Category: Colon Cancer

HM03 is a Potent and Selective HSPA5 Inhibitor

Heat shock protein 70 (HSP70) are chaperone proteins that protect proteins from stress and promote nascent polypeptide folding. They exist in both prokaryotic and eukaryotic organisms. The stress-inducible HSP70 is an emerging cancer target that directly inhibits apoptosis. Administration of the inhibitors for HSP90 induces the expression of HSP70....

TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect

Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...

NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity

Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...

MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C

KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...

MN58b is a Selective Choline Kinase α Inhibitor

Choline kinase (CHK) catalyzes the phosphorylation of choline by ATP in the presence of Mg2+, yielding phosphocholine. This enzyme step commits choline to the Kennedy pathway for the biosynthesis of phosphatidylcholine, the major phospholipid constituent in biomembranes. Phosphatidylcholine has an essential structural function as well as serving as a...

FR 180204 is an ATP-competitive and Selective ERK Inhibitor

An extracellular signal-regulated kinase (ERK) is a serine/threonine-protein kinase of the mitogen-activated protein kinase superfamily. Selective inhibition of ERK represents a potential approach for the treatment of cancer and other diseases. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...