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Volumn 1, Issue 2, 1997, Pages 254-259

Steroid 5α-reductase inhibitors in androgen-dependent disorders

Author keywords

[No Author keywords available]

Indexed keywords

ANDROGEN; ENZYME INHIBITOR; STEROID 5ALPHA REDUCTASE;

EID: 0031197126     PISSN: 13675931     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1367-5931(97)80017-8     Document Type: Article
Times cited : (43)

References (54)
  • 2
    • 0028173882 scopus 로고
    • Steroid 5α-reductase: Two genes/two enzymes
    • Russell DW, Wilson JD: Steroid 5α-reductase: two genes/two enzymes. Annu Rev Biochem 1994, 63:25-61.
    • (1994) Annu Rev Biochem , vol.63 , pp. 25-61
    • Russell, D.W.1    Wilson, J.D.2
  • 3
    • 0016359646 scopus 로고
    • Steroid 5α-reductase deficiency in man: An inherited form of male pseudohermaphroditism
    • Imperato-McGinley J, Guerrero L, Gautier T, Peterson RE: Steroid 5α-reductase deficiency in man: an inherited form of male pseudohermaphroditism. Science 1974, 27:1213-1215.
    • (1974) Science , vol.27 , pp. 1213-1215
    • Imperato-McGinley, J.1    Guerrero, L.2    Gautier, T.3    Peterson, R.E.4
  • 4
    • 0017343580 scopus 로고
    • Male pseudohermaphroditism due to steroid 5α-reductase deficiency
    • Peterson RE, Imperato-McGinley J, Gautier T, Sturla E: Male pseudohermaphroditism due to steroid 5α-reductase deficiency. Am J Med 1977, 62:170-191.
    • (1977) Am J Med , vol.62 , pp. 170-191
    • Peterson, R.E.1    Imperato-McGinley, J.2    Gautier, T.3    Sturla, E.4
  • 6
    • 0000464966 scopus 로고
    • Inherited 5α-reductase deficiency in man
    • Imperato-McGinley J, Gautier T: Inherited 5α-reductase deficiency in man. Trends Genet 1986, 2:130-133.
    • (1986) Trends Genet , vol.2 , pp. 130-133
    • Imperato-McGinley, J.1    Gautier, T.2
  • 7
    • 0002714801 scopus 로고    scopus 로고
    • Inhibitors of 5α-reductase
    • Frye SV: Inhibitors of 5α-reductase. Curr Pharm Des 1996, 2:59-84. This comprehensive review provides a description of the historical development of inhibitors of 5αR and an extensive discussion of the structure-activity relationships of steroidal and nonsteroidal inhibitors of this enzyme.
    • (1996) Curr Pharm des , vol.2 , pp. 59-84
    • Frye, S.V.1
  • 8
    • 0030913442 scopus 로고    scopus 로고
    • Pharmacological options in the treatment of benign prostatic hyperplasia
    • Kenny B, Ballard S, Blagg S, Fox D: Pharmacological options in the treatment of benign prostatic hyperplasia. J Med Chem 1997, 40:1293-1315.
    • (1997) J Med Chem , vol.40 , pp. 1293-1315
    • Kenny, B.1    Ballard, S.2    Blagg, S.3    Fox, D.4
  • 9
    • 0025278610 scopus 로고
    • Mechanistic studies with solubilized rat liver steroid 5α-reductase: Elucidation of the kinetic mechanism
    • Levy MA, Brandt J, Greway AT: Mechanistic studies with solubilized rat liver steroid 5α-reductase: elucidation of the kinetic mechanism. Biochemistry 1990, 29:2808-2815.
    • (1990) Biochemistry , vol.29 , pp. 2808-2815
    • Levy, M.A.1    Brandt, J.2    Greway, A.T.3
  • 11
    • 0028918929 scopus 로고
    • Chemical mechanism of the covalent modification of 5α-reductases by finasteride as probed by secondary tritium isotope effects
    • Tian G, Chen S-Y, Facchine KL, Prakash SR: Chemical mechanism of the covalent modification of 5α-reductases by finasteride as probed by secondary tritium isotope effects. J Am Chem Soc 1995, 117:2369-2370.
