A potent inhibitor of pancreatic elastase
Elastatinal is a potent inhibitor of pancreatic elastase (Ki = 240 nM) that is produced by various species of Actinomycetes. [1]? It more strongly inhibits pancreatic elastase versus the leukocyte-derived enzyme. [2] [3] Elastatinal reduces electrophoretic mobilities of 2A proteinases from poliovirus and human rhinovirus 14 in a dose-dependent manner, indicating substrate recognition by 2A proteinases is similar to that of pancreatic elastases.[4] It can also inhibit elastase-like protease collagenolytic protease from C. maenas digestive glands.[5]?
Reference:
[1]. Umezawa, H. Structures and activities of protease inhibitors of microbial origin. Methods Enzymol. 45, 678-695 (1976).
[2]. Feinstein, G., Malemud, C.J., and Janoff, A. The inhibition of human leucocyte elastase and chymotrypsin-like protease by elastatinal and chymostatin. Biochim Biophys. Acta. 429(3), 925-932 (1976).
[3]. Okumura, Y., Ogawa, K., and Uchiya, K. Characterization and primary structure of elastase inhibitor, AFLEI, from Aspergillus flavus. Nishon Ishinkin Gakkai Zasshi 48(1), 13-18 (2007).
[4]. Molla, A., Hellen, C.U.T., and Wimmer, E. Inhibition of proteolytic activity of poliovirus and rhinovirus 2A proteinases by elastase-specific inhibitors. J. Virol. 67(8), 4688-4695 (1993).
[5]. Roy, P., Colas, B., and Durand, P. Purification, kinetical and molecular characterizations of a serine collagenolytic protease from greenshore crag (Carcinus maenas) digestive gland. Comp. Biochem. Physiol. Biochem. Mol. Biol. 115(1), 87-95 (1996).
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