PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket
Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...
E3330, an APE1 Redox Inhibitor, Modulates Cell Migration and Invasion in Metastatic Cancer
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 function has detrimental effects on cancer cell viability. Furthermore, APE1 implicates in the transactivation of numerous seminal transcription factors involved...
TPCA-1, a Direct Dual Inhibitor of STAT3 and NF-κB, Regresses Mutant EGFR-Associated NSCLC
In previous blog, “TPCA-1, a Selective IKK-2 Inhibitor, Alleviates Rheumatoid Arthritis”, we identified TPCA-1 as a selective IKK-2 Inhibitor that alleviates rheumatoid arthritis. Today, I’d like to introduce the anti-tumor activity of TPCA-1. A study from Jing Nan identified that TPCA-1 is a direct dual inhibitor of STAT3 and...