Results 131 to 140 of about 79,838 (161)

Allosteric Site Inhibitors for Caspases

Science's STKE, 2004
The active sites of proteins with enzymatic activity are not always suitable for drug targeting. Hardy et al. report the application of a method called "Tethering" to identify an allosteric site inhibitor on the executioner caspases, caspase-3. Tethering, a commercial method, uses reversible disulfide bond formation
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Predicting Binding Sites by Analyzing Allosteric Effects

2011
This chapter describes a method for analyzing the allosteric influence of molecular interactions on protein conformational distributions. The method, called Dynamics Perturbation Analysis (DPA), generally yields insights into allosteric effects in proteins and is especially useful for predicting ligand-binding sites.
Dengming, Ming, Michael E, Wall
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Evolution of a kinase allosteric site

Science, 2020
Enzyme Regulation Enzyme activity is often regulated by conformational changes coupled to binding of an effector at an allosteric site, a feature especially important for enzymes involved in signaling cascades. Hadzipasic et al. studied the origins of allosteric regulation of Aurora A, a kinase involved in progression of the eukaryotic cell cycle ...
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Chemogenomics of allosteric binding sites in GPCRs

Drug Discovery Today: Technologies, 2013
Chemogenomic techniques connect the chemical and biological domains to establish ligand and target relationships not evident from the individual disciplines. Chemogenomics has been applied in lead generation, target classification, focused library design as well as selectivity and polypharmacology profiling.
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Allosteric Na⁺-binding site modulates CXCR4 activation

Physical Chemistry Chemical Physics, 2018
G protein-coupled receptors (GPCRs) control most cellular communications with the environment and are the largest protein family of drug targets.
Xiaojing Cong, Jérôme Golebiowski
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Allosteric binding sites on muscarinic receptors

Drug Development Research, 1997
The classical (acetylcholine) binding sites of all five subtypes of muscarinic receptors are known to be subject to allosteric regulation by a variety of small molecules. The hallmarks of such modula- tion in binding assays are that the allosteric ligands can alter both the affinities and the rates of association and dissociation of classical ligands ...
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Allosteric interactions among drug binding sites on calmodulin

Biochemical and Biophysical Research Communications, 1983
Felodipine is a fluorescent dihydropyridine Ca2+-antagonist. It binds to calmodulin in a Ca2+-dependent manner, and undergoes a fluorescence increase which allows us to monitor its interaction with calmodulin. Hydrophobic ligands including the calmodulin antagonist, R24571 and Ca2+ antagonists, prenylamine and diltiazem, bind to calmodulin and ...
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Cancer risk among World Trade Center rescue and recovery workers: A review

Ca-A Cancer Journal for Clinicians, 2022
Paolo Boffetta, Charles B Hall, Andrew C Todd   +2 more
exaly  

Splice site m6A methylation prevents binding of U2AF35 to inhibit RNA splicing

Cell, 2021
Kamila Delaney, Radha Raman Pandey, Kuan-Ming Chen   +2 more
exaly  

Site-Selective Cross-Coupling of Polyhalogenated Arenes and Heteroarenes with Identical Halogen Groups

Chemical Reviews, 2022
Vignesh Palani, Melecio A Perea, Richmond Sarpong   +2 more
exaly