Month: October 2021

Cytochalasin B is a Mycotoxin binding to the Barbed end of Actin Filaments

Actin, a family of globular multi-functional proteins, is the most abundant protein in most eukaryotic cells. It forms microfilaments in the cytoskeleton, and the thin filaments in muscle fibrils. Actin participates in many important cellular processes, including muscle contraction, cell motility, cell division and cytokinesis, vesicle and organelle movement,...

Atuveciclib is a Highly Selective and Orally Active PTEFb, CDK9 Inhibitor

Positive transcription elongation factor P-TEFb is a kinase composed of CDK9 and cyclin T. Specifically, P-TEFb plays an important role in the transcriptional regulation of RNA polymerase II (pol II) in eukaryotes. Besides, P-TEFb mediates the positive transcriptional extension of the new mRNA chain by phosphorylating the S2 residue...

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...

Sapanisertib is an Orally Active and ATP-Dependent mTOR Inhibitor

Acute myelogenous leukemia (AML) is a heterogeneous disease. It often relapses after standard chemotherapy or proves refractory to available treatments. Therefore, It needs novel therapies for AML. In AML, many signaling pathways are abnormally activated and lead to uncontrolled proliferation/survival of immature myeloid progenitors. The 50% to 80% of...

Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor

The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...

IACS-010759 is a Potent Inhibitor of Complex I of OXPHOS

Oxidative phosphorylation (OXPHOS) is a metabolic pathway in which cells use enzymes to oxidize nutrients. So it releases the chemical energy stored in nutrients to produce adenosine triphosphate (ATP). Besides, mitochondria are key players in the production and regulation of cellular bioenergy. Most adenosine triphosphate molecules are produced by...