Related kinases structural basis

Src and Src related kinases are included in the large family of cytoplasmic tyrosine kinases on the basis of their common domain structure acety-lated amino terminus, SH2 and SH3 domains, and highly conserved catalytic domain (Williams et al., 1998). Src kinase has little activity in cells in the absence of an activating signal, but many stimuli increase Src enzymatic activity via phosphorylation mechanisms (Cooper and Howell,... 

Designing specific enzyme inhibitors on a rational basis when one does not have a detailed three-dimensional crystal structure to which to relate is a rather sophisticated challenge. Some viable approaches to such a challenge are discussed in a review chapter by Santi and Kenyon (91) This discussion will focus on our rationale for the design of an affinity label for creatine kinase, namely N-(2,3-epoxypropyl)-N-amidinoglycine (epoxycreatine ) ... 

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