At the 2nd IRN I-GPCRnet Annual Meeting, Ghazl Al Hamwi (working group Prof. Dr. Christa E. Müller) presented her poster entitled "Development of the potent antagonist for the orphan MAS-related G protein-coupled receptor MRGPRX2". The clear, well-structures, and very appealing presentation of her scientific work inspired the visitors and the jury: more than 25 scientists discussed her work with her and she was awarded the poster prize of the sponsor CALIXAR🏅. A total of 44 posters were shown and six posters prizes were awared. The conference was held at the university of Würzburg on September 30 and October 01, 2022.
Congratulationto the young an aspiring scientist Ghazl Al Hamwi!
Ghazl Al Hamwi about her project:
📌 The project started by screening of an in-house compound library, consisting of diverse small molecules, at the orphan receptor MRGPRX2. Several hit compounds were identified to block MRGPRX2, and one was selected as tractable for further optimization. Subsequent synthetic efforts and structure-activity relationship studies resulted in a drug-like compound with potency in the low nanomolar range, blocking MRGPRX2-mediated calcium mobilization as well as β-arrestin recruitment. Some of the allosteric antagonists were found to be biased, preferably blocking G protein signaling. Selected antagonists display high metabolic stability in liver microsomal preparations. Candidates are currently further characterized in preclinical models. The first patent has recently been filed, and the compounds are further optimized as novel drugs for the treatment of MRGPRX2-related diseases, as atopic dermatitis, rosacea, urticaria, and pseudoallergic reactions....