The 5α-recluctase system and its inhibitors?

Dermatology

Volumn 193, Issue 3, 1997, Pages 177-184

  Chen, W ^a   Zouhoulis, Ch C ^a   Orfanos, C E ^a  

^a CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

Author keywords

5 and ; Reductase inhibitors; 5 and Reductase; Androgen receptor

Indexed keywords

4,7BETA DIMETHYL 4 AZACHOLESTAN 3 ONE; 8 CHLORO 1,2,3,4,4A,5,6,10B OCTAHYDRO 4 METHYLBENZO[F]QUINOLIN 3(2H) ONE; AMINO ACID; ANDROGEN RECEPTOR; ANDROSTANOLONE; FINASTERIDE; STEROID 5ALPHA REDUCTASE; STEROID 5ALPHA REDUCTASE INHIBITOR; TESTOSTERONE;

ACNE; AMINO ACID SEQUENCE; CHROMOSOME 2P; CHROMOSOME 5P; ENZYME ACTIVITY; ENZYME BINDING; ENZYME LOCALIZATION; EPIDIDYMIS; FIBROBLAST; GENITAL SYSTEM; HAIR FOLLICLE; HIRSUTISM; HORMONE METABOLISM; HUMAN; KERATINOCYTE; MALE TYPE ALOPECIA; PH; PRIORITY JOURNAL; PROSTATE; PROSTATE HYPERTROPHY; REVIEW; SEBORRHEA; SEMINAL VESICLE; SKIN CELL; SKIN DISEASE; SWEAT GLAND;

ACNE VULGARIS; ADULT; ALOPECIA; AMINO ACIDS; ANDROGENS; CHOLESTENONE 5 ALPHA-REDUCTASE; CHROMOSOMES, HUMAN, PAIR 2; CHROMOSOMES, HUMAN, PAIR 5; DERMATITIS, SEBORRHEIC; ENZYME INHIBITORS; EPIDERMIS; EPIDIDYMIS; FIBROBLASTS; FINASTERIDE; HAIR FOLLICLE; HIRSUTISM; HUMANS; ISOENZYMES; KERATINOCYTES; MALE; OXIDOREDUCTASES; PROSTATE; PROSTATIC HYPERPLASIA; SEBACEOUS GLANDS; SEMINAL VESICLES; SKIN; SKIN DISEASES; SWEAT GLANDS; TESTOSTERONE;

EID: 0029852637     PISSN: 10188665     EISSN: 14219832     Source Type: Journal    
DOI: 10.1159/000246242     Document Type: Article

References (57)

1. Flamigni C. Collins WP. Koullapis EN, et al: Androgen metabolism in human skin.,.1 Clin Endocrinol Melab 1971:32:737-743.
2. Evans RM: The steroid and thyroid hormone-receptor superfamily. Science 1988:240: 889-895.
3. Blauer M. Vaalasli A. Pauli SL.et al: Localization of androgen receptor in human skin. J Invest Dermatol 1991:97:264-268.
4. Thigpen AE. Silver RI. Guileyardo JM. et al: Molecular genetics of steroid 5a-reduetase 2 deficiency. J Clin Invest 1993;92:903-910.
5. Jenkins EP. Andersson S. Impcralo-McGinley J, et al: Genetic and pharmacological evidence of more than one human steroid 5a-rcduelase. 1 Clin Invest 1992:89:293-300.
6. Eicheler W, Aumiiller G. Happle R. Hoffmann R: Differential distribution of steroid Sa-re-ducutse isoenzymes in human skin. J Invest Dermatol 1994; 103:403.
7. Liang T. Rasmusson GH. Brooks JR: Biochemical and biological studies with 4-aza-steroidal 5ct-reducla.se inhibitors.,1 Steroid Biochem 1983; 19:385-390.
8. Cionnley GJ. Stoner E. Bruskewitz RC. et al: The effect of finasteride in men with benign prostatic hyperplasia. N Engl J Med 1992:327: 1185-1191.
9. Bakshi RK. Patel GF. Rasmusson GH, et al: 7[J-Melhyl-4-aza-cholestan-3-one (MK386) and related 4-azasleroids as selective inhibitors of human type 158-reductase.,1 Med Client 1994;37:3871-3874.
10. Grino PB. Griffin.IE, Wilson JD: Testosterone at high concentrations interacts with the human androgen receptor similarly to dihydrotestos-terone. Endocrinoloy 1990:126:1165-1172.
11. Bingham KD. Shaw DA: The metabolism of testosterone by human male scalp skin. J Endocrinol 1973:57:111-121.
12. Salman K. Spielvogel RL, Shulman LH. et al: Serum androstanediol glucuronide in women with facial hirsutism. J Am Acad Dermatol 1992:26:411-414.
13. Matteri RK. Stanczyk FZ. Gentzschein EE, et al: Androgen sulfate and glucuronide conjugates in nonhirsute and hirsute women with polycystic ovarian syndrome. Am J Obstet Gynecol 1989:161:1704-1709.
14. Savaya ME. Honig SL. Garland LD. Hsia SL: A-3p-Hydroxysteroid dehydrogenase activity in sebaceous gland in male pattern baldness. J Invest Dermatol 1988:91:101-105.
15. Vingler P. Filthath H. Baque A, et al: Direct quantitative digital autoradiography of testosterone metabolites in the pilosebaceous unit: An environmentally advantageous trace radioactive technology. Steroids 1993:58:429-438.
16. Impcralo-McGinley J. Guerrero L. Gautier T. Peterson RE: Steroid 5a-reducla.se deficiency in man: An inherited form of male pseudohermaphroditism. Science 1974:186:1213-1215.
17. Moore RJ. Wilson JD: Steroid Sot-reductase in cultured human fibroblasts: Biochemical and genetic evidence for two distinct enzyme activities. J Biol Chem 1976:251:5895-5900.
18. Andcrsson S. Russell DW: Structural and biochemical properties of cloned and expressed human and rat steroid 5oc-reductases. Proc Nall AcadSci USA 1990:87:3640-3644.
19. Andersson S. Berman DM. Jenkins EP. Russell DW: Deletion of steroid 5ot-reductasc 2 gene in male pseudohermaphroditism. Nature 1991: 354:159-161.
20. Normington K, Russell DW: Tissue distribution and kinetic characteristics of rat steroid 5oc-redueta.se isozymes. J Biol Chem 1992:267: 19548-19554.
21. Wilson JD. Griffin JE. Russell DW: Steroid 5(/.-reductase 2 deficiency. Endocrinol Rev 1993;14:577-593.
22. Hay JB. Hodgins MB: Metabolism of androgens in vitro by human facial and axillary skin. J Endrocrinol 1973:59:475-486.
23. Sansone G. Reisner RM: Differential rates of conversion of testosterone to dihydrotestosterone in acne and in normal human skin - A possible pathogenetic factor in acne. J Invest Dermatol 1971:56:366-372.
24. Takayasu S, Wakimoto H. Itami S, Sano S: Activity of testosterone 5oc-reductase in various tissues of human skin. J Invest Dermatol 1980: 74:187-191.
25. Itami S. Kurala S. Sonoda T. Takayasu S: Characterization of 5a-reductase in cultured human dermal papilla cells from beard and occipital scalp hair. J Invest Dermatol 1991:96:57-60.
26. Thigpen AE. Silver RI. Guileyardo JM. et al: Tissue distribution and ontogeny of steroid 5a-reductase isozyme expression. J Clin Invest 1993:92:903-910.
27. Luu-The V. Sugimoto Y. Puy L. et al: Characterization. expression and immunohistochemical localization of 5a-reducta.se in human skin. J Invest Dermatol 1994:102:221-226.
28. Caiman KC. Muir AV. Milne JA. Young II: Survey of the distribution of steroid dehydrogenase in sebaceous glands of human skin. Br J Dermatol 1970:82:567-571.
29. Liang T, Heiss CE, Cheung AH. et al: 4-Az.a-steroidal 5a-reduetase inhibitors without affinity of the androgen receptor. J Biol Chem 1984:259:734-739.
30. Russell DW. Wilson JD: Steroid Sot-reductase: Two genes/two enzymes. Annu Rev Biochcm 1994;63:25-61.
31. Brooks JR. Berman C. Pritnaka RL. el al: 5a-Reducta.sc inhibitory and anti-androgenic activities of some 4-azastcroids in the rat. Steroids 1986:47:1-19.
