Rosati F , Bardazzi I , De Blasi P , Simi L , Scarpi D , Guarna A , Serio M , Racchi ML , Danza G ( 2005 ) 5α-Reductase activity in Lycopersicon esculentum : Cloning and functional characterization of LeDET2 and evidence of the presence of two isoenzymes . J. Steroid. Biochem. ...
17-N, N-diethylcarbamoyl-4-methyl-4-aza-5-an-drostan-3-one (4-MA) inhibits 5-reductase activity in cultured human genital skin fibroblasts. Enzyme kinetic studies analyzed by Eadie-Hofstee plots demonstrated that 4-MA is a competitive inhibitor, with an apparent Ki of 15 nM. 4-MA had ...
Pharmacologically Relevant Receptor Binding Characteristics and 5α-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract 锯棕榈提取物(SPE)可以抑制大鼠肝脏中的II型5α-还原酶活性,半抑制浓度IC50为101μg/ ml。其中,...
Pharmacologically Relevant Receptor Binding Characteristics and 5α-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract 锯棕榈提取物(SPE)可以抑制大鼠肝脏中的II型5α-还原酶活性,半抑制浓度IC50为101μg/ ml。其中,除棕榈酸外,所有脂肪酸均抑制5α-还原酶活性,IC50值为42.1至6...
Fig. 1: Steroid 5α-reductase activity of PbSRD5A. aSteroid 5α-reductase family proteins can reduce Δ4carbon–carbon double bound to form α configuration at C5of products. These reactions can be inhibited by finasteride and dutasteride specifically.bTestosterone (T), 4-androstene-3,17-dione...
Lin, Theaflavin-3,3'-digallate and penta-O-galloyl-beta-D- glucose inhibit rat liver microsomal 5alpha-reductase activity and the expression of androgen receptor in LNCaP prostate cancer cells. Carcinogenesis, 2004. 25(7): p. 1109-18.
This observation is supported by a previous study showing that some mis- sense SRD5A2 mutations do not impair but increase the steroid 5a-reductase activity (Makridakis et al. 2004). On the other hand, the presence of this premature ter- mination signal predicts the expression of a truncated...
[14]. The A49T missense mutation significantly increases the risk of advanced prostate cancer in African-American and in Latino men, and increases the maximal steroid 5α-reductase activity (Vmax) fivefold in vitro[12]. Thus, the kinetic data provide a rational explanation for the increased ...
Disclosed are methods and compositions for the preparation of steroid 5&agr;-reductases by recombinant means, as well as for the use of these enzymes in screening assays for the identification of compounds which have the ability to inhibit or otherwise alter the enzymatic function of these enzymes...
Inhibition of the activity of 'basic' 5α-reductase (type 1) detected in DU 145 cells and expressed in insect cells The purpose of this study was 2-fold: (1) to identify the 5α-reductase (5α-R) isozyme(s) present in DU 145 cells, a human cell-line of low androgen sensi... ...