2c0i: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:2c0i.gif|left|200px]] | [[Image:2c0i.gif|left|200px]] | ||
'''SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-420983''' | {{Structure | ||
|PDB= 2c0i |SIZE=350|CAPTION= <scene name='initialview01'>2c0i</scene>, resolution 2.30Å | |||
|SITE= <scene name='pdbsite=AC1:Ca+Binding+Site+For+Chain+A'>AC1</scene> | |||
|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene> and <scene name='pdbligand=L1G:N-(4-{4-AMINO-1-[4-(4-METHYLPIPERAZIN-1-YL)-TRANS-CYCLOHEXYL]-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL}-2-METHOXYPHENYL)-1-METHYL-1H-INDOLE-2-CARBOXAMIDE'>L1G</scene> | |||
|ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.10.1_and_2.7.10.2 Transferred entry: 2.7.10.1 and 2.7.10.2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.112 2.7.1.112] | |||
|GENE= | |||
}} | |||
'''SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-420983''' | |||
==Overview== | ==Overview== | ||
| Line 7: | Line 16: | ||
==About this Structure== | ==About this Structure== | ||
2C0I is a [ | 2C0I 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=2C0I OCA]. | ||
==Reference== | ==Reference== | ||
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:[http:// | Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16216497 16216497] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| Line 34: | Line 43: | ||
[[Category: tyrosine-protein kinase]] | [[Category: tyrosine-protein kinase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:09:13 2008'' | ||
Revision as of 14:09, 20 March 2008
| |||||||||||||
| 2c0i, resolution 2.30Å | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sites: | AC1 | ||||||||||||
| Ligands: | CA and L1G | ||||||||||||
| Activity: | Transferred entry: 2.7.10.1 and 2.7.10.2, with EC number 2.7.1.112 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-420983
Overview
We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.
About this Structure
2C0I is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:16216497
Page seeded by OCA on Thu Mar 20 16:09:13 2008
