In This Section

Targeting Gq Signaling in Disease

Sunday April 03, 2022

8:00 am - 9:30 am Eastern Time (ET)



CVP DDD MP

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.

Speakers

Evi Kostenis - Institute of Pharmacobiology, University of Bonn

FR900359: Nature’s Weapon and Treasure Trove for Basic and Translational Research

Natural products have been a rich source of compounds for basic research and drug discovery. One such example is FR900359, a highly selective inhibitor of Gq family proteins. Along with the structurally close analog YM254890, both molecules offer the exciting perspective to interfere with Gq-dependent signaling in health and disease: in health to understand Gq contribution to complex signaling networks, in disease to treat pathologies caused by overactivity of Gq proteins. Dr. Kostenis, a leader in the use of depsipeptides to target Gq, will provide an update on her research in this area.

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.

Talks will be selected from submitted abstracts.

Last Updated: August 31, 2021
Key Dates
 
November 30, 2021

Abstract Submission Deadline

February 7, 2022

Early Registration Deadline

April 2 – 5, 2022

ASPET Annual Meeting at EB 2022

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