Target Information

Target General Infomation
Target ID
T59328
Former ID
TTDS00355
Target Name
Epidermal growth factor receptor
Gene Name
EGFR
Synonyms
EGFR-TK; Epidermal growth factor receptor ErbB-1; Epidermal growth factor receptor-tyrosine kinase; Receptor protein-tyrosine kinase ErbB-1; Proto-oncogene c-ErbB-1; EGFR
Target Type
Successful
Disease Advanced cancers [ICD9: 140-229; ICD10: C00-C96]
Adult primary hepatocellular carcinoma [ICD10: C22]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33]
Brain cancer; Glioblastoma multiforme [ICD9:191, 225.0; ICD10: C71, D33]
Colorectal cancer; Squamous Non-small-cell lung cancer [ICD9:153, 154, 140-229, 162, 204.0; ICD10: C18-C21, C33, C33-C34, C34, C91.0]
Cryptosporidium infection [ICD10: A07.2]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Colorectal cancer; Head and neck cancer [ICD9: 140-149, 153, 154; ICD10: C18-C21, C07-C14, C32-C33]
Colon cancer; Glioma; Breast cancer; Head and neck cancer [ICD9: 140-149, 140-229, 183, 191; ICD10: C00-C96, C07-C14, C32, C33, C56, C71]
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Chronic lymphocytic leukaemia [ICD10: C91]
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89]
Esophageal cancer [ICD9: 150; ICD10: C15]
Glioblastoma multiforme [ICD9: 191; ICD10: C71]
Gastric cancer [ICD9: 151; ICD10: C16]
Gastrointestinal disease [ICD10: K00-K93]
Glioma [ICD9: 191; ICD10: C71]
Gastric cancer; Non-small cell lung cancer [ICD9:151; ICD10: C16, C33-C34]
Head and neck cancer [ICD9: 140-149, 140-229; ICD10: C07-C14, C32-C33]
Head and neck squamous cell carcinoma [ICD9: 199; ICD10: C44]
Inflammatory breast cancer [ICD9: 174, 175; ICD10: C50]
Ischemia [ICD9: 459.89; ICD10: I99.8]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Locally advanced head and neck cancer [ICD9: 140-149; ICD10: C07-C14, C32, C33]
Lung cancer [ICD9: 162; ICD10: C33-C34]
Metastatic epithelial tumors [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Malignant tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Melanoma [ICD9: 172; ICD10: C43]
Metastatic colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Non-small cell lung cancer; Metastatic colorectal cancer [ICD9:153, 154; ICD10: C33-C34, C18-C21]
Non-small cell lung cancer [ICD10: C33-C34]
Ovarian cancer [ICD9: 183; ICD10: C56]
Psoriasis [ICD9: 696; ICD10: L40]
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25]
Refractory breast cancer [ICD9: 174, 175; ICD10: C50]
Recurrent squamous cell carcinoma of the hypopharynx [ICD10: D37]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Urethral cancer; Bladder cancer; Ovarian cancer; Prostate cancer; Breast cancer [ICD9: 140-229, 174, 175, 183, 188; ICD10: C50, C56, C67]
Vulnerary [ICD10: S00-T98]
Unspecified [ICD code not available]
Function
Receptor for egf, but also for other members of the egf family, as tgf-alpha, amphiregulin, betacellulin, heparin-binding egf-like growth factor, gp30 and vaccinia virus growth factor. Is involved in the control of cell growth and differentiation.
BioChemical Class
Kinase
Target Validation
T59328
UniProt ID
P00533
EC Number
EC 2.7.10.1
Sequence
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
Drugs and Mode of Action
Drug(s) BIBW 2992 Drug Info Approved Non-small cell lung cancer [529823], [541010]
Cetuximab Drug Info Approved Colorectal cancer [527466], [541939]
DWP-401 Drug Info Approved Diabetic foot ulcer [536297]
Epidermal growth factor Drug Info Approved Vulnerary [551871]
Erlotinib Drug Info Approved Non-small cell lung cancer [468098], [527466]
Gefitinib Drug Info Approved Cancer [468104], [536223]
HEGF Drug Info Approved Diabetic foot ulcer [536297]
Lapatinib Drug Info Approved Breast cancer [538586], [541034]
Necitumumab Drug Info Approved Colorectal cancer; Squamous Non-small-cell lung cancer [522790], [542964]
Panitumumab Drug Info Approved Colorectal cancer [528715], [541940]
SKI-758 Drug Info Approved Ischemia [532210], [551871]
Tyverb/Tykerb Drug Info Approved Refractory breast cancer [538585]
Vandetanib Drug Info Approved Solid tumours [531783], [541055]
Icotinib hydrochloride Drug Info Registered Non-small cell lung cancer [525134], [542624], [550337]
AZD9291 Drug Info Phase 3 Melanoma [525278], [542692]
Bevacizumab + Erlotinib Drug Info Phase 3 Non-small cell lung cancer; Metastatic colorectal cancer [553819], [554242]
CO-1686 Drug Info Phase 3 Non-small cell lung cancer [525036], [542882]
