A new series of proteolytic targeting chimeras (PROTACs) was designed by Zhejiang University of Technology scientists based on a previously described PD-L1 inhibitor, and systematic screening of ligands and linkers, combined with structure-activity relationship analysis of the degraders, led to the identification of compounds [I] and [II] as the most active candidates.
Suzhou Ribo Life Science Co. Ltd. recently reported on the development and preclinical characterization of a novel blood-brain barrier (BBB)-penetrating oligonucleotide drug, RBD-8088, for the treatment of glioblastoma.
Researchers from Maruho Co. Ltd. published data regarding the development and preclinical evaluation of a novel orally available bromodomain-containing protein 4 (BRD4) inhibitor for the treatment of melanoma.
Endometrial cancer (EC) accounts for 20% to 30% of most malignant tumors of the female reproductive system, making it one of the most common. Furthermore, the 5-year survival rate of patients with early-stage EC is 90%, but this number decreases to 20% in late-stage disease.
The University of Michigan has identified proteolysis targeting chimeric (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to a CREB-binding protein (CREBBP; CBP) and/or histone acetyltransferase KAT3B (p300)-targeting moiety through a linker. They are described as potentially useful for the treatment of cancer, autoimmune and inflammatory disorders.
Gan & Lee Pharmaceuticals Co. Ltd. has described new S-adenosylmethionine synthase isoform type-2 (Mat2A) inhibitors reported to be useful for the treatment of cancer.
Merck Sharp & Dohme LLC and Otsuka Pharmaceutical Co. Ltd. have patented cellular tumor antigen p53 (TP53) (Y220C mutant) activators reported to be useful for the treatment of cancer.
Zic family member 4 (ZIC4) is a tumor suppressive transcription factor that is epigenetically silenced in many types of cancers. In the current study, researchers from Children's Cancer Hospital Egypt (CCHE) and affiliated organizations investigated the epigenetic regulation function of ZIC4 in pediatric choroid plexus tumors (CPTs).
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have patented indazole compounds acting as membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (PKMYT1) inhibitors reported to be useful for the treatment of cancer.
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