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J. Biol. Chem., Vol. 268, Issue 20, 14583-14585, 07, 1993
W Lu, W Zhang, SS Molloy, G Thomas, K Ryan, Y Chiang, S Anderson and M Laskowski Jr
Turkey ovomucoid third domain with Leu18 in its reactive site is a potent
inhibitor of many serine proteinases: subtilisins, chymotrypsins, and
elastases. Previous studies showed that an L18K mutation made it a
moderately strong inhibitor of trypsin, while an L18E mutation made it a
strong inhibitor of Glu-specific Streptomyces griseus proteinase (GluSGP).
For human furin substrates the consensus optimal sequence is RXKR
decreases. Therefore the A15R, T17K, and L18R mutations were made in turkey
ovomucoid third domain. The mutant inhibits human furin with a Ka of 1.1 x
10(7) M-1. As human furin catalyzes an obligatory step in human
immunodeficiency virus proliferation, this inhibitor, along with the others
already available, deserves further study.
Arg15-Lys17-Arg18 turkey ovomucoid third domain inhibits human furin
Department of Chemistry, Purdue University, West Lafayette, Indiana 47907.
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