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
Authors: Gerst C.1; Dalko M.2; Pichaud P.2; Galey J.B.2; Buan B.1; Bernard B.A.1
Source: Experimental Dermatology, Volume 11, Number 1, 1 February 2002 , pp. 52-58(7)
Publisher: Blackwell Publishing
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: 5258. © 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.
Keywords: 5-reductase inhibitor; hair follicle; indole carboxylic acids
Document Type: Original article
DOI: 10.1034/j.1600-0625.2002.110106.x
Affiliations: 1: L'Oréal Recherche Avancée, Hair Biology Group, Centre de Recherche C.Zviak, Clichy and 2: Department of Chemistry, Aulnay sous Bois, France

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