Proteolysis targeting chimeras (PROTACs) are drugs that use cancer cells’ own proteasome to selectively degrade essential tumor-driver molecules through E3 ubiquitin ligase binding. Resistance to PROTAC therapy in cultured cells has been shown to involve genomic alterations in their E3 ligase targets.
A research team at Deciphera Pharmaceuticals LLC has discovered novel small-molecule colony-stimulating factor 1 receptor (CSF-1R) inhibitors for the treatment of cancer.
A germline change in a single nucleotide increased the risk by up to 6-fold of developing an isocitrate dehydrogenase (IDH) mutant low-grade glioma. The rs55705857 genotype could serve as a biomarker before surgery to identify an early glioma.
Nested Therapeutics Inc. emerged from stealth, revealing $125 million in equity funding and plans to bring precision oncology to the next level by probing the genomics and structural biology of key cancer targets more deeply than before, in an ambitious bid to find new driver mutations, new druggable pockets, and new chemistry that will expand the current arsenal of targeted therapies.
Lifearc and Provincial Health Services Authority (PHSA) have presented 7-morpholino-l,6-naphthyridin-5-yl derivatives acting as DNA-dependent protein kinase (DNA-PK) inhibitors reported to be useful for the treatment of cancer.
Blueprint Medicines Corp. has divulged new EGFR mutant inhibitors, particularly EGFR L858R mutant and EGFR del746-750 mutant, reported to be useful for the treatment of non-small-cell lung cancer.
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