Axys Pharmaceuticals, Inc.

University of California

Other

Schering Aktiengesellschaft

Arris Pharmaceutical Corporation

Bradley A Katz

Thomas E Jenkins

James M Clark

Robert M Stroud

William R Moore

Kyle C Elrod

Richard N Harkins

Marian Seto

The present invention relates to serine protease inhibitors having a P site binding moiety and a divalent cation(s) chelating moiety which are pre-prepared as divalent cation(s) complexes or combined with the serine protease in the presence of divalent cation(s) and methods for identifying and using the inhibitors. The compounds are shown to have high inhibitory activity when complexed to divalent cation(s) and are useful in various processes associated with serine protease isolation and inhibition.

Metal mediated serine protease inhibitors

A method is presented for determining if the inhibition of metal mediated serine proteases can be potentiated by cobalt or zinc ions.

Potentiating metal mediated serine protease inhibitors with cobalt or zinc ions

Serine protease inhibitors are provided comprising compounds having a P site binding moiety and a divalent cation(s) chelating moiety which are pre-prepared as divalent cation(s) complexes or combined with the serine protease in the presence of divalent cation(s). The compounds are shown to have high inhibitory activity when complexed to divalent cation(s) and find use in various processes associated with serine protease isolation and inhibition.

Metal complexed serine protease inhibitors

The invention provides for synthetic ligands that bind to class I receptor tyrosine kinases. The ligands are analogous in structure to naturally occurring ligands. The modified ligands however, have eliminated the mid-sequence (B) domain present in the native ligands and replaced it with a peptide bridge which links the amino (A) and carboxy (C) domains.

Modified ligands for receptor tyrosine kinases

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San Francisco, CA, United States of America

Bradley A Katz