Recent Publication: Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain

We are excited to share a recent publication, capturing the results of a long journey led by the collaboration between Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques (LCBPT) at Université Paris Cité, Institute of Functional Genomics (IGF) at University of Montpellier and BIOVIA team including Dr. @AC and Dr. @AG.

Using Discovery Studio, the team has identified the mode of action for XAP044, a unique negative allosteric modulator of metabotropic Glutamate 7 receptor (mGlu7). Inhibition of mGlu7 may help treat mood disorders including anxiety and depression, post-traumatic stress disorders or epilepsy. The results of this project, which has combined molecular modeling, pharmacological assays and mutagenesis, helped design more potent antagonists targeting mGlu7, with fewer possible off-target effects. This work will also be featured on the cover of Journal of Medicinal Chemistry!

Read the full article here: https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.3c01924?linkId=429856587.

Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain