In This Section

Targeting Gq Signaling in Disease

Sunday April 03, 2022

8:00 am - 9:30 am Central Time (CT)

113 C


Chair :

Jeffrey Benovic
Thomas Jefferson University

The heterotrimeric Gq protein family plays an important role in regulating signaling through a number of effectors. Gq signaling has been implicated in a number of diseases including asthma and uveal melanoma. Several inhibitors have been identified that can effectively and specifically inhibit Gq including constitutively active Gq mutants found in some cancers. The goal of this symposium is to provide: 1) insight into the development of Gq inhibitors that might be used to treat various diseases; 2) insight into the use of Gq inhibitors to treat disease; and 3) mechanistic insight into Gq inhibitor function.


Kirill Martemyanov - The Scripps Research Institute

Exploring pharmacological Inhibition of Gq/11 as an Analgesic Strategy

Kendall Blumer - Washington University

G Protein Inhibitors in Ocular Melanoma: Therapeutic Potential and Challenges

Dr. Blumer and his colleagues are exploring an inhibitor of Gq in ocular melanoma. He will present research describing the effects of the inhibitor in vitro and in vivo, challenges posed by the inhibitor, and efforts to produce inhibitor analogs that address these challenges.  

Philip Wedegaertner - Thomas Jefferson University

Mechanistic Insight into Gq Inhibitors

Natural product, cyclic depsipeptide Gq inhibitors, such as YM-254890 and FR900359, are exciting tools for inhibiting Gq signaling, and they function by locking Gq in the inactive GDP state. Dr. Wedegaertner will discuss a role for Gq localization in the effectiveness of these inhibitors in cells.

Joseph Loomis - University of Michigan

Abstract #2620 - Identifying Novel Signaling Mechanisms Downstream of Gq-Coupled Receptors

Last Updated: March 27, 2022
Key Dates

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