Tag: TNBC

DGY-06-116 is an Irreversible Covalent and Selective Src Inhibitor

Src kinase family is a family of non-receptor tyrosine kinases. DGY-06-116 is a selective Src inhibitor. DGY-06-116 is an SRC-directed covalent kinase inhibitor that displays efficient covalent target labeling and irreversible cellular inhibition of SRC signaling. Furthermore, DGY-06-116 inhibits SRC for an extended duration, likely due to its ability...

LJI308 is a Pan-Ribosomal S6 Kinase (RSK) Inhibitor

The cold shock protein Y-box binding protein-1 (YB-1) is a multifunctional protein. It shows relations in cell proliferation, survival, and stress response. Through translation and transcription of key proteins and regulation of DNA repair, YB-1 performs its functions in different cancers. YB-1 displays overexpression in many tumor entities, especially...

LYN-1604 is a Potent ULK1 Activator

UNC-51 like kinase 1 (ULK1) is the mammalian homolog of ATG1. ULK1 is an autophagic initiator that may decide the subsequent cell fate. In the autophagic process, ULK1 is a component of the ULK complex that is essential for autophagy induction in different types of cancer. Additionally, characterization of ULK1 expression...

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...

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...