Month: July 2022

Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor

HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because acetylation and de-acetylation can regulate DNA expression. Acetylation is controlled by two antagonistic enzyme families:...

AUTAC4 is a Mitochondria-targeting Autophagy-targeting Chimera (AUTAC).

AUTAC4 is a Mitochondria-targeting Autophagy-targeting Chimera (AUTAC). Besides, AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy. Autophagy-targeting chimera (AUTAC) degrades target proteins via a lysosomal pathway rather than the common proteasome pathway. Besides, One end of AUTAC is a target protein-ligand, the other end is a...

Henatinib is an Orally Active Multikinase Inhibitor with Broad Antitumor Activities

Tumor growth and development involve many complex pathways, such as malignant cell proliferation and angiogenesis. Kinases are the enzymes that control signal transduction in these pathways, including VEGF, PDGFR, c-kit, and so on. They are present in stromal vascular or cell-matrix, and when they are dysfunctional (such as overactivation), they...

PSB-SB-487 is a Potent  GPR55 Antagonist

GPR55 (G protein-coupled receptor 55) is a G protein-coupled receptor that in humans is encoded by the GPR55 gene. GPR55, along with GPR119 and GPR18, are novel cannabinoid receptors. Like the CB receptors, GPR55 belongs to the rhodopsin-like seven transmembranes G protein-coupled receptor (GPCR) superfamily. GPR55 and CB2 receptors...

Tiragolumab is An Immune Checkpoint Inhibitor Binding to T-cell Immunoglobulin and TIGIT

Tiragolumab is a potent TIGIT inhibitor. Tiragolumab alone or in combination with the PD-L1 inhibitor Atezolizumab has effects on solid cancers. Additionally, at two recent medical meetings, the agent achieves statistically significant results in multiple solid malignancies. Especially in small cell lung cancer (NSCLC). Lung cancer is the most...

LDN-211904 is a Potent and Selective EphB3 Inhibitor for Colorectal Cancer Research

LDN-211904  is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. Besides, LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. What’s more, LDN-211904 oxalate with cetuximab could effectively inhibit STAT3-activated CSC stemness and cetuximab resistance in colorectal cancer. LDN-211904 oxalate is a potent EphB3 inhibitor. Besides,...