Dacomitinib Drug Info Phase 3 Non-small cell lung cancer [523496], [542446]
DE-766 Drug Info Phase 3 Gastric cancer; Non-small cell lung cancer [550580], [550582]
Erlotinib Drug Info Phase 3 Pancreatic cancer [468098], [536361]
Gefitinib Drug Info Phase 3 Head and neck cancer [468104], [536223]
HKI-272 Drug Info Phase 3 Breast cancer [548009]
Rindopepimut Drug Info Phase 3 Brain cancer; Glioblastoma multiforme [523703]
Tyverb/Tykerb Drug Info Phase 3 Gastric cancer [538585]
Zalutumumab Drug Info Phase 3 Head and neck cancer [521892]
Indium-111 Drug Info Phase 2/3 Solid tumours [521975]
ABT-414 Drug Info Phase 2 Glioblastoma multiforme [542886], [549318]
ABX-EGF Drug Info Phase 2 Discovery agent [521640]
ASP8273 Drug Info Phase 2 Non-small cell lung cancer [525268]
Bevacizumab + Erlotinib Drug Info Phase 2 Adult primary hepatocellular carcinoma [523055], [553932], [554003], [555115], [555445], [555446]
BMS-599626 Drug Info Phase 2 Solid tumours [523940], [542630]
BMS-690514 Drug Info Phase 2 Chronic pain [528940]
CetuGEX Drug Info Phase 2 Cancer [531354]
CI-1033 Drug Info Phase 2 Lymphoma [525738], [541018]
Erlotinib Drug Info Phase 2 Colon cancer; Glioma; Breast cancer; Head and neck cancer [468098], [536361]
Gefitinib Drug Info Phase 2 Urethral cancer; Bladder cancer; Ovarian cancer; Prostate cancer; Breast cancer [468104], [536223]
HER1-VSSP vaccine Drug Info Phase 2 Cancer [525364], [528312]
HM-78136B Drug Info Phase 2 Solid tumours [524875], [542826]
Matuzumab Drug Info Phase 2 Gastric cancer [521578]
MEHD-7945A Drug Info Phase 2 Solid tumours [523994]
MEHD7945A Drug Info Phase 2 Colorectal cancer; Head and neck cancer [523994], [889373]
Panitumumab Drug Info Phase 2 Locally advanced head and neck cancer [538382], [541940]
Pazopanib + Tyverb/Tykerb Drug Info Phase 2 Inflammatory breast cancer [532156]
Pelitinib Drug Info Phase 2 Lymphoma [521571], [542627]
SYM-004 Drug Info Phase 2 Head and neck cancer [524673]
TT-100 Drug Info Phase 2 Non-small cell lung cancer [548064]
Tyverb/Tykerb Drug Info Phase 2 Head and neck squamous cell carcinoma [538585]
VATALANIB Drug Info Phase 2 Solid tumours [521851], [541046]
Bevacizumab + Erlotinib Drug Info Phase 1/2 Recurrent squamous cell carcinoma of the hypopharynx [553734]
EGF816 Drug Info Phase 1/2 Non-small cell lung cancer [524707]
EMD 55900 Drug Info Phase 1/2 Glioma [534148]
SN-32793 Drug Info Phase 1/2 Non-small cell lung cancer [523961]
Varlitinib Drug Info Phase 1/2 Breast cancer [522608], [542628]
S-222611 Drug Info Phase 1b Malignant tumor [551683]
AMG 595 Drug Info Phase 1 Glioblastoma multiforme [547942]
Anti-HER3/EGFR DAF Drug Info Phase 1 Metastatic epithelial tumors [550794]
AST-1306 Drug Info Phase 1 Cancer [549107]
BIBX-1382 Drug Info Phase 1 Chronic lymphocytic leukaemia [521457], [542629]
Cipatinib Drug Info Phase 1 Cancer [523370]
CUDC-101 Drug Info Phase 1 Solid tumours [533101]
HER-2/HER-1 vaccine Drug Info Phase 1 Solid tumours [533315]
IMGN289 Drug Info Phase 1 Solid tumours [524477]
JNJ-26483327 Drug Info Phase 1 Cancer [522319]
LY3164530 Drug Info Phase 1 Advanced cancers [889401]
MR1-1 Drug Info Phase 1 Brain cancer [522845]
111In-hEGF Drug Info Preclinical Breast cancer [528222], [533321]
EGFR/IGFR tandem adnectin Drug Info Preclinical Cancer [548559]
PKI166 Drug Info Discontinued in Phase 2 Esophageal cancer [542625], [547182]
RG7160 Drug Info Discontinued in Phase 2 Metastatic colorectal cancer [548810]
AZD4769 Drug Info Discontinued in Phase 1 Solid tumours [548344]
PD-153035 Drug Info Discontinued in Phase 1 Psoriasis [545893]
TAK165 Drug Info Discontinued in Phase 1 Cancer [541276], [547786]
AZD-9935 Drug Info Terminated Solid tumours [547683]
CGP-52411 Drug Info Terminated Cancer [545834]
CGP-53353 Drug Info Terminated Discovery agent [468226], [546079]
Heparin-EGF-like factor Drug Info Terminated Gastrointestinal disease [533768], [533866]
Inhibitor (3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine Drug Info [533683]
(3-Bromo-phenyl)-quinazolin-4-yl-amine Drug Info [534127]
(E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin Drug Info [530002]
(S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate Drug Info [551353]
10-hydroxy-18-methoxybetaenone Drug Info [525806]
2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile Drug Info [528244]
2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile Drug Info [528244]
