Target Information

Target General Infomation
Target ID
T95913
Former ID
TTDR00356
Target Name
Phosphoinositide 3 kinase
Gene Name
PIK3CG
Synonyms
PI 3-kinase; PI3K; Phosphoinositol-3 kinase; PI3-kinase p110 subunit gamma; PI3K; PI3Kgamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphoinositide 3-Kinase gamma; PtdIns-3-kinase p110; PIK3CG
Target Type
Successful
Disease Advanced solid tumor; Non-hodgkin's lymphoma [ICD9: 140-199, 200, 202, 202.8, 210-229; ICD10: C00-C75, C7A, C7B, C81-C86, C82-C85, D10-D36, D3A]
Angioedema; Myocardial infarction [ICD9: 277.6, 410, 995.1; ICD10: D84.1, I21, I22, T78.3]
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Cardiovascular disorder [ICD10: I00-I99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Diffuse large B-cell lymphoma [ICD9: 200; ICD10: C83.3]
Enthesopathy; Type 2 diabetes [ICD9:726, 250; ICD10: M76-M77.9, E11]
Endometrial cancer [ICD9: 182; ICD10: C54.1]
Glioma [ICD9: 191; ICD10: C71]
Hematologic malignancies [ICD9: 200-209; ICD10: C81-C86]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Metastatic breast cancer; Endometrial cancer; Lymphoma [ICD9: 140-199, 140-229, 174, 175, 182.0, 202.8, 210-229; ICD10: C50, C81-C86]
Non-hodgkin's lymphoma [ICD10: C85]
Prostate cancer [ICD9: 185; ICD10: C61]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4- phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5- bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation in breast cancer cells through the PDPK1- AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Has also serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS.
BioChemical Class
Kinase
Target Validation
T17917
UniProt ID
P48736
EC Number
EC 2.7.11.1
Sequence
MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLH
VAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLD
CLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGL
VTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDT
PGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNG
EEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRK
FRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKI
KDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEY
VLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEG
DRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQ
QEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYL
LQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAY
LRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLP
ESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQ
DMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTG
AFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNL
FHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLAL
RHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGW
TVQFNWFLHLVLGIKQGEKHSA
Structure
1E8Y; 1E8Z; 1HE8; 2A4Z; 2A5U; 2CHW; 2CHX; 2CHZ; 2V4L; 3APC; 3APD; 3APF; 3CSF; 3CST; 3DBS; 3DPD; 3ENE; 3IBE; 3L08; 3L13; 3L16; 3L17; 3L54; 3LJ3; 3MJW; 3ML8; 3ML9; 3NZS; 3NZU; 3OAW; 3P2B; 3PRE; 3PRZ; 3PS6; 3QAQ; 3QAR; 3QJZ; 3QK0; 3R7Q; 3R7R; 3S2A; 3SD5; 3T8M; 3TJP; 3TL5; 3ZVV; 3ZW3; 4ANU; 4ANV; 4ANW; 4ANX; 4AOF; 4DK5; 4EZJ; 4EZK; 4EZL; 4F1S; 4FA6; 4FAD; 4FHJ; 4FHK; 4FJY; 4FJZ; 4FLH; 4FUL; 4G11; 4GB9; 4HLE; 4HVB; 4J6I; 4KZ0; 4KZC; 4PS3; 4PS7; 4PS8; 4URK; 4WWN; 4WWO; 4WWP; 2ENQ; 2RD0; 3HHM; 3HIZ; 3ZIM; 4JPS; 4L1B; 4L23; 4L2Y; 4OVU; 4OVV; 4TUU; 4TV3; 4WAF
Drugs and Mode of Action
Drug(s) CHU Drug Info Registered Enthesopathy; Type 2 diabetes [548663]
BAY 80-6946 Drug Info Phase 3 Non-hodgkin's lymphoma [542801], [549051]
Buparlisib Drug Info Phase 3 Breast cancer [523929], [542804]
