Drug General Information
Drug ID D0SV8E
Drug Name Methotrexate
Synonyms methotrexate; 1959/5/2; Rheumatrex; Amethopterin; Metatrexan; Hdmtx; Abitrexate; Mexate; Methylaminopterinum; Methotrexatum; Antifolan; Metotrexato; Methylaminopterin; MTX; (S)-2-(4-(((2,4-Diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioic acid; Methotrexat; Amethopterine; Maxtrex; Rasuvo; L-Amethopterin; A-Methopterin; A-Methpterin; Amethopterin L-; Folex-Pfs; Methotrexat-Ebewe; N-Bismethylpteroylglutamic acid; Methotrexate, L-; Metotressato [DCIT]; Methotextrate; Mexate-Aq; [3H]methotrexate
Drug Type Small molecular drug
Structure D0SV8E
Drug Resistance Mutations
Target Name Folate transporter 1 (SLC19A1) Target Info
Gene Name SLC19A1
Uniprot ID S19A1_HUMAN
Species Homo sapiens
Reference Sequence MVPSSPAVEKQVPVEPGPDPELRSWRHLVCYLCFYGFMAQIRPGESFITPYLLGPDKNFT
REQVTNEITPVLSYSYLAVLVPVFLLTDYLRYTPVLLLQGLSFVSVWLLLLLGHSVAHMQ
LMELFYSVTMAARIAYSSYIFSLVRPARYQRVAGYSRAAVLLGVFTSSVLGQLLVTVGRV
SFSTLNYISLAFLTFSVVLALFLKRPKRSLFFNRDDRGRCETSASELERMNPGPGGKLGH
ALRVACGDSVLARMLRELGDSLRRPQLRLWSLWWVFNSAGYYLVVYYVHILWNEVDPTTN
SARVYNGAADAASTLLGAITSFAAGFVKIRWARWSKLLIAGVTATQAGLVFLLAHTRHPS
SIWLCYAAFVLFRGSYQFLVPIATFQIASSLSKELCALVFGVNTFFATIVKTIITFIVSD
VRGLGLPVRKQFQLYSVYFLILSIIYFLGAMLDGLRHCQRGHHPRQPPAQGLRSAAEEKA
AQALSVQDKGLGGLQPAQSPPLSPEDSLGAVGPASLEQRQSDPYLAQAPAPQAAEFLSPV
TTPSPCTLCSAQASGPEAADETCPQLAVHPPGVSKLGLQCLPSDGVQNVNQ [Homo sa
piens]
Targeted Disease Leukemia
Drug Resistance Mutations
Mutation info Missense: S309F [1]
Level of Resistance Confer 35 fold resistance
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 Leukemia
Drug Resistance Mutations
Mutation info Missense: R482G [2]
References
REF 1 Discrimination among reduced folates and methotrexate as transport substrates by a phenylalanine substitution for serine within the predicted eight... Biochem Pharmacol. 1999 Nov 15;58(10):1615-24.
REF 2 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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