Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.

Androsterone derivatives substituted at position 3 were synthesized starting from dihydrotestosterone in a short sequence of reactions. They proved to be potent inhibitors (IC50 = 57-147 nM) of type 3 17beta-hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transformation of androstenedione to steroid active androgen testosterone.

N-glycosylation and residue 96 are involved in the functional properties of UDP-glucuronosyltransferase enzymes.

The recent cloning of several human and monkey UDP-glucuronosyltransferase (UGT) 2B proteins has allowed the characterization of these steroid metabolic enzymes. However, relatively little is known about the structure-function relationship, and the potential post-translational modifications of these proteins. The mammalian UGT2B proteins contain at least one consensus asparagine-linked glycosylation site NX(S/T).

Evaluation of prostatic specific antigen and digital rectal examination as screening tests for prostate cancer.

Background: The 11,811 first visits and 46,751 annual follow-up visits performed since 1988 were analyzed in order to assess the efficacy of serum prostatic specific antigen (PSA) and digital rectal examination (DRE) for diagnosis of prostate cancer.

Methods: At first visit, screening included DRE and measurement of PSA using 3.0 ng/ml as upper limit of normal, demonstrated as optimal value in the course of the study.