Category: Triple-Negative Breast Cancer

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...

UPGL00004 is a Potent Allosteric and Orally Active Glutaminase C Inhibitor

The Warburg effect in cancer cells refers to the significant alteration of the glycolytic pathway. It increases the generation of lactate, decreases mitochondrial metabolism of pyruvate, and accompanying with the reduction in oxidative phosphorylation. The Warburg effect has a significant consequence. Cancer cells need to develop alternative mechanisms that...

LSN 3213128 is an Orally Active AICARFT Inhibitor

Antifolates are a group of antimetabolite agents, which block the functions of folic acid. Folic acid is a cofactor to different kinds of methyltransferases. The latter are related to serine, methionine, thymidine and purine biosynthesis. Thus, antifolates are able to inhibit cell division, DNA/RNA synthesis and repair as well...

OTS186935 is a Protein Methyltransferase SUV39H2 Inhibitor

SUV39H2 (Suppressor of variegation 3-9 homolog 2), also known as KMT1B, is a member of the SUV39 subfamily of lysine methyltransferases (KMTs). SUV39H2 results in heterochromatin formation and transcriptional repression. In addition, it is report that SUV39H2 methylate histone H2AX at lysine 134 and enhance the formation of phosphorylated...