2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile Drug Info [551353]
2-cyano-3-(3,4-dihydroxyphenyl)acrylamide Drug Info [551353]
2-methoxy-4-(2-nitrovinyl)phenol Drug Info [551353]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Drug Info [528032]
3,4-diphenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one Drug Info [525445]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-Pyridin-4-yl-quinoline-6,7-diol Drug Info [533872]
4-(2-nitroprop-1-enyl)benzene-1,2-diol Drug Info [551353]
4-(2-nitrovinyl)benzene-1,2-diol Drug Info [551353]
4-(2-nitrovinyl)phenol Drug Info [551353]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Drug Info [551331]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Drug Info [551331]
4-(3-Bromo-phenylamino)-quinazoline-6,7-diol Drug Info [534127]
4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid Drug Info [551353]
4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline Drug Info [529134]
4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Drug Info [527849]
4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline Drug Info [529046]
4557W Drug Info [526072]
5,6-Bis-p-tolylamino-isoindole-1,3-dione Drug Info [533915]
5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Drug Info [527849]
6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline Drug Info [529046]
6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline Drug Info [529046]
6,7-diethoxy-4-styrylquinazoline Drug Info [529046]
6,7-dimethoxy-4-(2-phenylethynyl)quinazoline Drug Info [529046]
6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline Drug Info [529046]
6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline Drug Info [529046]
6,7-dimethoxy-N-m-tolylquinazolin-4-amine Drug Info [529935]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Drug Info [530473]
AG 112 Drug Info [533080]
AG 9 Drug Info [533080]
AG-213 Drug Info [529134]
AG-538 Drug Info [551353]
ASP8273 Drug Info [549984]
AZD4769 Drug Info [550288]
AZD9291 Drug Info [532797]
Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine Drug Info [534127]
Benzyl-quinazolin-4-yl-amine Drug Info [533683]
Bevacizumab + Erlotinib Drug Info [551607]
BIBW 2992 Drug Info [550386]
BMS-599626 Drug Info [530678], [536474]
BMS-690514 Drug Info [530732]
BPIQ-I Drug Info [534127]
CGP-52411 Drug Info [534180]
CGP-53353 Drug Info [533915]
CI-1033 Drug Info [536474]
CL-387785 Drug Info [529935]
Cochliobolic acid Drug Info [534313]
compound 38 Drug Info [532836]
compound 56 Drug Info [534095]
EGF816 Drug Info [532489]
EGFR inhibitor Drug Info [529213]
EGFR/IGFR tandem adnectin Drug Info [550011]
Epitinib Drug Info [543485]
Erlotinib Drug Info [537629]
Gefitinib Drug Info [535899], [535901]
HDS-029 Drug Info [528037]
HKI-272 Drug Info [528774]
HM-61713B Drug Info [543485]
HM-78136B Drug Info [531542]
HTS-00213 Drug Info [529935]
HTS-02876 Drug Info [529935]
HTS-05058 Drug Info [529213]
IMGN289 Drug Info [544376]
JNJ-26483327 Drug Info [550422]
Lapatinib Drug Info [536331], [537224]
LAVENDUSTIN A Drug Info [533837]
MDP-01 Drug Info [543485]
MT-062 Drug Info [543485]
N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine Drug Info [534127]
N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine Drug Info [526895]
N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine Drug Info [533683]
N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine Drug Info [534120]
N-(4-(phenylamino)quinazolin-6-yl)acrylamide Drug Info [528707]
N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Drug Info [525502]
N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide Drug Info [525502]
N4-(3-chlorophenyl)quinazoline-4,6-diamine Drug Info [528809]
N4-(3-methylphenyl)-4,6-quinazolinediamine Drug Info [528236]
NRC-2694 Drug Info [543485]
ON-128 Drug Info [543485]
OSI-75 Drug Info [535318]
Pazopanib + Tyverb/Tykerb Drug Info [550963]
PD-0166326 Drug Info [525862]
PD-0173956 Drug Info [525862]
PD-0180970 Drug Info [525862]
PD-158780 Drug Info [534120]
PD-168393 Drug Info [528707]
PD182905 Drug Info [535233]
PP121 Drug Info [529744]
RG-50810 Drug Info [551353]
RM-6427 Drug Info [543485]
Ro-4396686 Drug Info [528018]
S-222611 Drug Info [551683]
SKI-758 Drug Info [528584]
SN-32793 Drug Info [543485]
TAK165 Drug Info [536474]
Theliatinib Drug Info [543485]
TT-100 Drug Info [549834]
TYRPHOSTIN AG-1478 Drug Info [525445]
