Development of a Potent and Selective G2A (GPR132) Agonist
Victor Hernandez-Olmos,
Jan Heering,
Beatrice Marinescu
et al.
Abstract:G protein-coupled receptor G2A was postulated to be a promising target for the development of new therapeutics in neuropathic pain, acute myeloid leukemia, and inflammation. However, there is still a lack of potent, selective, and drug-like G2A agonists to be used as a chemical tool or as the starting matter for the development of drugs. In this work, we present the discovery and structure−activity relationship elucidation of a new potent and selective G2A agonist scaffold. Systematic optimization resulted in … Show more
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