Gain-of-function mutations and overexpression of the EZH2 gene lead to H3K27Me3 accumulation, which in turn initiates tumorigenesis and tumor progression, thus making it a promising target for therapy.
Activin receptor-like kinase 5 (ALK5) is a member of the transforming growth factor-β (TGF-β) family associated with tumor development and progression that impacts cancer immune response within the tumor microenvironment.
Nonselective poly(ADP-ribose) polymerase (PARP) inhibitors have shown antitumoral activity, but they are tied to hematotoxicity, most probably due to PARP2 inhibition. Instead, selective PARP inhibitors retain antitumoral activity without risking PARP2-related toxicity.
Researchers from Zymeworks Inc. recently reported preclinical data for ZW-220, an antibody-drug conjugate (ADC) consisting of humanized IgG1 monoclonal antibody targeting sodium-dependent phosphate transport protein 2B (SLC34A2, NaPi2b) conjugated to a topoisomerase I inhibitor, being developed for the treatment of cancer.
KAT6 is a histone lysine acetyl transferase involved in the epigenetic regulation of oncogenes and it is often dysregulated in cancer, including breast cancer. Inhibiting KAT6 blocks the transcription of genes such as ESR1 and CCND1 and the use of KAT6 inhibitors together with endocrine therapy and CDK4/6 inhibitor therapy may enhance the effectiveness in cancer.
The inhibition of hematopoietic progenitor kinase 1 (HPK1), predominantly expressed in immune cells, has proven effective in reducing tumor growth across cancer immune response modulation.
Data from preclinical studies conducted to evaluate the activity of NKT-3964, a first-in-class, orally bioavailable CDK2-selective PROTAC degrader being developed for the potential treatment of cancer, were reported by Nikang Therapeutics Inc.
SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS, and recent preclinical studies have demonstrated that combining KRAS and EGFR inhibitors with SOS1 inhibitors can overcome resistance and achieve durable responses.
Anti-HER2 antibody-drug conjugates (ADCs) have proven effective in multiple tumor types. However, between 64% and 85% of HER2+ breast and gastric cancer patients retain HER2 expression after treatment with trastuzumab deruxtecan (T-Dxd), which includes a topoisomerase I inhibitor payload.
Nimbus Therapeutics LLC reported the identification of an allosteric, potent, selective, highly efficacious and noncovalent Werner syndrome helicase (WRN) inhibitor, NTX-452, for the potential treatment of microsatellite instability high (MSI-H) tumors.
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