5 alpha-reductase in intact DU145 cells: Evidence for isozyme I and evaluation of novel inhibitors

Citation
W. Reichert et al., 5 alpha-reductase in intact DU145 cells: Evidence for isozyme I and evaluation of novel inhibitors, ARCH PHARM, 333(7), 2000, pp. 201-204
Citations number
18
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARCHIV DER PHARMAZIE
ISSN journal
03656233 → ACNP
Volume
333
Issue
7
Year of publication
2000
Pages
201 - 204
Database
ISI
SICI code
0365-6233(200007)333:7<201:5AIIDC>2.0.ZU;2-8
Abstract
The epithelial-like human prostatic carcinoma cell line DU145, which expres ses 5 alpha-reductase type I isozyme, was used to test a series of potentia l 5 alpha-reductase inhibitors. The exclusive expression of the type I isoz yme was confirmed by PCR and subsequent DNA sequence analysis. Culture cond itions were optimized for high conversion rates. Using this whole cell assa y finasteride, 4MA, and 65 steroidal and non-steroidal compounds synthesize d in our group were tested fur their inhibitory activity. Inhibitors with I C50 values in the nanomolar range could be identified.