Category: Colorectal Cancer

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...

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...

BI8622 is a HUWE1 Ubiquitin Ligase Inhibitor for Colorectal Cancer

HUWE1 is a colonic tumor suppressor. Especially, HUWE1 is a critical colonic tumour suppressor gene that prevents MYC signalling, DNA damage accumulation and tumor initiation. HUWE1 is a pleiotropic E3 ubiquitin ligase that modulates the function of several proteins involved in oncogenesis and DNA damage response including MYC, MYCN,...

A Potent and Specific Tankyrase Inhibitor RK-287107, Blocks Colorectal Cancer Cell Growth

Wnt/β-catenin signaling is activated in over 90% of human colorectal cancer. In particular, loss-of-function mutations of the tumor suppressor adenomatous polyposis coli (APC), a key negative regulator of Wnt/β-catenin signaling, occur in 90% of patients. The secreted Frizzled-related proteins (sFRPs) and Wnt inhibitory protein (WIF) regulate Wnt/b-catenin signaling. Both...

MRTX-1257 is a KRAS G12C Inhibitor with Antitumor Efficacy

A study from Matthew A. Marx, et al found that, MRTX-1257 is a selective, covalent KRAS G12C inhibitor, with antitumor efficacy. KRAS (K-ras or Ki-ras) is a gene that acts as an on/off switch in cell signaling. During the last several decades, the ability to target and block the...

AZ304, a Dual BRAF Inhibitor Against Cancer

Cancer is the most serious disease in the world. Gene mutation always exhibits in many of human cancers, especially oncogenic BRAF mutations. Non-small cell lung cancer, ovarian cancer, leukaemia, gliomas and other malignancies have had BRAF mutations already. Although several BRAF inhibitors are launched to market, we need to...