CXC chemokine receptor 4 (CXCR4) is a receptor overexpressed in several tumor types and associated with tumor aggressiveness and risk of metastasis, resistance and recurrence. A novel PET radiopharmaceutical tracer and CXCR4 ligand, [68Ga]NOTA-R-54, was developed and tested for potential use in the treatment of lung cancer.
Recent evidence suggests the gastrin/cholecystokinin-2 receptor (CCK2R) is a potential target for radiolabeled theranostics in cancer, but the stability of minigastrin analogues remains unresolved. Researchers from the National University of Singapore aimed to develop a peptide with improved tumor uptake and prolonged retention in CCK2R+ cancers.
Researchers from Opko Health Inc. and Entera Bio Ltd. recently presented preclinical pharmacokinetic data on OPK-8801003, an oral GLP-2 analogue developed for the treatment of short bowel syndrome.
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.
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.
RSS
