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...
AZD4635 (HTL1071) is a Selective and Orally Active A2AR Antagonist
Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes (A1R, A2AR, A2BR, A3R) have been cloned and identified in different tissues. Adenosine receptors play an important role in sleep, the development of cancers and hearing...
Rapamycin is a Specific mTOR Inhibitor
mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...
Nimotuzumab is a Humanized IgG1 Monoclonal Antibody Targeting EGFR
The epidermal growth factor receptor (EGFR) is a transmembrane protein. The dimerization of EGFR stimulates the activity of intracellular protein tyrosine kinase. Therefore, several tyrosine (y) residues in the C-terminal domain of EGFR undergo autophosphorylation. These include y992, y1045, y1068, y1148, and y1173, as shown in the adjacent chart....
GGTI-2154 is a Selective Geranylgeranyltransferase I (GGTase I) Inhibitor
The Ras superfamily of low molecular weight GDP/GTP-binding GTPases is critical in the regulation of many important biological events. They include the cell division cycle, survival and death, differentiation, and development. These GTPases also show a relation with oncogenesis, Ras and Rho proteins mediate malignant transformation, invasion, and metastasis....
LP-261 is a Potent and Orally Active Anti-Mitotic Agent
In this article, we will introduce a potent anti-mitotic agent, LP-261. LP-261 shows inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. Firstly, in vitro, LP-261 exhibits potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01 μM to 0.38 μM. Besides, the...