Targeted protein degradation (TPD) is an alternative to conventional protein inhibition that is gaining attention due to advantages such as ensuring complete elimination of the target protein, reduced off-target effects or the potential to target previously inaccessible or “undruggable” proteins. Proteolysis targeting chimeras (PROTACs) are agents used for TPD that have proven effective for degradation of histone deacetylase (HDAC), among other different proteins.
Aptamers are single-stranded DNA or RNA molecules with unique 3D structures that allow for specific binding to a wide variety of ions and molecules. Due to their unique properties, aptamers have been extensively studied for the precise detection and treatment of cancer; however, their susceptibility to nuclease degradation and rapid renal clearance represent challenges that limit theranostic time window and effectiveness. Researchers from Huazhong University of Science and Technology evaluated the potential of a novel albumin-conjugation strategy that would improve tumor targeting of the aptamers.
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has described molecular glue compounds acting as eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) degradation inducers reported to be useful for the treatment of cancer.
Chengdu Chipscreen Pharmaceutical Ltd. has synthesized protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of cancer.
Sunshine Lake Pharma Co. Ltd. has disclosed poly(ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of cancer.
Elevated expression of DHX9 has been reported in multiple cancer types and it is associated with poor prognosis. In a recently published study, researchers from Accent Therapeutics Inc. evaluated aimed to assess the role of DHX9 in cancer using the tool compound ATX-968, designed as a potent and selective small-molecule inhibitor of DHX9.
Io Biotech Aps has presented preclinical data regarding their Arg1-derived peptide cancer vaccine IO-112 as a potential immunotherapeutic that would allow controlling the tumor microenvironment.
Researchers from Tianjin University have published data regarding development and preclinical characterization of a new anti-PD-L1/CD40 bispecific antibody (BsAb), BA-4415, designed to activate CD40 signaling specifically in the context of PD-L1 while simultaneously blocking PD-1/PD-L1 signaling.
Epitopea Ltd. has signed a license and research collaboration agreement with MSD (Merck & Co. Inc.) to identify Cryptigen tumor-specific antigens in an undisclosed solid tumor. Cryptigen TSAs are shared, nonmutated, aberrantly expressed antigens that are derived from what were thought to be noncoding regions of the genome.
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