IPI-145 Drug Info Phase 3 Arthritis [532543], [542746]
Rigosertib Drug Info Phase 3 Solid tumours [532659], [542777]
BEZ235 Drug Info Phase 2 Solid tumours [542866], [548508]
CLR-1404 Drug Info Phase 2 Cancer [524202]
GDC0941 Drug Info Phase 2 Advanced solid tumor; Non-hodgkin's lymphoma [541027], [548661]
PF-04691502 Drug Info Phase 2 Endometrial cancer [523615], [542851]
PF-05212384 Drug Info Phase 2 Cancer [533132], [542855]
PX-866 Drug Info Phase 2 Cancer [523422], [542856]
SAR245409 Drug Info Phase 2 Cancer [524422]
XL147 Drug Info Phase 2 Cancer [533087], [542879]
BGT226 Drug Info Phase 1/2 Solid tumours [531639], [542867]
CLR-1401 Drug Info Phase 1/2 Cancer [523773]
CLR457 Drug Info Phase 1/2 Advanced solid tumor [524832]
TG100-115 Drug Info Phase 1/2 Angioedema; Myocardial infarction [536497], [541054]
CH-5132799 Drug Info Phase 1 Solid tumours [531469], [542708]
CUDC-907 Drug Info Phase 1 Diffuse large B-cell lymphoma [550573]
DS-7423 Drug Info Phase 1 Solid tumours [549261]
GDC-0980 Drug Info Phase 1 Advanced solid tumor; Non-hodgkin's lymphoma [550796]
GSK2126458 Drug Info Phase 1 Lymphoma [533074]
P-7170 Drug Info Phase 1 Cancer [524177]
PA-799 Drug Info Phase 1 Solid tumours [549160]
Perifosine Drug Info Phase 1 Solid tumours [521489], [542448]
PQR309 Drug Info Phase 1 Pain [543099]
SAR245408 + MSC1936369B Drug Info Phase 1 Solid tumours [523487]
SAR245409/MSC1936369B combination therapy Drug Info Phase 1 Solid tumours [523487]
SF1126 Drug Info Phase 1 Solid tumours [548503]
VS-5584 Drug Info Phase 1 Solid tumours [532167], [543098]
ZSTK474 Drug Info Phase 1 Cancer [532539], [542881]
Adyvia Drug Info Discontinued in Phase 2 Type 2 diabetes [547734]
GDC-0084 Drug Info Discontinued in Phase 1 Glioma [549369]
GSK1059615 Drug Info Discontinued in Phase 1 Metastatic breast cancer; Endometrial cancer; Lymphoma [548760]
LY294002 Drug Info Terminated Cancer [541270], [546293]
PX-867 Drug Info Terminated Cardiovascular disorder [548762]
SCR-44001 Drug Info Terminated Cancer [548121]
Wortmannin Drug Info Terminated Hematologic malignancies [541309], [546241]
Inhibitor 2-(4-Morpholinyl)-8-Phenyl-4h-1-Benzopyran-4-One Drug Info [551393]
3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol Drug Info [528931]
5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE Drug Info [551374]
AEZS-126 Drug Info [543561]
AS-604850 Drug Info [527706]
BAG956 Drug Info [537458]
Buparlisib Drug Info [537633]
CH-5132799 Drug Info [531469]
CHU Drug Info [543562]
CLR-1401 Drug Info [543561]
CLR-1404 Drug Info [543561]
CU-906 Drug Info [543561]
CZC 24832 Drug Info [531889]
CZC-19091 Drug Info [543562]
Dual PI3K/mTOR inhibitors Drug Info [543561]
GDC-0084 Drug Info [544240]
GDC0941 Drug Info [537458], [537633]
GSK1059615 Drug Info [537633]
Her2- and PSA-targeted TGX-D1 Drug Info [531442]
HM-5016699 Drug Info [543561]
HS-173 Drug Info [531383]
KU-0060648 Drug Info [532428]
LOR-220 Drug Info [543561]
LY-292223 Drug Info [526022]
LY-293646 Drug Info [526022]
LY294002 Drug Info [550797]
Multiform PI3K inhibitors Drug Info [543561]
Myricetin Drug Info [551393]
P-6915 Drug Info [543561]
P-7170 Drug Info [543561]
PF-03772304 Drug Info [532819]
PF-4989216 Drug Info [543561]
PI-103 Drug Info [537458]
PI-3065 Drug Info [532839]
PIK-75 Drug Info [528931]
PKI-402 Drug Info [530561]
PP121 Drug Info [529744]
PQR309 Drug Info [543561]
PX-866 Drug Info [537633]
SAR245408 + MSC1936369B Drug Info [543562]
SAR245409 Drug Info [551615]
SAR245409/MSC1936369B combination therapy Drug Info [543562]
SCR-44001 Drug Info [531187]
TG100-115 Drug Info [536301], [536380], [536962]
