1bhh

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{{STRUCTURE_1bhh| PDB=1bhh | SCENE= }}
{{STRUCTURE_1bhh| PDB=1bhh | SCENE= }}
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'''FREE P56LCK SH2 DOMAIN'''
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===FREE P56LCK SH2 DOMAIN===
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==Overview==
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The crystal structure of human p56(lck) SH2 domain in complex with an inhibitor containing the singly charged p-(carboxymethyl)phenylalanine residue (cmF) as a phosphotyrosine (Tyr(P) or pY) replacement has been determined at 1.8 A resolution. The binding mode of the acetyl-cmF-Glu-Glu-Ile (cmFEEI) inhibitor is very similar to that of the pYEEI inhibitor, confirming that the cmFEEI inhibitor has a similar mechanism of SH2 domain inhibition despite its significantly reduced potency. Observed conformational differences in the side chain of the cmF residue can be interpreted in terms of maintaining similar interactions with the SH2 domain as the Tyr(P) residue. The crystal structure of the free p56(lck) SH2 domain has been determined at 1.9 A resolution and shows an open conformation for the BC loop and an open phosphotyrosine binding pocket, in contrast to earlier studies on the src SH2 domain that showed mostly closed conformation. The structural information presented here suggests that the carboxymethyl-phenylalanine residue may be a viable Tyr(P) replacement and represents an attractive starting point for the design and development of SH2 domain inhibitors with better pharmaceutical profiles.
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(as it appears on PubMed at http://www.pubmed.gov), where 9685372 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9685372}}
==About this Structure==
==About this Structure==
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[[Category: Sh2 domain]]
[[Category: Sh2 domain]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:31:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:10:32 2008''

Revision as of 16:10, 30 June 2008

Image:1bhh.png

Template:STRUCTURE 1bhh

FREE P56LCK SH2 DOMAIN

Template:ABSTRACT PUBMED 9685372

About this Structure

1BHH is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Carboxymethyl-phenylalanine as a replacement for phosphotyrosine in SH2 domain binding., Tong L, Warren TC, Lukas S, Schembri-King J, Betageri R, Proudfoot JR, Jakes S, J Biol Chem. 1998 Aug 7;273(32):20238-42. PMID:9685372

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