Resistance mutation info of drug

Drug General Information
Drug ID D0B7EB
Drug Name Etoposide Drug Info
Synonyms Eposide; Eposin; Etopol; Etoposido; Etoposidum; Etosid; Lastet; Toposar; VePesid; Vepeside; Zuyeyidal; Demethyl EpipodophyllotoxinEthylidine Glucoside; Vepesid J; E0675; NK 171; VP 16; VP 16213; Demethyl-epiodophyllotoxin ethylidene glucoside; Epipodophyllotoxin VP-16213; Eposin (TN); Etopophos (TN); Etopophos (phosphate salt);Etoposide (VP16); Etoposido [INN-Spanish]; Etoposidum [INN-Latin]; Trans-Etoposide; VP 16 (pharmaceutical); VP 16-213; VP-16; VePESID (TN); Vepesid (TN); DEMETHY-EPIPODOPHYLLOTOXIN, ETHYLIDENE GLUCOSIDE; VP-16 (TN); VP-16-213; Demethylepipodophyllotoxin-beta-D-ethylideneglucoside; Etoposide (JP15/USP/INN); Etoposide [USAN:INN:BAN:JAN]; Eposin, Vepesid, VP-16, Toposar, Etoposide; Epipodophyllotoxin, 4'-demethyl-, 4,6-O-ethylidene-beta-D-glucopyranoside; Epipodophyllotoxin, 4'-demethyl-, 4,6-O-ethylidene-beta-D-glucopyranoside (8CI); Epipodophyllotoxin, 4'-demethyl-, 4,6-O-ethylidene-.beta.-D-glucopyranoside; Epipodophyllotoxin, 4'-demethyl-, 9-(4,6-O-ethylidene-beta-D-glucopyranoside); Epipodophyllotoxin, 4'-demethyl-, 9-(4,6-O-ethylidene-.beta.-D-glucopyranoside); (-)-Etoposide; 4'-Demethyl-epipodophyllotoxin 9-[4,6-O-(R)-ethylidene-beta-D-glucopyranoside; 4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylidene-beta-D-glucopyranoside); 4'-Demethylepipodophyllotoxin 9-(4,6-O-ethylidene-beta-D-glucopyranoside); 4'-Demethylepipodophyllotoxin ethylidene-.beta.-D-glucoside; 4'-O-Demethyl-1-O-(4,6-O-ethylidene-beta-D-glucopyranosyl)epipodophyllotoxin; 4-Demethylepipodophyllotoxin beta-D-ethylideneglucoside; 4-Demethylepipodophyllotoxin-.beta.-D-ethylideneglucoside
Drug Type Small molecular drug
Therapeutic Class Anticancer Agents
Company Bristol Myers Squibb Co Pharmaceutical Research Institute
Structure D0B7EB
Drug Resistance Mutations
Target Name ATP-binding cassette sub-family G member 2 (ABCG2) Target Info
Gene Name ABCG2
Uniprot ID ABCG2_HUMAN
Species Homo sapiens
Reference Sequence MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS [Hom
o sapiens]
Targeted Disease Cancer
Drug Resistance Mutations
Mutation info Missense: R482* [1559283]
References
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 541897(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6815).
Ref 1559283Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein.

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