Thiomethylene group-containing aldehyde cysteine and serine prot

Chemistry: molecular biology and microbiology – Enzyme – proenzyme; compositions thereof; process for... – Enzyme inactivation by chemical treatment

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435219, 564162, 514618, C12N 999, C12N 948, C07C32100, A01N 3718

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active

057443394

ABSTRACT:
The present invention is directed to thiomethylene group-containing aldehyde inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

REFERENCES:
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Puri et al. "Modulation of thrombin-induced platelet aggregation by inhibition of calpain by a synthetic peptide derived from the thiol-protease inhibitory sequence of kininogens and S-(3-nitro-2-pyridinesulfenyl)-cysteine", Eur. J. Biochem. (1993) vol. 2, pp. 233-241.
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Greene, T.W. and Wuts, P.G.M., Protective Groups in Organic Synthesis, 2d. Ed., Wiley & Sons, 1991. Publ. in NY.
Lee, W.J. et al., "Factors Influencing the Bindingof Calpain I to Human Erythrocyte Inside-Out Vesicles", Biochem Int'l., 1990, 22(1), 163-171.
Lehninger, Biochemistry, Second Edition, Worth Publishers, Inc., 1975, 73-75, Published in NY.
Luly, J. R. et al., "A Synthesis of Protected, Aminoalkyl Epoxides from .alpha.-Amino Acids", J. Org. Chem., 1987, 52, 1487-1492.
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Chatterjee, et al., "Potent Fluoromethyl Ketone Inhibitors of Recombinant Human Calpain I.sup.+ ", Bioorganic & Medicinal Chem.Letters, 1996, 6, 1237-1240.

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