Category: Cancer

APS-2-79 is a KSR-Dependent Antagonist of RAF-Mediated MEK Phosphorylation

Deregulation of the Ras-MAPK pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Kinase suppressor of Ras (KSR) is a MAPK scaffold. KSR exhibits allosteric regulation through dimerization with RAF. In this study, researchers developed a class of compounds that...

Retro-2 is a Selective Inhibitor of Retrograde Protein Trafficking

Viruses critically depend on host cellular factors to establish a productive infection. Retro-2 is an inhibitor of endosome-to-Golgi retrograde transport of the plant toxin ricin and bacterial Shiga toxin. However, the efficacy of Retro-2 also has been examined against enveloped viruses, such as filoviruses. As a result, Retro-2 is...

Stafib-1 is the First Selective Inhibitor of the STAT5b SH2 Domain

The transcription factor STAT5A/B controls leukemic cell survival and disease progression. Especially, STAT5B as major STAT5 isoform driving BCR/ABL+ leukemia. Besides, STAT5B enables transformation by suppressing IFN-α/γ, thereby facilitating leukemogenesis. STAT5b might serve as an anticancer target in ductal pancreatic adenocarcinoma. Stafib-1 acts as the first selective inhibitor of...

BIM-23190 is a Selective SSTR2 and SSTR5 Agonist

Somatostatin (SST) is a peptide hormone, which can regulate the endocrine system. Specifically, Somatostatin affects neurotransmission and cell proliferation by interacting with G protein-coupled somatostatin receptors and inhibiting multiple releases. Besides, Somatostatin inhibits insulin and glucagon secretion. Moreover, Somatostatin is produced by neuroendocrine neurons in the hypothalamic extraperitoneal nucleus....

Z-LE(OMe)TD(OMe)-FMK is a Selective Caspase-8 Inhibitor

Cysteine proteases implicate in apoptosis and cytokine processing. Caspase-8 is a member of the cysteine proteases. In particular, Caspase-8 is the molecular switch for apoptosis, necroptosis and pyroptosis. Z-LE(OMe)TD(OMe)-FMK is a selective caspase-8 inhibitor. Besides, Z-LE(OMe)TD(OMe)-FMK shows its antiproliferative and cytotoxic activity via induction of apoptosis. Caspase-8 is the...

BrBzGCp2 is a Glyoxalase 1 Inhibitor, with Antitumor and Neuroprotective Activity

The glyoxalase system is a ubiquitous enzymatic network that plays important role in biological life. The glyoxalase system consists of glyoxalase 1 (GLO1), glyoxalase 2 (GLO2), and reduced glutathione (GSH). They perform an essential metabolic function in cells by detoxifying methylglyoxal (MG). GLO performs an essential metabolic function by...

GW806742X, an ATP mimetic, is a Potent MLKL and VEGFR2 Inhibitor

The pseudokinase Mixed Lineage Kinase domain-like (MLKL) is an essential effector protein in the necroptotic cell death pathway downstream of the protein kinase Receptor Interacting Protein Kinase-3 (RIPK3).  RIPK3–mediated phosphorylation of the activation loop in MLKL trips a molecular switch to induce necroptotic cell death. The structure of mouse MLKL...