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Molecule Details

General Information of the Molecule
Name
Multidrug resistance protein 1 (ABCB1)
Synonyms
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
Gene Name
ABCB1
Gene ID
5243
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
Function
Translocates drugs and phospholipids across the membrane. Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins. Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
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Uniprot ID
MDR1_HUMAN
EC Number
EC: 7.6.2.2 ; EC: 7.6.2.1
TC Number
TC: 3.A.1.201.1
Pfam
PF00664 ; PF00005
KEGG ID
hsa5243
TTD ID
T25258
VARIDT ID
DTD0003
A List of Drug Combination(s) Able to Regulate This Molecule
          Activity Regulation     Click to Show/Hide the Drug Combination Regulating This Molecule
                 Down-regulation     Click to Show/Hide
                    Drug Combination 1 Down-regulating the Activity of This Molecule [1]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Aloe emodin   NP Info  + Doxorubicin   Drug Info 
                    Structure +
          Expression Regulation     Click to Show/Hide the Drug Combination Regulating This Molecule
                 Down-regulation     Click to Show/Hide
                    Drug Combination 1 Down-regulating the Expression of This Molecule [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Curcumin   NP Info  + 5-fluorouracil   Drug Info 
                    Structure +
                    Drug Combination 2 Down-regulating the Expression of This Molecule [3]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Quercetin   NP Info  + Cisplatin   Drug Info 
                    Structure +
                    Drug Combination 3 Down-regulating the Expression of This Molecule [4]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Ellagic acid   NP Info  + Bevacizumab   Drug Info 
                    Structure +
                    Drug Combination 4 Down-regulating the Expression of This Molecule [5]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Resveratrol   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 5 Down-regulating the Expression of This Molecule [6]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Schisandrol B   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 6 Down-regulating the Expression of This Molecule [7]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Hesperidin   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 7 Down-regulating the Expression of This Molecule [8]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Cinchonine + Hydrocinchonine + Quinidine
    Click to Show/Hide the Each NP or Drug Structure of This Combination
Cinchonine   NP Info     Drug Info 
   Drug Info 
                    Drug Combination 8 Down-regulating the Expression of This Molecule [9]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Schisandrin A   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 9 Down-regulating the Expression of This Molecule [10]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Neferine   NP Info  + Imatinib   Drug Info 
                    Structure +
                    Drug Combination 10 Down-regulating the Expression of This Molecule [11]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Gambogic acid   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 11 Down-regulating the Expression of This Molecule [12]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Epigallocatechin gallate   NP Info  + 5-fluorouracil   Drug Info 
                    Structure +
                    Drug Combination 12 Down-regulating the Expression of This Molecule [13]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Cinchonine   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 13 Down-regulating the Expression of This Molecule [14]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Ursolic acid   NP Info  + Oxaliplatin   Drug Info 
                    Structure +
                    Drug Combination 14 Down-regulating the Expression of This Molecule [15]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Thymoquinone   NP Info  + Imatinib   Drug Info 
                    Structure +
                    Drug Combination 15 Down-regulating the Expression of This Molecule [16]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Fisetin   NP Info  + Cabazitaxel   Drug Info 
                    Structure +
                    Drug Combination 16 Down-regulating the Expression of This Molecule [17]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Curcumin   NP Info  + Cytarabine   Drug Info 
                    Structure +
                    Drug Combination 17 Down-regulating the Expression of This Molecule [18]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Kaempferol   NP Info  + Sorafenib   Drug Info 
                    Structure +
                    Drug Combination 18 Down-regulating the Expression of This Molecule [19]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Thymoquinone   NP Info  + Cisplatin   Drug Info 
                    Structure +
                    Drug Combination 19 Down-regulating the Expression of This Molecule [20]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Roxithromycin   NP Info  + Cyclophosphamide   Drug Info 
                    Structure +
                    Drug Combination 20 Down-regulating the Expression of This Molecule [21]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Epigallocatechin gallate   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 21 Down-regulating the Expression of This Molecule [22]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Quercetin   NP Info  + Doxorubicin   Drug Info 
                    Structure +
                    Drug Combination 22 Down-regulating the Expression of This Molecule [23]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Cardamonin   NP Info  + 5-fluorouracil   Drug Info 
                    Structure +
                    Drug Combination 23 Down-regulating the Expression of This Molecule [24]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Pentagalloylglucose   NP Info  + 5-fluorouracil   Drug Info 
