Design and synthesis of novel monocyclic β-lactam inhibitors of prostate specific antigen

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 13, 1997, Pages 1689-1694

  Adlington, Robert M ^a   Baldwin, Jack E ^a   Chen, Beining ^a   Cooper, Stephen L ^a   McCoull, William ^a   Pritchard, Gareth J ^a   Howe, Trevor J ^b   Becker, Gerald W ^b   Hermann, Robert B ^b   McNulty, Ann M ^b   Neubauer, Blake L ^b  

^a UNIVERSITY OF OXFORD   (United Kingdom)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA LACTAM DERIVATIVE; PROSTATE SPECIFIC ANTIGEN; SERINE PROTEINASE INHIBITOR;

ARTICLE; DRUG CONFORMATION; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITOR INTERACTION; MOLECULAR DYNAMICS; MOLECULAR MODEL; PROSTATE CARCINOMA; STEREOCHEMISTRY;

EID: 0030860598     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00285-0     Document Type: Article

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27. 10 μl of each inhibitor was pre-incubated with 10 μl of PSA (40 nM), in 10 μl of phosphate buffered saline/bovine serum albumen (BSA) (6.3μg/ml BSA), for two hours at 37 °C. 70 μl of 1mM substrate was added and serial dilution to give half-maximal effect of cleavage evaluated.