2aob

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[[Image:2aob.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2aob| PDB=2aob | SCENE= }}
{{STRUCTURE_2aob| PDB=2aob | SCENE= }}
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'''Crystal structures of a high-affinity macrocyclic peptide mimetic in complex with the Grb2 SH2 domain'''
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===Crystal structures of a high-affinity macrocyclic peptide mimetic in complex with the Grb2 SH2 domain===
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==Overview==
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The high-affinity binding of the growth factor receptor-bound protein 2 (Grb2) SH2 domain to tyrosine-phosphorylated cytosolic domains of receptor tyrosine kinases (RTKs) is an attractive target for therapeutic intervention in many types of cancer. We report here two crystal forms of a complex between the Grb2 SH2 domain and a potent non-phosphorus-containing macrocyclic peptide mimetic that exhibits significant anti-proliferative effects against erbB-2-dependent breast cancers. This agent represents a "second generation" inhibitor with greatly improved binding affinity and bio-availability compared to its open-chain counterpart. The structures were determined at 2.0A and 1.8A with one and two domain-swapped dimers per asymmetric unit, respectively. The mode of binding and specific interactions between the protein and the inhibitor provide insight into the high potency of this class of macrocylic compounds and may aid in further optimization as part of the iterative rational drug design process.
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The line below this paragraph, {{ABSTRACT_PUBMED_16165154}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16165154 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16165154}}
==About this Structure==
==About this Structure==
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[[Category: Kinase signalling]]
[[Category: Kinase signalling]]
[[Category: Peptide mimetic]]
[[Category: Peptide mimetic]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:16:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:18:21 2008''

Revision as of 16:18, 28 July 2008

Image:2aob.png

Template:STRUCTURE 2aob

Crystal structures of a high-affinity macrocyclic peptide mimetic in complex with the Grb2 SH2 domain

Template:ABSTRACT PUBMED 16165154

About this Structure

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

Reference

Crystal structures of a high-affinity macrocyclic peptide mimetic in complex with the Grb2 SH2 domain., Phan J, Shi ZD, Burke TR Jr, Waugh DS, J Mol Biol. 2005 Oct 14;353(1):104-15. PMID:16165154

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