Copper is an essential trace element with critical roles in several biological processes; therefore, its levels are tightly regulated by multiple mechanisms. Researchers from Sun Yat-Sen University (Guangzhou, China) and collaborators recently described the design of a series of novel copper ionophores with varying n-alkyl chain lengths.
Triple-negative breast cancer (TNBC) lacks hormone receptors and HER2 amplification, limiting the effectiveness of targeted therapies and contributing to its aggressive clinical behavior. As aberrant activation of STAT3 is a key driver of TNBC growth, strategies aimed at suppressing STAT3 signaling are emerging as a potential treatment approach.
The receptor tyrosine kinase-like orphan 1 (ROR1) is a transmembrane protein expressed during embryonic development. Moreover, it is highly expressed on the surface of several cancer cell types, including B-cell malignancies and solid tumors such as triple-negative breast cancer (TNBC). Researchers from The University of Queensland and collaborating institutions recently reported the development of a single-chain fragment variable (scFvs) specifically targeting the membrane proximal region of ROR1 rather than the Ig-like domain, aiming to reduce cross-reactivity with other surface proteins expressed in normal tissues.
Researchers from Chimerix, now part of Jazz Pharmaceuticals, presented preclinical data on ONC-206, a compound that functions as both an agonist of the mitochondrial protease Caseinolytic peptidase P (CLPP) and an antagonist of the G protein-coupled receptor DRD2, in models of triple-negative breast cancer (TNBC).
Triple-negative breast cancer (TNBC) is a highly aggressive subtype affecting 15%-20% of breast cancer patients. TNBC patients harboring breast cancer susceptibility gene 1/2 (BRCA1/2) mutations have shown improved therapeutic response to poly(ADP-ribose) polymerase (PARP) inhibitors (PARPi).
Triple-negative breast cancer (TNBC) is notoriously difficult to treat because it is quite aggressive and the tumors do not express the three major surface hormone receptors that can be targeted with available drugs. A potential target for treating this cancer may be glutathione peroxidase 4 (GPX4), which normally protects cells from ferroptosis, an iron-mediated form of cell death triggered by high oxidative stress.
Bakuchiol, a phenolic meroterpenoid from the seeds of Psoralea corylifolia L., has shown promise as an antitumor drug, so researchers at Bengbu Medical University synthesized novel derivatives of bakuchiol bearing modifications on the aromatic ring.
Triple-negative breast cancer, which accounts for 15-20% of all cases of breast cancer, is particularly difficult to treat. It is driven in part by epidermal growth factor receptor (EGFR), yet EGFR inhibitors that are effective against other cancers somehow fail to be effective against triple-negative breast cancer.
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.
Pinotbio Inc. recently reported a novel antibody-drug conjugate (ADC), named PBX-004, consisting of an ITGB6-targeting antibody conjugated to a potent topoisomerase I (TOP1) inhibitor payload.