Tyverb/Tykerb Drug Info [550963]
Vandetanib Drug Info [536474], [550288]
VATALANIB Drug Info [528774]
WHI-P154 Drug Info [529228]
WZ-3146 Drug Info [543485]
Modulator 111In-hEGF Drug Info [525767]
AGT-2000 Drug Info [543485]
AL-6802 Drug Info [543485]
AMG 595 Drug Info [533230]
Anti-HER3/EGFR DAF Drug Info
AST-1306 Drug Info [531575]
Cipatinib Drug Info [1572591]
CO-1686 Drug Info [533226]
CUDC-101 Drug Info [533101]
DE-766 Drug Info [543485]
Epidermal growth factor Drug Info [543485]
Heparin-EGF-like factor Drug Info [533768], [533866]
Imaging-theranostic nanoemulsion agents Drug Info [543485]
LA22-radioimmunoconjugates Drug Info [543485]
LY3164530 Drug Info [889442]
MEHD-7945A Drug Info [1572591]
MEHD7945A Drug Info [889442]
MG-111 Drug Info
MR1-1 Drug Info [550395]
Necitumumab Drug Info [531296]
PD-153035 Drug Info
Pelitinib Drug Info
PF 5208766 Drug Info
PKI166 Drug Info
RG7160 Drug Info [532140]
Rindopepimut Drug Info [531296]
Small-molecule cetuximab binding mimics Drug Info [543485]
SYM-011 Drug Info [543485]
TGF alpha Drug Info [543485]
Varlitinib Drug Info [1572591]
Antagonist AZD-9935 Drug Info [550140]
BIBX-1382 Drug Info [526329]
Dacomitinib Drug Info [543485]
EDP-13 Drug Info [543485]
Icotinib hydrochloride Drug Info [531288]
IPS-01003 Drug Info [543485]
RX-1792 Drug Info [543485]
Activator DWP-401 Drug Info [536297]
HEGF Drug Info [536297]
Suppressor Panitumumab Drug Info [537616]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
DRM DRM Info
Pathways
KEGG Pathway MAPK signaling pathway
ErbB signaling pathway
Ras signaling pathway
Rap1 signaling pathway
Calcium signaling pathway
Cytokine-cytokine receptor interaction
HIF-1 signaling pathway
FoxO signaling pathway
Endocytosis
PI3K-Akt signaling pathway
Dorso-ventral axis formation
Focal adhesion
Adherens junction
Gap junction
Regulation of actin cytoskeleton
GnRH signaling pathway
Estrogen signaling pathway
Oxytocin signaling pathway
Epithelial cell signaling in Helicobacter pylori infection
Hepatitis C
Pathways in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Melanoma
Bladder cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
Choline metabolism in cancer
NetPath Pathway IL4 Signaling Pathway
EGFR1 Signaling Pathway
PANTHER Pathway Cadherin signaling pathway
EGF receptor signaling pathway
Pathway Interaction Database LPA receptor mediated events
Signaling events mediated by PTP1B
Arf6 signaling events
Signaling events mediated by TCPTP
Thromboxane A2 receptor signaling
SHP2 signaling
Regulation of Telomerase
EGF receptor (ErbB1) signaling pathway
EGFR-dependent Endothelin signaling events
Posttranslational regulation of adherens junction stability and dissassembly
Direct p53 effectors
ErbB1 downstream signaling
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
E-cadherin signaling in keratinocytes
ErbB receptor signaling network
Internalization of ErbB1
Stabilization and expansion of the E-cadherin adherens junction
a6b1 and a6b4 Integrin signaling
Syndecan-3-mediated signaling events
Reactome Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
SHC1 events in ERBB2 signaling
PLCG1 events in ERBB2 signaling
PIP3 activates AKT signaling
GRB2 events in EGFR signaling
GAB1 signalosome
SHC1 events in EGFR signaling
EGFR downregulation
GRB2 events in ERBB2 signaling
PI3K events in ERBB2 signaling
EGFR Transactivation by Gastrin
Constitutive Signaling by Aberrant PI3K in Cancer
Constitutive Signaling by EGFRvIII
RAF/MAP kinase cascade
WikiPathways ErbB Signaling Pathway
Regulation of Actin Cytoskeleton
EGF/EGFR Signaling Pathway
MAPK Signaling Pathway
Focal Adhesion
Aryl Hydrocarbon Receptor Pathway
Extracellular vesicle-mediated signaling in recipient cells
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
Cytodifferentiation (Part 3 of 3)
Bladder Cancer
Induction (Part 1 of 3)
Signaling by ERBB4
Signaling by ERBB2
Gastrin-CREB signalling pathway via PKC and MAPK
PIP3 activates AKT signaling
Nanoparticle-mediated activation of receptor signaling
Aryl Hydrocarbon Receptor
Spinal Cord Injury
Integrated Pancreatic Cancer Pathway
Gastric cancer network 2
AGE/RAGE pathway
Signaling Pathways in Glioblastoma
Arylhydrocarbon receptor (AhR) signaling pathway
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
Integrated Breast Cancer Pathway
Signaling by EGFR
L1CAM interactions
References
Ref 468098(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4920).