32. Holt DA. Oh HJ. Levy MA, Metcalf BW: Synthesis of a steroidal A ring aromatic sulfonic acid as an inhibitor of steroid Sa-reductase. Steroids 1991:56:4-7.
33. Stoner E: The clinical development of a.Sa-reductase inhibitor, finasteride. J Steroid Bio-chem Mol Biol 1990;37:375-378.
34. Peters DH, Sorkin EM: Finasteride: A review of its potential in the treatment of benign prostatic hyperplasia. Drugs 1993:46:177-208.
35. Tian G. Stuart JD. Moss ML. el al: l7[5-(n-tert-butylcarbamoyl)-4-az.a-5a-androstan-1 -en-3-onc is an active site-directed slow time-dependent inhibitor of human steroid 5a-reduelase I. Biochemistry 1994:33:2291-2296.
36. Gonnley GJ. Stoner E. Rittmaster RS. ct al: Effects of finasteride (MK-906), a 5a-reductase inhibitor, on circulating androgens in male volunteers. J Clin Endocrinol Metab 1990:70: 1136-1141.
37. Stoner E: Maintenance of clinical efficacy with finasteride therapy for 24 months in patients with benign prostatic hyperplasia. Arch Intern Med 1994:154:83-88.
38. Imperato-McGinley J, Gauerro L. Gautier T, et al: The androgen control of sebum production. Studies of subjects with dihydrotestosterone deficiency and complete androgen insensitivity. J Clin Endocrinol Metab 1993:76: 524-528.
39. Wong IL. Morris RS. Chang L. Spahn MA. Stanczy FZ. Lobo RA: A prospective randomized trial comparing finasteride to spironolactone in the treatment of hirsute women. J Clin Endocrinol Metab 1995:80:233-238.
40. Moghetti P. Castello R, Magnani CM. et al: Clinical and hormonal effects of the Sa-reductase inhibitor finasteride in idiopathic hirsutism. J Clin Endocrinol Metab 1994:79: 1115-1121.
41. Dal lob AL. Sadick NS. Unger W. et al: The effect of finasteride, a 5a-rcducta.se inhibitor, on scalp skin testosterone and dihydrotestosterone concentration in patients with male pattern baldness. J Clin Endocrinol Metab 1994: 79:703-706.
42. Di Salle E. Giudiei D. Briatico G. et al; Hormonal effects of turosteride, a 5a-rcducta.se inhibitor. in the rat. J Steroid Biochcm Mol Biol 1993:46:549-555.
43. Ichlc C. Délos S. Guirou O. Tate R. Raynaud J-P. Martin P-M: Human prostatic steroid Sa-reductase isoforms - A comparative study of selective inhibitors. J Steroid Biochem Mol Biol 1995:54:273-279.
44. Di Salle E, Briatico G. Giudiei D, et al: Endocrine properties of the testosterone Sa-reductase inhibitor, turosteride (FCE 26037). J Steroid Biochcm Mol Biol 1994:48:241-248.
45. Schwartz, Jl. Laskin OL. Meetcr CA, et al: Pharmacodynamics of MK-0963, a new 5a-re-duck.sc inhibitor: Effects on serum androgen concentrations. Clin Pharmacol Ther 1994:55: 50-54.
46. Van llecken A. Depre M. Schwartz Jl, et al: Plasma concentrations and effect on testosterone metabolism after single doses of MK-0434. a steroid 5-alpha-reductase inhibitor, in healthy subjects. Eur J Clin Pharmacol 1994: 46:123-126.
47. Levy MA. Brandi M. Sheedy KM. et al: Epris-teride is a selective and specific uncompetitive inhibitor of human steroid 5a-reducta.se isoform 2. J Steroid Biochem Mol Biol 1994:48: 197-206.
48. Liao S. Hiipakka RA: Selective inhibition of steroid 5a-reductasc isozymes by tea cpicate-chin-3-gallate and epigallocatechin-3-gallate. Biochem Biophys Res Commun 1995:214: 833-838.
49. Hirsch KS. Jones CD. Audia JE. et al: LY191704: A selective, nonsteroidal inhibitor of human steroid 5a-reducta.se type I. Proc Natl Acad Sci USA 1993:90:5277-5281.
50. Jones CD. Audia JE, Lawhorn DE, et al: Nonsteroidal inhibitors of human type I steroid Sa-reductase. J Med Chem 1993:36:421-423.
51. Hirosumi J. Nakayama O. Fagan T. et al: FK 143. a novel nonsteroidal inhibitor of steroid.Sa-reductase 1. In vitro effects on human and animal prostatic enzymes. J Steroid Biochem Mol Biol 1995:52:357-363.
52. Kojo H. Nakayama O. Hirosumi J. Chida N. Notsu Y. Okuhara M: Novel steroid Sa-reductase inhibitor FK 143: Its dual inhibition against the two isozymes and its effect on transcription of the isozyme genes. Mol Pharmacol 1995:48: 401-406.
53. Liang T. Liao S: Inhibition of steroid.Sa-reductase by specific aliphatic unsaturated fatty acids. Biochem J 1992:285:557-562.
54. Demctree JW. Safer LF. Artis WM: The effect of zinc on sebum secretion rate. Acta Derm Venereol (Stockh) 1980:60:166-169.
55. Stamatiadis D. Bulleau-Portois M-C. Mows-zowicz I: Inhibition of Sa-reductase activity in human skin by zinc and azelaic acid. Br J Dermatol 1988:119:627-632.
56. Sugimoto Y. Lopez-Solache I. Labri F. Luu-The V: Cations inhibit specifically type I.Sa-reductase found in human skin. J Invest Dermatol 1995:104:775-778.
57. Fahim MS, Wang M. Sutcu MF. Fahim II: Zinc arginine, a Sa-reductase inhibitor, reduces rat ventral prostate weight and DNA without affecting testicular function. Andrologia 1993: 25:369-375.