Exploring Innovative Frontiers: Harnessing Novel Targets for Pain Therapies with Professor Corey R. Hopkins, Ph.D., University of Nebraska Medical Center

Abstract:

Work in the Hopkins Laboratory centers around the synthesis and optimization of novel chemical tool compounds aimed at tackling unmet medical needs.  This talk will cover two projects in my lab: 1. Characterization of novel GIRK1/2 activators for the treatment of neuropathic pain, and 2. The synthesis, optimization and biological characterization of a series of sigma 1 modulators derived from dopamine 4 antagonists and their use in animal models of pain.

GIRK1/2 activators are a class of compounds that can modulate G-protein-coupled inwardly rectifying potassium channels, which are involved in pain signaling pathways. By enhancing GIRK channel activity, these activators have shown potential in reducing pain perception and providing analgesic effects in preclinical animal models. The work presented herein outlines the ongoing structure-activity relationship (SAR) studies centered around a potent, efficacious, and selective positive allosteric modulators (PAM) of the GIRK1/2 channel. Sigma 1 antagonists have gained attention for their potential to modulate pain by blocking the sigma-1 receptor, which is involved in various cellular processes, including pain transmission. Preclinical studies suggest that these antagonists may reduce nociceptive signaling, offering a novel approach to pain management. In the second part, I’ll describe our efforts at the identification of novel dopamine 4 receptor antagonists and how that effort morphed into the discovery of potent and selective sigma 1 modulators.

Biography:

Corey R. Hopkins, Ph.D.
Professor and Interim Chair, Department of Pharmaceutical Sciences
Director, UNMC Center for Drug Design and Innovation
University of Nebraska Medical Center

Dr. Hopkins is a Professor and Interim Chair in the Department of Pharmaceutical Sciences in the College of Pharmacy at the University of Nebraska Medical Center and the Director of the newly designated UNMC Center for Drug Design and Innovation (CDDI). Corey completed his doctorate in 2002 at the University of Pittsburgh in the area of natural product total synthesis and he developed a novel ring expansion methodology to make pharmacophore analogs of dnacin. Dr. Hopkins moved to Aventis Pharmaceuticals in 2001 and later became Senior Research Investigator in Medicinal Chemistry. In 2008, Dr. Hopkins served as Associate Director of Medicinal Chemistry for the Vanderbilt Center for Neuroscience Drug Discovery where he led the chemistry efforts on multiple projects that led to pharmaceutical partnerships and a first-in-class clinical candidates. He is the author of more than 110 peer reviewed articles and an inventor on >25 patents. In addition, he has been named to Stanford/Elsevier’s Top 2% scientist rankings for the past 8 years.

Dr. Hopkins has expertise in medicinal chemistry and drug discovery. Dr. Hopkins’ laboratory focuses on the development of chemical probes to elucidate the mechanisms in therapeutic areas such as pain, Parkinson’s disease and cancer.