Ref 468104(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4941).
Ref 468226(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5163).
Ref 521457ClinicalTrials.gov (NCT00003980) BIBX 1382 in Treating Patients With Solid Tumors. U.S. National Institutes of Health.
Ref 521571ClinicalTrials.gov (NCT00067548) Study Evaluating EKB-569 in Advanced Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 521578ClinicalTrials.gov (NCT00073541) A Study of the Safety and Effects of EMD 72000 in Subjects With Recurrent Ovarian Cancer. U.S. National Institutes of Health.
Ref 521640ClinicalTrials.gov (NCT00111761) Evaluating Panitumumab (ABX-EGF) in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
Ref 521851ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health.
Ref 521892ClinicalTrials.gov (NCT00382031) Zalutumumab in Patients With Non-curable Head and Neck Cancer. U.S. National Institutes of Health.
Ref 521975ClinicalTrials.gov (NCT00442533) Safety and Efficacy Study of In-111 Pentetreotide to Treat Neuroendocrine Tumors. U.S. National Institutes of Health.
Ref 522319ClinicalTrials.gov (NCT00676299) A Safety and Dose-finding Study of JNJ-26483327, a Drug in Development for Cancer, for Patients With Advanced and/or Refractory Solid Malignancies.. U.S. National Institutes of Health.
Ref 522608ClinicalTrials.gov (NCT00862524) A Study of ARRY-334543 and Gemcitabine in Patients With Advanced Cancer and Pancreatic Cancer. U.S. National Institutes of Health.
Ref 522790ClinicalTrials.gov (NCT00981058) First-line Treatment of Participants With Stage IV Squamous Non-Small Cell Lung Cancer With Necitumumab and Gemcitabine-Cisplatin. U.S. National Institutes of Health.
Ref 522845ClinicalTrials.gov (NCT01009866) Study of Immunotoxin, MR1-1. U.S. National Institutes of Health.
Ref 523055ClinicalTrials.gov (NCT01130519) A Phase II Study of Bevacizumab and Erlotinib in Subjects With Advanced Hereditary Leiomyomatosis and Renal Cell Cancer (HLRCC) or Sporadic Papillary Renal Cell Cancer. U.S. National Institutes of Health.
Ref 523370ClinicalTrials.gov (NCT01301911) Study of Cipatinib in Patients With HER2 Positive or Uncertain Advanced Breast Cancer. U.S. National Institutes of Health.
Ref 523496ClinicalTrials.gov (NCT01360554) ARCHER 1009 : A Study Of Dacomitinib (PF-00299804) Vs. Erlotinib In The Treatment Of Advanced Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 523703ClinicalTrials.gov (NCT01480479) Phase III Study of Rindopepimut/GM-CSF in Patients With Newly Diagnosed Glioblastoma. U.S. National Institutes of Health.
Ref 523940ClinicalTrials.gov (NCT01614522) A Clinical Trial Evaluating the Effect of ASLAN001 in Patients With Recurrent/Metastatic Gastric Cancer Whose Tumors Are Either HER-2 Amplified or Co-expressing HER-1and HER-2. U.S. National Institutes of Health.
Ref 523961ClinicalTrials.gov (NCT01631279) A Dose Escalation Trial of PR610 Treating Patients With Solid Tumors. U.S. National Institutes of Health.
Ref 523994ClinicalTrials.gov (NCT01652482) A Study of MEHD7945A + FOLFIRI Versus Cetuximab + FOLFIRI in Second Line in Patients With KRAS Wild-Type Metastatic Colorectal Cancer. U.S. National Institutes of Health.
Ref 524477ClinicalTrials.gov (NCT01963715) A Phase 1 Study of IMGN289 in Adult Patients With EGFR-positive Solid Tumors. U.S. National Institutes of Health.
Ref 524673ClinicalTrials.gov (NCT02083653) Sym004 vs Standard of Care in Subjects With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
Ref 524707ClinicalTrials.gov (NCT02108964) A Phase I/II, Multicenter, Open-label Study of EGFRmut-TKI EGF816, Administered Orally in Adult Patients With EGFRmut Solid Malignancies. U.S. National Institutes of Health.
Ref 524875ClinicalTrials.gov (NCT02216916) Phase II Trial of HM781-36B in Patients With Metastatic/Recurrent Head and Neck Squamous Cell Carcinoma (HNSCC) After Failure of or Unfit for Platinum-containing Therapy. U.S. National Institutes of Health.
