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2pzy

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2pzy, resolution 2.90Å ()
Ligands: ,
Gene: MAPKAPK2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Structure of MK2 Complexed with Compound 76

Publication Abstract from PubMed

The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors., Wu JP, Wang J, Abeywardane A, Andersen D, Emmanuel M, Gautschi E, Goldberg DR, Kashem MA, Lukas S, Mao W, Martin L, Morwick T, Moss N, Pargellis C, Patel UR, Patnaude L, Peet GW, Skow D, Snow RJ, Ward Y, Werneburg B, White A, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4664-9. Epub 2007 Jun 7. PMID:17576063

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

2pzy is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Wu JP, Wang J, Abeywardane A, Andersen D, Emmanuel M, Gautschi E, Goldberg DR, Kashem MA, Lukas S, Mao W, Martin L, Morwick T, Moss N, Pargellis C, Patel UR, Patnaude L, Peet GW, Skow D, Snow RJ, Ward Y, Werneburg B, White A. The discovery of carboline analogs as potent MAPKAP-K2 inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4664-9. Epub 2007 Jun 7. PMID:17576063 doi:10.1016/j.bmcl.2007.05.101

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