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.
Antibody-drug conjugates (ADCs) are effective anti-cancer agents in a wide variety of solid and hematologic cancers. CD30 (TNFRSF8), a member of the TNF receptor superfamily is the target of antibody drug conjugate Adcetris (brentuximab vedotin/BV, Seagen Inc.) approved for use in multiple CD30-expressing lymphomas.
Researchers from Bridge Biotherapeutics Inc. have presented the discovery and preclinical characterization of BBT-4437, a novel brain-penetrable and reversible pan-transcriptional enhancer factor (TEAD) inhibitor, designed to target the Hippo signaling pathway in solid tumors.
KRAS is a GTP-binding protein involved in cell growth control that requires post-translational farnesylation to be active. KRAS G12D mutations are mostly associated with pancreatic, colorectal and non-small-cell lung cancers and occur less commonly in other cancers. There are currently no therapies approved to specifically target this mutation.
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