2pzy
From Proteopedia
| Line 4: | Line 4: | ||
|PDB= 2pzy |SIZE=350|CAPTION= <scene name='initialview01'>2pzy</scene>, resolution 2.900Å | |PDB= 2pzy |SIZE=350|CAPTION= <scene name='initialview01'>2pzy</scene>, resolution 2.900Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=B18:(4R)-N-[4-({[2-(DIMETHYLAMINO)ETHYL]AMINO}CARBONYL)-1,3-THIAZOL-2-YL]-4-METHYL-1-OXO-2,3,4,9-TETRAHYDRO-1H-BETA-CARBOLINE-6-CARBOXAMIDE'>B18</scene> | + | |LIGAND= <scene name='pdbligand=B18:(4R)-N-[4-({[2-(DIMETHYLAMINO)ETHYL]AMINO}CARBONYL)-1,3-THIAZOL-2-YL]-4-METHYL-1-OXO-2,3,4,9-TETRAHYDRO-1H-BETA-CARBOLINE-6-CARBOXAMIDE'>B18</scene>, <scene name='pdbligand=STU:STAUROSPORINE'>STU</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span> |
|GENE= MAPKAPK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= MAPKAPK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2pzy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pzy OCA], [http://www.ebi.ac.uk/pdbsum/2pzy PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2pzy RCSB]</span> | ||
}} | }} | ||
| Line 45: | Line 48: | ||
[[Category: White, A.]] | [[Category: White, A.]] | ||
[[Category: Wu, J P.]] | [[Category: Wu, J P.]] | ||
| - | [[Category: B18]] | ||
| - | [[Category: STU]] | ||
[[Category: mk2]] | [[Category: mk2]] | ||
[[Category: protein kinase]] | [[Category: protein kinase]] | ||
[[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 Mon Mar 31 04:42:52 2008'' |
Revision as of 01:42, 31 March 2008
| |||||||
| , resolution 2.900Å | |||||||
|---|---|---|---|---|---|---|---|
| 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 | ||||||
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. 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 Mon Mar 31 04:42:52 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. | Mk2 | Protein kinase | Transferase
