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The design, synthesis, and characterization of tight-binding inhibitors of calmodulin

✍ Scribed by William F. DeGrado; Frank G. Prendergast; Henry R. Wolfe Jr.; Jos A. Cox

Publisher: John Wiley and Sons
Year: 1985
Tongue: English
Weight: 637 KB
Volume: 29
Category: Article
ISSN: 0730-2312
DOI: 10.1002/jcb.240290204

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✦ Synopsis

Based on a consideration of the probable structure of calmodulin and some natural peptides known to interact with it, two calmodulin-binding peptides were designed. These peptides bind to calmodulin in helical conformations and are capable of forming electrostatic and hydrophobic interactions with calmodulin. Their dissocation constants for binding ( < 2 10 and 400 pM) place them as the tightestbinding inhibitors of calmodulin thus far reported. The study of the interactions of these and similar peptides with calmodulin will provide valuable insights into the mechanisms whereby calmodulin binds to target enzymes, and it also serves as an excellent model system for exploring the physical chemistry of proteinprotein interaction.

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