Researchers from Cardiff University have discovered a new class of highly potent and selective inhibitors targeting the LIM domain kinases (LIMKs), a family of enzymes that play a critical role in regulating actin filament turnover. This turnover is involved in the cytoskeletal remodeling, proliferation and migration.
At last week’s American Chemical Society meeting, Novartis AG presented the discovery of IID-432, a highly efficacious and safe inhibitor of Trypanosoma cruzi topoisomerase 2 (Top2), offering a short-duration curative treatment for Chagas disease.
Researchers from Arkansas State University synthesized a library of thiazole derivatives, and these compounds were subsequently screened for their antibacterial activity both in vitro and in vivo.
Hepatocellular carcinomas (HCCs) are challenging to diagnose due to the tumor heterogeneity and unnoticeable early symptoms. Researchers from Anhui Medical University have developed a novel gallium 68 (68Ga)-labeled radiotracer, named [68Ga]DOTA-AngII, designed to improve the precision of HCC imaging.
Endoplasmic reticulum oxidoreductase 1 (ERO1) has traditionally been associated with proper protein folding in the endoplasmic reticulum, but it has recently been linked to platelet activation and aggregation in arterial thrombosis and ischemic stroke.
The sialyltransferase ST6GAL1 is upregulated in several types of cancer and its expression is particularly elevated in triple-negative breast cancer, which is extremely aggressive and associated with very poor prognosis.
Graves disease (GD)-associated hyperthyroidism is an autoimmune disorder characterized by the presence of autoantibodies that stimulate the thyroid-stimulating hormone receptor (TSHR), leading to excessive production of thyroid hormones.
Targeting SHP2 has emerged as a promising approach for treating cancers driven by receptor tyrosine kinases. Although allosteric SHP2 inhibitors have shown strong antitumor activity in preclinical studies, their clinical efficacy as monotherapies has been limited. Recent studies indicate that combining SHP2 inhibitors with kinase inhibitors may enhance treatment effectiveness and help overcome therapeutic resistance.
Neuroinflammation is a common hallmark in several neurodegenerative disorders, including Alzheimer’s and Parkinson’s diseases, among others, where TREM2 (triggering receptor expressed on myeloid cells 2) is a crucial member involved in this biological process and is mainly expressed in microglial cells, being thus an attractive target for diagnostic imaging.
A team of researchers at the University of British Columbia investigated the potential of radiopharmaceutical therapy based on Terbium-161 (161Tb) both in vitro and in vivo using a novel tracer, [161Tb]Tb-BL34L20S, which uses the C-X-C chemokine receptor type 4 (CXCR4)-targeting peptide BL34L20S labeled to 161Tb.
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