Results 61 to 70 of about 151,004 (296)

Allosteric modulators targeting GPCRs

open access: yes, 2020
The remarkable precision of the pharmacological modulation, including high degree of specificity, probe dependence, and signaling bias, confers to GPCR allosteric modulators unique advantages over orthosteric classical ligands.
María L. López-Rodríguez   +5 more
core   +1 more source

Evolutionarily Conserved Allosteric Communication in Protein Tyrosine Phosphatases [PDF]

open access: yes, 2018
Protein tyrosine phosphatases (PTPs) are an important class of regulatory enzymes that exhibit aberrant activities in a wide range of diseases. A detailed mapping of allosteric communication in these enzymes could, thus, reveal the structural basis of ...
Michael K., Hjortness   +6 more
core   +2 more sources

Deciphering the Allosteric Process of Phaeodactylum tricornutum Aureochrome 1a LOV Domain [PDF]

open access: yes, 2020
The conformational-driven allosteric protein diatom Phaeodactylum tricornutum aureochrome 1a (PtAu1a) di ers from other light-oxygen-voltage (LOV) proteins for its uncommon structural topology. The mechanism of signaling transduction in PtAu1a LOV domain
Francesco, Trozzi   +3 more
core   +1 more source

The Shewanella oneidensis Fic enzyme SoFic targets the switch‐I region of EF‐Tu for AMPylation

open access: yesFEBS Letters, EarlyView.
Fic enzymes mediate diverse post‐translational modifications across all domains of life, including AMPylation. Prokaryotic EF‐Tu can be AMPylated and deAMPylated by the conserved Fic enzyme SoFic. Structural and biochemical approaches were used to characterize the effect of AMPylation on EF‐Tu, SoFic's enzymatic activities, and the enzyme‐target ...
Svenja Runge   +6 more
wiley   +1 more source

The positive allosteric modulator of NMDA receptors, GNE‐9278, blocks the ethanol‐induced decrease of excitability in developing retrosplenial cortex neurons from mice

open access: yesNeuropsychopharmacology Reports, 2023
Binge‐like exposure to ethanol during the brain growth spurt triggers apoptotic neurodegeneration in multiple brain regions, including the retrosplenial cortex, a brain region that is part of the hippocampal‐diencephalic‐cingulate memory network. This is
Clark W. Bird, Carlos F. Valenzuela
doaj   +1 more source

Prospecting the protein design landscape

open access: yesFEBS Letters, EarlyView.
This review outlines the current state of various protein design approaches. We discuss the current possibilities enabled by recently released tools, highlight future avenues to pursue in protein design, and underscore the crucial role of key databases and resources for successful protein design workflows.
Jakob R. Riccabona   +4 more
wiley   +1 more source

Schild Analysis of the Interaction between Parthenolide and Cocaine Suggests an Allosteric Relationship for Their Effects on Planarian Motility

open access: yesBiomolecules
The freshwater planarian is an emerging animal model in neuroscience due to its centralized nervous system that closely parallels closely parallels the nervous system of vertebrates.
Jyothi Kakuturu   +2 more
doaj   +1 more source

Coevolution-based prediction of key allosteric residues for protein function regulation

open access: yeseLife, 2023
Allostery is fundamental to many biological processes. Due to the distant regulation nature, how allosteric mutations, modifications, and effector binding impact protein function is difficult to forecast.
Juan Xie   +4 more
doaj   +1 more source

Supramolecular Allostery Achieves Tunable Luminescence Aromatic Bridged Phenothiazine Noncovalent Frameworks. [PDF]

open access: yesAdv Sci (Weinh)
Tunable luminescent supramolecular organic framework enabled by multiple allosteric effects, composed of a tetracation vinylphenylpyridinium‐modified aromatic‐bridged phenothiazine guest and cucurbit[8]uril, not only exhibits unique guest oxidation‐driven NIR luminescence blue‐shift and effectively enhances the quantum yield by 46‐fold to 22.2% but ...
Lu X, Chen J, Yu J.
europepmc   +2 more sources

Allosteric activation mechanism of bovine chymosin revealed by bias-exchange metadynamics and molecular dynamics simulations [PDF]

open access: yes, 2016
The aspartic protease, bovine chymosin, catalyses the proteolysis of κ-casein proteins in milk. The bovine chymosin–κ-casein complex is of industrial interest as the enzyme is widely employed in the manufacturing of processed dairy products. The apo form
Andrea Coletta   +17 more
core   +1 more source

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