Results 11 to 20 of about 151,004 (296)
Profiling Allosteric Modulators of CB 1 R with an Allosteric Fluoroprobe [PDF]
Angewandte ChemieAbstract Allosteric modulation of cannabinoid receptor type 1 (CB 1 R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs).
Miroslav Kosar +12 more
openaire +6 more sources
Coarse-grained models of biomolecule dynamics and allostery [PDF]
, 2010 Recently, it has become increasingly accepted that thermal fluctuations take active part in functional tasks of biological molecules. We employ a set of coarse-grained models to investigate the mechanism of transmission of allosteric signal via spatial ...
Toncrova, Hedvika
core +7 more sources
Sensing the allosteric force [PDF]
Nature Communications, 2020 AbstractAllosteric regulation is an innate control in most metabolic and signalling cascades that enables living organisms to adapt to the changing environment by tuning the affinity and regulating the activity of target proteins. For a microscopic understanding of this process, a protein system has been designed in such a way that allosteric ...
Bozovic, Olga +2 more
openaire +5 more sources
Allosterism in the PDZ Family [PDF]
International Journal of Molecular Sciences, 2022 Dynamic allosterism allows the propagation of signal throughout a protein. The PDZ (PSD-95/Dlg1/ZO-1) family has been named as a classic example of dynamic allostery in small modular domains. While the PDZ family consists of more than 200 domains, previous efforts have primarily focused on a few well-studied PDZ domains, including PTP-BL PDZ2, PSD-95 ...
Stevens, Amy O., He, Yi
openaire +2 more sources
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
core +2 more sources
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation. The identification and development of PTH1R non-peptide allosteric modulators have obtained widespread attention.
Mengrong Li +5 more
openaire +3 more sources
Frontiers in Chemistry, 2020 The Src homology-2 (SH2) domain-containing protein tyrosine phosphatase 2 (SHP2, encoded by PTPN11) is a critical allosteric phosphatase for many signaling pathways.
Quan Wang +3 more
doaj +1 more source
Novel Putative Positive Modulators of α4β2 nAChRs Potentiate Nicotine Reward-Related Behavior
Molecules, 2021 The popular tobacco and e-cigarette chemical flavorant (−)-menthol acts as a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs), and contributes to multiple physiological effects that exacerbates nicotine addiction ...
Skylar Y. Cooper +3 more
doaj +1 more source
PASSer: Prediction of Allosteric Sites Server [PDF]
, 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
Pharmaceuticals, 2023 Increases in antibiotic usage and antimicrobial resistance occurrence have caused a dramatic reduction in the effectiveness of many frontline antimicrobial treatments.
Scott Grossman +2 more
doaj +1 more source