Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0SO0T)
Name
Multidrug resistance protein 1 (ABCB1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
ATP-binding cassette sub-family B member 1; CD243; CD243 antigen; MDR1; Multidrug resistance protein 1; P-glycoprotein 1; PGY1; Phospholipid transporter ABCB1
Family Primary active transporter (PAT)  >>  ATP-binding cassette transporter (ABC)
Organism
Homo sapiens (Human)
Gene Name ABCB1 Gene ID
5243
UniProt ID MDR1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T25258 (click to find more therapeutic target data of this DBT)
VARIDT ID DTD0003 (click to find more drug transporter data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAII
HGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSG
IGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVS
KINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFT
DKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIG
AAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARG
AAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSG
QTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLF
ATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIA
IARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAG
FDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRS
SLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAII
NGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKA
GEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNI
ANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEA
IENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFG
AYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDS
YSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVV
QLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVV
SQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLD
EATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQL
LAQKGIYFSMVSVQAGTKRQ
Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glyceryl monooleate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Bioadhesive material; Emollient; Emulsifying agent; Emulsion stabilizing agent; Gelling agent; Modified-release agent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation = 39.1 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 39 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 63 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Glyceryl monostearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emollient; Emulsifying agent; Emulsion stabilizing agent; Solubilizing agent; Surfactant; Viscosity-controlling agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation = 52.3 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 46 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 47 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyethylene glycol 2000 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 40 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyethylene glycol 20000 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 72 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyethylene glycol 300 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 54 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 90 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 94 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyethylene glycol 3350 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation (tested by experiment) [5]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN
          DIG Name: Polyethylene glycol 400 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 28 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 64 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyoxyl 35 castor oil Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 5 mg.mL-1 (tested by experiment) [6]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 61 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 100 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polyoxyl 40 stearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 72.1 % (tested by experiment) [8]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polysorbate 20 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.25 mg.mL-1 (tested by experiment) [6]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 240 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Polysorbate 80 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.31 mg.mL-1 (tested by experiment) [6]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 60 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 250 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Propylene glycol monostearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emollient; Emulsifying agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 25 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Sorbitan monolaurate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emulsifying agent; Solubilizing agent; Surfactant; Suspending agent; Vaccine adjuvant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 70 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Tocophersolan Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant; Binding agent; Emulsifying agent; Ointment base; Solubilizing agent; Surfactant; Suspending agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 50 % (tested by experiment) [9]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 200 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Laureth-23 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emulsifying agent; Gelling agent; Penetration agent; Solubilizing agent; Surfactant; Viscosity-controlling agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 72 % (tested by experiment) [10]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 81.7 % (tested by experiment) [10]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 89.7 % (tested by experiment) [10]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Laureth-4 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emulsifying agent; Gelling agent; Penetration agent; Solubilizing agent; Surfactant; Viscosity-controlling agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 230 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Propylene glycol monolaurate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emollient; Emulsifying agent; Oleaginous vehicle; Penetration agent; Solubilizing agent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 55 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 45 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Cremophor RH Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Other agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 70 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Pluronic F123 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 85 % (tested by experiment) [11]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Pluronic P85 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 150 % (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
          DIG Name: Pregelatinized starch Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Binding agent; Diluent; Disintegrant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation (tested by experiment) [5]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN
          DIG Name: Propylene glycol monooleate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emollient; Emulsifying agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 45 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
References
1 Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.
2 Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm. 2006 Apr 26;313(1-2):49-56.
3 The effect of polyoxyethylene polymers on the transport of ranitidine in Caco-2 cell monolayers. Int J Pharm. 2011 May 16;409(1-2):164-8.
4 A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci. 2002 Sep;91(9):1991-2002.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 Reversal of multidrug resistance by surfactants. Br J Cancer. 1992 Jul;66(1):62-8.
7 Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
8 Effects of polyoxyethylene (40) stearate on the activity of P-glycoprotein and cytochrome P450. Eur J Pharm Sci. 2009 Jul 12;37(5):573-80.
9 Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res. 1999 Dec;16(12):1812-7.
10 Intestinal transport of bis(12)-hupyridone in Caco-2 cells and its improved permeability by the surfactant Brij-35. Biopharm Drug Dispos. 2011 Apr;32(3):140-50.
11 Effect of pluronic P123 and F127 block copolymer on P-glycoprotein transport and CYP3A metabolism. Arch Pharm Res. 2011 Oct;34(10):1719-28.

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