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1pkg

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{{STRUCTURE_1pkg| PDB=1pkg | SCENE= }}
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'''Structure of a c-Kit Kinase Product Complex'''
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===Structure of a c-Kit Kinase Product Complex===
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==Overview==
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The c-Kit proto-oncogene is a receptor protein-tyrosine kinase associated with several highly malignant human cancers. Upon binding its ligand, stem cell factor (SCF), c-Kit forms an active dimer that autophosphorylates itself and activates a signaling cascade that induces cell growth. Disease-causing human mutations that activate SCF-independent constitutive expression of c-Kit are found in acute myelogenous leukemia, human mast cell disease, and gastrointestinal stromal tumors. We report on the phosphorylation state and crystal structure of a c-Kit product complex. The c-Kit structure is in a fully active form, with ordered kinase activation and phosphate-binding loops. These results provide key insights into the molecular basis for c-Kit kinase transactivation to assist in the design of new competitive inhibitors targeting activated mutant forms of c-Kit that are resistant to current chemotherapy regimes.
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(as it appears on PubMed at http://www.pubmed.gov), where 12824176 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12824176}}
==About this Structure==
==About this Structure==
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[[Category: Structure]]
[[Category: Structure]]
[[Category: Transactivation]]
[[Category: Transactivation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:11:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 14:05:08 2008''

Revision as of 11:05, 28 July 2008

Image:1pkg.png

Template:STRUCTURE 1pkg

Structure of a c-Kit Kinase Product Complex

Template:ABSTRACT PUBMED 12824176

About this Structure

1PKG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of a c-kit product complex reveals the basis for kinase transactivation., Mol CD, Lim KB, Sridhar V, Zou H, Chien EY, Sang BC, Nowakowski J, Kassel DB, Cronin CN, McRee DE, J Biol Chem. 2003 Aug 22;278(34):31461-4. Epub 2003 Jun 24. PMID:12824176

Page seeded by OCA on Mon Jul 28 14:05:08 2008

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