Fructose-1, 6-bisphosphatase (FBPase), a rate-limiting enzyme involved in the pathway of gluconeogenesis, can catalyze the hydrolysis of fructose-1, 6-bisphosphate to fructose-6-phosphate. Upon inhibiting the activity of FBPase, the production of endogenous glucose can be decreased and the level of blood glucose lowered. Therefore, inhibitors of FBPase are expected to be novel potential therapeutics for the treatment of type II diabetes. Recent research efforts were reviewed in the field of developing allosteric inhibitors interacting with the AMP binding site of FBPase.
Adenosine Monophosphate ; chemistry ; Allosteric Site ; Animals ; Binding Sites ; Blood Glucose ; metabolism ; Diabetes Mellitus, Type 2 ; blood ; Enzyme Inhibitors ; chemistry ; pharmacology ; Fructose-Bisphosphatase ; antagonists & inhibitors ; chemistry ; metabolism ; Fructosediphosphates ; metabolism ; Fructosephosphates ; metabolism ; Humans

Glutamate receptor channels have been classified into three major subtypes, the alpha-amino-3 - hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), kainite and N-Methyl-D-aspartate (NMDA) receptor channels. The NMDA receptor channel differs in fundamental ways from the non-NMDA receptor channels, and these properties relate directly to its physiological roles. NMDA ion channels play important roles in various physiological or pathologic functions in neuroprotection, neurodegeneration, long-term potentiation, memory, cognition, neurological disorders, psychiatric disorders, and neuropathic pain syndromes. The NMDA receptor channel is gated in a unique manner both by ligands and by voltage. The voltage dependence is caused by Mg2+ block within the ion channel. The NMDA receptor is highly permeable to Ca2+ unlike most other ions. In addition, it can be modulated at a number of sites other than glutamate recognition site. Among these sites, an allosteric site through glycine modulates the NMDA response. The molecular cloning and diversity of the NMDA receptor channel have been identified. The mechanisms that control the opening and closing, or gating, of the channel of NMDA receptors are among the most basic determinants of receptor function, and yet are not well understood. This review summarizes from a molecular perspective the recent advances in our understanding of the pharmacological properties of NMDA receptor channels.
Allosteric Site ; Cloning, Molecular ; Cognition ; Diethylpropion ; Glutamic Acid ; Glycine ; Ion Channels ; Ions ; Ligands ; Long-Term Potentiation ; Memory ; N-Methylaspartate ; Nervous System Diseases ; Neuralgia ; Polymethacrylic Acids ; Propionates ; Receptors, N-Methyl-D-Aspartate