TGX-221 Drug Info [527515]
VE-822 Drug Info [532144]
Wortmannin Drug Info [535473], [535536], [537458]
WX-037 Drug Info [543561]
Modulator Adyvia Drug Info
BAY 80-6946 Drug Info
BEZ235 Drug Info
BGT226 Drug Info [531639]
CLR457 Drug Info [1572591]
CUDC-907 Drug Info
DS-7423 Drug Info [532664]
GDC-0980 Drug Info [531658]
GSK2126458 Drug Info
IPI-145 Drug Info [532543]
PA-799 Drug Info
Perifosine Drug Info
PF-04691502 Drug Info
PF-05212384 Drug Info [533132]
PX-867 Drug Info [532491]
Rigosertib Drug Info [532659]
SF1126 Drug Info
VS-5584 Drug Info [532167]
XL147 Drug Info
ZSTK474 Drug Info [532539]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Inositol phosphate metabolism
ErbB signaling pathway
Ras signaling pathway
Rap1 signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
HIF-1 signaling pathway
FoxO signaling pathway
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK signaling pathway
Apoptosis
Adrenergic signaling in cardiomyocytes
VEGF signaling pathway
Osteoclast differentiation
Focal adhesion
Signaling pathways regulating pluripotency of stem cells
Platelet activation
Toll-like receptor signaling pathway
Jak-STAT signaling pathway
Natural killer cell mediated cytotoxicity
T cell receptor signaling pathway
B cell receptor signaling pathway
Fc epsilon RI signaling pathway
Fc gamma R-mediated phagocytosis
TNF signaling pathway
Leukocyte transendothelial migration
Neurotrophin signaling pathway
Cholinergic synapse
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Regulation of lipolysis in adipocytes
Type II diabetes mellitus
Non-alcoholic fatty liver disease (NAFLD)
Aldosterone-regulated sodium reabsorption
Carbohydrate digestion and absorption
Bacterial invasion of epithelial cells
Chagas disease (American trypanosomiasis)
Toxoplasmosis
Amoebiasis
Hepatitis C
Hepatitis B
Measles
Influenza A
HTLV-I infection
Epstein-Barr virus infection
Pathways in cancer
Viral carcinogenesis
Proteoglycans in cancer
MicroRNAs in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Melanoma
Chronic myeloid leukemia
Acute myeloid leukemia
Small cell lung cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
Choline metabolism in cancer
PathWhiz Pathway Inositol Metabolism
Phosphatidylinositol Phosphate Metabolism
Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Fc Epsilon Receptor I Signaling in Mast Cells
Reactome PI3K Cascade
GPVI-mediated activation cascade
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
PI3K events in ERBB4 signaling
PIP3 activates AKT signaling
GAB1 signalosome
PI3K events in ERBB2 signaling
PI3K/AKT activation
Role of phospholipids in phagocytosis
Tie2 Signaling
Constitutive Signaling by Aberrant PI3K in Cancer
DAP12 signaling
Role of LAT2/NTAL/LAB on calcium mobilization
Nephrin interactions
Costimulation by the CD28 family
CD28 dependent PI3K/Akt signaling
gamma signalling through PI3Kgamma
G alpha (q) signalling events
G alpha (12/13) signalling events
VEGFA-VEGFR2 Pathway
Interleukin-3, 5 and GM-CSF signaling
Constitutive Signaling by EGFRvIII
FGFR1
FGFR2
FGFR3
FGFR4
Interleukin receptor SHC signaling
Regulation of signaling by CBL
WikiPathways Toll-like receptor signaling pathway
Serotonin HTR1 Group and FOS Pathway
DNA Damage Response (only ATM dependent)
G13 Signaling Pathway
Regulation of Actin Cytoskeleton
Insulin Signaling
IL-4 Signaling Pathway
Copper homeostasis
Signaling of Hepatocyte Growth Factor Receptor
Transcriptional activation by NRF2
IL1 and megakaryotyces in obesity
Signaling by ERBB4
Signaling by ERBB2
Fc epsilon receptor (FCERI) signaling
PI Metabolism
Interleukin-2 signaling
