GPCR Therapeutics Announces Publication in Nature Scientific Reports on Novel Anticancer Therapy

CXCR4-HRH1 heteromer identified as a potential therapeutic target for anticancer therapy

SEOUL, Korea and REDWOOD CITY, Calif., March 15, 2023 (GLOBE NEWSWIRE) -- GPCR Therapeutics, Inc., a clinical stage, international biopharmaceutical company focused on targeting G Protein Coupled Receptors (GPCR) pairs, announced publication of a paper in Nature Scientific Reports (1), in collaboration with the School of Biological Sciences, Seoul National University (Seoul, Republic of Korea). The paper is entitled ‘Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration.’

CXC chemokine receptor 4 (CXCR4) is a well-known GPCR overexpressed in more than 23 types of cancer and plays an important role in tumor metastasis. The team, led by Professor Won-Ki Huh, shows that another GPCR known as histamine receptor H1 (HRH1) is widely expressed in various cancer cell lines and cancer tissues, and that the level of co-expression of CXCR4 and HRH1 is related to poor prognosis in breast cancer patients. The simultaneous expression of both receptors leads to the formation of CXCR4-HRH1 heteromer, and this complex demonstrates enhanced signalling and migration capabilities.

These findings suggest the interaction of CXCR4 and HRH1 may play an important role in cancer progression, thus serving as a potential therapeutic target for anticancer therapy.

Dr. Michel Bouvier, a world-renowned expert in the field of GPCRs working as a professor and CEO at the Institute for Research in Immunology and Cancer (IRIC) at Université de Montréal said, “This paper shows that the co-expression of the CXCR4 chemokine receptor and the H1 histamine receptor is associated to a poor prognostic and shorter overall and progression-free survival in breast cancer patients. This synergism between CXCR4 and HRH1 was observed not only in breast cancer cells but also in other cancer cells in which both receptors are expressed, suggesting a possible generalization of this cross-talk mechanism in oncogenesis. The observation that CXCR4 and HRH1 can form heterodimers in live cells suggest that such heterodimerization may underlie the observed synergism between the two receptors and open the possibility of targeting such heterodimer for the development of anti-cancer drugs.”

“We are on a scientific journey to find more efficacious cancer treatments, delivering better patient outcomes,” commented Dr. Dong Seung Seen, GPCR’s founder and CEO. “We believe understanding the interactions between GPCRs is the key to overcoming the current hurdles of drug discovery. This publication is significant as it represents the first case for our co-targeting drug development strategy to be peer-reviewed and validated in academia. In addition to the ongoing combination treatment program using a CXCR4 inhibitor, GPC-100, and an ADRB2 inhibitor, Propranolol, we plan to expand our pipeline by targeting the interaction of CXCR4 and other GPCRs in the development of anticancer drugs."

GPCR recently announced the launch of a US phase 2 trial of GPC-100 in combination with Propranolol for stem cell mobilization in patients with multiple myeloma (2).


(1) Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration:


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About GPCR Therapeutics

GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.

GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for multiple solid tumors as well as hematological malignancies. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, and has demonstrated safety and efficacy in US Phase 2 clinical trial. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation. This combination therapy is currently undergoing Phase 2 clinical trial in the US. The company is collaborating with Australia’s AdAlta on novel cancer therapeutics.

GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit and follow us on LinkedIn.