Target Information
| Target General Information | Top | |||||
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| Target ID |
T25258
(Former ID: TTDR00007)
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| Target Name |
Multidrug resistance protein 1 (ABCB1)
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| Synonyms |
PGY1; P-glycoprotein 1; P-gp; Pgp; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
Click to Show/Hide
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| Gene Name |
ABCB1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Lung cancer [ICD-11: 2C25] | |||||
| Function |
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Click to Show/Hide
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| BioChemical Class |
ABC transporter
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| UniProt ID | ||||||
| EC Number |
EC 7.6.2.2
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| Sequence |
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAII
HGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSG IGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVS KINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFT DKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIG AAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARG AAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSG QTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLF ATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIA IARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAG FDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRS SLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAII NGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKA GEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNI ANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEA IENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFG AYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDS YSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVV QLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVV SQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLD EATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQL LAQKGIYFSMVSVQAGTKRQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A02145 ; BADD_A04856 ; BADD_A06316 | |||||
| HIT2.0 ID | T50WOV | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | EDP-322 | Drug Info | Phase 1 | Bacterial infection | [2] | |
| 2 | W-198 | Drug Info | Phase 1 | Solid tumour/cancer | [3] | |
| Discontinued Drug(s) | [+] 8 Discontinued Drugs | + | ||||
| 1 | CBT-1 | Drug Info | Discontinued in Phase 3 | Non-small-cell lung cancer | [4] | |
| 2 | LY335979 | Drug Info | Discontinued in Phase 3 | Acute myeloid leukaemia | [5] | |
| 3 | Biricodar | Drug Info | Discontinued in Phase 2 | Ovarian cancer | [6] | |
| 4 | S-9788 | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [7] | |
| 5 | Tariquidar | Drug Info | Discontinued in Phase 2 | Adrenocortical carcinoma | [8] | |
| 6 | Elacridar | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [9] | |
| 7 | ONT-093 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [10] | |
| 8 | XR-9051 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [11] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 12 Inhibitor drugs | + | ||||
| 1 | EDP-322 | Drug Info | [12] | |||
| 2 | Elacridar | Drug Info | [19] | |||
| 3 | ONT-093 | Drug Info | [20] | |||
| 4 | XR-9051 | Drug Info | [21] | |||
| 5 | 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl | Drug Info | [22] | |||
| 6 | 6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol | Drug Info | [22] | |||
| 7 | TRISMETHOXYRESVERATROL | Drug Info | [22] | |||
| 8 | XR-9456 | Drug Info | [23] | |||
| 9 | XR-9504 | Drug Info | [23] | |||
| 10 | XR-9544 | Drug Info | [23] | |||
| 11 | XR-9577 | Drug Info | [23] | |||
| 12 | [1,1':2',1'']-terphenyl-4,3'',5''-triol | Drug Info | [22] | |||
| Modulator | [+] 6 Modulator drugs | + | ||||
| 1 | W-198 | Drug Info | [13] | |||
| 2 | CBT-1 | Drug Info | [14] | |||
| 3 | LY335979 | Drug Info | [15] | |||
| 4 | Biricodar | Drug Info | [6] | |||
| 5 | S-9788 | Drug Info | [16] | |||
| 6 | Tariquidar | Drug Info | [17], [18] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Vincristine | Ligand Info | |||||
