1cj1 Citations

Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.

J. Med. Chem. 42 2358-63 (1999)
Cited: 1 times
EuropePMC logo PMID: 10395476


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.

Articles - 1cj1 mentioned but not cited (1)

  1. Binding modes of peptidomimetics designed to inhibit STAT3. Dhanik A, McMurray JS, Kavraki LE. PLoS ONE 7 e51603 (2012)