Current Enzyme Inhibition - Volume 4, Issue 3, 2008

The discoveries of the pluripotent role of glycogen synthase kinase-3 (GSK-3) are pointing to GSK-3 as a potential target for therapy of neurodegenerative disorders and type 2 diabetes. GSK-3 is a constitutively active protein kinase that is inhibited in response to various extracellular signals. Lithium has been found to be an important inhibitor of GSK-3 activity and its use as a laboratory tool has contributed to the unde Read More

Liver steatosis, or fatty liver, is characterized by the excess accumulation of triglycerides and fatty acids within hepatocytes. This accumulation is marked by an imbalance between the import/synthesis and export/degradation of fat in the liver. Liver steatosis is typically a benign condition, but is associated with severe complications following major liver surgery, as well as the progression of the liver to fibrosis, cirrhosis, and hep Read More

Ezetimibe is the first lipid-lowering drug which selectively inhibits the intestinal uptake of dietary and biliary cholesterol by binding to the cholesterol transporter protein Niemann-Pick C1 Like 1 (NPC1L1). This drug is an effective new tool for cholesterol lowering and allows to better investigate the mechanisms involved in cholesterol absorption by small intestine. Ezetimibe is rapidly absorbed after oral administration and extensively Read More

Enzyme inhibition is a fundamental process to preserve the orderly sequence of events required for life, from seed germination to apoptosis. This review will verse on recent findings showing the various ways in which enzyme inhibition has been incorporated into the arsenal of many organisms, either as an effective defensive weapon or as a factor needed for the establishment of infection, parasitism and/or symbiotic Read More

The chromosome passenger complex (CPC) is composed of five proteins: Aurora B kinase, Borealin, INCENP, Survivin and TD-60. CPC functions as an oligo-enzyme, each member activating the catalytic subunit, Aurora B kinase. CPC controls chromosome congression, bidirectional tension on kinetochores and spindle checkpoint signalling as well as cytokinesis completion. CPC is thus a key regulator during mitosis; CPC proteins Read More