4,4,14 alpha-trimethyl9 beta,19-cyclo-5 alpha-26-homocholesta-24,26-dien-3beta-ol: A potent mechanism-based inactivator of Delta(24(25))- to Delta(25(27))-sterol methyl transferase

Authors
Nes, WD He, L Mangla, AT
Citation
Wd. Nes et al., 4,4,14 alpha-trimethyl9 beta,19-cyclo-5 alpha-26-homocholesta-24,26-dien-3beta-ol: A potent mechanism-based inactivator of Delta(24(25))- to Delta(25(27))-sterol methyl transferase, BIOORG MED, 8(24), 1998, pp. 3449-3452
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
24
Year of publication
1998
Pages
3449 - 3452
Database
ISI
SICI code
0960-894X(199812)8:24<3449:4ABA>2.0.ZU;2-D
Abstract
The title compound (4A) was synthesized and tested as a mechanism-based ina ctivator of the sterol methyl transferase (SMT) enzyme from Prototheca wick erhamii. Using cycloartenol as substrate, 4A was found to exhibit time-depe ndent inactivation kinetics, generating a K-i value of 30 mu M and K-inact value of 0.30 min(-1). (C) 1998 Elsevier Science Ltd. All rights reserved.