Results 71 to 80 of about 4,452,404 (339)

Bias-inducing allosteric binding site in mu-opioid receptor signaling

open access: yesSN Applied Sciences, 2021
G-protein-biased agonism of the mu-opioid receptor (μ-OR) is emerging as a promising strategy in analgesia. A deep understanding of how biased agonists modulate and differentiate G-protein-coupled receptors (GPCR) signaling pathways and how this is ...
Andrés F. Marmolejo-Valencia   +2 more
doaj   +1 more source

Interplay between RNA‐protein interactions and RNA structures in gene regulation

open access: yesFEBS Open Bio, EarlyView.
Methodological advances in mapping transcriptome‐wide RNA‐protein interactions and RNA structures have started to uncover the potential of RNP conformations in gene regulation. Competing RNA–RNA, RNA‐protein and protein–protein interactions shape the compaction and function of RNPs throughout their lifetime and may provide novel therapeutic targets in ...
Jenni Rapakko   +2 more
wiley   +1 more source

Allostery Inhibition of BACE1 by Psychotic and Meroterpenoid Drugs in Alzheimer’s Disease Therapy

open access: yesMolecules, 2022
In over a century since its discovery, Alzheimer’s disease (AD) has continued to be a global health concern due to its incurable nature and overwhelming increase among older people. In this paper, we give an overview of the efforts of researchers towards
Samuel C. Ugbaja   +5 more
doaj   +1 more source

HSP70 governs permeability and mechanotransduction in primary human endothelial cells

open access: yesFEBS Open Bio, EarlyView.
HSP70 chemical inhibition reduces endothelial cell proliferation and increases permeability, the latter supported by normal interendothelial junctional protein distribution. HSP70 also plays a role in shear stress response, a hemodynamic force naturally present in blood vessels and correlated with vessel protection.
Andrea Pinto‐Martinez   +5 more
wiley   +1 more source

Illuminating the mechanism and allosteric behavior of NanoLuc luciferase

open access: yesNature Communications, 2023
NanoLuc, a superior β-barrel fold luciferase, was engineered 10 years ago but the nature of its catalysis remains puzzling. Here experimental and computational techniques are combined, revealing that imidazopyrazinone luciferins bind to an intra-barrel ...
Michal Nemergut   +17 more
doaj   +1 more source

Allosteric crosstalk in modular proteins: Function fine-tuning and drug design

open access: yesComputational and Structural Biotechnology Journal, 2023
Modular proteins are regulatory proteins that carry out more than one function. These proteins upregulate or downregulate a biochemical cascade to establish homeostasis in cells.
Suman Abhishek   +4 more
doaj   +1 more source

Allosteric Site Inhibitor Disrupting Auto-Processing of Malarial Cysteine Proteases

open access: yesScientific Reports, 2018
Falcipains are major haemoglobinases of Plasmodium falciparum required for parasite growth and development. They consist of pro- and mature domains that interact via ‘hot-spot’ interactions and maintain the structural integrity of enzyme in zymogen state.
A. Pant   +12 more
semanticscholar   +1 more source

Molecular determinants of signal transduction in tropomyosin receptor kinases

open access: yesFEBS Open Bio, EarlyView.
Tropomyosin receptor kinases control critical neuronal functions, but how do the same receptors produce diverse cellular responses? This review explores the structural mechanisms behind Trk signaling diversity, focusing on allosteric modulation and ligand bias.
Giray Enkavi
wiley   +1 more source

Current Advances in Allosteric Modulation of Muscarinic Receptors

open access: yesBiomolecules, 2020
Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter.
Jan Jakubik, Esam E. El-Fakahany
doaj   +1 more source

Reversing allosteric communication: From detecting allosteric sites to inducing and tuning targeted allosteric response

open access: yesPLOS Computational Biology, 2018
The omnipresence of allosteric regulation together with the fundamental role of structural dynamics in this phenomenon have initiated a great interest to the detection of regulatory exosites and design of corresponding effectors. However, despite a general consensus on the key role of dynamics most of the earlier efforts on the prediction of allosteric
Wei-Ven Tee   +2 more
openaire   +4 more sources

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