Biopsies from up to 14% of patients with non-small-cell lung cancer (NSCLC) showing resistance to epidermal growth factor receptor (EGFR) tyrosine kinase therapy ascertain histologic transformation (HT) to SCLC, which is estimated to kill around 250,000 patients globally, every year. In a study published in Science on Feb. 9, 2024, researchers from Weill Cornell Medicine have dissected that complex process using a genetically engineered mouse model of pulmonary HT.
Bruton tyrosine kinase (BTK) enzyme inhibitors used to treat B-cell cancers, including chronic lymphocytic leukemia and non-Hodgkin lymphoma, also produce resistance by causing mutations in the protein. Now, a study on the BTK degrader NX-2127 showed the compound could be effective in eliminating BTK regardless of its mutations.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have patented phosphorylpurinone compounds acting as Toll-like receptor 7 (TLR7) agonists reported to be useful for the treatment of cancer.
Incyte Corp. has developed fused tricyclic compounds acting as GTPase KRAS (mutant) inhibitors. As such, they are reported to be useful for the treatment of cancer, inflammation and immunological disorders.
Protein arginine N-methyltransferase 5 (PRMT5) inhibitors have been disclosed in an Abbisko Therapeutics Co. Ltd. patent and described as potentially useful for the treatment of cancer.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have described new 5’-nucleotidase (CD73) inhibitors reported to be useful for the treatment of cancer.
Researchers from National Taiwan University combined the structural features of purine-type microtubule-disrupting compounds and histone deacetylase (HDAC) inhibitors, which led to the discovery of a novel series of dual-targeting compounds, with the purine-hydroxamate conjugate [I] selected as the lead candidate.
Mitochondrial DNA (mtDNA) is comprised of two strands, the light and the heavy one. The latter is rich in guanine and tends to form G-quadruplexes (mtG4s) which are more prevalent in cancer cells and are considered an emerging therapeutic target in cancer treatment.
Eli Lilly & Co. has selected FHD-909, a first-in-class oral BRM-selective inhibitor, for clinical development from its 2021 collaboration with Foghorn Therapeutics Inc. Lilly plans to file an IND for FHD-909 in the second quarter of this year. The primary target patient population is BRG1-mutated non-small-cell lung cancer.
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