1cj1: Difference between revisions

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|PDB= 1cj1 |SIZE=350|CAPTION= <scene name='initialview01'>1cj1</scene>, resolution 3.0&Aring;
|PDB= 1cj1 |SIZE=350|CAPTION= <scene name='initialview01'>1cj1</scene>, resolution 3.0&Aring;
|SITE=  
|SITE=  
|LIGAND= <scene name='pdbligand=C78:[1-[1-(6-CARBAMOYL-CYCLOHEX-2-ENYLCARBAMOYL)-CYCLOHEXYLCARBAMOYL]-2-(4-PHOSPHONOOXY-PHENYL)- ETHYL]-CARBAMIC ACID 3-AMINOBENZYLESTER'>C78</scene>
|LIGAND= <scene name='pdbligand=C78:[1-[1-(6-CARBAMOYL-CYCLOHEX-2-ENYLCARBAMOYL)-CYCLOHEXYLCARBAMOYL]-2-(4-PHOSPHONOOXY-PHENYL)-+ETHYL]-CARBAMIC+ACID+3-AMINOBENZYLESTER'>C78</scene>
|ACTIVITY=  
|ACTIVITY=  
|GENE=  
|GENE=  
|DOMAIN=
|RELATEDENTRY=
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1cj1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1cj1 OCA], [http://www.ebi.ac.uk/pdbsum/1cj1 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1cj1 RCSB]</span>
}}
}}


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==Overview==
==Overview==
Previous efforts in the search for molecules capable of blocking the associations between the activated tyrosine kinase growth factor receptors and the SH2 domain of Grb2 had resulted in the identification of 3-amino-Z-pTyr-Ac6c-Asn-NH2, a high-affinity and selective antagonist of this SH2 domain. In the present paper, we report the successful replacement of asparagine in this compound by a beta-amino acid mimetic, which brings us closer to our objective of identifying a Grb2-SH2 antagonist suitable for pharmacological investigations.
Previous efforts in the search for molecules capable of blocking the associations between the activated tyrosine kinase growth factor receptors and the SH2 domain of Grb2 had resulted in the identification of 3-amino-Z-pTyr-Ac6c-Asn-NH2, a high-affinity and selective antagonist of this SH2 domain. In the present paper, we report the successful replacement of asparagine in this compound by a beta-amino acid mimetic, which brings us closer to our objective of identifying a Grb2-SH2 antagonist suitable for pharmacological investigations.
==Disease==
Known diseases associated with this structure: Central hypoventilation syndrome, congenital OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=100790 100790]], Haddad syndrome OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=100790 100790]]


==About this Structure==
==About this Structure==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Rahuel, J.]]
[[Category: Rahuel, J.]]
[[Category: C78]]
[[Category: phosphotyrosine]]
[[Category: phosphotyrosine]]
[[Category: sh2 domain]]
[[Category: sh2 domain]]
[[Category: signal transduction]]
[[Category: signal transduction]]


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