Type I protein arginine methyltransferases (PRMTs) are an attractive target for inhibiting growth of triple-negative breast cancer. Several small-molecule inhibitors of these enzymes are in various stages of preclinical development, while clinical trials of the inhibitor GSK-3368715 had to be terminated early because of poor efficacy and toxicity.
Researchers from Prospect Therapeutics Inc. have discovered PSTA-5204, a novel oral KRAS G12D(ON) inhibitor that exhibits potent in vitro activity, strong in vivo efficacy and high selectivity over wild-type KRAS.
Aurigene Oncology Ltd. recently provided details on the discovery and preclinical characterization of AUR-243, a novel CBL-B inhibitor with a distinct therapeutic profile and best-in-class potential compared to other inhibitors. AUR-243 was described as a structurally distinct, oral small molecule demonstrating excellent potency, functional activity and superior efficacy.
Researchers at Triana Biomedicines Inc. presented the preclinical characterization of TRI-611, a CNS-penetrant molecular glue degrader targeting ALK in models of ALK fusion-positive non-small-cell lung cancer.
Researchers from Chemdiv Inc. and Eilean Therapeutics LLC recently presented preclinical data on ZE77-0273, an AI-designed, reversible pan-EGFR inhibitor developed to address a key unmet need in the treatment of EGFR-mutant non-small-cell lung cancer.
Prospect Therapeutics Inc.’s PSTA-2413 is a newly developed oral pan-RAS inhibitor that demonstrates selectivity over wild-type KRAS, along with strong in vitro potency and in vivo antitumor efficacy.
Loss of FOCAD in cells impairs normal mRNA surveillance, creating a dependency on the HBS1L/PELO complex for ribosome rescue and identifying HBS1L as a potential synthetic lethal target and therapeutic vulnerability.
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.
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