Category: Breast Cancer

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...

ASP4132 is an Orally Active AMPK Activator

Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is an enzyme that plays a role in cellular energy homeostasis. Specifically, it is important in largely to activate glucose and fatty acid uptake and oxidation when cellular energy is low. Besides, AMP or adenosine diphosphate (ADP) levels increase during metabolic stress such...

ZINC69391 is a Specific Rac1 Inhibitor and Apoptosis Inducer

Rho-GTPases are molecular switches that cycle between an inactive GDP-bound form and an active GTP-bound form. Guanine nucleotide exchange factors (GEFs) catalyze nucleotide exchange and mediate activation in this cycle, While GTPase-activating proteins (GAPs) stimulate GTP hydrolysis and inactivate the GTPase. Only the active GTP-bound state binds to downstream...

HSD1590 is Potent ROCK Inhibitor with Low Cell Toxicity

Rho-associated protein kinases (ROCKs) are serine-threonine kinases contain isoforms ROCK1 and ROCK2. ROCK1 and ROCK2 exhibit 60% sequence homology and 90% kinase domain homology. The 2 isoforms exist in many organs/tissues but have different expression levels. ROCK1 mainly expresses in thymus, tongue, spleen, and cervix, et al. ROCK2 exists...

Zotatifin is a Selective and Well-Tolerated eIF4A (Protein Biogenesis) Inhibitor

In this article, we will introduce a potent, selective, and well-tolerated eIF4A inhibitor, Zotatifin. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM). Zotatifin is able to induce the formation of a stable ternary complex [eIF4A-RNA-eFT226]. Additionally, it increases the residence time for...

MK-2206 is an Orally Active and Selective Allosteric Akt Inhibitor

Nasopharyngeal carcinoma (NPC) is a squamous cell carcinoma arising from the epithelium lining of the posterior nasopharynx. In a word, NPC causes very serious health problems in these areas. NPC is highly sensitive to radiation and chemotherapy. However, even with combined radiation and chemotherapy treatment, the prognosis for the...