Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl) carbonyl] piperidin-4-yl} propan-2-ol: a novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase …

K Watanabe, A Kakefuda, M Yasuda, K Enjo…

Index: Watanabe, Kazushi; Kakefuda, Akio; Yasuda, Minoru; Enjo, Kentaro; Kikuchi, Aya; Furutani, Takashi; Naritomi, Yoichi; Otsuka, Yukio; Okada, Minoru; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 17 p. 5261 - 5270

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Citation Number: 6

Abstract

Abstract Type 5 17β-hydroxysteroid dehydrogenase (17β-HSD5), also known as aldo-keto reductase 1C3 (AKR1C3), is a member of the aldo-keto reductase superfamily of enzymes and is expressed in the human prostate. One of the main functions of 17β-HSD5 is to catalyze the conversion of the weak androgen, androstenedione, to the potent androgen, testosterone. The concentration of intraprostatic 5α-dihydrotestosterone (DHT) in patients ...