HIV Mutation Detail Information

> C280A Search Result

Mutation Information

Mutation Site	C280A
Mutation Type	Amino acid level
Gene/Protein/Region Type	RT

Literature Information

PubMed PMID	33143469
Published Year	2020
Journal	Journal of enzyme inhibition and medicinal chemistry
Title	Scaffold hopping and optimisation of 3',4'-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H.
Author	Tocco G,Esposito F,Caboni P,Laus A,Beutler JA,Wilson JA,Corona A,Le Grice SFJ,Tramontano E
Evidence	In addition, by using a panel of drug-resistant and -sensitive recombinant enzymes we could identify several thienopyrimidinone derivatives which retained activity against drug-resistant variants and 2-(3,4-dihydroxyphenyl)-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one 1 emerged as the best compound (wt RT RNase H IC50 = 0.26 muM and C280A RT RNase H IC50 = 0.32 muM).

Contents
Description

Mutation Information Note

Gene/Protein/Region Type: Virus Gene (e.g. LMP-1) or Virus Protein (e.g. Rep 68) or Virus Region (e.g. S, X)

Literature Information Note

Evidence: sentence contains this mutation information in the citation