Target General Information
Target ID T56556
Target Name ATP-binding cassette sub-family G member 2 (ABCG2)
Gene Name ABCG2
Species Homo sapiens
UniProt ID ABCG2_HUMAN
Sequence MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS [Hom
o sapiens]
Drug and Corresponding Resistance Mutations
Mutation Info Missense: R482*
Drugs
Drug Name Teniposide Drug Info [3]
Targeted Disease Cancer
Drug Name Etoposide Drug Info [3]
Targeted Disease Cancer
Mutation Info Missense: R482G
Drugs
Drug Name Mitoxantrone Drug Info [4]
Targeted Disease Breast Cancer
Drug Name Methotrexate Drug Info [5]
Targeted Disease Leukemia; Cancer
Mutation Info Missense: R482M
Drugs
Drug Name Zidovudine Drug Info [2]
Targeted Disease HIV infection
Mutation Info Missense: R482T
Drugs
Drug Name Anthracycline Drug Info [1]
Targeted Disease Cancer
Drug Name SN-38 Drug Info [1]
Targeted Disease Cancer
Drug Name Anthracycline Drug Info [1]
Targeted Disease T-lineage acute lymphoblastic leukaemia
Drug Name Topotecan Drug Info [1]
Targeted Disease Cancer
References
REF 1 Acquired mutations in the MXR/BCRP/ABCP gene alter substrate specificity in MXR/BCRP/ABCP-overexpressing cells. Cancer Res. 2001 Sep 15;61(18):6635-9.
REF 2 Induction of cellular resistance to nucleoside reverse transcriptase inhibitors by the wild-type breast cancer resistance protein. Biochem Pharmacol. 2004 Oct 1;68(7):1363-70.
REF 3 Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primar... Cancer Res. 2003 Mar 15;63(6):1339-44.
REF 4 Arginine482 to threonine mutation in the breast cancer resistance protein ABCG2 inhibits rhodamine 123 transport while increasing binding. Biochem J. 2004 Sep 1;382(Pt 2):711-6.
REF 5 Arginine-482 is not essential for transport of antibiotics, primary bile acids and unconjugated sterols by the human breast cancer resistance prote... Biochem J. 2005 Jan 15;385(Pt 2):419-26.

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