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...
ADH-503 is an Orally Active and Allosteric CD11b Agonist
Integrin αMβ2 (CD11b/CD18) is a multifunctional integrin expressed on myeloid cells. In addition, CD11b/CD18 is an integrin molecule and plays an important role in their trafficking and cellular functions in inflamed tissues. Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal malignancy in which very limited responses to immunotherapy have been observed....
PKI-166 is a Selective and Orally Bioavailable EGFR Autophosphorylation Inhibitor
Human pancreatic cancer cells can secrete the proangiogenic molecules, such as VEGF, IL-8, and basic fibroblast growth factor. VEGF is the major proangiogenic factor in most types of human cancer. Therefore, in this article, we will introduce a potent, selective and orally active EGFR tyrosine kinase inhibitor, PKI-166. Firstly,...
FPA-124 is a Selective Akt Inhibitor and Induces Apoptosis
Copper complexes play an important role in the active sites of a large number of metalloproteins in biological systems. Copper complexes also have a potential application for numerous catalytic processes in living organisms. In addition, copper complexes involve electron transfer reactions or activation of some antitumor substances. In this...