Results 21 to 30 of about 130,472 (328)

Novel allosteric inhibition of phosphoribulokinase identified by ensemble kinetic modeling of Synechocystis sp. PCC 6803 metabolism

open access: yesMetabolic Engineering Communications, 2020
The present study attempted a computer simulation of the metabolism of a model cyanobacteria, Synechocystis sp. PCC 6803 (PCC 6803) to predict allosteric inhibitions that are likely to occur in photoautotrophic and mixotrophic conditions as well as in a ...
Hiroki Nishiguchi   +3 more
doaj   +1 more source

Activity modulation and allosteric control of a scaffolded DNAzyme using a dynamic DNA nanostructure. [PDF]

open access: yes, 2016
Recognition of the fundamental importance of allosteric regulation in biology dates back to not long after its discovery in the 1960s. Our ability to rationally engineer this potentially useful property into normally non-allosteric catalysts, however ...
Fan, Chunhai   +7 more
core   +1 more source

Design, Synthesis and Characterization of a New Series of Fluorescent Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulators

open access: yesMolecules, 2020
In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation ...
Víctor Fernández-Dueñas   +6 more
doaj   +1 more source

Allosteric Inhibition of Factor XIIIa. Non-Saccharide Glycosaminoglycan Mimetics, but Not Glycosaminoglycans, Exhibit Promising Inhibition Profile [PDF]

open access: yes, 2016
Factor XIIIa (FXIIIa) is a transglutaminase that catalyzes the last step in the coagulation process. Orthostery is the only approach that has been exploited to design FXIIIa inhibitors.
Afosa, Daniel K.   +4 more
core   +7 more sources

Dynamic allosteric control of noncovalent DNA catalysis reactions [PDF]

open access: yes, 2008
Allosteric modulation of catalysis kinetics is prevalent in proteins and has been rationally designed for ribozymes. Here, we present an allosteric DNA molecule that, in its active configuration, catalyzes a noncovalent DNA reaction.
Winfree, Erik, Zhang, David Yu
core   +1 more source

Light-regulated allosteric switch enables temporal and subcellular control of enzyme activity

open access: yeseLife, 2020
Engineered allosteric regulation of protein activity provides significant advantages for the development of robust and broadly applicable tools. However, the application of allosteric switches in optogenetics has been scarce and suffers from critical ...
Mark Shaaya   +14 more
doaj   +1 more source

Mutations in the PKM2 exon-10 region are associated with reduced allostery and increased nuclear translocation. [PDF]

open access: yes, 2019
PKM2 is a key metabolic enzyme central to glucose metabolism and energy expenditure. Multiple stimuli regulate PKM2's activity through allosteric modulation and post-translational modifications.
Chen, Tsan-Jan   +11 more
core   +3 more sources

Conformational spread as a mechanism for cooperativity in the bacterial flagellar switch [PDF]

open access: yes, 2010
The bacterial flagellar switch that controls the direction of flagellar rotation during chemotaxis has a highly cooperative response. This has previously been understood in terms of the classic two-state, concerted model of allosteric regulation.
F. Bai   +29 more
core   +3 more sources

Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]

open access: yes, 2012
Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Badura, Susanne   +8 more
core   +1 more source

Structurally distributed surface sites tune allosteric regulation [PDF]

open access: yeseLife, 2021
Our ability to rationally optimize allosteric regulation is limited by incomplete knowledge of the mutations that tune allostery. Are these mutations few or abundant, structurally localized or distributed? To examine this, we conducted saturation mutagenesis of a synthetic allosteric switch in which Dihydrofolate reductase (DHFR ...
James W. McCormick   +4 more
openaire   +3 more sources

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