A perspective on the discovery of enzyme activators
SLAS Discovery, 2022 Enzyme activation remains a largely under-represented and poorly exploited area of drug discovery despite some key literature examples of the successful application of enzyme activators by various mechanisms and their importance in a wide range of ...
Antonia Turberville +4 more
doaj +1 more source
Iron-Dependent Trafficking of 5-Lipoxygenase and Impact on Human Macrophage Activation
Frontiers in Immunology, 2019 5-lipoxygenase (5-LOX) is a non-heme iron-containing dioxygenase expressed in immune cells that catalyzes the two initial steps in the biosynthesis of leukotrienes.
Beatrice Dufrusine +13 more
doaj +1 more source
Cyclic nucleotide specificity of the activator and catalytic sites of a cGMP-stimulated cGMP phosphodiesterase from Dictyostelium discoideum [PDF]
, 1985 The cellular slime mold Dictyostelium discoideum has an intracellular phosphodiesterase which specifically hydrolyzes cGMP. The enzyme is activated by low cGMP concentrations, and is involved in the reduction of chemoattractant-mediated elevations of ...
Baraniak, Janina, +8 more
core +2 more sources
Scientific Reports, 2023 The assembly state of enzymes is gaining interest as a mechanism for regulating the function of enzymes in living cells. One of the current topics in enzymology is the relationship between enzyme activity and the assembly state due to liquid–liquid phase
Tomoto Ura +7 more
doaj +1 more source
How does conformational flexibility influence key structural features involved in activation of anaplastic lymphoma kinase? [PDF]
, 2014 Anaplastic Lymphoma Kinase (ALK) plays a major role in developing tumor processes and therefore has emerged as a validated therapeutic target. Applying atomistic molecular dynamics simulations on the wild type enzyme and the nine most frequently ...
Adcock +28 more
core +1 more source
Pharmacologic or Genetic Targeting of Glutamine Synthetase Skews Macrophages toward an M1-like Phenotype and Inhibits Tumor Metastasis. [PDF]
, 2017 Glutamine-synthetase (GS), the glutamine-synthesizing enzyme from glutamate, controls important events, including the release of inflammatory mediators, mammalian target of rapamycin (mTOR) activation, and autophagy.
Castegna, Alessandra +12 more
core +5 more sources
Activation of oxidoreductases by the formation of enzyme assembly
Scientific Reports, 2023 Biological properties of protein molecules depend on their interaction with other molecules, and enzymes are no exception. Enzyme activities are controlled by their interaction with other molecules in living cells.
Tomoto Ura +6 more
doaj +1 more source
Substrate specificity and the effect of calcium on Trypanosomabrucei metacaspase 2 [PDF]
, 2013 Metacaspases are cysteine peptidases found only in yeast, plants and lower eukaryotes, including the protozoa. To investigate the extended substrate specificity and effects of Ca<sup>2+</sup> on the activation of these enzymes, detailed ...
Juliano, L. +7 more
core +1 more source
Scanning Electron Microscopic Study of the Tongue Papillae Formation
Central Asian Journal of Medical Sciences, 2017 Objectives: To clarify the morphology of the tongue papillae formation and the metabolic characteristics along the papillae distribution in rats. Methods: The experiment was designed as a cross-sectional study and included; a scanning electron and light ...
Shine-Od Dalkhsuren +2 more
doaj +1 more source
Protein dynamics in the reductive activation of a B12-containing enzyme [PDF]
, 2017 B12-dependent proteins are involved in methyl transfer reactions ranging from the biosynthesis of methionine in humans to the formation of acetyl-CoA in anaerobic bacteria.
Goetzl, Sebastian +6 more
core +1 more source