2c30: Difference between revisions
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==Overview== | ==Overview== | ||
p21-activated kinases have been classified into two groups based on their, domain architecture. Group II PAKs (PAK4-6) regulate a wide variety of, cellular functions, and PAK deregulation has been linked to tumor, development. Structural comparison of five high-resolution structures, comprising all active, monophosphorylated group II catalytic domains, revealed a surprising degree of domain plasticity, including a number of, catalytically productive and nonproductive conformers. Rearrangements of, helix alphaC, a key regulatory element of kinase function, resulted in an, additional helical turn at the alphaC N terminus and a distortion of its C, terminus, a movement hitherto unseen in protein kinases. The observed, structural changes led to the formation of interactions between conserved, .. | p21-activated kinases have been classified into two groups based on their, domain architecture. Group II PAKs (PAK4-6) regulate a wide variety of, cellular functions, and PAK deregulation has been linked to tumor, development. Structural comparison of five high-resolution structures, comprising all active, monophosphorylated group II catalytic domains, revealed a surprising degree of domain plasticity, including a number of, catalytically productive and nonproductive conformers. Rearrangements of, helix alphaC, a key regulatory element of kinase function, resulted in an, additional helical turn at the alphaC N terminus and a distortion of its C, terminus, a movement hitherto unseen in protein kinases. The observed, structural changes led to the formation of interactions between conserved, residues that structurally link the glycine-rich loop, alphaC, and the, activation segment and firmly anchor alphaC in an active conformation., Inhibitor screening identified six potent PAK inhibitors from which a, tri-substituted purine inhibitor was cocrystallized with PAK4 and PAK5. | ||
==About this Structure== | ==About this Structure== | ||
2C30 is a | 2C30 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PO4 and CL as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C30 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
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