3ccn
From Proteopedia
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'''X-ray structure of c-Met with triazolopyridazine inhibitor.''' | '''X-ray structure of c-Met with triazolopyridazine inhibitor.''' | ||
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| + | ==Overview== | ||
| + | Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
3CCN 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=3CCN OCA]. | 3CCN 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=3CCN OCA]. | ||
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| + | ==Reference== | ||
| + | Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase., Albrecht BK, Harmange JC, Bauer D, Berry L, Bode C, Boezio AA, Chen A, Choquette D, Dussault I, Fridrich C, Hirai S, Hoffman D, Larrow JF, Kaplan-Lefko P, Lin J, Lohman J, Long AM, Moriguchi J, O'Connor A, Potashman MH, Reese M, Rex K, Siegmund A, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Bellon SF, J Med Chem. 2008 May 22;51(10):2879-82. Epub 2008 Apr 22. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18426196 18426196] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Receptor protein-tyrosine kinase]] | [[Category: Receptor protein-tyrosine kinase]] | ||
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[[Category: Transmembrane]] | [[Category: Transmembrane]] | ||
[[Category: Tyrosine-protein kinase]] | [[Category: Tyrosine-protein kinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 28 09:37:59 2008'' |
Revision as of 06:38, 28 May 2008
X-ray structure of c-Met with triazolopyridazine inhibitor.
Contents |
Overview
Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity.
Disease
Known disease associated with this structure: Hepatocellular carcinoma, childhood type OMIM:[164860], Renal cell carcinoma, papillary, familial and sporadic OMIM:[164860], Autism, suseptibility to, 9 OMIM:[164860]
About this Structure
3CCN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase., Albrecht BK, Harmange JC, Bauer D, Berry L, Bode C, Boezio AA, Chen A, Choquette D, Dussault I, Fridrich C, Hirai S, Hoffman D, Larrow JF, Kaplan-Lefko P, Lin J, Lohman J, Long AM, Moriguchi J, O'Connor A, Potashman MH, Reese M, Rex K, Siegmund A, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Bellon SF, J Med Chem. 2008 May 22;51(10):2879-82. Epub 2008 Apr 22. PMID:18426196 Page seeded by OCA on Wed May 28 09:37:59 2008
Categories: Homo sapiens | Receptor protein-tyrosine kinase | Single protein | Abrecht, B K. | Bauer, D. | Bellon, S F. | Dussault, I. | Harmange, J C. | Long, A. | Atp-binding | C-met kinase triazolopyridazine | Glycoprotein | Membrane | Nucleotide-binding | Phosphoprotein | Proto-oncogene | Receptor | Transferase | Transmembrane | Tyrosine-protein kinase
