Gain Therapeutics Presents Data at 36?? EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics Demonstrating Identification of Allosteric Inhibitors Targeting DDR2
GT-03842, Identified by the Company’s Magellan Drug Discovery Platform, Effectively Hinders Phosphorylation and Activation of DDR2
GT-03842 May Offer Potential Favourable Therapeutic Attributes for Oncology Compared to Traditional Kinase Inhibitors
BETHESDA, Md., Oct. 23, 2024 (GLOBE NEWSWIRE) -- Gain Therapeutics, Inc. (Nasdaq: GANX) (“Gain”, or the “Company”), a clinical-stage biotechnology company leading the discovery and development of the next generation of allosteric small molecule therapies, today announced the presentation of a poster at the 36th EORTC-NCI-AACR (ENA) Symposium on molecular targets and cancer therapeutics that details the use of the Company’s Magellan drug discovery platform to identify allosteric inhibitors targeting discoidin domain receptor 2 (DDR2). ENA 2024 is being held October 23-25 in Barcelona, Spain.
“We believe the identification of allosteric small molecule inhibitors targeting DDR2 validates the Company’s Magellan platform. Our belief is strengthened that this innovative approach can one day result in much-needed novel therapeutics for people with DDR2-driven malignancies,” commented Joanne Taylor, Ph.D., Senior Vice President of Research at Gain.
The poster, “Identification of allosteric inhibitors targeting Discoidin Domain Receptor 2 (DDR2),” which was presented on-site on October 23 by Sara Cano-Crespo, Ph.D., Senior Scientist of Biology at Gain, detailed how the 3D structure of DDR2 guided a high-throughput virtual screening and subsequent experimental validation that resulted in GT-03842 and additional analogue compounds. Upon binding to collagen, DDR2 undergoes autophosphorylation, triggering its activation and initiating downstream signaling cascades. After conducting a phosphorylation assay based on AlphaLISA with HEK293 cells overexpressing DDR2, GT-03842 and its analogues were found to inhibit DDR2 phosphorylation in a dose-dependent manner.
Aberrant DDR2 phosphorylation is associated with various cancer types and is involved in critical processes in tumor progression, including proliferation, migration, invasion, metastasis, epithelial-mesenchymal transition, and immunotherapy resistance. In a metastatic breast cancer model, GT-03842 also reduced DDR2 phosphorylation. Additionally, GT-03842 inhibits DDR2 activity without targeting the kinase domain, showing the potential to overcome resistance and offer enhanced selectivity and safety compared to traditional kinase inhibitors.
A PDF of the poster presented at the 36th ENA Symposium on molecular targets and cancer therapeutics is available on the Science and Technology section of the Company’s website at https://gaintherapeutics.com/science-and-technology/posters.
About Gain Therapeutics, Inc. Gain Therapeutics, Inc. is a clinical-stage biotechnology company leading the discovery and development of next generation allosteric therapies. Gain’s lead drug candidate, GT-02287 is currently being evaluated for the treatment of Parkinson’s disease with or without a GBA1 mutation. Results from a Phase 1 study of GT-02287 in healthy volunteers demonstrated favorable safety and tolerability, plasma exposure in the projected therapeutic range, CNS exposure, and target engagement and modulation of GCase enzyme.
Gain’s unique approach enables the discovery of novel, allosteric small molecule modulators that can restore or disrupt protein function. Deploying its highly advanced Magellan? platform, Gain is accelerating drug discovery and unlocking novel disease-modifying treatments for untreatable or difficult-to-treat disorders including neurodegenerative diseases, rare genetic disorders and oncology.
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