Design and testing of bicyclic inhibitors of Grb7-are two cycles better than one?

• Published in: Biopolymers Vol. 100; no. 5; pp. 543 - 549
• Main Authors: Gunzburg, Menachem J., Ambaye, Nigus D., Del Borgo, Mark P., Perlmutter, Patrick, Wilce, Jacqueline A.
• Format: Journal Article
• Language: English
• Published: United States Blackwell Publishing Ltd 01.09.2013
• Subjects: Affinity; Antineoplastic Agents - pharmacology; bicyclic peptide; Binding; Biopolymers; Cell Movement - drug effects; GRB7 Adaptor Protein - metabolism; Humans; Inhibitors; ITC; Linkages; Peptides; Peptides - pharmacology; Protein Binding; Reproduction; ring closing methathesis; Scaffolds; SH2 domain inhibitor; SPR; src Homology Domains; ring closing methathesis; ITC; SPR; SH2 domain inhibitor; bicyclic peptide

ABSTRACT Grb7 is an adapter protein involved in the propagation of signals in cancer cell migration and proliferation, and is thus a target for the development of novel anti‐cancer agents. An 11‐residue thioether‐cyclized peptide known as G7‐18NATE has previously been developed, that inhibits Grb7 v...