2gqg

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:2gqg.gif|left|200px]]
+
{{Seed}}
 +
[[Image:2gqg.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_2gqg| PDB=2gqg | SCENE= }}
{{STRUCTURE_2gqg| PDB=2gqg | SCENE= }}
-
'''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===
-
==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.
+
The line below this paragraph, {{ABSTRACT_PUBMED_16740718}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 16740718 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_16740718}}
==About this Structure==
==About this Structure==
Line 25: Line 29:
[[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 Jul 28 02:01:17 2008''

Revision as of 23:01, 27 July 2008

Image:2gqg.png

Template:STRUCTURE 2gqg

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

Template:ABSTRACT PUBMED 16740718

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 Mon Jul 28 02:01:17 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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