KPT-6566 is a Selective PIN1 Inhibitor
PIN1 is a prolyl isomerase, which binds to several proteins, acts as a post phosphorylation control and regulates protein function. PIN1 targets proteins containing phosphorylated S/T-P sites firstly via the…
PIN1 is a prolyl isomerase, which binds to several proteins, acts as a post phosphorylation control and regulates protein function. PIN1 targets proteins containing phosphorylated S/T-P sites firstly via the…
Phospholipase D (PLD) belongs to the phospholipase superfamily, which widely exists in animals, plants, yeast, bacteria, and viruses. In mammalian cells, there are two PLD isoforms, PLD1 and PLD2. The…
The Warburg effect in cancer cells refers to the significant alteration of the glycolytic pathway. It increases the generation of lactate, decreases mitochondrial metabolism of pyruvate, and accompanying with the…
Breast cancer represents an aggressive disease with a high prevalence that can develop invasive capability, then rapidly metastasize to other organs. Breast cancer metastasis is a complex process. The initial…
AP endonuclease 1 (APE1; also known as REF-1) is a dual-function protein. It contains a redox domain and a DNA repair domain. Several human cancers overexpress APE1. Disruption of APE1…
Breast cancer cells usually develop resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). TRAIL shows cancer-selective killing activity. TRAIL ligand selectively kills cancer cells by initiating apoptotic signaling through the…
Phosphoglycerate dehydrogenase (PHGDH) is an essential enzyme catalyzing the synthesis of amino acid serine. PHGDH is important for maintaining the poorly differentiated, stem-like state of cancer stem-like cells (CSLCs). Typically,…
In previous blog “MSX-122 is a Partial Antagonist of CXCR4”, I described MSX-122 as an orally available, specific small molecule antagonist of CXCR4/CXCL12. And it has good anti-inflammatory properties. However,…
Antifolates are a group of antimetabolite agents, which block the functions of folic acid. Folic acid is a cofactor to different kinds of methyltransferases. The latter are related to serine,…
Heat shock protein 70 (Hsp70/HSPA1A) is a molecular chaperone. It plays important roles in protein homeostasis and cell survival. The expression of Hsp70 strongly correlates with tumor grade, metastasis, and…