Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...
YUM70, a Selective GRP78 Inhibitor, Induces ER Stress-Induced Apoptosis
GRP78 (Glucose-regulated protein, 78 kDa) is a key regulator of endoplasmic reticulum (ER) stress signaling. In this study, researchers describe the discovery of a series of GRP78 inhibitors. YUM70 is an ER stress inducer and kills cells by activating the apoptosis pathway. Especially, YUM70 treatment induces ER stress and...
AES-135 is a Potent HDAC Inhibitor
Pancreatic cancer is cancer that’s found anywhere in the pancreas. Histone deacetylases (HDACs) regulate the post-translational modification of histones and consequent gene expression. HDACs act as transcriptional repressors and overexpress in several types of cancer, including pancreatic cancer. HDAC inhibitors are effective in killing pancreatic cancer cells. In this...
Senaparib is a Selective and Orally Active PARP1/2 Inhibitor
Poly(ADP-ribose) polymerase (PARP) is an important protein in DNA repair pathways especially the base excision repair. . PARP proteins compose of two ribose moieties and two phosphates per unit polymer. PARP inhibitors represent a successful example of precision medicine as the first drugs targeting DNA damage response to have...
ZZW-115, a NUPR1 Inhibitor, Possesses Anticancer Activity via Inducing Necroptosis and Apoptosis
NUPR1 is an intrinsically disordered protein (IDP) with an entirely disordered conformation. It binds to DNA in a manner similar to other chromatin proteins to control the expression of gene targets. At the cellular level, NUPR1 participates in many cancer-associated processes, including cell-cycle regulation, apoptosis, senescence, cell migration and...
PIK-75 is a Reversible DNA-PK and p110α Selective Inhibitor
PI3Ks catalyze the phosphorylation of the D-3 position of the inositol headgroup of phosphatidylinositol leading to the synthesis of second messengers PtdIns3P, PtdIns(3,4)P2, PtdIns(3,5)P2 and PtdIns(3,4,5)P3. The p110α and p110β are the main forms in insulin target tissues. Especially, p110α isoform (PIK3CA) plays the predominant role in insulin signaling....
AGN194204 is an Orally Active and Selective RXR Agonist
Rexinoids are selective ligands for the retinoid X receptors (RXRα, RXRβ, and RXRγ). Specifically, rexinoids are multifunctional drugs that are useful for both the prevention and treatment of lung and breast cancer in preclinical animal models. Besides, retinoid X receptors heterodimerize with other receptors in the nuclear receptor superfamily. They modulate the activities of numerous steroid-like...