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: Wiley-Blackwell

Buy & download fulltext article:

Price: $48.00 plus tax (Refund Policy)

Abstract:

Gerst C, Dalko M, Pichaud P, Galey JB, Buan B, Bernard BA. Type-1 steroid 5 agr

-reductase is functionally active in the hair follicle as evidenced by new selective inhibitors of either type-1 or type-2 human steroid 5 agr

-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 agr

-reductase, namely type-1 and type-2 5 agr

-reductase (5 agr

-R1 and 5

-R2, respectively), have prompted studies directed towards the synthesis of selective 5 agr

-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 agr

-reductase activity. We have demonstrated that this class of molecules were potent inhibitors of either 5 agr

-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 agr

-R1 or 5

-R1/R2 inhibitors were able to inhibit 5 agr

-reductase activity in plucked hairs from female volunteers or in freshly isolated female hair follicles, selective 5 agr

-R2 inhibitors being inactive.

Keywords: 5-reductase inhibitor; hair follicle; indole carboxylic acids

Document Type: Original article

DOI: http://dx.doi.org/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

Publication date: 2002-02-01