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.
Mitochondria In Motion Inc. has identified new N-(trans-4-hydroxycyclohexyl)-6-phenylhexanamide derivatives acting as mitofusin activators and reported to be useful for the treatment of Alzheimer’s, Parkinson’s and Huntington’s disease, cancer, amyotrophic lateral sclerosis, stroke, mitochondrial myopathy and Charcot-Marie-Tooth disease, among others.
Regeneron Pharmaceuticals Inc. has patented rapamycin analogues acting as peptidyl-prolyl cis-trans isomerase FKBP1A (FKBP12; Rotamase) ligands reported to be useful for the treatment of Alzheimer’s disease, graft-vs.-host disease, cancer, sarcopenia and more.
Scientists from INSERM and affiliated organizations presented findings from their work that aimed to investigate the involvement of heat shock protein 27 (HSP27) in the activation and pathological accumulation of parietal epithelial cells (PEC) during crescentic glomerulonephritis (CrGN).
The PLN-R14del mutation is often tied to dilated or arrhythmogenic cardiomyopathy, which can progress to end-stage heart failure. Cardiac phospholamban (PLN) plays a crucial role in calcium modulation in cardiomyocytes, which is disrupted by the PLN-R14del mutation.
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).
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