Fcgamma receptor (FCGR) dependent phagocytosis
Signaling by SCF-KIT
DAP12 interactions
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
Gastrin-CREB signalling pathway via PKC and MAPK
PIP3 activates AKT signaling
Integrated Pancreatic Cancer Pathway
Prostate Cancer
Signaling Pathways in Glioblastoma
TSLP Signaling Pathway
Regulation of Microtubule Cytoskeleton
TSH signaling pathway
SREBP signalling
TCR signaling
Signaling by PDGF
Signaling by Insulin receptor
Signaling by FGFR
Signaling by EGFR
NGF signalling via TRKA from the plasma membrane
Nephrin interactions
Interleukin-3, 5 and GM-CSF signaling
GPVI-mediated activation cascade
GPCR downstream signaling
Costimulation by the CD28 family
Cell surface interactions at the vascular wall
MicroRNAs in cardiomyocyte hypertrophy
Angiogenesis
Regulation of toll-like receptor signaling pathway
AMPK Signaling
References
Ref 521489ClinicalTrials.gov (NCT00019656) Perifosine in Treating Patients With Refractory Solid Tumors or Hematologic Cancer. U.S. National Institutes of Health.
Ref 523422ClinicalTrials.gov (NCT01331083) A Phase II Study of PX-866 in Patients With Recurrent or Metastatic Castration Resistant Prostate Cancer. U.S. National Institutes of Health.
Ref 523487ClinicalTrials.gov (NCT01357330) Oral SAR245408 (XL147) and Oral MSC1936369B in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.
Ref 523615ClinicalTrials.gov (NCT01430585) Pre-Operative Study of PF-4691502 With Letrozole Compared To Letrozole Alone In Patients With Early Breast Cancer. U.S. National Institutes of Health.
Ref 523773ClinicalTrials.gov (NCT01516905) PET/CT Imaging of Malignant Brain Tumors With a Novel Radioiodinated Phospholipid Ether Analogue 124I-NM404. U.S. National Institutes of Health.
Ref 523929ClinicalTrials.gov (NCT01610284) Phase III Study of BKM120/Placebo With Fulvestrant in Postmenopausal Patients With Hormone Receptor Positive HER2-negative Locally Advanced or Metastatic Breast Cancer Refractory to Aromatase Inhibitor. U.S. National Institutes of Health.
Ref 524177ClinicalTrials.gov (NCT01762410) Clinical Study of Oral PI3K/mTOR Inhibitor in Patients With Advanced Refractory Solid Tumors. U.S. National Institutes of Health.
Ref 524202ClinicalTrials.gov (NCT01778088) Open-Label Study of I-131-CLR1404 in Subjects With Recurrent Glioma. U.S. National Institutes of Health.
Ref 524422ClinicalTrials.gov (NCT01936363) Trial of Pimasertib With SAR245409 or Placebo in Ovarian Cancer. U.S. National Institutes of Health.
Ref 524832ClinicalTrials.gov (NCT02189174) Study of CLR457 Administered Orally in Adult Patients With Advanced Solid Malignancies. U.S. National Institutes of Health.
Ref 531469The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
Ref 531639Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8.
Ref 532167VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61.
Ref 532539Combination of the PI3K inhibitor ZSTK474 with a PSMA-targeted immunotoxin accelerates apoptosis and regression of prostate cancer. Neoplasia. 2013 Oct;15(10):1172-83.
Ref 532543PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
Ref 532659Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
Ref 533074Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma. Mol Cancer Ther. 2015 Feb;14(2):429-39.
Ref 533087Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma. Gynecol Oncol. 2015 Feb;136(2):246-53.
Ref 533132First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95.
Ref 536497Pharmacologic therapeutics for cardiac reperfusion injury. Expert Opin Emerg Drugs. 2007 Sep;12(3):367-88.
