The Conformation of a Peptidyl Methyl Ketone Inhibitor Bound to the Human Cytomegalovirus Protease.

Angew Chem Int Ed Engl

Departments of Chemistry and Biological Sciences, Bio-Méga Research Division, Boehringer Ingelheim (Canada) Ltd., 2100 Cunard St., Laval, Québec, H7S 2G5 (Canada), Fax: (+1) 514-682-8434.

Published: October 1998

A weak inhibitor means faster exchange! Since the methyl ketone MK2 is a weak noncovalent peptidyl inhibitor of the human cytomegalovirus protease, exchange between the free and enzyme-bound forms is rapid. This allows for the use of transferred NOE NMR methods and molecular modeling, which show that the bound conformation of MK2 is an extended peptide. This is confirmed by the results of an X-ray crystallographic analysis of a related enzyme-inhibitor complex.

Download full-text PDF

Source
http://dx.doi.org/10.1002/(SICI)1521-3773(19981016)37:19<2729::AID-ANIE2729>3.0.CO;2-4DOI Listing

Publication Analysis

Top Keywords

methyl ketone
8
human cytomegalovirus
8
cytomegalovirus protease
8
conformation peptidyl
4
peptidyl methyl
4
ketone inhibitor
4
inhibitor bound
4
bound human
4
protease weak
4
weak inhibitor
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!