Category: Triple-Negative Breast Cancer

SP-146 is a Selective and non-ATP-Competitive Aurora B Inhibitor

Aurora B Kinase is a serine-threonine kinase and plays an important role in mitosis. This kinase also plays an important role in mitosis as a serine-threonine kinase. It also a part of the chromosomal passenger complex (CPC).  Overexpression of Aurora B has been reported in several cancers, such as...

HJC0416 is a Highly Potent and Orally Active STAT3 Inhibitor

Signal transducer and activator of transcription 3 (STAT3) is involved in the regulation of early embryonic development, angiogenesis, immune response, cell proliferation, and apoptosis. Additionally, STAT3 overexpresses in many cancers. As a result, it becomes an attractive therapeutic target for various cancer treatment studies. However, despite much intensive researches...

Targapremir-210, a Selective miR-210 Inhibitor, Targets the Dicer Site in Pre-miR-210

Hypoxia is a non-physiological level of oxygen tension, a phenomenon common in a majority of malignant tumors. Hypoxia associates with tumor progression, resistance to therapy, and metastasis in cancer. Numerous pathways play critical roles in cancer maintenance, including noncoding RNAs such as microRNA (miR)-210 that regulates hypoxia-inducible factors. In...

Telaglenastat is a Selective and Orally Active Inhibitor of Glutaminase 1

Tumor cells use a variety of oncogenically- and environmentally driven metabolic pathways. That aims to meet the bioenergetic and biosynthetic demands of rapid and sustained growth. One of the key nutrients is the amino acid glutamine. It is the most abundant amino acid in plasma. Small-molecule inhibitors, suppressing the...

SR-4835 is a Highly Selective and ATP Competitive Dual Inhibitor of CDK12/CDK13

Breast cancer is the most frequently diagnosed cancer of women worldwide. The feature of triple-negative breast cancers (TNBCs) is the absence of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor 2 receptor (HER2/ERBB2) overexpression. Although early-stage TNBC responds well to treatment, the advanced disease is worse overall...

PK11007, an Anti-p53 drug for TNBC Treatment, Reactivates Mutant p53

The p53 function in cell cycle arrest, DNA repair, senescence and apoptosis induction in response to mutagenic stimuli, and, to exert those functions, p53 acts as a transcriptional factor. P53 is a transcription factor able to regulate several intracellular pathways involved in cell survival, DNA-repair, apoptosis, and senescence. Most...

MS645, a Bivalent BET BrD Inhibitor, Inhibits BRD4 Transcriptional Activity

Bromodomains (BrDs) in transcription proteins bind acetyl-lysine in histones and transcription factors to direct gene transcription in biology and disease conditions.  BRD4 contains two characteristic tandem BrDs. Meanwhile, BRD4 is a major drug target owing to its implicated functions in oncogenesis and inflammation. BET protein BRD4 in gene transcription...