A2A-04 / A2A Pharma, OncoCube Therap - LARVOL DELTA

Isoxazole-pyrimidine derivatives as TACC3 inhibitors: A novel modality to targeted cancer therapy. (PubMed, Bioorg Chem) - "Inhibiting the function of transforming acidic coiled-coil 3 (TACC3) offers a promising therapeutic approach for various cancers, such as breast, ovarian, and lung cancers.Our previous work introduced BO-264 as a novel chemotype for inhibiting TACC3 function, though it exhibited relatively low metabolic stability...13b markedly increased the levels of p-Histone H3 (Ser10), cleaved PARP, and p-H2AX (Ser139), indicative of mitotic arrest, apoptosis, and DNA damage, respectively. In addition, the protein-drug binding assay, DARTS, identified TACC3 as a biologically significant target of 13b, positioning it as an advanced lead compound for further development of clinically relevant TACC3 inhibitors in cancers with elevated TACC3 expression."

Journal • Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • TACC3