@article {Gerst:1 February 2002:0906-6705:52,
author = "Gerst C.",
author = "Dalko M.",
author = "Pichaud P.",
author = "Galey J.B.",
author = "Buan B.",
author = "Bernard B.A.",
title = "Type-1 steroid 5alpha-reductase is functionally active in the hair follicle as evidenced by new selective inhibitors of either type-1 or type-2 human steroid 5alpha-reductase",
journal = "Experimental Dermatology",
volume = "11",
year = "1 February 2002",
abstract = "Gerst C, Dalko M, Pichaud P, Galey JB, Buan B, Bernard BA. Type-1 steroid 5
-reductase is functionally active in the hair follicle as evidenced by new selective inhibitors of either type-1 or type-2 human steroid 5-reductase. Exp Dermatol 2002: 11: 52–58. © Munksgaard, 2002Abstract:Steroid 5-reductase catalyzes the reduction of testosterone (T) into the very potent androgen dihydrotestosterone (DHT). The different tissue expression patterns of the two isoforms of 5-reductase, namely type-1 and type-2 5-reductase (5-R1 and 5-R2, respectively), have prompted studies directed towards the synthesis of selective 5-R1 or 5-R2 inhibitors. In this present work, we have performed a structure/activity study on the inhibitory potential of indole carboxylic acids against hair follicle 5-reductase activity. We have demonstrated that this class of molecules were potent inhibitors of either 5-R1 or 5-R2 or both depending on (i) substituents in positions 4, 5 or 6 and (ii) the presence of a free carboxylic group. We have also found that only 5-R1 or 5-R1/R2 inhibitors were able to inhibit 5-reductase activity in plucked hairs from female volunteers or in freshly isolated female hair follicles, selective 5-R2 inhibitors being inactive.",
pages = "52-58(7)",
url = "http://www.ingentaconnect.com/content/mksg/exd/2002/00000011/00000001/art00006"
doi = "doi:10.1034/j.1600-0625.2002.110106.x"
}