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- W2076457673 abstract "Six phosphorus-containing peptide analogues of the form Cbz-NHCH2PO2--L-Leu-Y (Y = D-Ala, NH2, Gly, L-Phe, L-Ala, L-Leu) have been prepared and evaluated as inhibitors of thermolysin. The Ki values for these compounds range from 1.7 microM to 9.1 nM and correlate well with the Km/kcat values for the corresponding peptide substrates [Morihara, K., & Tsuzuki, H. (1970) Eur. J. Biochem. 15, 374-380] but not with the Km values alone. The correlation noted between inhibitor Ki and substrate Km/kcat is the most extensive one of this type, providing strong evidence that the phosphonamidates are transition-state analogues and not simply multisubstrate ground-state analogues. Cbz-NH2CH2PO2--L-Leu-L-Leu (Ki = 9.1 nM) is the most potent inhibitor yet reported for thermolysin." @default.
- W2076457673 created "2016-06-24" @default.
- W2076457673 creator A5005741296 @default.
- W2076457673 creator A5045592322 @default.
- W2076457673 date "1983-09-27" @default.
- W2076457673 modified "2023-10-10" @default.
- W2076457673 title "Phosphonamidates as transition-state analog inhibitors of thermolysin" @default.
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- W2076457673 doi "https://doi.org/10.1021/bi00289a002" @default.
- W2076457673 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/6626519" @default.
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