2pzy
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The discovery of a series of potent, carboline-based MK2 inhibitors is | + | 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== | ==About this Structure== | ||
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[[Category: Emmanuel, M.]] | [[Category: Emmanuel, M.]] | ||
[[Category: Gautschi, E.]] | [[Category: Gautschi, E.]] | ||
| - | [[Category: Goldberg, D | + | [[Category: Goldberg, D R.]] |
| - | [[Category: Kashem, M | + | [[Category: Kashem, M A.]] |
[[Category: Lukas, S.]] | [[Category: Lukas, S.]] | ||
[[Category: Mao, W.]] | [[Category: Mao, W.]] | ||
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[[Category: Moss, N.]] | [[Category: Moss, N.]] | ||
[[Category: Pargellis, C.]] | [[Category: Pargellis, C.]] | ||
| - | [[Category: Patel, U | + | [[Category: Patel, U R.]] |
[[Category: Patnaude, L.]] | [[Category: Patnaude, L.]] | ||
| - | [[Category: Peet, G | + | [[Category: Peet, G W.]] |
[[Category: Skow, D.]] | [[Category: Skow, D.]] | ||
| - | [[Category: Snow, R | + | [[Category: Snow, R J.]] |
[[Category: Wang, J.]] | [[Category: Wang, J.]] | ||
[[Category: Ward, Y.]] | [[Category: Ward, Y.]] | ||
[[Category: Werneburg, B.]] | [[Category: Werneburg, B.]] | ||
[[Category: White, A.]] | [[Category: White, A.]] | ||
| - | [[Category: Wu, J | + | [[Category: Wu, J P.]] |
[[Category: B18]] | [[Category: B18]] | ||
[[Category: STU]] | [[Category: STU]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:34:40 2008'' |
Revision as of 16:34, 21 February 2008
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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 and 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
Categories: 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
