Category: Colon Cancer

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...

AAPK-25 is a Selective and Dual Aurora/PLK Inhibitor

The occurrence of many cancers is due to mismatch of chromosome. It leads to the formation of aneuploidy and incomplete genes, and hence triggering imbalance of cell cycles or divisions in the mitotic phase. Aurora and Polo-like kinases (PLKs) control the G2/M phase in cell mitosis. They are crucial...

BI-882370 is a Novel Orally Active RAF Kinase Inhibitor

Cancers arise owing to the accumulation of mutations in critical genes that alter normal programmes of cell proliferation, differentiation and death. The RAS–RAF–MEK–ERK–MAP kinase pathway mediates cellular responses to growth signals. Three RAF genes code for cytoplasmic serine/threonine kinases. Whereas mutations in ARAF and CRAF are very rare, BRAF...