ABCG2 p.Gln126Thr
| ClinVar: |
c.376C>T
,
p.Gln126*
?
, association
|
| Predicted by SNAP2: | A: D (71%), C: D (66%), D: D (80%), E: D (75%), F: D (80%), G: D (80%), H: D (63%), I: D (75%), K: D (80%), L: D (80%), M: D (63%), N: D (75%), P: D (85%), R: D (85%), S: D (75%), T: D (75%), V: D (71%), W: D (85%), Y: D (75%), |
| Predicted by PROVEAN: | A: D, C: D, D: D, E: D, F: D, G: D, H: D, I: D, K: D, L: D, M: D, N: D, P: D, R: D, S: D, T: D, V: D, W: D, Y: D, |
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[hide] Drug transporters: recent advances concerning BCRP... Br J Cancer. 2008 Mar 11;98(5):857-62. Epub 2008 Feb 5. Lemos C, Jansen G, Peters GJ
Drug transporters: recent advances concerning BCRP and tyrosine kinase inhibitors.
Br J Cancer. 2008 Mar 11;98(5):857-62. Epub 2008 Feb 5., 2008-03-11 [PMID:18253130]
Abstract [show]
Multidrug resistance is often associated with the (over)expression of drug efflux transporters of the ATP-binding cassette (ABC) protein family. This minireview discusses the role of one selected ABC-transporter family member, the breast cancer resistance protein (BCRP/ABCG2), in the (pre)clinical efficacy of novel experimental anticancer drugs, in particular tyrosine kinase inhibitors.
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No. Sentence Comment
45 Breedveld et al (2005) showed that Table 1 BCRP substrates and polymorphisms Substrates Classical anticancer drugs Novel targeted drugs Mitoxantrone Canertinib (CI-1033)a Anthracyclinesb Imatiniba Camptothecins Nilotiniba Antifolatesb Gefitiniba Erlotinib Flavopiridol Polymorphismsc Variant Amino-acid change Effect G34A Val12Met (V12M) No change C376T Gln126stop (Q126T) No active BCRP protein C421A Gln141Lys (Q141K) Decreased protein levels and drug resistance Increased gefitinib-associated toxicity (diarrhoea) Increased imatinib accumulation in vitro, but no changes in the pharmacokinetic parameters of imatinib in vivo G1322A Ser441Asn (S441N) Decreased protein levels and different subcellular localisation BCRP ¼ breast cancer resistance protein.
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ABCG2 p.Gln126Thr 18253130:45:366
status: NEW115 Another SNP, the C376T, replaces glutamine by a stop codon at position 126 (Q126T), and was found in 3 out of the 124 Japanese population (Imai et al, 2002).
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ABCG2 p.Gln126Thr 18253130:115:76
status: NEW