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PDBsum entry 1cj1
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Signaling protein
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PDB id
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1cj1
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Contents |
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* Residue conservation analysis
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References listed in PDB file
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Key reference
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Title
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Structure-Based design, Synthesis, And X-Ray crystallography of a high-Affinity antagonist of the grb2-Sh2 domain containing an asparagine mimetic.
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Authors
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P.Furet,
C.García-Echeverría,
B.Gay,
J.Schoepfer,
M.Zeller,
J.Rahuel.
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Ref.
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J Med Chem, 1999,
42,
2358-2363.
[DOI no: ]
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PubMed id
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Abstract
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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.
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