It has been previously demonstrated that the two coding variants in the APOL1 gene (G1 and G2) are associated with a greater risk of progressive, proteinuric kidney disease; however, there currently are no therapies to address the causal genetic drivers of this disease. Researchers from Maze Therapeutics Inc. presented the discovery and preclinical characterization of a novel small-molecule inhibitor of APOL1, MZ-302, and they evaluated its efficacy in a new transgenic model of APOL1-mediated kidney disease (AKD).
Researchers from Aligos Therapeutics Inc. have presented the discovery and preclinical evaluation of a novel next-generation liver targeted PD-L1 small molecule inhibitor, ALG-094103, which is being developed for the treatment of chronic hepatitis B and liver cancer.
A new derivative of coumarin, a natural plant product abundant in cinnamon, could hold the key to healthy aging. Researchers at the Buck Institute have shown that it extended life span and prevented neurodegenerative disease in worms and mice. The drug, a TFEB gene inducer called MIC, promoted mitochondria recycling (mitophagy) but also interacted with lysosomes, which could have multiple applications. The scientists published the results of this aging and mitophagy study on Nov. 13, 2023, in Nature Aging.
G1 and G2 genetic variants of the human APOL1 gene have been previously associated with an increased risk of developing chronic kidney diseases (CKD) in the African American population, and recent studies have shown that inhibition of APOL1 ion channel function could represent a novel therapeutic strategy for the treatment of patients with APOL1-like nephropathies.
The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor involved in tumor initiation, progression, and metastasis whose endogenous ligands are highly expressed in the tumor microenvironment of aggressive tumors.
Antibiotic resistance represents a global threat that leads to high morbidity and mortality. There is an urgent need for new strategies to combat persistent and resistant bacteria.
Researchers from Neophore Ltd. presented the discovery and preclinical evaluation of NP-1867, a small molecule inhibitor of DNA mismatch repair (MMR) protein PMS2, being developed for the treatment of cancer.
Glutaminyl-peptide cyclotransferase-like protein (QPCTL) is a modulator of CD47-SIRPα binding and can be targeted to achieve antitumor responses through myeloid checkpoint blockade. At the recent ESMO meeting in Madrid, researchers from Insilico Medicine Inc. reported the preclinical characterization of ISM-8207, a QPCTL inhibitor with activity against triple-negative breast cancer (TNBC) and diffuse large B-cell lymphoma (DLBCL).
Researchers from Loxo Oncology at Eli Lilly and Co. recently reported the discovery and preclinical evaluation of a new highly potent and selective pan-KRAS inhibitor, LY-4066434, being developed for the treatment of cancer.
Researchers from Hefei Institutes of Physical Science Chinese Academy of Sciences and affiliated organizations have reported the discovery of IHMT-PI3K-455, a novel potent and selective PI3Kγ/δ dual inhibitor as a potential anticancer agent.
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