Ahmed, Sabbir and Denison, Sophie (1998) Mechanism based representation of the active site of 5-[alpha]-reductase (5AR). Bioorganic & Medicinal Chemistry Letters, 8(18), pp. 2615-2620. ISSN (print) 0960-894X
Full text not available from this archive.Abstract
In the present study, we have attempted to determine a detailed representation of the 5 alpha-Reductase (5AR) active site involving the elucidation of the transition state for the steroid delta 4 reduction reaction (the 'NADPH-substrate' complex), onto which steroidal and non-steroidal inhibitors were superimposed. We conclude that: (i) there is a requirement for groups to mimic the steroid substrate A-ring; (ii) the area about C(3), C(4), C(5) and C(6) of T appears to be sterically hindered, and; (iii) the area of the active site about the C(17) of the steroid substrate does not possess hydrogen bonding groups and is not restricted.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | steroid 5-alpha-reductase, inhibition |
| Research Area: | Pharmacy |
| Faculty, School or Research Centre: | Faculty of Science (until 2011) > School of Pharmacy and Chemistry |
| Related URLs: | |
| Depositing User: | Kim Forbes |
| Date Deposited: | 24 Jul 2008 |
| Last Modified: | 14 Apr 2011 11:55 |
| URI: | http://eprints.kingston.ac.uk/id/eprint/2455 |
Actions (Repository Editors)
 |
Item Control Page |