Surprisingly few GPCR-targeted therapies have been developed for oncology, despite frequent disregulation of the receptors and their signaling mediators that control pro-survival and stress signaling pathways that are important in cancer.

These complex transmembrane receptors control several signaling pathways that are critical for cancer cells and are frequently hijacked by malignant cells. In recent years, researchers have increasingly implicated specific GPCRs as promising therapeutic targets for oncology, resulting in an increased focus on targeting these receptors. There is also an increasing appreciation that pharmacological engagement of GPCRs provides an opportunity to safely block an array of diverse oncogenic signals.

On February 9, 2017, Dr. Joshua Allen of Oncoceutics, Inc. presented a webinar that addressed discovering GPCR targets for oncology therapies.  In this webinar, Dr. Allen walked through:

• Opportunities and challenges for targeting GPCR’s in oncology
• Presented examples of GPCR-targeting investigational therapies for oncology
• Discussed Imipridones, selective GPCR-targeting small molecules, that are in preclinical and clinical development for oncology
• Highlighted how PathHunter^® Screening and Profiling services were used to discover that ONC201 selectively and competitively antagonized DRD2/3 and this was subsequently confirmed using Schild analysis.

In addition to his discussion on ONC201, Dr. Allen also summarized how the PathHunter Screening platform was used to discover ONC212, another imipridone which is a selective agonist of GPR132, an established tumor suppressor in leukemia.

Missed the live webinar?  Watch the recording below!

Want to learn more about the discovery of ONC201?  Read the publication “First-In-Class Small Molecule ONC201 Induces DR5 and Cell Death in Tumor but Not Normal Cells to Provide a Wide Therapeutic Index as an Anti-Cancer Agent“, Allen, et al., Plos One 2015.