Results 81 to 90 of about 139,314 (301)

Q94 is not a selective modulator of proteinase-activated receptor 1 (PAR1) in platelets

open access: yesPlatelets, 2022
Thrombin is a potent platelet activator, acting through proteinase-activated receptors −1 and −4 (PAR1 and PAR4). Of these, PAR-1 is activated more rapidly and by lower thrombin concentrations.
Luc R. A. Francis   +3 more
doaj   +1 more source

Genetic dissection of human ABCE1 in yeast reveals separable requirements for ribosome recycling and suppression of aberrant reinitiation

open access: yesFEBS Open Bio, EarlyView.
Human ABCE1 cannot functionally replace its yeast ortholog. Yeast–human chimera analysis identified NBD1 as a major interspecies barrier. Genetic screening yielded hABCE1 revertants that rescue yeast viability but fail to suppress aberrant translation reinitiation in the 3′ UTR.
Eriko Nakata   +3 more
wiley   +1 more source

A Silent Allosteric Modulator

open access: yesMolecular Medicine Communications, 2022
Deterioration in cognitive dysfunction in Alzheimer’s disease (AD) patients is associated with microglia-mediated synaptic destruction. Using AD mouse models Spurrier and colleagues discerned the function of the metabotropic glutamate receptor 5 (mGluR5) on synaptic loss and demonstrated that a silent allosteric modulator (SAM) of mGLuR5 when given ...
openaire   +1 more source

Novobiocin as an Allosteric Modulator of Ste2p [PDF]

open access: yes, 2013
G protein-coupled receptors (GPCRs) are the target of 30-50% of all prescribed drugs for human medicine and are therefore the subject of intense study by the scientific community.
Becker, Jeffrey M   +2 more
core  

Concentration dependence of the interaction of two allosteric modulators that compete for the same allosteric site.

open access: yes, 2019
Upper row, simulation of tracer binding (ordinate) in the presence of two allosteric modulators A and B competing for the same allosteric site, where α is either less than one (left) or greater than one (right) and B is negative allosteric modulator ...
Esam E. El-Fakahany (339452)   +3 more
core   +1 more source

PASSer: Prediction of Allosteric Sites Server [PDF]

open access: yes, 2020
Allostery is considered important in regulating protein\u27s activity. Drug development depends on the understanding of allosteric mechanisms, especially the identification of allosteric sites, which is prerequisite in drug discovery and design.
Xi, Jiang, Peng, Tao, Hao, Tian
core   +1 more source

DNA‐Templated 2D Heterostructures as Phototriggered Dynamic Nanohybrids: From Releasing Molecular Loads to Controlling Enzyme Biocatalytic Function

open access: yesAdvanced Functional Materials, EarlyView.
DNA strands are employed both as dynamic linkers and nanoscale templates for the integration of Ag2S nanoparticles on MoS2, which in turn imparted photothermal responsiveness; this feature permits the selective cargo (fluorophore, quantum dots or an enzyme) release from the MoS2 surface in response to local heat induced by light irradiation.
Kai Chen   +3 more
wiley   +1 more source

In Vivo Non-radioactive Assessment of mGlu5 Receptor-Activated Polyphosphoinositide Hydrolysis in Response to Systemic Administration of a Positive Allosteric Modulator

open access: yesFrontiers in Pharmacology, 2018
mGlu5 receptor-mediated polyphosphoinositide (PI) hydrolysis is classically measured by determining the amount of radioactivity incorporated in inositolmonophosphate (InsP) after labeling of membrane phospholipids with radioactive inositol. Although this
Anna R. Zuena   +9 more
doaj   +1 more source

Molecular Modeling Study of Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex

open access: yes, 2022
Allosteric modulators (AMs) are always the hotspot in research for their higher selectivity and various effects on the orthosteric ligands (OL), whereas AMs are also classified in terms of its functionalities as positive, negative, or silent allosteric ...
Jiang, Chen
core  

Conformational Switching of Proteins on Material Surfaces Enabled by Peptide‐Oriented Adsorption

open access: yesAdvanced Functional Materials, EarlyView.
Responsive biointerfaces could be achieved using conformationally responsive proteins; however, their interconversion can be lost upon surface adsorption. Herein, we demonstrate that the incorporation a Au binding peptide into calmodulin allows for binding control on Au wherein the protein retains conformational switching. This capability was confirmed
Sakthirupini Ramamurthy   +7 more
wiley   +1 more source

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