A loss of allosteric
regulation on the CBS enzyme activity by AdoMet was found to increase the homocysteine level .
He adds that the technique could be applied not only to protein folding intermediates, but any conformational change in proteins including allosteric
transitions and macromolecular assembly.
Thus it provides a simple and convenient method to describe both negative and positive allosteric
moderation of (biological) reaction networks.
Cambridge, Mass.-based Anchor Therapeutics announced the publication of new research that describes the identification and characterization of a pepducin-based allosteric
agonist that targets CXCR4, a chemokinc G protein-coupled receptor (GPCR) found on hematopoietic stem cells and other bone marrow-derived cells.
Chapters deal with pharmacological subjects such as allosteric
modulators, receptor dimerization, GPCR deorphanization, G protein activation, and the Frizzled family; methods to screen GPCR using biochemical techniques, cell phenotype, resonance energy transfer, label-free detection, and ultra-high-throughput screening; new ways to express and crystallize the receptors; computational studies such as modeling and rational drug design; and the use of pharmacological chaperones for diseases caused by GPCR mutations.
regulation of enzyme activity is widely used by living cells to control diverse physiological processes [1,2].
Eszopiclone is a non-benzodiazepine type allosteric
GABA agonist discovered by Sepracor.
The Ii-Key motif from the Ii protein acts at an allosteric
site adjacent to the MHC class II antigenic peptide-binding trough to enhance presentation of covalently linked epitopes 200-500 times in vitro.
The topics covered in the subsequent chapters include characterization of enzyme activity by the equilibrium and steady-state models; reversible, irreversible, and mechanism-based (alternate and suicide inhibition) enzyme inhibition; effects of pH on enzyme reactions; mechanisms of enzyme reactions; two- and multisubstrate reactions; immobilized, interfacial, and allosteric
enzymes; transient phases of enzyme reactions; and enzyme stability.
This platform allows us to identify novel pharmacologically active compounds, such as inverse agonists and allosteric
modulators, that regulate GPCR function," stated Dominic Behan, one of Arena's founders and Vice President, Research.
The oxygen binding affinity of natural human hemoglobin is too high when it is free in the blood stream (not contained within erythrocytes) because of a lack of allosteric
This property is allostery, and a protein is allosteric
if it can increase or decrease its ability to participate in a reaction.