| Structure Description | Nanodisc reconstituted human ABCB1 in complex with MRK16 Fab and vincristine | PDB:7A69 | ||||
| Method | Electron microscopy | Resolution | 3.20 Å | Mutation | Yes | [24] |
| PDB Sequence |
PTVSVFSMFR
41 YSNWLDKLYM51 VVGTLAAIIH61 GAGLPLMMLV71 FGEMTDIFAN81 AGNLFMNLEE 109 DMTRYAYYYS119 GIGAGVLVAA129 YIQVSFWCLA139 AGRQIHKIRK149 QFFHAIMRQE 159 IGWFDVHDVG169 ELNTRLTDDV179 SKINEGIGDK189 IGMFFQSMAT199 FFTGFIVGFT 209 RGWKLTLVIL219 AISPVLGLSA229 AVWAKILSSF239 TDKELLAYAK249 AGAVAEEVLA 259 AIRTVIAFGG269 QKKELERYNK279 NLEEAKRIGI289 KKAITANISI299 GAAFLLIYAS 309 YALAFWYGTT319 LVLSGEYSIG329 QVLTVFFSVL339 IGAFSVGQAS349 PSIEAFANAR 359 GAAYEIFKII369 DNKPSIDSYS379 KSGHKPDNIK389 GNLEFRNVHF399 SYPSRKEVKI 409 LKGLNLKVQS419 GQTVALVGNS429 GCGKSTTVQL439 MQRLYDPTEG449 MVSVDGQDIR 459 TINVRFLREI469 IGVVSQEPVL479 FATTIAENIR489 YGRENVTMDE499 IEKAVKEANA 509 YDFIMKLPHK519 FDTLVGERGA529 QLSGGQKQRI539 AIARALVRNP549 KILLLDEATS 559 ALDTESEAVV569 QVALDKARKG579 RTTIVIAHRL589 STVRNADVIA599 GFDDGVIVEK 609 GNHDELMKEK619 GIYFKLVTMQ629 TPVSFWRIMK702 LNLTEWPYFV712 VGVFCAIING 722 GLQPAFAIIF732 SKIIGVFTRI742 DDPETKRQNS752 NLFSLLFLAL762 GIISFITFFL 772 QGFTFGKAGE782 ILTKRLRYMV792 FRSMLRQDVS802 WFDDPKNTTG812 ALTTRLANDA 822 AQVKGAIGSR832 LAVITQNIAN842 LGTGIIISFI852 YGWQLTLLLL862 AIVPIIAIAG 872 VVEMKMLSGQ882 ALKDKKELEG892 AGKIATEAIE902 NFRTVVSLTQ912 EQKFEHMYAQ 922 SLQVPYRNSL932 RKAHIFGITF942 SFTQAMMYFS952 YAGCFRFGAY962 LVAHKLMSFE 972 DVLLVFSAVV982 FGAMAVGQVS992 SFAPDYAKAK1002 ISAAHIIMII1012 EKTPLIDSYS 1022 TEGLMPNTLE1032 GNVTFGEVVF1042 NYPTRPDIPV1052 LQGLSLEVKK1062 GQTLALVGSS 1072 GCGKSTVVQL1082 LERFYDPLAG1092 KVLLDGKEIK1102 RLNVQWLRAH1112 LGIVSQEPIL 1122 FDCSIAENIA1132 YGDNSRVVSQ1142 EEIVRAAKEA1152 NIHAFIESLP1162 NKYSTKVGDK 1172 GTQLSGGQKQ1182 RIAIARALVR1192 QPHILLLDEA1202 TSALDTESEK1212 VVQEALDKAR 1222 EGRTCIVIAH1232 RLSTIQNADL1242 IVVFQNGRVK1252 EHGTHQQLLA1262 QKGIYFSMVS 1272 VQAG
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LEU65
3.793
MET68
3.612
MET69
3.396
PHE303
4.293
ILE306
3.793
TYR310
3.320
PHE336
4.616
LEU339
3.662
ILE340
3.973
PHE343
3.401
SER344
3.315
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| Ligand Name: Taxol | Ligand Info | |||||
| Structure Description | Nanodisc reconstituted human ABCB1 in complex with UIC2 fab and taxol | PDB:6QEX | ||||
| Method | Electron microscopy | Resolution | 3.60 Å | Mutation | Yes | [25] |
| PDB Sequence |
PTVSVFSMFR
41 YSNWLDKLYM51 VVGTLAAIIH61 GAGLPLMMLV71 FGEMTDIFAN81 AGNLEDLMSN 91 ITNRSDINDT101 GFFMNLEEDM111 TRYAYYYSGI121 GAGVLVAAYI131 QVSFWCLAAG 141 RQIHKIRKQF151 FHAIMRQEIG161 WFDVHDVGEL171 NTRLTDDVSK181 INEGIGDKIG 191 MFFQSMATFF201 TGFIVGFTRG211 WKLTLVILAI221 SPVLGLSAAV231 WAKILSSFTD 241 KELLAYAKAG251 AVAEEVLAAI261 RTVIAFGGQK271 KELERYNKNL281 EEAKRIGIKK 291 AITANISIGA301 AFLLIYASYA311 LAFWYGTTLV321 LSGEYSIGQV331 LTVFFSVLIG 341 AFSVGQASPS351 IEAFANARGA361 AYEIFKIIDN371 KPSIDSYSKS381 GHKPDNIKGN 391 LEFRNVHFSY401 PSRKEVKILK411 GLNLKVQSGQ421 TVALVGNSGC431 GKSTTVQLMQ 441 RLYDPTEGMV451 SVDGQDIRTI461 NVRFLREIIG471 VVSQEPVLFA481 TTIAENIRYG 491 RENVTMDEIE501 KAVKEANAYD511 FIMKLPHKFD521 TLVGERGAQL531 SGGQKQRIAI 541 ARALVRNPKI551 LLLDEATSAL561 DTESEAVVQV571 ALDKARKGRT581 TIVIAHRLST 591 VRNADVIAGF601 DDGVIVEKGN611 HDELMKEKGI621 YFKLVTMQTP694 VSFWRIMKLN 704 LTEWPYFVVG714 VFCAIINGGL724 QPAFAIIFSK734 IIGVFTRIDD744 PETKRQNSNL 754 FSLLFLALGI764 ISFITFFLQG774 FTFGKAGEIL784 TKRLRYMVFR794 SMLRQDVSWF 804 DDPKNTTGAL814 TTRLANDAAQ824 VKGAIGSRLA834 VITQNIANLG844 TGIIISFIYG 854 WQLTLLLLAI864 VPIIAIAGVV874 EMKMLSGQAL884 KDKKELEGAG894 KIATEAIENF 904 RTVVSLTQEQ914 KFEHMYAQSL924 QVPYRNSLRK934 AHIFGITFSF944 TQAMMYFSYA 954 GCFRFGAYLV964 AHKLMSFEDV974 LLVFSAVVFG984 AMAVGQVSSF994 APDYAKAKIS 1004 AAHIIMIIEK1014 TPLIDSYSTE1024 GLMPNTLEGN1034 VTFGEVVFNY1044 PTRPDIPVLQ 1054 GLSLEVKKGQ1064 TLALVGSSGC1074 GKSTVVQLLE1084 RFYDPLAGKV1094 LLDGKEIKRL 1104 NVQWLRAHLG1114 IVSQEPILFD1124 CSIAENIAYG1134 DNSRVVSQEE1144 IVRAAKEANI 1154 HAFIESLPNK1164 YSTKVGDKGT1174 QLSGGQKQRI1184 AIARALVRQP1194 HILLLDEATS 1204 ALDTESEKVV1214 QEALDKAREG1224 RTCIVIAHRL1234 STIQNADLIV1244 VFQNGRVKEH 1254 GTHQQLLAQK1264 GIYFSMVSVQ1274 AG
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LEU65
4.516
MET68
4.100
MET69
3.545
TRP232
3.891
PHE303
4.008
ILE306
4.010
TYR307
3.152
TYR310
2.871
PHE336
3.122
LEU339
3.727
ILE340
3.341
PHE343
3.396
SER344
3.222
