Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase.
Crystal structure of HIV-RT in complex with a DNA template:primer and a dTTP leads us to design and synthesize a new class of nucleoside analog inhibitors containing a branched 3'-group against HIV-RT. An in vitro primer extension assay indicates that three out of five compounds are effective HIV-RT inhibitors.
Department of Biochemistry, School of Molecular and Cellular Biology, University of Illinois at Urbana-Champaign, 600 South Mathews Avenue, Urbana, IL 61801, USA.
Xianjun
X
Liu
Wei
W
Xie
Raven H
RH
Huang
D001483:Base Sequence; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D008969:Molecular Sequence Data; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase