Current Enzyme Inhibition - Volume 3, Issue 1, 2007

MET (hepatocyte growth factor receptor) and RON (recepteur d'origine Nantaise) are members of the MET proto-oncogene family of receptor tyrosine kinases (RTKs). Signalling from MET or RON activates multiple signalling pathways and ultimately promotes tumorigenesis and the formation of metastases. Mutations in MET have been detected in abundance in squamous cell carcinoma of the head and neck (SCCHN Read More

Lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P) are bioactive lysophospholipid mediators with a wide variety of biological actions. G-protein-coupled receptors for LPA and S1P have been identified, and physiological and pathological significances of the lysophospholipids and their receptors are under intensive investigation. Furthermore, specific agonists and antagonists for the receptors have been developed for cl Read More

In most organisms around 2% of the genes code for peptidases being this number only surmounted by the genes that code for transcriptional factors. This ubiquitous presence is almost unequaled and has for long fascinated biochemists. Although peptidases have been classified in four mechanistic classes (aspartic-, cysteine-, serine- and metallo-peptidases), the more recent MEROPS database recognizes 42 evolutionar Read More

Aldose reductase (E.C. 1.1.1.21), an intracellular enzyme of polyol pathway, catalyzes NADPHdependent reduction of glucose to sorbitol. Under normoglycemia, most of the cellular glucose is phosphorylated into glucose-6-phosphate by hexokinase. A minor part of non-phosphorylated glucose enters the polyol pathway, the alternate route of glucose metabolism. However, under hyperglycemia, because of saturation of Read More

We found that fat-soluble vitamins (i.e., vitamins A, D, E and K) have novel functions such as anticancer activity, and we therefore investigated the inhibitory activity of DNA polymerases (pols) from various species by vitamins and their related compounds. In vitamin A-related compounds, fucoxanthin, astaxanthin (provitamin A), all-trans retinal (vitamin A aldehyde) and all-trans retinoic acid (vitamin A acid) inhibited the acti Read More

The GHMP kinases are a structurally related family of small molecule kinases named after four of its members - galactokinase, homoserine kinase, mevalonate kinase and phosphomevalonate kinase. The group also includes the enzymes N-acetylgalactosamine kinase, arabinose kinase, mevalonate 5-diphosphate decarboxylase, archeal shikimate kinase and 4-(cytidine 5'-diphospho)-2-c-methyl-D-erythritol kinase. In addi Read More