Work at Acelink Therapeutics Inc. has led to the identification of Kelch-like ECH-associated protein 1 (Keap1)/Nrf2 interaction inhibitors reported to be useful for the treatment of cancer, lung, mitochondrial and sickle cell diseases, cardiovascular, inflammatory, neurological and renal disorders.
The c-MYB oncogene plays a key role in hematopoietic cell differentiation and proliferation. Genetic abnormalities and dysregulation of MYB have been found in several cancers, including adenoid cystic carcinoma (ACC) (80% of cases), making it an attractive druggable target for ACC treatment.
PARP1 is critical for repairing DNA single-strand breaks. First-generation PARP1/2 inhibitors have proven effective in the treatment of tumors with mutations in the essential homologous recombination repair (HR) genes including BRCA mutations. However, hematological toxicity associated with PARP2 emphasizes the need to find second-generation compounds with better safety profiles.
Researchers from Abbisko Therapeutics Inc. presented the preclinical characterization of ABSK-141, a potent bioavailable small-molecule KRAS G12D inhibitor.
Researchers from Astrazeneca plc recently reported preclinical data for AZD-3470, a second-generation MTA-cooperative PRMT5 inhibitor currently in early clinical development for the treatment of patients with MTAP-deficient solid tumors (NCT06130553) and hematological cancers (NCT06137144).
Researchers from Liaoning Jinqiu Hospital and affiliated organizations explored potential new genetic targets in heart failure and breast cancer through combining genetic inference and single-cell expression analysis. Genome-wide association study (GWAS) identified multiple genetic variants that were causally related in heart failure and breast cancer.
Biosplice Therapeutics Inc. has discovered dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitors reported to be useful for the treatment of cancer, diabetes and Alzheimer’s disease.
Researchers from Mariana Oncology Inc. reported preclinical data on MC-339, a DLL3-targeting macrocyclic peptide in several tumor models. Delta-like ligand 3 (DLL3) is overexpressed on the cell surface of small-cell lung cancer (SCLC), neuroendocrine prostate cancer (NEPC) and metastatic melanoma.
Bruton tyrosine kinase (BTK) inhibitors are commonly used in the treatment of hematological cancers. However, approximately 67% of patients with relapsed chronic lymphocytic leukemia (CLL) develop resistance to acalabrutinib and ibrutinib due to mutations in BTK, initially most often C481S.
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