ABCMdb

PMID: 16178819

Breier A, Barancik M, Sulova Z, Uhrik B
P-glycoprotein--implications of metabolism of neoplastic cells and cancer therapy.
Curr Cancer Drug Targets. 2005 Sep;5(6):457-68., [PubMed]

Sentences

No. Mutations Sentence Comment

183 ABCB1 p.Val338Ala ABCB1 p.Gly341Val This is also supported by the results of a site directed mutagenesis study of the transmembrane domain 6 of P-gp [133]: (i) replacement of valine 338 by alanine resulted in a mutant P-gp with enhanced resistance to colchicine and reduced resistance to vinblastine; (ii) replacement of glycine 341 by valine resulted in mutant P-gp with reduced resistance to colchicine or doxorubicin, but remaining resistance to vinblastine or actinomycin D; (iii) replacement of alanine 342 by leucine resulted in mutant P-gp with reduced resistance to all four drugs; (iv) replacement of serine 344 by alanine, threonine, cysteine, or tyrosine resulted in mutant P-gp unable to confer drug resistance. Login to comment 185 ABCB1 p.Phe983Ala Several other authors described modulation of drug efflux capacity of mutant P-gp after site directed mutagenesis of an amino acid in the transmembrane domains, e.g. histidine 61 in domain 1 [134], single serines replacements by phenylalanines in transmembrane domain 11 [135], leucine 975, valine 981 and phenylalanine 983 by alanine in transmembrane domain 12 [136]. Login to comment