    • (1995) J Am Chem Soc , vol.117 , pp. 2369-2370
    • Tian, G.1    Chen, S.-Y.2    Facchine, K.L.3    Prakash, S.R.4
  • 13
    • 0029937631 scopus 로고    scopus 로고
    • Mechanism-based inhibition of human steroid 5α-reductase by finasteride: Enzyme catalyzed formation of NADP-dihydrofinasteride, a potent bisubstrate analog inhibitor
    • Bull HG, Garcia-Calvo M, Andersson SA, Baginsky WF, Chan HK, Ellsworth D, Miller R, Stearns RA, Bakshi RK, Rasmusson GH et al.: Mechanism-based inhibition of human steroid 5α-reductase by finasteride: enzyme catalyzed formation of NADP-dihydrofinasteride, a potent bisubstrate analog inhibitor. J Am Chem Soc 1996, 118:2359-2365. This paper provides compelling evidence that the mechanism of inhibition of the human 5αR by finasteride is intimately related to catalysis. A mechanism of inhibition is proposed whereby finasteride is processed by the enzyme as an alternate substrate and ultimately forms an adduct with NADP.
    • (1996) J Am Chem Soc , vol.118 , pp. 2359-2365
    • Bull, H.G.1    Garcia-Calvo, M.2    Andersson, S.A.3    Baginsky, W.F.4    Chan, H.K.5    Ellsworth, D.6    Miller, R.7    Stearns, R.A.8    Bakshi, R.K.9    Rasmusson, G.H.10
  • 14
    • 0029098816 scopus 로고
    • 4-aza-3-oxo-5α-androst-1-ene-17β-N-aryl-carboxamides as dual inhibitors of human type 1 and 2 steroid 5α-reductatses. Dramatic effect of N-aryl substituents on type 1 and 2 5α-reductase inhibitory potency
    • Bakshi RK, Rasmusson GH, Patel GF, Mosley RT, Chang B, Ellsworth K, Harris GS, Tolman RL: 4-aza-3-oxo-5α-androst-1-ene-17β-N-aryl-carboxamides as dual inhibitors of human type 1 and 2 steroid 5α-reductatses. Dramatic effect of N-aryl substituents on type 1 and 2 5α-reductase inhibitory potency. J Med Chem 1995, 38:3189-3192.
    • (1995) J Med Chem , vol.38 , pp. 3189-3192
    • Bakshi, R.K.1    Rasmusson, G.H.2    Patel, G.F.3    Mosley, R.T.4    Chang, B.5    Ellsworth, K.6    Harris, G.S.7    Tolman, R.L.8
  • 15
    • 0028807269 scopus 로고
    • Mechanism of time-dependent inhibition of 5α-reductase by D1-4-azasteroids: Toward perfection of rates of time-dependent inhibition by using ligand binding energies
    • Tian G, Mook RA Jr, Moss ML, Frye SV: Mechanism of time-dependent inhibition of 5α-reductase by D1-4-azasteroids: toward perfection of rates of time-dependent inhibition by using ligand binding energies. Biochemistry 1995, 34:13433-13459.
    • (1995) Biochemistry , vol.34 , pp. 13433-13459
    • Tian, G.1    Mook R.A., Jr.2    Moss, M.L.3    Frye, S.V.4
  • 18
    • 0028806780 scopus 로고
    • Finasteride: A clinical review
    • Gormley GJ: Finasteride: a clinical review. Biomed Pharmacother 1995, 49:319-324.
    • (1995) Biomed Pharmacother , vol.49 , pp. 319-324
    • Gormley, G.J.1
  • 21
    • 0026503988 scopus 로고
    • Finasteride, an inhibitor of 5α-reductase suppresses prostatic dihydrotestosterone in men with benign prostatic hyperplasia
    • McConnell JD, Wilson JD, George FW, Geller J, Pappas F, Stoner E: Finasteride, an inhibitor of 5α-reductase suppresses prostatic dihydrotestosterone in men with benign prostatic hyperplasia. J Clin Endocrinol Metab 1992, 74:505-508.
