2pzy | pdb_00002pzy
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Structure of MK2 Complexed with Compound 76
Overview
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.
About this Structure
2PZY is a Single protein structure of sequence from Homo sapiens with B18 and STU as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Thu Feb 21 18:34:40 2008
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- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- Abeywardane, A.
- Andersen, D.
- Emmanuel, M.
- Gautschi, E.
- Goldberg, D R.
- Kashem, M A.
- Lukas, S.
- Mao, W.
- Martin, L.
- Morwick, T.
- Moss, N.
- Pargellis, C.
- Patel, U R.
- Patnaude, L.
- Peet, G W.
- Skow, D.
- Snow, R J.
- Wang, J.
- Ward, Y.
- Werneburg, B.
- White, A.
- Wu, J P.
- B18
- STU
- Mk2
- Protein kinase
- Transferase
