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Updated: Jun 25, 2026

Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells
Published on: November 6, 2021
Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase
Leila Malik1, Nicholas M Kelly, Jian-Nong Ma
1ACADIA Pharmaceuticals AB, Medeon Science Park, S-205 12 Malmö, Sweden.
Abstract:
A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active class, tetracyclic benzimidazoles, was undertaken. The solid-phase chemistry was found to be superior both for the synthesis of analogs and for the synthesis of gram quantities.
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