Crucial amides for dimerization inhibitors of HIV-1 protease.
An inhibitor based on crosslinked peptides from the interfacial region of HIV-1 protease, previously shown to act by dimerization inhibition, was modified by N-methylation to ascertain the importance of the amide hydrogens on inhibition. The effects of N-methylation on HIV-1 protease inhibition, as well as the effects on degradation by proteases are described.
Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Michael J
MJ
Bowman
Jean
J
Chmielewski
D000577:Amides / Q000737:chemistry* / Q000378:metabolism*; D019281:Dimerization; D016333:HIV Protease / Q000378:metabolism*; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*
D000577:Amides; D017320:HIV Protease Inhibitors; D016333:HIV Protease