Synthetic non-peptide inhibitors of HIV protease.
We have studied the inhibition of HIV protease by the antifungal antibiotic cerulenin, as well as by several related synthetic, structurally simpler analogs. The effect of these compounds on HIV protease was conveniently studied by monitoring the cleavage of an authentic single peptide bond in a synthetic nonapeptide corresponding to a natural cleavage site in HIV-1 gag precursor polyprotein. The relative inhibitory effects of these compounds have afforded an insight into the structural characteristics which impart antiprotease activity.
Blumenstein
J J
JJ
Laboratory of Chemical and Physical Carcinogenesis, NCI-Frederick Cancer Research Facility MD 21701.
Copeland
T D
TD
Oroszlan
S
S
Michejda
C J
CJ
D000935:Antifungal Agents / Q000494:pharmacology*; D002569:Cerulenin / Q000494:pharmacology*; D010450:Endopeptidases / Q000378:metabolism; D016333:HIV Protease; D006868:Hydrolysis; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D011480:Protease Inhibitors; D002569:Cerulenin; D010450:Endopeptidases; D016333:HIV Protease