New technologies enabling the industrialization of allosteric modulator discovery.
Allosteric modulators (AMs) are a promising avenue towards safe and selective drugs. AMs can interact selectively with unique domains distinct from the endogenous ligand binding site of receptors, up- or downregulating the response to receptor activation. Emphasis is placed in this article on the latest development in high-sensitivity technologies designed to identify AMs of G-protein coupled receptors. In addition to new pharmacological approaches, encouraging results in the crystal resolution of these targets enable use of more rational approaches to identification and optimization of AMs.
Robert
R
Lütjens
Benjamin
B
Perry
Dominik
D
Schelshorn
Jean-Philippe
JP
Rocher
D000494:Allosteric Regulation; D000818:Animals; D055808:Drug Discovery; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000378:metabolism*
D043562:Receptors, G-Protein-Coupled