1opl
From Proteopedia
(New page: 200px<br /> <applet load="1opl" size="450" color="white" frame="true" align="right" spinBox="true" caption="1opl, resolution 3.42Å" /> '''Structural basis fo...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1opl. | + | [[Image:1opl.jpg|left|200px]]<br /><applet load="1opl" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1opl" size=" | + | |
caption="1opl, resolution 3.42Å" /> | caption="1opl, resolution 3.42Å" /> | ||
'''Structural basis for the auto-inhibition of c-Abl tyrosine kinase'''<br /> | '''Structural basis for the auto-inhibition of c-Abl tyrosine kinase'''<br /> | ||
| Line 11: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1OPL 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 MYR and P16 as [http://en.wikipedia.org/wiki/ligands ligands]. The following page contains interesting information on the relation of 1OPL with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb43_1.html Src Tyrosine Kinase]]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http:// | + | 1OPL 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=MYR:'>MYR</scene> and <scene name='pdbligand=P16:'>P16</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. The following page contains interesting information on the relation of 1OPL with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb43_1.html Src Tyrosine Kinase]]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1OPL OCA]. |
==Reference== | ==Reference== | ||
| Line 32: | Line 31: | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:35:02 2008'' |
Revision as of 14:35, 15 February 2008
|
Structural basis for the auto-inhibition of c-Abl tyrosine kinase
Contents |
Overview
c-Abl is normally regulated by an autoinhibitory mechanism, the disruption, of which leads to chronic myelogenous leukemia. The details of this, mechanism have been elusive because c-Abl lacks a phosphotyrosine residue, that triggers the assembly of the autoinhibited form of the closely, related Src kinases by internally engaging the SH2 domain. Crystal, structures of c-Abl show that the N-terminal myristoyl modification of, c-Abl 1b binds to the kinase domain and induces conformational changes, that allow the SH2 and SH3 domains to dock onto it. Autoinhibited c-Abl, forms an assembly that is strikingly similar to that of inactive Src, kinases but with specific differences that explain the differential, ability of the drug STI-571/Gleevec/imatinib (STI-571) to inhibit the, catalytic activity of Abl, but not that of c-Src.
Disease
Known diseases associated with this structure: Leukemia, Philadelphia chromosome-positive, resistant to imatinib OMIM:[189980]
About this Structure
1OPL is a Single protein structure of sequence from Homo sapiens with and as ligands. The following page contains interesting information on the relation of 1OPL with [Src Tyrosine Kinase]. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 Full crystallographic information is available from OCA.
Reference
Structural basis for the autoinhibition of c-Abl tyrosine kinase., Nagar B, Hantschel O, Young MA, Scheffzek K, Veach D, Bornmann W, Clarkson B, Superti-Furga G, Kuriyan J, Cell. 2003 Mar 21;112(6):859-71. PMID:12654251
Page seeded by OCA on Fri Feb 15 16:35:02 2008