Ref 525036ClinicalTrials.gov (NCT02322281) TIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemotherapy. U.S. National Institutes of Health.
Ref 525134ClinicalTrials.gov (NCT02404675) High Dose Icotinib in Advanced Non-small Cell Lung Cancer Patients With EGFR 21 Exon Positive. U.S. National Institutes of Health.
Ref 525268ClinicalTrials.gov (NCT02500927) A Study of ASP8273 in Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-Naïve Patients With Non-Small Cell Lung Cancer Harboring EGFR Mutations.
Ref 525278ClinicalTrials.gov (NCT02511106) AZD9291 Versus Placebo in Patients With Stage IB-IIIA Non-small Cell Lung Carcinoma, Following Complete Tumour Resection With or Without Adjuvant Chemotherapy.
Ref 525364HER1-ECD vaccination dispenses with emulsification to elicit HER1-specific anti-proliferative effects. Hum Vaccin. 2009 Mar;5(3):158-65. Epub 2009 Mar 6.
Ref 525738Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97.
Ref 5274662004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
Ref 528222Preclinical pharmacokinetic, biodistribution, toxicology, and dosimetry studies of 111In-DTPA-human epidermal growth factor: an auger electron-emitting radiotherapeutic agent for epidermal growth factor receptor-positive breast cancer. J Nucl Med. 2006 Jun;47(6):1023-31.
Ref 528312Active antimetastatic immunotherapy in Lewis lung carcinoma with self EGFR extracellular domain protein in VSSP adjuvant. Int J Cancer. 2006 Nov 1;119(9):2190-9.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 528940A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62.
Ref 529823BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs. 2008 Dec;9(12):1336-46.
Ref 531354Molecular mechanisms of resistance to the EGFR monoclonal antibody cetuximab. Cancer Biol Ther. 2011 May 1;11(9):777-92. Epub 2011 May 1.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 532156A randomized phase II study of lapatinib + pazopanib versus lapatinib in patients with HER2+ inflammatory breast cancer. Breast Cancer Res Treat. 2013 Jan;137(2):471-82.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 533101A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73.
Ref 533315Anti-Tumor Effects of Peptide Therapeutic and Peptide Vaccine Antibody Co-targeting HER-1 and HER-2 in Esophageal Cancer (EC) and HER-1 and IGF-1R in Triple-Negative Breast Cancer (TNBC). Vaccines (Basel). 2015 Jul 6;3(3):519-43.
Ref 533321A comparison of non-biologically active truncated EGF (EGFt) and full-length hEGF for delivery of Auger electron-emitting 111In to EGFR-positive breast cancer cells and tumor xenografts in athymic mice. Nucl Med Biol. 2015 Aug 19. pii: S0969-8051(15)00147-X.
Ref 533768The heparin-binding domain of heparin-binding EGF-like growth factor can target Pseudomonas exotoxin to kill cells exclusively through heparan sulfate proteoglycans. J Cell Sci. 1994 Sep;107 ( Pt 9):2599-608.
Ref 533866Heparin-binding epidermal growth factor-like growth factor is an autocrine growth factor for human keratinocytes. J Biol Chem. 1994 Aug 5;269(31):20060-6.
Ref 534148Multiple infusions of anti-epidermal growth factor receptor (EGFR) monoclonal antibody (EMD 55,900) in patients with recurrent malignant gliomas. Eur J Cancer. 1996 Apr;32A(4):636-40.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538382FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (BLA) 125147.
Ref 538585FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
Ref 538586FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
Ref 541010(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5667).
Ref 541018(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5675).
Ref 541034(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5692).
Ref 541046(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5705).
Ref 541055(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5717).
Ref 541276(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6011).
Ref 541939(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6882).
Ref 541940(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6883).
Ref 542446(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7422).
Ref 542624(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7641).
Ref 542625(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7642).
Ref 542627(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7644).
Ref 542628(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7645).
Ref 542629(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7646).
Ref 542630(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7647).
Ref 542692(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7719).
Ref 542826(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7903).
Ref 542882(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7966).
Ref 542886(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7970).
Ref 542964(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8090).
Ref 545834Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004971)
Ref 545893Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005268)
Ref 546079Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006215)
Ref 547182Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013689)
Ref 547683Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018392)
Ref 547786Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019257)
Ref 547942Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020588)
Ref 548009Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154)
Ref 548064Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021633)
Ref 548344Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024847)
Ref 548559Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026610)
Ref 548810Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029052)
Ref 549107Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032292)
Ref 549318Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035129)
Ref 550337Clinical pipeline report, company report or official report of Beta Pharma.
Ref 550580Clinical pipeline report, company report or official report of Daiichi Sankyo.
Ref 550582Clinical pipeline report, company report or official report of Daiichi Sankyo.
Ref 550794Clinical pipeline report, company report or official report of Genentech (2011).
