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GPCR Therapeutics Announces Publication in PNAS Using Cutting Edge Spectroscopy to Detect GPCR Heteromers on Live Cancer Cells
[April 01, 2024]

GPCR Therapeutics Announces Publication in PNAS Using Cutting Edge Spectroscopy to Detect GPCR Heteromers on Live Cancer Cells


GPCR Therapeutics, Inc., a clinical-stage, international biopharmaceutical company, is pleased to announce the publication in the esteemed scientific journal, Proceedings of the National Academy of Sciences (PNAS) that was spearheaded by Dr. Niña Caculitan, Director of Clinical Development.

This research underscores the company's commitment to targeting diseases with cutting-edge approaches against GPCRs and discovering novel therapeutics. Detection of multimeric complexes by CXCR4 with other GPCRs in a live-cell environment validates the dual GPCR targeting hypothesis. The paper, authored in collaboration with Prof. Adam Smith, Associate Professor at Texas Tech University, is titled "The ß2-adrenergic receptor associates with CXCR4 multimers in human cancer cells."

Both CXCR4 and ß2AR receptors play active roles in oncogenesis. The work uses time-resolved fluorescence spectroscopy to quantify CXCR4 and ß2AR interactions as they form complexes in live cells under physiological conditions. Differential propensities of GPCRs to cluster in non-cancer versus cancer cell lines was observed, suggesting that GPCR multimerization is significantly affected by the plasma membane environment. Furthermore, the ligand for ß2AR, epinephrine, increases the CXCR4-ß2AR heteromerization. Thus, antagonizing its binding could decrease heteromerization and may have therapeutic benefits that can be missed by targeting only CXCR4. This supports the development of new drugs to treat CXCR4-positive cancers using combination therapies.



Dr. Dong Seung Seen, Founder and CEO of GPCR Therapeutics based in Seoul, spoke about Dr. Caculitan's accomplishments. "Dr. Caculitan represents the highest ideals that our entire team strive for. It is this level of understanding complex science that will lead us to success with the unique approach upon which our company was founded."

References:
(2024). The ß2-adrenergic receptor associates with CXCR4 multimers in human cancer cells. Proceedings of the National Academy of Sciences, 121(14), e2304897121.
https://doi.org/10.1073/pnas.2304897121


About GPCR Therapeutics

GPCR Therapeutics, Inc. is a clinical-stage biopharmaceutical company developing therapeutics built on its proprietary GPCR data. GPCR Therapeutics has its HQ in Seoul and a subsidiary in the San Francisco Bay Area, USA. The company's lead asset, GPC-100/Burixafor, targets CXCR4. GPCR has a US phase 2 trial of GPC-100, G-CSF and Propranolol, a beta blocker, for stem cell mobilization in multiple myeloma patients (NCT05561751). For more information, please visit gpcr.co.kr and follow us on LinkedIn.


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