Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0WB6S)
Name
Multidrug resistance protein 2 (ABCC2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
ATP-binding cassette sub-family C member 2; ATP-binding cassette, sub-family C, member 2; CMOAT; CMOAT1; CMRP; Canalicular multidrug resistance protein; Canalicular multispecific organic anion transporter 1; MRP2; Multidrug resistance-associated protein 2
Family Primary active transporter (PAT)  >>  ATP-binding cassette transporter (ABC)
Organism
Homo sapiens (Human)
Gene Name ABCC2 Gene ID
1244
UniProt ID MRP2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T61792 (click to find more therapeutic target data of this DBT)
VARIDT ID DTD0002 (click to find more drug transporter data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MLEKFCNSTFWNSSFLDSPEADLPLCFEQTVLVWIPLGYLWLLAPWQLLHVYKSRTKRSS
TTKLYLAKQVFVGFLLILAAIELALVLTEDSGQATVPAVRYTNPSLYLGTWLLVLLIQYS
RQWCVQKNSWFLSLFWILSILCGTFQFQTLIRTLLQGDNSNLAYSCLFFISYGFQILILI
FSAFSENNESSNNPSSIASFLSSITYSWYDSIILKGYKRPLTLEDVWEVDEEMKTKTLVS
KFETHMKRELQKARRALQRRQEKSSQQNSGARLPGLNKNQSQSQDALVLEDVEKKKKKSG
TKKDVPKSWLMKALFKTFYMVLLKSFLLKLVNDIFTFVSPQLLKLLISFASDRDTYLWIG
YLCAILLFTAALIQSFCLQCYFQLCFKLGVKVRTAIMASVYKKALTLSNLARKEYTVGET
VNLMSVDAQKLMDVTNFMHMLWSSVLQIVLSIFFLWRELGPSVLAGVGVMVLVIPINAIL
STKSKTIQVKNMKNKDKRLKIMNEILSGIKILKYFAWEPSFRDQVQNLRKKELKNLLAFS
QLQCVVIFVFQLTPVLVSVVTFSVYVLVDSNNILDAQKAFTSITLFNILRFPLSMLPMMI
SSMLQASVSTERLEKYLGGDDLDTSAIRHDCNFDKAMQFSEASFTWEHDSEATVRDVNLD
IMAGQLVAVIGPVGSGKSSLISAMLGEMENVHGHITIKGTTAYVPQQSWIQNGTIKDNIL
FGTEFNEKRYQQVLEACALLPDLEMLPGGDLAEIGEKGINLSGGQKQRISLARATYQNLD
IYLLDDPLSAVDAHVGKHIFNKVLGPNGLLKGKTRLLVTHSMHFLPQVDEIVVLGNGTIV
EKGSYSALLAKKGEFAKNLKTFLRHTGPEEEATVHDGSEEEDDDYGLISSVEEIPEDAAS
ITMRRENSFRRTLSRSSRSNGRHLKSLRNSLKTRNVNSLKEDEELVKGQKLIKKEFIETG
KVKFSIYLEYLQAIGLFSIFFIILAFVMNSVAFIGSNLWLSAWTSDSKIFNSTDYPASQR
DMRVGVYGALGLAQGIFVFIAHFWSAFGFVHASNILHKQLLNNILRAPMRFFDTTPTGRI
VNRFAGDISTVDDTLPQSLRSWITCFLGIISTLVMICMATPVFTIIVIPLGIIYVSVQMF
YVSTSRQLRRLDSVTRSPIYSHFSETVSGLPVIRAFEHQQRFLKHNEVRIDTNQKCVFSW
ITSNRWLAIRLELVGNLTVFFSALMMVIYRDTLSGDTVGFVLSNALNITQTLNWLVRMTS
EIETNIVAVERITEYTKVENEAPWVTDKRPPPDWPSKGKIQFNNYQVRYRPELDLVLRGI
TCDIGSMEKIGVVGRTGAGKSSLTNCLFRILEAAGGQIIIDGVDIASIGLHDLREKLTII
PQDPILFSGSLRMNLDPFNNYSDEEIWKALELAHLKSFVASLQLGLSHEVTEAGGNLSIG
QRQLLCLGRALLRKSKILVLDEATAAVDLETDNLIQTTIQNEFAHCTVITIAHRLHTIMD
SDKVMVLDNGKIIECGSPEELLQIPGPFYFMAKEAGIENVNSTKF
Function
May function as a cellular cisplatin transporter. Mediates hepatobiliary excretion of numerous organic anions.
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 for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 62 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_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 for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 76 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Antipyrine 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 IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Benzocaine 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
Lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Bronopol 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Caffeine 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 IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Diatrizoic acid 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 IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Undecylenic acid 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 133000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Poloxamer 188 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 Inhibition ratio = 53 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 55 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_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 (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 72 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 73 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_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 = 67 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 73 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_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 Inhibition ratio = 51 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 73 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Alpha-monopalmitin 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 = 45 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_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 (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 46 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 64 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
          DIG Name: Transcutol 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
Solubilizing agent; Solvent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio = 50 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 55 % (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID MRP2_HUMAN
References
1 Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
2 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov; 136(1):216-41.
3 Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients. J Pharm Pharm Sci. 2014;17(4):447-60.
4 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.

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