Researchers from Jiangsu Hengrui Pharmaceuticals Co. Ltd. reported the discovery of SHR-3591, an orally bioavailable AR proteolysis targeting chimera (PROTAC) designed to treat prostate tumors.
PARP inhibitors have been approved for the treatment of several cancers, including ovarian, breast, pancreatic and prostate cancers with BRCA mutations or other homologous recombination repair deficiencies (HRD). However, their therapeutic potential is limited by challenges such as hematologic toxicity and lack of target selectivity.
Programmed cell death protein 1 (PD-1) and vascular endothelial growth factor (VEGF) are often co-expressed in the tumor microenvironment. The combination of anti-PD-1 and anti-VEGF agents has been evaluated in patients with advanced non-small-cell lung cancer, with promising results from agents like ivonescimab, a PD-1/VEGF bispecific antibody.
The transcriptional repressor B-cell lymphoma 6 (BCL6) plays a central role in the development and progression of various B-cell malignancies, particularly diffuse large B-cell lymphoma (DLBCL), where it is associated with poor prognosis and resistance to standard immunochemotherapy.
SMARCA4 and SMARCA2 are essential subunits of the SWI/SNF complex, functioning as ATP-dependent chromatin remodelers that regulate gene expression and maintain cellular homeostasis. Recent research has shown that selectively targeting SMARCA2 is an effective cancer treatment strategy, with several compounds already in early clinical testing.
Aberrant signaling by fibroblast growth factor receptors (FGFRs) drives tumor cell survival and proliferation in several cancers, making them promising therapeutic targets.
Researchers from Violet Therapeutics Inc. presented the discovery of VTT-001, a novel EPHB3 inhibitor designed to target astrocyte-mediated disease mechanisms.
Overexpression of focal adhesion kinase (FAK) has been observed in several types of cancer, including gastric, esophageal and colorectal cancers. Several FAK inhibitors have advanced to clinical evaluation for the treatment of cancer, however, none have entered the market.
The specific tau isoforms, such as 3-repeat (3R) and 4-repeat (4R) isoforms, and the distinct conformational strains that misfolded tau can adopt are determinants of the molecular and clinical heterogeneity observed across tauopathies.
Using its proprietary FBDD platform, Blacksmith discovered FG-2101, the prodrug form of FG-960, the first known non-hydroxamate LpxC inhibitor that exerted activity against LpxC at the nanomolar range.
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