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Macrocyclic compounds as strategy for kinase-related chemical probe development


Recent advances have highlighted the advantages of using macrocyclic compounds as a basis for protein kinase inhibitors. However, the design and synthesis methodologies for such macrocyclic inhibitors are at an early stage. SGC-Unicamp works on inhibitor development for several protein kinases which are good candidates for development of macrocyclic inhibitors. Those candidate kinases can bind inhibitors with small hinge-binding groups and sometimes, can also accommodate ligands in a teardrop binding mode. Additionally, new macrocyclic compounds can be screened against the SGC-Unicamp in-house panel of 40+ human protein kinases to identify new opportunities for inhibitor development. Whenever possible, SGC-Unicamp will perform co-crystallization trials and solve co-crystal structures for the target proteins in complex with the macrocyclic inhibitors. (AU)

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