    • (1992) J Clin Endocrinol Metab , vol.74 , pp. 505-508
    • McConnell, J.D.1    Wilson, J.D.2    George, F.W.3    Geller, J.4    Pappas, F.5    Stoner, E.6
  • 22
    • 10144251748 scopus 로고    scopus 로고
    • Effect of MK-386, a novel inhibitor of type 1 5α-reductase, alone and in combination with finasteride, on serum DHT (dihydrotestosterone) concentrations in men
    • Schwartz JI, Vanhecken A, Deschepper PJ, De Lepeleire I, Lasseter KC, Cooper Shamblen E, Winchell GA, Constanzer ML, Chavez CM et al.: Effect of MK-386, a novel inhibitor of type 1 5α-reductase, alone and in combination with finasteride, on serum DHT (dihydrotestosterone) concentrations in men. J Clin Endocrinol Metab 1996, 81:2942-2947. This manuscript presents clinical data demonstrating that inhibition of 5αR1 with MK-386 decreases serum and sebum DHT. Furthermore, it is reported that combined inhibition of 5αR1 with MK-386 and 5αR2 with finasteride drops circulating DHT to the limit of detection.
    • (1996) J Clin Endocrinol Metab , vol.81 , pp. 2942-2947
    • Schwartz, J.I.1    Vanhecken, A.2    Deschepper, P.J.3    De Lepeleire, I.4    Lasseter, K.C.5    Cooper Shamblen, E.6    Winchell, G.A.7    Constanzer, M.L.8    Chavez, C.M.9
  • 23
    • 0029684628 scopus 로고    scopus 로고
    • 5α-reductase inhibitors/finasteride
    • Stoner E: 5α-reductase inhibitors/finasteride. Prostate 1996, 6:82-87.
    • (1996) Prostate , vol.6 , pp. 82-87
    • Stoner, E.1
  • 26
    • 0029893171 scopus 로고    scopus 로고
    • Screening for prostate cancer: Opportunities for prevention
    • Thompson IM, Coltman CA: Screening for prostate cancer: opportunities for prevention. Semin-Urol-Oncol. 1996, 14 (suppl 2):4-10.
    • (1996) Semin-Urol-Oncol. , vol.14 , Issue.2 SUPPL. , pp. 4-10
    • Thompson, I.M.1    Coltman, C.A.2
  • 27
    • 0001040796 scopus 로고
    • Effect of multiple doses of epristeride (E) a steroid 5α-reductase inhibitor on serum dihydrotestosterone in older male subjects
    • Audet P, Nurcombe H, Lamb Y, Jorasky D, Lloyd-Davis K, Morris R: Effect of multiple doses of epristeride (E) a steroid 5α-reductase inhibitor on serum dihydrotestosterone in older male subjects. Clin Pharmacol Ther 1993, 53:231.
    • (1993) Clin Pharmacol Ther , vol.53 , pp. 231
    • Audet, P.1    Nurcombe, H.2    Lamb, Y.3    Jorasky, D.4    Lloyd-Davis, K.5    Morris, R.6
  • 28
    • 0006527843 scopus 로고    scopus 로고
    • Effects of GI198745 (GG745), a novel 5-alpha-reductase (5αR) inhibitor on dihydrotestosterone (DHT)
    • Hermann DJ, Davis IM, Wilson TH: Effects of GI198745 (GG745), a novel 5-alpha-reductase (5αR) inhibitor on dihydrotestosterone (DHT). Clin Pharmacol Ther 1996, 59:192. This abstract provides evidence that combined inhibition of 5αR1 and 5αR2 with a single agent leads to significantly greater decreases in serum DHT than is obtained with finasteride, a selective inhibitor of 5αR2.
    • (1996) Clin Pharmacol Ther , vol.59 , pp. 192
    • Hermann, D.J.1    Davis, I.M.2    Wilson, T.H.3
  • 33
    • 0000268324 scopus 로고    scopus 로고
    • Clinical studies on the effects of oral finasteride, a type II 5α-reductase inhibitor, on scalp hair in men with male pattern baldness
    • Edited by Van Neste DJ, Randall VA. Amsterdam: Elsevier
    • Kaufman KD: Clinical studies on the effects of oral finasteride, a type II 5α-reductase inhibitor, on scalp hair in men with male pattern baldness. In Hair Research for the Next Millennium. Edited by Van Neste DJ, Randall VA. Amsterdam: Elsevier; 1996:363-365.
    • (1996) Hair Research for the next Millennium , pp. 363-365
    • Kaufman, K.D.1
  • 35
    • 0029101544 scopus 로고
    • Activity of the type , 5α-reductase exhibits regional differences in isolated sebaceous glands and whole skin
    • Thiboutot D, Harris G, Iles V, Cimis G, Gilliland K, Hagari S: Activity of the type , 5α-reductase exhibits regional differences in isolated sebaceous glands and whole skin. J Invest Dermatol 1995, 105:209-214.