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| ABC transporters | hsa02010 | Affiliated Target |
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| Class: Environmental Information Processing => Membrane transport | Pathway Hierarchy | ||
| Bile secretion | hsa04976 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 1.89E-03 |
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| Closeness centrality | 2.30E-01 | Radiality | 1.40E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 1.42E+02 | Topological coefficient | 5.00E-01 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | ABC transporters | |||||
| 2 | Bile secretion | |||||
| 3 | MicroRNAs in cancer | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | IL2 Signaling Pathway | |||||
| 2 | TCR Signaling Pathway | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | HIF-1-alpha transcription factor network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | ABC-family proteins mediated transport | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | Nuclear Receptors in Lipid Metabolism and Toxicity | |||||
| 2 | Abacavir transport and metabolism | |||||
| 3 | Multi Drug Resistance Protein 1 (Glycoprotein 1) Regulation | |||||
| 4 | Integrated Pancreatic Cancer Pathway | |||||
| 5 | Allograft Rejection | |||||
| 6 | Drug Induction of Bile Acid Pathway | |||||
| 7 | Codeine and Morphine Metabolism | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Clin Cancer Res. 2004 Mar 1;10(5):1826-34. | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028928) | |||||
| REF 3 | Pharmacokinetics and safety of bromotetrandrine (BrTet,W198) after single-dose intravenous administration in healthy Chinese volunteers. Journal of Clinical Pharmacy and Therapeutics (2010) 35, 113-119. | |||||
| REF 4 | ClinicalTrials.gov (NCT00437749) A Study of CBT-1 and Paclitaxel With Carboplatin in Patients With Advanced Inoperable Non-small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005159) | |||||
| REF 6 | ClinicalTrials.gov (NCT00003847) VX-710, Doxorubicin, and Vincristine for the Treatment of Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002565) | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010214) | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002537) | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011621) | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007052) | |||||
| REF 12 | In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother. 2015 Jan;70(1):173-7. | |||||
| REF 13 | Mechanisms of tetrandrine and 5-bromotetrandrine in reversing multidrug resistance may relate to down-regulation of multidrug resistance associated protein 7 expression. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):558-63. | |||||
| REF 14 | A pharmacodynamic study of the P-glycoprotein antagonist CBT-1 in combination with paclitaxel in solid tumors. Oncologist.2012;17(4):512. | |||||
| REF 15 | A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxoru... Clin Cancer Res. 2004 May 15;10(10):3265-72. | |||||
| REF 16 | In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients. Cancer Chemother Pharmacol. 1995;36(3):195-203. | |||||
| REF 17 | Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).Biochem Pharmacol.2008 Mar 15;75(6):1302-12. | |||||
| REF 18 | The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).ACS Chem Neurosci.2011 Feb 16;2(2):82-9. | |||||
| REF 19 | 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J Med Chem. 2008 Dec 11;51(23):7602-13. | |||||
| REF 20 | A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. | |||||
| REF 21 | Communication between multiple drug binding sites on P-glycoprotein. Mol Pharmacol. 2000 Sep;58(3):624-32. | |||||
| REF 22 | Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8. | |||||
| REF 23 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. Bioorg Med Chem. 2008 Mar 1;16(5):2448-62. | |||||
| REF 24 | Cryo-EM structures reveal distinct mechanisms of inhibition of the human multidrug transporter ABCB1. Proc Natl Acad Sci U S A. 2020 Oct 20;117(42):26245-26253. | |||||
| REF 25 | Structural insight into substrate and inhibitor discrimination by human P-glycoprotein. Science. 2019 Feb 15;363(6428):753-756. | |||||
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