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 553734ClinicalTrials.gov (NCT00055913) Bevacizumab and Erlotinib in Treating Patients With Recurrent or Metastatic Head and Neck Cancer
Ref 553819ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer
Ref 553932ClinicalTrials.gov (NCT00287222) Bevacizumab and Erlotinib in Inoperable and Metastatic Hepatocellular Carcinoma
Ref 554003ClinicalTrials.gov (NCT00365391) Bevacizumab and Erlotinib in Treating Patients With Advanced Liver Cancer
Ref 554242ClinicalTrials.gov (NCT00598156) Chemotherapy and Avastin Followed by Maintenance Treatment With Avastin +/- Tarceva
Ref 555115ClinicalTrials.gov (NCT02655536) Bevacizumab and Erlotinib in Lung Cancer With Brain Metastases, a Phase II Trial
Ref 555445Combined inhibition of vascular endothelial growth factor and epidermal growth factor signaling in non-small-cell lung cancer therapy. Clin Lung Cancer. 2009 Mar;10 Suppl 1:S17-23. doi: 10.3816/CLC.2009.s.003.
Ref 555446Efficacy of bevacizumab plus erlotinib versus erlotinib alone in advanced non-small-cell lung cancer after failure of standard first-line chemotherapy (BeTa): a double-blind, placebo-controlled, phase 3 trial. Lancet. 2011 May 28;377(9780):1846-54. doi: 10.1016/S0140-6736(11)60545-X.
Ref 889373ClinicalTrials.gov (NCT01577173) A Study of MEHD7945A Versus Cetuximab in Patients With Recurrent/Metastatic Squamous Cell Carcinoma of The Head And Neck
Ref 889401ClinicalTrials.gov (NCT02221882) A Study of LY3164530 in Participants With Cancer
Ref
Ref 525445J Med Chem. 1999 Mar 25;42(6):1018-26.Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.
Ref 525502J Med Chem. 1999 May 20;42(10):1803-15.Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding siteof the epidermal growth factor receptor.
Ref 525767A comparison of EGF and MAb 528 labeled with 111In for imaging human breast cancer. J Nucl Med. 2000 May;41(5):903-11.
Ref 525806J Nat Prod. 2000 Jun;63(6):739-45.Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 526072Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Ref 526329Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80.
Ref 526895J Med Chem. 2003 Dec 4;46(25):5546-51.Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept.
Ref 527849Bioorg Med Chem Lett. 2006 Jan 15;16(2):469-72. Epub 2005 Nov 3.Acryloylamino-salicylanilides as EGFR PTK inhibitors.
Ref 528018Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Ref 528032J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
Ref 528037J Med Chem. 2006 Feb 23;49(4):1475-85.Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Ref 528236J Med Chem. 2006 Jun 15;49(12):3544-52.The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).
Ref 528244J Med Chem. 1991 Jun;34(6):1896-907.Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Ref 528312Active antimetastatic immunotherapy in Lewis lung carcinoma with self EGFR extracellular domain protein in VSSP adjuvant. Int J Cancer. 2006 Nov 1;119(9):2190-9.
Ref 528584J Med Chem. 2006 Dec 28;49(26):7868-76.Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.
Ref 528707Nat Chem Biol. 2007 Apr;3(4):229-38. Epub 2007 Mar 4.Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
Ref 528774Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Ref 528809J Med Chem. 2007 May 31;50(11):2605-8. Epub 2007 May 2.Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.
Ref 529046Bioorg Med Chem Lett. 2007 Nov 1;17(21):5863-7. Epub 2007 Aug 15.Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.
Ref 529134Eur J Med Chem. 2008 Jul;43(7):1478-88. Epub 2007 Sep 29.Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.
Ref 529213Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Ref 529228The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. Epub 2007 Dec 19.
Ref 529407Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Cancer Cell. 2008 Apr;13(4):365-73.
Ref 529744Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
Ref 529935J Med Chem. 2009 Feb 26;52(4):964-75.Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.
Ref 530002Eur J Med Chem. 2009 Sep;44(9):3471-9. Epub 2009 Feb 7.5-Benzylidene-hydantoins: synthesis and antiproliferative activity on A549 lung cancer cell line.
Ref 530473Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Ref 530678AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61.
Ref 530732Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
Ref 531288Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 2011 Aug;73(2):195-202.
Ref 531296Rindopepimut, a 14-mer injectable peptide vaccine against EGFRvIII for the potential treatment of glioblastoma multiforme. Curr Opin Mol Ther. 2010 Dec;12(6):741-54.
Ref 531354Molecular mechanisms of resistance to the EGFR monoclonal antibody cetuximab. Cancer Biol Ther. 2011 May 1;11(9):777-92. Epub 2011 May 1.
Ref 531542Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54.
Ref 531575AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.
Ref 532140GA201 (RG7160): a novel, humanized, glycoengineered anti-EGFR antibody with enhanced ADCC and superior in vivo efficacy compared with cetuximab. Clin Cancer Res. 2013 Mar 1;19(5):1126-38.
