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.
Researchers from Nankai University and collaborating institutions have identified a novel proteolysis targeting chimera (PROTAC) molecule that effectively and selectively degrades multiple cyclin-dependent kinases (CDKs) to inhibit the proliferation of triple-negative breast cancer (TNBC) cells, offering a potential targeted therapy for this form of breast cancer.
Taxanes such as paclitaxel are among the standard chemotherapies for triple-negative breast cancer, one of the most aggressive forms of this tumor type. However, numerous processes can contribute to paclitaxel resistance. As a next-generation drug that could help overcome such resistance, researchers at six universities in China, including Ningxia Medical University, examined the crystal structure of protein arginine methyltransferase 1 (PRMT1) and developed, in silico, a pharmacophore that could bind tightly to it. PRMT1, which acts as an epigenetic regulator, is overexpressed in various cancers and its levels correlate inversely with survival.
Forx Therapeutics AG presented data on their PARG inhibitor – FORX-428 – for the treatment of cancer. FORX-428 is a highly potent, selective and orally bioavailable PARG inhibitor that showed strong and reversible binding to the catalytic domain of the human PARG enzyme.
Breast cancer accounts for nearly one-third of all cancers in women, and one of the most aggressive subtypes is triple-negative breast cancer (TNBC). Researchers at Nanjing University and Nantong University developed the β-carboline derivative [I] and showed that it inhibited the growth of various types of TNBC cells in culture as well as growth of TNBC 4T1 xenografts in mice.
