Results 41 to 50 of about 137,279 (309)

Allosteric modulators targeting GPCRs

, 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, Bellinda Benhamú, López Rodríguez, María Luz, Henar Vázquez-Villa, Benhamú Salama, Bellinda, Vázquez Villa, María Del Henar   +5 more
core   +1 more source

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

, 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, Mcintyre, Susan, Mark Marsden, Rehab AlJamal-Naylor, Fiona Rossi, Harrison, Beth, Marsden, Mark, Linda Wilson, Aljamal-naylor, Rehab, Wilson, Linda, David J. Harrison, Beth Harrison, Rossi, Fiona, Harrison, David J.   +13 more
core   +1 more source

Light-regulated allosteric switch enables temporal and subcellular control of enzyme activity

eLife, 2020
Engineered allosteric regulation of protein activity provides significant advantages for the development of robust and broadly applicable tools. However, the application of allosteric switches in optogenetics has been scarce and suffers from critical ...
Mark Shaaya, Jordan Fauser, Anastasia Zhurikhina, Jason E Conage-Pough, Vincent Huyot, Martin Brennan, Cameron T Flower, Jacob Matsche, Shahzeb Khan, Viswanathan Natarajan, Jalees Rehman, Pradeep Kota, Forest M White, Denis Tsygankov, Andrei V Karginov   +14 more
doaj   +1 more source

Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines [PDF]

Journal of the Serbian Chemical Society, 2016
A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-(piperidin-4-ylmethyl)piperazine.
Penjišević Jelena Z., Šukalović Vladimir V., Andrić Deana B., Roglić Goran M., Novaković Irena T., Šoškić Vukić, Kostić-Rajačić Slađana V.   +6 more
doaj   +1 more source

A Novel High-Throughput Assay Reveals That the Temperature Induced Increases in Transphosphatidylation of Phospholipase D Are Dependent on the Alcohol Acceptor Concentration

Biomolecules, 2022
Phospholipase D reacts with alcohols or water, transphosphatidylating or hydrolysing lipids such as phosphatidylcholine, generating phosphatidylalcohols or phosphatidic acid, respectively.
Hengzhang Yang, Rüdiger Woscholski
doaj   +1 more source

Allostery: allosteric networks and allosteric signaling bias

Quarterly Reviews of Biophysics
Abstract Allosteric communication is established by networks through which strain energy generated at the allosteric site by an allosteric event, such as ligand binding, can propagate to the functional site. Exerted on multiple molecules in the cell, it can wield a biased function. Here, we discuss
Ruth Nussinov, Bengi R. Yavuz, Hyunbum Jang   +2 more
openaire   +2 more sources

The autoregulation of a eukaryotic DNA transposon

eLife, 2013
How do DNA transposons live in harmony with their hosts? Bacteria provide the only documented mechanisms for autoregulation, but these are incompatible with eukaryotic cell biology.
Corentin Claeys Bouuaert, Karen Lipkow, Steven S Andrews, Danxu Liu, Ronald Chalmers   +4 more
doaj   +1 more source

PASSer2.0: Accurate Prediction of Protein Allosteric Sites Through Automated Machine Learning

, 2021
Allostery is a fundamental process in regulating proteins’ activity. The discovery, design and development of allosteric drugs demand for better identification of allosteric sites.
Sian, Xiao, Peng, Tao, Hao, Tian
core   +1 more source

Multitargeting nature of muscarinic orthosteric agonists and antagonists

Frontiers in Physiology, 2022
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj   +1 more source

Cooperativity of Allosteric Receptors

Journal of Molecular Biology, 2013
Cooperativity of ligand binding to allosteric receptors can be quantified using the Hill coefficient (nH) to measure the sigmoidal character of the binding curve. However, for measurements of the transition between conformational states, nH values can be misleading due to ambiguity of the reference state.
Edelstein, Stuart J., Le Novère, Nicolas   +1 more
openaire   +2 more sources