Publications by authors named "Shoghag B Panjarian"
Article Synopsis
- * The inactive form of c-Abl kinase has a compact structure stabilized by the N-cap and has specific interactions that, when mutated, lead to kinase activation.
- * X-ray scattering studies show that one mutation (A356N) maintains a similar structure to the wild-type active state, while another (T315I) alters the structure, indicating that c-Abl activation can occur with or without significant structural changes.
Allosteric kinase inhibitors hold promise for revealing unique features of kinases that may not be apparent using conventional ATP-competitive inhibitors. Here we explore the activity of a previously reported allosteric inhibitor of BCR-Abl kinase, GNF-2, against two cellular isoforms of Abl tyrosine kinase: one that carries a myristate in the N terminus and the other that is deficient in N-myristoylation. Our results show that GNF-2 inhibits the kinase activity of non-myristoylated c-Abl more potently than that of myristoylated c-Abl by binding to the myristate-binding pocket in the C-lobe of the kinase domain.
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