918129-61-0Relevant academic research and scientific papers
Design and synthesis of conformationally constrained, extended and reverse turn pseudopeptides as Grb2-SH2 domain antagonists
Plake, Hilary R.,Sundberg, Thomas B.,Woodward, Angela R.,Martin, Stephen F.
, p. 1571 - 1574 (2003)
A series of conformationally constrained and flexible pseudopeptide derivatives of the tripeptide pYVN were prepared as potential antagonists of interactions of phosphotyrosine peptides with the Grb2-SH2 domain. The conformationally constrained compounds
Ligand preorganization may be accompanied by entropic penalties in protein-ligand interactions
Benfield, Aaron P.,Teresk, Martin G.,Plake, Hilary R.,DeLorbe, John E.,Millspaugh, Laura E.,Martin, Stephen F.
, p. 6830 - 6835 (2006)
(Figure Presented) Fact or fiction? It is generally assumed that preorganization of a flexible ligand in the 3D shape it adopts when bound to a macromolecular receptor will provide a derivative with an increased binding affinity that benefits entropically
Thermodynamic and structural effects of conformational constraints in protein-ligand interactions. Entropic paradoxy associated with ligand preorganization
DeLorbe, John E.,Clements, John H.,Teresk, Martin G.,Benfield, Aaron P.,Plake, Hilary R.,Millspaugh, Laura E.,Martin, Stephen F.
supporting information; experimental part, p. 16758 - 16770 (2010/03/04)
Succinate- and cyclopropane-derived phosphotyrosine (pY) replacements were incorporated into a series of Grb2 SH2 binding ligands wherein the pY+1 residue was varied to determine explicitly how variations in ligand preorganization affect binding energetic
