On October 9, 2024 BridGene Biosciences, a leader in the discovery of small molecule drugs for traditionally "hard-to-drug" targets, reported it will present three groundbreaking posters at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) 2024 Annual Meeting in Barcelona, on October 25, 2024 (Press release, Bridgene Biosciences, OCT 9, 2024, View Source [SID1234647116]). The posters will showcase the company’s latest advancements in the development of covalent inhibitors for key oncogenic targets, including cMyc, ADAR1, and PAX8, each representing promising new treatment avenues for various cancers.
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"These three presentations represent significant strides in our mission to develop novel therapeutics for cancer patients," said Ping Cao, Ph.D., Co-Founder and CEO of BridGene Biosciences. "By focusing on these high-value, historically hard-to-drug targets, we aim to create first-in-class therapies that address critical gaps in cancer treatment. Our platform continues to unlock new possibilities in drug discovery, and we are excited to share these advancements with the scientific community at AACR (Free AACR Whitepaper)."
BridGene’s work on cMyc, titled "Discovery of a Covalent Inhibitor Targeting the Undruggable Oncogene cMyc," focuses on overcoming the challenges posed by its intrinsically disordered structure, which has historically rendered the protein hard-to-drug. Through its proprietary Isobaric Mass Tagged Affinity Characterization (IMTAC) platform, BridGene identified two hit compounds, which effectively inhibit cMyc signaling. These inhibitors showed potent activity in reducing transcriptional function and offering a potential therapeutic strategy for cancers driven by cMyc amplification, which accounts for nearly one-third of all tumors.
In addition to its work on cMyc, BridGene will present research titled "Discovery of a Novel Covalent ADAR1 Inhibitor," focusing on a novel covalent inhibitor targeting ADAR1, an enzyme that plays a critical role in RNA editing and immune suppression in cancer. By inhibiting ADAR1, BridGene’s compounds, could be expected to enhance the efficacy of immune checkpoint blockade therapies. This research highlights the potential for ADAR1 inhibitors to reshape the tumor microenvironment, paving the way for more effective immunotherapies.
BridGene’s third poster presentation, "Discovery of a Novel Covalent PAX8 Inhibitor," will unveil a covalent inhibitor of PAX8, a transcription factor linked to poor prognosis in renal cell carcinoma and ovarian cancer. Utilizing its IMTAC platform, BridGene discovered a compound that disrupts the DNA binding activity of PAX8. This discovery opens the door to new therapeutic strategies for cancers with elevated PAX8 expression, which have traditionally been difficult to target.