Advancing Drug Discovery and Characterization in GPCR Research

TOPICAL COLLECTIONS

Guest Editor

Oleh Durydivka

University of Chemistry and Technology Prague, Czech Republic

Oleh Durydivka, Ph.D., is a biochemist specializing in molecular pharmacology and GPCR signaling. He earned his doctorate in 2023 from the Institute of Molecular Genetics at the Czech Academy of Sciences, where he investigated the molecular mechanisms regulating cannabinoid receptor 1 (CB1R). His research employed Bioluminescence Resonance Energy Transfer (BRET)-based assays, confocal and Total Internal Reflection Fluorescence (TIRF) microscopy, immunocytochemistry, immunoblotting, and behavioral studies in animal models to explore CB1R activity and its modulation by SGIP1. During his internship at the Institute for Research in Immunology and Cancer at the Université de Montréal, he worked with various BRET-based biosensors for GPCR signaling and contributed to the development of novel biosensors. In 2024, he joined the Forensic Laboratory of Biologically Active Substances at the University of Chemistry and Technology Prague, where he evaluates the activity and safety of novel psychoactive compounds. His work includes assays for G protein and β-arrestin signaling, neurotransmitter transporter activity, enzymatic inhibition, cell viability, and ecotoxicity.

Collection Overview

G protein-coupled receptors (GPCRs) are among the most significant drug targets, regulating diverse physiological functions and playing critical roles in numerous diseases. Despite the development of many GPCR-targeted drugs, challenges persist in understanding receptor dynamics, achieving selectivity, and optimizing drug efficacy and safety. Advances in structural biology, molecular pharmacology, and computational modeling have provided more profound insights into GPCR mechanisms, yet translating these discoveries into therapeutics requires continued methodological and technological innovation.

This collection aims to bring together methodological advancements and original research findings that enhance GPCR-targeted drug discovery and characterization. It will cover diverse approaches to ligand screening, receptor structure-function analysis, signaling modulation, and computational strategies for drug design. Contributions exploring GPCR roles in health and disease, novel therapeutic strategies, and interdisciplinary approaches integrating emerging technologies are encouraged.

The collection will provide a platform for knowledge exchange, foster collaboration, and accelerate the development of safer and more effective GPCR-targeted therapeutics. By bridging fundamental research with clinical applications, this collection aims to advance our understanding of GPCR biology and drive innovation in drug discovery.