Prostate specific antigen inhibitor

Veinberg G, Vorona M, Shestakova I, Kanepe I, Lukevics E (2003) Some of the more notable advances concern the development of mechanism-based serine protease inhibitors of elastase, cytomegalovirus protease, thrombin, prostate specific antigen, and cell metastasis and as inhibitors of acyl-CoA cholesterol acyl transferase. Curr Med Chem 10 1741... 

In 2002, the condensation of the titanium enolate derived from 2-pyridylthio acetoxyacetate with /V-4-methoxvphenvlimine of (S)-0,0-cyclohexylidene protected glyceraldehyde has been reported to give (35.4/C4 A)-p-lactam as a single product in 65% isolated yield (Scheme 52), [137]. A reactions sequence at C-3 and C-4 led in good yield to the p-lactam inhibitor of the serine protease prostate-specific antigen. 

Scheme 52 Stereoselective synthesis of (3-lactam inhibitor of the serine protease prostate-specific antigen...

Christensson A, Lilja H. Complex formation between protein C inhibitor and prostate-specific antigen in vitro and in human semen. Eur J Biochem 1994 220 45-53. 

Christensson A, Laurell CB, Lilja H. Enzymatic activity of prostate-specific antigen and its reactions with extracellular serine proteinase inhibitors. Eur J Biochem. 1990 194 755-763. 

Prostate Volume and Serum Prostate-Specific Antigen Predictors of Responsiveness to 5a-Reductase Inhibitors in Men with Benign Prostatic Hyperplasia... 

Several inhibitors bind and inactivate prostate-specific antigen (PSA), including aj-antitrypsin, ai-inacroglobulin, and aj-antiplasmin. ai-Anticliymotrypsin complexes are usually the predominant ones in serum or plasma, probably because of rapid clearance of the others. Levels of compiexed PSA are increased in most patients with prostatic cancer, compared with normal individuals or those with benign prostatic hypertrophy. Quantitative and qualitative (functional) deficiencies reported. 

Adlington RM, Baldwin JE, Chen B, Cooper SL, McCoull W, Pritchard GJ, Howe TJ, Becker GW, Hermann RB, McNulty AM, Neubauer BL. Design and synthesis of novel monocyclic /i-lactam inhibitors of prostate specific antigen. Bioorg. Med. Chem. Lett. 1997 7 1689-1694. 

---