Scholars@Duke publication: Photoreactivation of Irreversibly Inhibited Serine Proteinases

Photoreactivation of Irreversibly Inhibited Serine Proteinases

Publication , Journal Article

Turner, AD; Pizzo, SV; Porter, NA; Rozakis, G

Published in: Journal of the American Chemical Society

January 1, 1988

The p-amidinophenyl ester of o-hydroxy-α-methylcinnamic acid has been synthesized and characterized. This compound irreversibly inhibits thrombin, Factor Xa, and trypsin. Inhibition by this derivative is, however, reversible (80-100%) upon irradiation of the enzyme in the presence of excess compound. Photolysis of the inactive 1:1 acylenzyme complexes of all three enzymes (purified to homogeneity) also regenerated full enzymatic activity in 15 min or less. Thrombin clotting times for a-thrombin inactivated with this inhibitor were >120 s (essentially incapable of clotting) prior to irradiation and 20 s (identical with controls) after complete photoreactivation. This derivative is the first example of a photosensitive inhibitor of the vitamin K dependent proteinases. © 1988, American Chemical Society. All rights reserved.

Duke Scholars

Author Salvatore Vincent Pizzo Pathology

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Published In

Journal of the American Chemical Society

DOI

10.1021/ja00209a040

EISSN

1520-5126

ISSN

0002-7863

Publication Date

January 1, 1988

Volume

110

Issue

Start / End Page

244 / 250

Related Subject Headings

General Chemistry
40 Engineering
34 Chemical sciences
03 Chemical Sciences

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Turner, A. D., Pizzo, S. V., Porter, N. A., & Rozakis, G. (1988). Photoreactivation of Irreversibly Inhibited Serine Proteinases. Journal of the American Chemical Society, 110(1), 244–250. https://doi.org/10.1021/ja00209a040

Turner, A. D., S. V. Pizzo, N. A. Porter, and G. Rozakis. “Photoreactivation of Irreversibly Inhibited Serine Proteinases.” Journal of the American Chemical Society 110, no. 1 (January 1, 1988): 244–50. https://doi.org/10.1021/ja00209a040.

Turner AD, Pizzo SV, Porter NA, Rozakis G. Photoreactivation of Irreversibly Inhibited Serine Proteinases. Journal of the American Chemical Society. 1988 Jan 1;110(1):244–50.

Turner, A. D., et al. “Photoreactivation of Irreversibly Inhibited Serine Proteinases.” Journal of the American Chemical Society, vol. 110, no. 1, Jan. 1988, pp. 244–50. Scopus, doi:10.1021/ja00209a040.

Turner AD, Pizzo SV, Porter NA, Rozakis G. Photoreactivation of Irreversibly Inhibited Serine Proteinases. Journal of the American Chemical Society. 1988 Jan 1;110(1):244–250.

Published In

Journal of the American Chemical Society

DOI

10.1021/ja00209a040

EISSN

1520-5126

ISSN

0002-7863

Publication Date

January 1, 1988

Volume

110

Issue

Start / End Page

244 / 250

Related Subject Headings

General Chemistry
40 Engineering
34 Chemical sciences
03 Chemical Sciences