Category: Colon Cancer

Tivantinib is a Selective c-Met Tyrosine Kinase Inhibitor

c-Met (hepatocyte growth factor receptor, HGFR) is a type of receptor tyrosine kinase which belongs to the MET family.  c-Met exsists in the surfaces of various epithelial cells. Hepatocyte growth factor (HGF) is the ligand for c-Met. HGF belongs to the soluble cytokine family and is also a member...

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Bestatin is a Broad-Spectrum, and Competitive Aminopeptidase Inhibitor

Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein or peptide substrates. Regarding catalytic mechanism, most of the aminopeptidases are metallo-enzymes. In addition, aminopeptidase is widely present in animal and plant kingdomsis widely present in , found in many subcellular organelles, in cytoplasm, and as...

CBL0137 is an Histone Chaperone FACT Inhibitor

Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...

A 83-01 is a Potent Inhibitor of TGF-β Type I Receptor ALK5 Kinase

TGF-β, activin, nodal, and bone morphogenetic proteins (BMPs) belong to the TGF-β superfamily. It regulates a wide range of cellular responses, including cell proliferation, differentiation, adhesion, migration, and apoptosis. TGF-β and related proteins transduce signals through two distinct serine/threonine kinase receptors, including type I and type II. The function...

SN-38 (NK012) is an Active Metabolite of the Topoisomerase I Inhibitor Irinotecan

DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. Top1 binds supercoiled DNA, nicks a DNA strand allowing its rotation around the intact strand, and then relegates the DNA. Camptothecins bind and stabilize the Top1-DNA cleavage complexes, thus...

ML-00253764 is a Brain Penetrant Melanocortin Receptor 4 Antagonist

The involuntary weight loss that occurs as some diseases poses a serious medical problem. For example, sarcopenia, cancer cachexia, rheumatoid arthritis, and hip fractures can lead to involuntary weight loss. The melanocortin 4 receptor (MC4R) plays a key role in body weight regulation and energy homeostasis. The signaling of...