Breaking the Dogma of the Metal-Coordinating Carboxylate Group in Integrin Ligands: Introducing Hydroxamic Acids to the MIDAS To Tune Potency and Selectivity

Angewandte Chemie, 2009, 48, 24, 4436 - 40 published on 02.06.2009
Angewandte Chemie,   online article

A suitable substitute: All integrin receptors bind their ligands, which contain an aspartate residue, in the metal-ion- dependent adhesion site (MIDAS). So far all attempts to replace the carboxyl group of aspartate with other, pharmacologically favorable isosteric groups have failed. Now it has been shown that a hydroxamic acid group can replace the carboxyl group; the resulting ligand retains its high binding activity. The picture shows one such ligand in the binding site of v3.

Campus Movie 2020

CIPSM Movie

Campus Movie 2012

CIPSM Movie
LMUexcellent
TU München
MPG
Helmholtz München
MPI of Neurobiology
MPI of Biochemistry