2osc

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[[Image:2osc.gif|left|200px]]<br /><applet load="2osc" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2osc.gif|left|200px]]
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caption="2osc, resolution 2.8&Aring;" />
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'''Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors'''<br />
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{{Structure
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|PDB= 2osc |SIZE=350|CAPTION= <scene name='initialview01'>2osc</scene>, resolution 2.8&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=MUH:N-{4-METHYL-3-[(3-PYRIMIDIN-4-YLPYRIDIN-2-YL)AMINO]PHENYL}-3-(TRIFLUOROMETHYL)BENZAMIDE'>MUH</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1]
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|GENE= TEK, TIE2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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}}
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'''Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2OSC is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MUH:'>MUH</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OSC OCA].
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2OSC 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=2OSC OCA].
==Reference==
==Reference==
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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors., Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H, Bioorg Med Chem Lett. 2007 May 15;17(10):2886-9. Epub 2007 Feb 25. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17350837 17350837]
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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors., Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H, Bioorg Med Chem Lett. 2007 May 15;17(10):2886-9. Epub 2007 Feb 25. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17350837 17350837]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Receptor protein-tyrosine kinase]]
[[Category: Receptor protein-tyrosine kinase]]
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[[Category: kinase domain tie-2]]
[[Category: kinase domain tie-2]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:21:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:03:51 2008''

Revision as of 16:03, 20 March 2008

Image:2osc.gif


PDB ID 2osc

Drag the structure with the mouse to rotate
, resolution 2.8Å
Ligands:
Gene: TEK, TIE2 (Homo sapiens)
Activity: Receptor protein-tyrosine kinase, with EC number 2.7.10.1
Coordinates: save as pdb, mmCIF, xml



Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors


Contents

Overview

A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.

Disease

Known diseases associated with this structure: Venous malformations, multiple cutaneous and mucosal OMIM:[600221]

About this Structure

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

Reference

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors., Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H, Bioorg Med Chem Lett. 2007 May 15;17(10):2886-9. Epub 2007 Feb 25. PMID:17350837

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