Ref 532489Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Dec;3(12):1404-15.
Ref 532540Sym004, a novel EGFR antibody mixture, can overcome acquired resistance to cetuximab. Neoplasia. 2013 Oct;15(10):1196-206.
Ref 532797AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.
Ref 532836Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28.
Ref 533080Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52.
Ref 533101A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73.
Ref 533159Characterization of ABT-806, a Humanized Tumor-Specific Anti-EGFR Monoclonal Antibody. Mol Cancer Ther. 2015 May;14(5):1141-51.
Ref 533226Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9.
Ref 533230AMG 595, an Anti-EGFRvIII Antibody-Drug Conjugate, Induces Potent Antitumor Activity against EGFRvIII-Expressing Glioblastoma. Mol Cancer Ther. 2015 Jul;14(7):1614-24.
Ref 533683J Med Chem. 1995 Sep 1;38(18):3482-7.Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.
Ref 533768The heparin-binding domain of heparin-binding EGF-like growth factor can target Pseudomonas exotoxin to kill cells exclusively through heparan sulfate proteoglycans. J Cell Sci. 1994 Sep;107 ( Pt 9):2599-608.
Ref 533837J Med Chem. 1994 Nov 25;37(24):4079-84.Novel antiproliferative agents derived from lavendustin A.
Ref 533866Heparin-binding epidermal growth factor-like growth factor is an autocrine growth factor for human keratinocytes. J Biol Chem. 1994 Aug 5;269(31):20060-6.
Ref 533872J Med Chem. 1994 Aug 19;37(17):2627-9.5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.
Ref 533915J Med Chem. 1994 Apr 1;37(7):1015-27.Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.
Ref 534095Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.
Ref 534120J Med Chem. 1996 Apr 26;39(9):1823-35.Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor.
Ref 534127J Med Chem. 1996 Feb 16;39(4):918-28.Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Ref 534180Retinoic acid-induced RB (retinoblastoma) hypophosphorylation enhanced by CGP 52411 (4,5-dianilinophthalimide), an EGF family tyrosine kinase receptor inhibitor. Eur J Cell Biol. 1996 Apr;69(4):327-34.
Ref 534313J Nat Prod. 1997 Jan;60(1):6-8.Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay.
Ref 535233Growth factors and their receptors: new targets for prostate cancer therapy. Urology. 2001 Aug;58(2 Suppl 1):114-22.
Ref 535318Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37.
Ref 535397Epidermal growth factor receptors as a target for cancer treatment: the emerging role of IMC-C225 in the treatment of lung and head and neck cancers. Semin Oncol. 2002 Feb;29(1 Suppl 4):27-36.
Ref 535418Monoclonal antibodies to target epidermal growth factor receptor-positive tumors: a new paradigm for cancer therapy. Cancer. 2002 Mar 1;94(5):1593-611.
Ref 535602Epidermal growth factor receptor-targeted therapy for pancreatic cancer. Semin Oncol. 2002 Oct;29(5 Suppl 14):31-7.
Ref 535628Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol Cancer Ther. 2002 May;1(7):507-14.
Ref 535899Targeting' the epidermal growth factor receptor tyrosine kinase with gefitinib (Iressa) in non-small cell lung cancer (NSCLC). Semin Cancer Biol. 2004 Feb;14(1):33-40.
Ref 535901Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
Ref 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536331Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28.
Ref 536474A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 537224Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
Ref 537616Integration of panitumumab into the treatment of colorectal cancer. Crit Rev Oncol Hematol. 2009 Jul 16.
Ref 537629Quantitative Prediction of Fold Resistance for Inhibitors of EGFR. Biochemistry. 2009 Jul 23.
Ref 543485(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
Ref 544371Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development. Mar Drugs. 2014 January; 12(1): 255-278.
Ref 544376World Antibody-Drug Conjugate Summit, October 15-16, 2013, San Francisco, CA. MAbs. 2014 January 1; 6(1): 18-29.
Ref 549834BiPar Sciences Co-founder Reunites Management Team At TriAct Therapeutics to Advance Clinical Stage Cancer Programs. TriAct Therapeutics. Sept. 10, 2009.
Ref 549984Phase I dose escalation study of ASP8273, a mutant-selective irreversible EGFR inhibitor, in subjects with EGFR mutation positive NSCLC, Journal of Clinical Oncology, Vol 33, No 15_suppl (May 20 Supplement), 2015: 8083.
Ref 550011Clinical pipeline report, company report or official report of Bristol-Myers Squibb.
Ref 550140WO patent application no. 2009,0582,67, Benzomorpholine derivatives and methods of use.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550386Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
Ref 550395A Phase I Study of Immunotoxin, MR1-1. Duke University report.
Ref 550422National Cancer Institute Drug Dictionary (drug id 596693).
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551331A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997).
Ref 551353Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60.
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).
Ref 551683Clinical pipeline report, company report or official report of Shionogi (2011).
Ref 889442Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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