Drug discovery and chemical genetic efforts typically focus on the identification and design of inhibitors or loss-of-function probes as a means to perturb enzyme function. These tools are effective in determining the physiological consequence of ablating the activity of a specific enzyme. Remarkably, nearly a dozen examples of non-natural small molecules that activate enzyme catalysis have bee...

Abstract In December 2019, a novel respiratory tract infection, from severe acute syndrome coronavirus 2 (SARS-CoV-2), was detected in China that rapidly spread around the world. This virus possesses spike (S) glycoproteins on surface of mature virions, like other members coronaviridae. The S glycoprotein is crucial viral protein for binding, fusion, and entry into target cells. Binding recepto...

The activity of protein kinase C is reversibly regulated by an autoinhibitory pseudosubstrate, which blocks the active site of the enzyme in the absence of activators. However, before it can be allosterically regulated, protein kinase C must first be processed by three ordered phosphorylations, the first of which is modification of the activation loop catalyzed by the phosphoinositide-dependent...

A rapid method for the preparation of crystalline 5’-adenylic acid deaminase from rabbit skeletal muscle is presented. The enzyme remains bound to cellulose phosphate under conditions at which apparently no other proteins are bound; thus it was possible to develop, in essence, a one-step method for its purification. The crystalline preparation is homogeneous as indicated by its elution profile,...

An enzyme that catalyzes the hydrolysis of folic acid and the antifolate methotrexate nearly 20 times more rapidly than the hydrolysis of 5-methyltetrahydrofolate was extraced from a gram-negative bacterium tentatively identified as a Flavobacterium sp. The enzyme was purified 500-fold and found to have a molecular weight of about 53,000. Apparently a metallo-enzyme, it is inhibited by citrate ...

Following a previous report on physicochemical properties, the enzymological properties of a homogeneously purified preparation of pantothenate synthetase were described. The optimum pH was 10.0 and optimum temperature 30 degrees C. The lyophilized enzyme was very stable on standing at -20 degrees C. K+ or NH4+ and Mg2+ were required as activators; other cations examined were inhibitive to vari...

A rapid method for the preparation of crystalline 5’-adenylic acid deaminase from rabbit skeletal muscle is presented. The enzyme remains bound to cellulose phosphate under conditions at which apparently no other proteins are bound; thus it was possible to develop, in essence, a one-step method for its purification. The crystalline preparation is homogeneous as indicated by its elution profile,...

Ischemia is a blockage of blood supply due to an embolism or a hemorrhage in a blood vessel. When an organ cannot receive oxygenated blood and can therefore no longer replenish its blood supply due to ischemia, stresses, such as the disruption of blood glucose homeostasis, hypoglycemia and hypoxia, activate the AMPK complex. LKB1 and CaMKKβ are essential activators of the AMPK signaling pathway...

NAD malic enzyme (EC 1.1.1.39), which is involved in C(4) photosynthesis, was purified to electrophoretic homogeneity from leaves of Eleusine coracana and to near homogeneity from leaves of Panicum dichotomiflorum. The enzyme from each C(4) species was found to have only one type of subunit by SDS polyacrylamide gel electrophoresis. The M(r) of subunits of the enzme from E. coracana and P. dich...