2pzy: Difference between revisions

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[[Image:2pzy.jpg|left|200px]]<br /><applet load="2pzy" size="350" color="white" frame="true" align="right" spinBox="true"
[[Image:2pzy.jpg|left|200px]]
caption="2pzy, resolution 2.900&Aring;" />
 
'''Structure of MK2 Complexed with Compound 76'''<br />
{{Structure
|PDB= 2pzy |SIZE=350|CAPTION= <scene name='initialview01'>2pzy</scene>, resolution 2.900&Aring;
|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> and <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]
|GENE= MAPKAPK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
}}
 
'''Structure of MK2 Complexed with Compound 76'''
 


==Overview==
==Overview==
Line 7: Line 16:


==About this Structure==
==About this Structure==
2PZY 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 <scene name='pdbligand=B18:'>B18</scene> and <scene name='pdbligand=STU:'>STU</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2PZY OCA].  
2PZY is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2PZY OCA].  


==Reference==
==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17576063 17576063]
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:[http://www.ncbi.nlm.nih.gov/pubmed/17576063 17576063]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: transferase]]
[[Category: transferase]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:34:40 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:20:01 2008''

Revision as of 16:20, 20 March 2008

File:2pzy.jpg


Drag the structure with the mouse to rotate
2pzy, resolution 2.900Å
Ligands: B18 and STU
Gene: MAPKAPK2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
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

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