Ref 541027(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: 5682).
Ref 541054(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: 5715).
Ref 541270(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: 6004).
Ref 541309(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: 6060).
Ref 542448(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: 7424).
Ref 542708(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: 7743).
Ref 542746(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: 7795).
Ref 542777(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: 7833).
Ref 542801(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: 7875).
Ref 542804(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: 7878).
Ref 542851(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: 7936).
Ref 542855(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: 7940).
Ref 542856(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: 7941).
Ref 542866(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: 7950).
Ref 542867(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: 7951).
Ref 542879(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: 7963).
Ref 542881(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: 7965).
Ref 543098(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: 8382).
Ref 543099(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: 8383).
Ref 546241Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007058)
Ref 546293Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007287)
Ref 547734Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018893)
Ref 548121Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022134)
Ref 548503Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026065)
Ref 548508Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026094)
Ref 548661Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027517)
Ref 548663Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027532)
Ref 548760Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028447)
Ref 548762Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028453)
Ref 549051Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031792)
Ref 549160Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033063)
Ref 549261Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034336)
Ref 549369Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035804)
Ref 550573Clinical pipeline report, company report or official report of Curis.
Ref 550796Clinical pipeline report, company report or official report of Genentech (2011).
Ref
Ref 526022Bioorg Med Chem Lett. 2001 Apr 9;11(7):909-13.LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.
Ref 527515PI 3-kinase p110beta: a new target for antithrombotic therapy. Nat Med. 2005 May;11(5):507-14. Epub 2005 Apr 17.
Ref 527706Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28.
Ref 528931Bioorg Med Chem. 2007 Sep 1;15(17):5837-44. Epub 2007 Jun 6.Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.
Ref 529744Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
Ref 530561J Med Chem. 2010 Jan 28;53(2):798-810.Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
Ref 531187Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice. PLoS One. 2010 Sep 24;5(9):e12965.
Ref 531383Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. J Med Chem. 2011 Apr 14;54(7):2455-66.
Ref 531442Development of a peptide-drug conjugate for prostate cancer therapy. Mol Pharm. 2011 Jun 6;8(3):901-12.
Ref 531469The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
Ref 531639Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8.
Ref 531658GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36.
Ref 531889A selective inhibitor reveals PI3Kgamma dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82.
Ref 532144Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis. 2012 Dec 6;3:e441.
Ref 532167VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61.
Ref 5324281-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
Ref 532491Pharmacologic profiling of phosphoinositide 3-kinase inhibitors as mitigators of ionizing radiation-induced cell death. J Pharmacol Exp Ther. 2013 Dec;347(3):669-80.
Ref 532539Combination of the PI3K inhibitor ZSTK474 with a PSMA-targeted immunotoxin accelerates apoptosis and regression of prostate cancer. Neoplasia. 2013 Oct;15(10):1172-83.
Ref 532543PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
Ref 532659Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
Ref 532664Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.
Ref 532819Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7.
Ref 532839Inactivation of PI(3)K p110delta breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;510(7505):407-11.
Ref 533132First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95.
Ref 535473Estrogen regulation of c-fos gene expression through phosphatidylinositol-3-kinase-dependent activation of serum response factor in MCF-7 breast cancer cells. Biochem Biophys Res Commun. 2002 Jun 7;294(2):384-94.
Ref 535536Phosphatidylinositol 3-kinase/Akt signaling in the response of vascular endothelium to ionizing radiation. Cancer Res. 2002 Aug 15;62(16):4671-7.
Ref 536301PI3Kgamma inhibition: towards an 'aspirin of the 21st century'? Nat Rev Drug Discov. 2006 Nov;5(11):903-18. Epub 2006 Oct 13.
Ref 536380Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans. 2007 Apr;35(Pt 2):204-6.
Ref 536962Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. Epub 2008 Dec 4.
Ref 537458The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9.
Ref 537633Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
Ref 543561(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: 2155).
Ref 543562(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: 2156).
Ref 544240Current clinical development of PI3K pathway inhibitors in glioblastoma. Neuro Oncol. 2012 July; 14(7): 819-829.
Ref 550797Clinical pipeline report, company report or official report of Genentech (2009).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551615Clinical pipeline report, company report or official report of Sanofi Oncology.
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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