Stereoselective binding of an enantiomeric pair of stromelysin-1 inhibitors caused by conformational entropy factors

Authors
Parker, MH Ortwine, DF O'Brien, PM Lunney, EA Banotai, CA Mueller, WT McConnell, P Brouillette, CG
Citation
Mh. Parker et al., Stereoselective binding of an enantiomeric pair of stromelysin-1 inhibitors caused by conformational entropy factors, BIOORG MED, 10(21), 2000, pp. 2427-2430
Citations number
31
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2427 - 2430
Database
ISI
SICI code
0960-894X(20001106)10:21<2427:SBOAEP>2.0.ZU;2-Q
Abstract
Isothermal titration calorimetry was used to analyze the binding of an enan tiomeric pair of inhibitors to the stromelysin-1 catalytic domain. Differen ces in binding affinity are attributable to different conformational entrop y penalties suffered upon binding. Two possible explanations for these diff erences are proposed. (C) 2000 Elsevier Science Ltd. All rights reserved.