                    Structure +
                    Drug Combination 24 Down-regulating the Expression of This Molecule [25]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Beta asarone   NP Info  + Temozolomide   Drug Info 
                    Structure +
                 Up-regulation     Click to Show/Hide
                    Drug Combination 1 Up-regulating the Expression of This Molecule [26]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Name Arsenic trioxide   NP Info  + Etoposide   Drug Info 
                    Structure +
Natural Product(s) of This Target
1 Tangeretin  NP Info  Investigative Citrus reticulata
References
Reference 1 The effects and mechanisms of aloe-emodin on reversing adriamycin-induced resistance of MCF-7/ADR cells. Phytother Res. 2021 Jul;35(7):3886-3897.
Reference 2 Curcumin enhances cytotoxicity of chemotherapeutic agents in prostate cancer cells by inducing p21(WAF1/CIP1) and C/EBPbeta expressions and suppressing NF-kappaB activation. Prostate. 2002 May 15;51(3):211-8.
Reference 3 Effects of Quercetin on the Efficacy of Various Chemotherapeutic Drugs in Cervical Cancer Cells. Drug Des Devel Ther. 2021 Feb 15;15:577-588.
Reference 4 Ellagic Acid Enhances the Antitumor Efficacy of Bevacizumab in an In Vitro Glioblastoma Model. World Neurosurg. 2019 Dec;132:e59-e65.
Reference 5 Resveratrol enhances the cytotoxic profile of docetaxel and doxorubicin in solid tumour cell lines in vitro. Cell Prolif. 2011 Dec;44(6):591-601.
Reference 6 Enhanced antitumour efficacy of functionalized doxorubicin plus schisandrin B co-delivery liposomes via inhibiting epithelial-mesenchymal transition. J Liposome Res. 2021 Jun;31(2):113-129.
Reference 7 Hesperidin as a preventive resistance agent in MCF-7 breast cancer cells line resistance to doxorubicin. Asian Pac J Trop Biomed. 2014 Mar;4(3):228-33.
Reference 8 Hydrocinchonine, cinchonine, and quinidine potentiate paclitaxel-induced cytotoxicity and apoptosis via multidrug resistance reversal in MES-SA/DX5 uterine sarcoma cells. Environ Toxicol. 2011 Aug;26(4):424-31.
Reference 9 Schisandrin A reverses doxorubicin-resistant human breast cancer cell line by the inhibition of P65 and Stat3 phosphorylation. Breast Cancer. 2018 Mar;25(2):233-242.
Reference 10 Neferine increases STI571 chemosensitivity via inhibition of P-gp expression in STI571-resistant K562 cells. Leuk Lymphoma. 2011 Apr;52(4):694-700.
Reference 11 Suppression of NF-KappaB signaling and P-glycoprotein function by gambogic acid synergistically potentiates adriamycin -induced apoptosis in lung cancer. Curr Cancer Drug Targets. 2014;14(1):91-103.
Reference 12 Reversal of 5-fluorouracil resistance by EGCG is mediate by inactivation of TFAP2A/VEGF signaling pathway and down-regulation of MDR-1 and P-gp expression in gastric cancer. Oncotarget. 2017 Sep 6;8(47):82842-82853.
Reference 13 Apoptosis induced by doxorubicin and cinchonine in P388 multidrug-resistant cells. J Pharm Pharmacol. 2001 Jul;53(7):1029-39.
Reference 14 Ursolic acid synergistically enhances the therapeutic effects of oxaliplatin in colorectal cancer. Protein Cell. 2016 Aug;7(8):571-85.
Reference 15 Thymoquinone chemosensitizes human colorectal cancer cells to imatinib via uptake/efflux genes modulation. Clin Exp Pharmacol Physiol. 2021 Jun;48(6):911-920.
Reference 16 Fisetin Enhances Chemotherapeutic Effect of Cabazitaxel against Human Prostate Cancer Cells. Mol Cancer Ther. 2016 Dec;15(12):2863-2874.
Reference 17 Synergism of Curcumin and Cytarabine in the Down Regulation of Multi-Drug Resistance Genes in Acute Myeloid Leukemia. Anticancer Agents Med Chem. 2016;16(1):128-35.
Reference 18 Kaempferol-Mediated Sensitization Enhances Chemotherapeutic Efficacy of Sorafenib Against Hepatocellular Carcinoma: An In Silico and In Vitro Approach. Adv Pharm Bull. 2020 Jul;10(3):472-476.
Reference 19 Thymoquinone and cisplatin as a therapeutic combination in lung cancer: In vitro and in vivo. J Exp Clin Cancer Res. 2010 Jul 1;29(1):87.
Reference 20 Mechanisms of venoocclusive disease resulting from the combination of cyclophosphamide and roxithromycin. Ther Drug Monit. 2006 Dec;28(6):766-74.
Reference 21 In vivo reversal of doxorubicin resistance by (-)-epigallocatechin gallate in a solid human carcinoma xenograft. Cancer Lett. 2004 May 28;208(2):179-86.
Reference 22 Quercetin potentiates the effect of adriamycin in a multidrug-resistant MCF-7 human breast-cancer cell line: P-glycoprotein as a possible target. Cancer Chemother Pharmacol. 1994;34(6):459-64.
Reference 23 Cardamonin, a natural chalcone, reduces 5-fluorouracil resistance of gastric cancer cells through targeting Wnt/beta-catenin signal pathway. Invest New Drugs. 2020 Apr;38(2):329-339.
Reference 24 Inhibitory effects and molecular mechanisms of pentagalloyl glucose in combination with 5-FU on aggressive phenotypes of HepG2 cells. Nat Prod Res. 2021 Mar;35(5):815-818.
Reference 25 Beta-Asarone promotes Temozolomide's entry into glioma cells and decreases the expression of P-glycoprotein and MDR1. Biomed Pharmacother. 2017 Jun;90:368-374.
Reference 26 Arsenic trioxide potentiates the effectiveness of etoposide in Ewing sarcomas. Int J Oncol. 2016 Nov;49(5):2135-2146.
Reference 27 Tangeretin, a citrus pentamethoxyflavone, antagonizes ABCB1-mediated multidrug resistance by inhibiting its transport function. Pharmacol Res. 2016 Aug;110:193-204.
Cite NPCDR
Visitor Map
Correspondence

X. N. Sun, Y. T. Zhang, Y. Zhou, X. C. Lian, L. L. Yan, T. Pan, T. Jin, H. Xie, Z. M. Liang, W. Q. Qiu, J. X. Wang, Z. R. Li, F. Zhu*, X. B. Sui*. NPCDR: natural product-based drug combination and its disease-specific molecular regulation. Nucleic Acids Research. 50(D1): 1324-1333 (2020). PMID: 34664659

Prof. Feng ZHU  (zhufeng@zju.edu.cn)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China


Prof. Xinbing SUI  (hzzju@hznu.edu.cn)

School of Pharmacy and Department of Medical Oncology, the Affiliated Hospital of Hangzhou Normal University, Hangzhou Normal University, Hangzhou, China