Results 41 to 50 of about 139,314 (301)

Modulation of Allosteric Control and Evolution of Hemoglobin

open access: yesBiomolecules, 2023
Allostery arises when a ligand-induced change in shape of a binding site of a protein is coupled to a tertiary/quaternary conformational change with a consequent modulation of functional properties. The two-state allosteric model of Monod, Wyman and Changeux [J. Mol. Biol.
Maurizio Brunori, Adriana Erica Miele
openaire   +4 more sources

Effect of γ value on binding of allosteric modulator to two allosteric sites.

open access: yes, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452)   +3 more
core   +1 more source

Allosteric Modulation of Beta1 Integrin Function Induces Lung Tissue Repair [PDF]

open access: yes, 2012
The cellular cytoskeleton, adhesion receptors, extracellular matrix composition, and their spatial distribution are together fundamental in a cell's balanced mechanical sensing of its environment.
Susan McIntyre   +13 more
core   +1 more source

Allosteric modulation of glycine receptors [PDF]

open access: yesBritish Journal of Pharmacology, 2011
Inhibitory (or strychnine-sensitive) glycine receptors (GlyRs) are anion-selective transmitter-gated ion channels of the cys-loop superfamily, which includes among others also the inhibitory γ-aminobutyric acid receptors (GABA(A) receptors). While GABA mediates fast inhibitory neurotransmission throughout the CNS, the action of glycine as a fast ...
Yévenes, G E, Zeilhofer, Hanns Ulrich
openaire   +4 more sources

In Silico Prediction and Validation of CB2 Allosteric Binding Sites to Aid the Design of Allosteric Modulators

open access: yesMolecules, 2022
Although the 3D structures of active and inactive cannabinoid receptors type 2 (CB2) are available, neither the X-ray crystal nor the cryo-EM structure of CB2-orthosteric ligand-modulator has been resolved, prohibiting the drug discovery and development ...
Jiayi Yuan   +7 more
doaj   +1 more source

Concentration dependence of binding of allosteric modulator to two allosteric sites.

open access: yes, 2019
Simulation of tracer binding (ordinate) in the presence an allosteric modulator binding to two allosteric sites for various combinations of positive and negative cooperativity with the tracer indicated at headings of individual plots.
Esam E. El-Fakahany (339452)   +3 more
core   +1 more source

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

open access: yesFEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang   +2 more
wiley   +1 more source

Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters

open access: yesData in Brief, 2017
The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative ...
Carolina L. Haass-Koffler   +7 more
doaj   +1 more source

Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]

open access: yes, 2015
Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
Dhankher, P   +4 more
core  

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

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