    • (1995) J Invest Dermatol , vol.105 , pp. 209-214
    • Thiboutot, D.1    Harris, G.2    Iles, V.3    Cimis, G.4    Gilliland, K.5    Hagari, S.6
  • 36
    • 0029123708 scopus 로고
    • Immunohistochemical evidence for differential distribution of 5α-reductase isoenzymes in human skin
    • Eichler W, Dreher M, Hoffmann R, Happle R, Aumuller G: Immunohistochemical evidence for differential distribution of 5α-reductase isoenzymes in human skin. Br J Dermatol 1995, 133:371-376.
    • (1995) Br J Dermatol , vol.133 , pp. 371-376
    • Eichler, W.1    Dreher, M.2    Hoffmann, R.3    Happle, R.4    Aumuller, G.5
  • 38
    • 85003125189 scopus 로고
    • Male hormone substance: A prime factor in acne
    • Hamilton JB: Male hormone substance: a prime factor in acne. J Endocrinol Metab 1941, 1:507-592.
    • (1941) J Endocrinol Metab , vol.1 , pp. 507-592
    • Hamilton, J.B.1
  • 39
    • 0027520707 scopus 로고
    • The androgen control of sebum production. Studies of subjects with dihydrotestosterone deficiency and complete androgen insensitivity
    • Imperato-McGinley J, Gautier T, Cai LQ, Yee B, Epstein J, Pochi P: The androgen control of sebum production. Studies of subjects with dihydrotestosterone deficiency and complete androgen insensitivity. J Clin Endocrinol Metab 1993, 76:524-528.
    • (1993) J Clin Endocrinol Metab , vol.76 , pp. 524-528
    • Imperato-McGinley, J.1    Gautier, T.2    Cai, L.Q.3    Yee, B.4    Epstein, J.5    Pochi, P.6
  • 40
    • 0030982034 scopus 로고    scopus 로고
    • MK-386, an inhibitor of 5-alpha-reductase type 1, reduces dihydrotestosterone concentrations in serum and sebum without affecting dihydrotestosterone concentrations in semen
    • Schwartz JI, Tanaka WK, Wang DZ, Ebel DL, Geissler LA, Dallob A, Hafkin B, Gertz BJ: MK-386, an inhibitor of 5-alpha-reductase type 1, reduces dihydrotestosterone concentrations in serum and sebum without affecting dihydrotestosterone concentrations in semen. J Clin Endocrinol Metabol 1997, 82:1373-1377. These investigators demonstrate that a differential response is obtained in serum, sebum and semen DHT upon selective inhibition of 5αR1 or 5αR2 with MK-386 or finasteride, respectively. It is suggested that mainly 5αR1 contributes to sebum DHT, 5αR2 is important for semen DHT and both isozymes contribute to serum DHT.
    • (1997) J Clin Endocrinol Metabol , vol.82 , pp. 1373-1377
    • Schwartz, J.I.1    Tanaka, W.K.2    Wang, D.Z.3    Ebel, D.L.4    Geissler, L.A.5    Dallob, A.6    Hafkin, B.7    Gertz, B.J.8
  • 42
    • 0028897316 scopus 로고
    • Clinical relevance of testosterone and dihydrotestosterone metabolism in women
    • Rittmaster RS: Clinical relevance of testosterone and dihydrotestosterone metabolism in women. Am J Med 1995, 98(suppl 1A):17S-21S.
    • (1995) Am J Med , vol.98 , Issue.SUPPL. 1A
    • Rittmaster, R.S.1
  • 44
    • 0028844434 scopus 로고
    • A practical approach to hirsutism
    • Gilchrist VJ, Hecht BR: A practical approach to hirsutism. Am Fam Physician 1995, 52:1837-1844.
    • (1995) Am Fam Physician , vol.52 , pp. 1837-1844
    • Gilchrist, V.J.1    Hecht, B.R.2
  • 45
    • 0022885593 scopus 로고
    • Treatment of hirsutism with sprionolactone
    • Tremblay RR: Treatment of hirsutism with sprionolactone. J Clin Endocrinol Metab 1986, 15:363-371.
