2gqg

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2gqg.gif|left|200px]]
[[Image:2gqg.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2gqg |SIZE=350|CAPTION= <scene name='initialview01'>2gqg</scene>, resolution 2.400&Aring;
+
The line below this paragraph, containing "STRUCTURE_2gqg", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=1N1:N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE'>1N1</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE= ABL1, ABL, JTK7 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_2gqg| PDB=2gqg | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2gqg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gqg OCA], [http://www.ebi.ac.uk/pdbsum/2gqg PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2gqg RCSB]</span>
+
-
}}
+
'''X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain'''
'''X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain'''
Line 27: Line 24:
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Klei, H E.]]
[[Category: Klei, H E.]]
-
[[Category: kinase]]
+
[[Category: Kinase]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:24:10 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:20:06 2008''
+

Revision as of 02:24, 4 May 2008

Image:2gqg.gif

Template:STRUCTURE 2gqg

X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain


Overview

Chronic myeloid leukemia (CML) is caused by the constitutively activated tyrosine kinase breakpoint cluster (BCR)-ABL. Current frontline therapy for CML is imatinib, an inhibitor of BCR-ABL. Although imatinib has a high rate of clinical success in early phase CML, treatment resistance is problematic, particularly in later stages of the disease, and is frequently mediated by mutations in BCR-ABL. Dasatinib (BMS-354825) is a multitargeted tyrosine kinase inhibitor that targets oncogenic pathways and is a more potent inhibitor than imatinib against wild-type BCR-ABL. It has also shown preclinical activity against all but one of the imatinib-resistant BCR-ABL mutants tested to date. Analysis of the crystal structure of dasatinib-bound ABL kinase suggests that the increased binding affinity of dasatinib over imatinib is at least partially due to its ability to recognize multiple states of BCR-ABL. The structure also provides an explanation for the activity of dasatinib against imatinib-resistant BCR-ABL mutants.

About this Structure

2GQG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants., Tokarski JS, Newitt JA, Chang CY, Cheng JD, Wittekind M, Kiefer SE, Kish K, Lee FY, Borzillerri R, Lombardo LJ, Xie D, Zhang Y, Klei HE, Cancer Res. 2006 Jun 1;66(11):5790-7. PMID:16740718 Page seeded by OCA on Sun May 4 05:24:10 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2gqg"
Personal tools