3cth
From Proteopedia
(New page: '''Unreleased structure''' The entry 3cth is ON HOLD until Paper Publication Authors: Sack, J. Description: Crystal structure of the tyrosine kinase domain of the hepatocyte growth fac...) |
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| + | {{STRUCTURE_3cth| PDB=3cth | SCENE= }} | ||
| - | + | '''Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-met in complex with a aminopyridine based inhibitor''' | |
| - | Description: Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-met in complex with a aminopyridine based inhibitor | ||
| + | ==Overview== | ||
| + | A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model. | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 11 | + | ==Disease== |
| + | Known disease associated with this structure: Hepatocellular carcinoma, childhood type OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=164860 164860]], Renal cell carcinoma, papillary, familial and sporadic OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=164860 164860]], Autism, suseptibility to, 9 OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=164860 164860]] | ||
| + | |||
| + | ==About this Structure== | ||
| + | 3CTH 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=3CTH OCA]. | ||
| + | |||
| + | ==Reference== | ||
| + | Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors., Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM, Bioorg Med Chem Lett. 2008 Jun 1;18(11):3224-9. Epub 2008 Apr 25. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18479916 18479916] | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Receptor protein-tyrosine kinase]] | ||
| + | [[Category: Single protein]] | ||
| + | [[Category: Sack, J.]] | ||
| + | [[Category: Atp-binding]] | ||
| + | [[Category: Glycoprotein]] | ||
| + | [[Category: Grb2]] | ||
| + | [[Category: Membrane]] | ||
| + | [[Category: Nucleotide-binding]] | ||
| + | [[Category: Phosphoprotein]] | ||
| + | [[Category: Proto-oncogene]] | ||
| + | [[Category: Receptor tyrosine kinase]] | ||
| + | [[Category: Shc]] | ||
| + | [[Category: Signal transduction]] | ||
| + | [[Category: Transferase]] | ||
| + | [[Category: Transmembrane]] | ||
| + | [[Category: Tyrosine-protein kinase]] | ||
| + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 11 10:50:19 2008'' | ||
Revision as of 07:50, 11 June 2008
Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-met in complex with a aminopyridine based inhibitor
Contents |
Overview
A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.
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
3CTH is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors., Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM, Bioorg Med Chem Lett. 2008 Jun 1;18(11):3224-9. Epub 2008 Apr 25. PMID:18479916 Page seeded by OCA on Wed Jun 11 10:50:19 2008
Categories: Homo sapiens | Receptor protein-tyrosine kinase | Single protein | Sack, J. | Atp-binding | Glycoprotein | Grb2 | Membrane | Nucleotide-binding | Phosphoprotein | Proto-oncogene | Receptor tyrosine kinase | Shc | Signal transduction | Transferase | Transmembrane | Tyrosine-protein kinase