    • (1986) J Clin Endocrinol Metab , vol.15 , pp. 363-371
    • Tremblay, R.R.1
  • 46
    • 0029859309 scopus 로고    scopus 로고
    • Outcome of long-term treatment with the 5α-reductase inhibitor finasteride in idiopathic hirsutism: Clinical and hormonal effects during a 1-year course of therapy and 1-year follow-up
    • Castello R, Tosi F, Perone G, Negri C, Muggeo M, Moghetti P: Outcome of long-term treatment with the 5α-reductase inhibitor finasteride in idiopathic hirsutism: clinical and hormonal effects during a 1-year course of therapy and 1-year follow-up. Fertil Steril 1996, 66:734-740. In this manuscript the authors present evidence that treatment of hirsute women with finasteride for one year led to a significant improvement in hirsutism scores.
    • (1996) Fertil Steril , vol.66 , pp. 734-740
    • Castello, R.1    Tosi, F.2    Perone, G.3    Negri, C.4    Muggeo, M.5    Moghetti, P.6
  • 48
    • 0028852761 scopus 로고
    • Androgenic regulation of bone mass in women
    • Gasperino J: Androgenic regulation of bone mass in women. Clin Orthop Rel Res 1995, 311:278-286.
    • (1995) Clin Orthop Rel Res , vol.311 , pp. 278-286
    • Gasperino, J.1
  • 50
    • 0026674814 scopus 로고
    • Prolonged treatment with finasteride (a 5 alpha-reductase inhibitor) does not affect bone density and metabolism
    • Matzkin H, Chen J, Weisman Y, Goldray D, Pappas F, Jaccard N, Braf Z: Prolonged treatment with finasteride (a 5 alpha-reductase inhibitor) does not affect bone density and metabolism. Clin Endocrinol 1992, 37:432-436.
    • (1992) Clin Endocrinol , vol.37 , pp. 432-436
    • Matzkin, H.1    Chen, J.2    Weisman, Y.3    Goldray, D.4    Pappas, F.5    Jaccard, N.6    Braf, Z.7
  • 51
    • 0029961690 scopus 로고    scopus 로고
    • Finasteride therapy does not alter bone turnover in men with benign prostatic hyperplasia - A Clinical Research Center study
    • Tollin SR, Rosen HN, Zurowski K, Saltzman B, Zeind AJ, Berg S, Greenspan SL: Finasteride therapy does not alter bone turnover in men with benign prostatic hyperplasia - a Clinical Research Center study. J Clin Endocrinol Metab 1996, 81:1031-1034.
    • (1996) J Clin Endocrinol Metab , vol.81 , pp. 1031-1034
    • Tollin, S.R.1    Rosen, H.N.2    Zurowski, K.3    Saltzman, B.4    Zeind, A.J.5    Berg, S.6    Greenspan, S.L.7
  • 52
    • 85047696604 scopus 로고
    • Polycystic ovary syndrome as a form of functional ovarian hyperandrogenism due to dysregulation of androgen secretion
    • Ehrmann DA, Barnes RB, Rosenfield RL: Polycystic ovary syndrome as a form of functional ovarian hyperandrogenism due to dysregulation of androgen secretion. Endocrine Rev 1995, 16:322-353.
    • (1995) Endocrine Rev , vol.16 , pp. 322-353
    • Ehrmann, D.A.1    Barnes, R.B.2    Rosenfield, R.L.3
  • 53
    • 0029842832 scopus 로고    scopus 로고
    • A mechanism of the suppression of estrogen production in polycystic ovary syndrome
    • Agarwal SK, Judd HL, Magoffin DA: A mechanism of the suppression of estrogen production in polycystic ovary syndrome. J Clin Endocrinol Metabol 1996, 81:3686-3691.
    • (1996) J Clin Endocrinol Metabol , vol.81 , pp. 3686-3691
    • Agarwal, S.K.1    Judd, H.L.2    Magoffin, D.A.3
  • 54
    • 0030255859 scopus 로고    scopus 로고
    • 5α-reductase 1 and 2 expression and activity in human ovarian follicles, stroma and corpus luteum as compared to neonatal foreskin
    • Haning RC Jr, Tantravahi U, Zhao Q, Hackett RJ, Canick JA: 5α-reductase 1 and 2 expression and activity in human ovarian follicles, stroma and corpus luteum as compared to neonatal foreskin. J Steroid Biochem Mol Biol 1996, 59:199-204.
    • (1996) J Steroid Biochem Mol Biol , vol.59 , pp. 199-204
    • Haning R.C., Jr.1    Tantravahi, U.2    Zhao, Q.3    Hackett, R.J.4    Canick, J.A.5


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