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2 results on '"TR-FRET, time resolved fluorescence resonance energy transfer"'

1. Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer

Author

Katlin B. Massirer, Lewis E. Pennicott, Fiona Scott, Jonathan M. Elkins, Simon E. Ward, Tristan Reuillon, and A.M. Fala

Subjects
Models, Molecular, HATU, hexafluorophosphate azabenzotriazole tetramethyl uronium, PARP, poly(ADP-ribose) polymerase, Chemical tool, Clinical Biochemistry, Pharmaceutical Science, IC50, half maximal inhibitory concentration, Chemical probe, PRK, protein kinase C-related kinase, DMSO, dimethyl sulfoxide, Crystallography, X-Ray, PRO2, glutamate 5-kinase Pro2, EGTA, egtazic acid, Benzimidazole, 01 natural sciences, Biochemistry, GST, glutathione S-transferase, CDI, 1,1′-carbonyldiimidazole, AGC, protein kinase A/G/C families, DNA, deoxyribonucleic acid, Neoplasms, CLK, CDC2-like kinase, DMF, N,N-dimethyl-formamide, Drug Discovery, PDB, protein databank, Kinome, Ki, inhibitor constant, Protein Kinase C, Cancer, ChEMBL, European Molecular Biology Laboratory Chemical database, Molecular Structure, Kinase, Chemistry, PRK2, KD, dissociation constant, PAK2, p21 activated kinase 2, DCM, dichloromethane, SFM, scanning force microscopy, Agc kinase, Molecular Medicine, THF, tetrahydrofuran, EtOH, ethanol, SDS, sodium dodecyl sulfate, ATP, adenosine triphosphate, TCEP, tris(2-carboxyethyl)phosphine, Antineoplastic Agents, Kinases, Heart failure, STK, serine/threonine kinase, Article, Structure-Activity Relationship, Protein kinase N2, Drug Development, TR-FRET, time resolved fluorescence resonance energy transfer, AcOH, acetic acid, PKC, protein kinase C, DIPEA, N,N-diisopropylethylamine, medicine, Humans, NMR, nuclear magnetic resonance, Protein kinase A, Protein Kinase Inhibitors, Molecular Biology, PAGE, polyacrylamide gel electrophoresis, ComputingMethodologies_COMPUTERGRAPHICS, PKN2, Inflammation, Dose-Response Relationship, Drug, EDTA, ethylenediaminetetraacetic acid, 010405 organic chemistry, Organic Chemistry, HEPES, 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid, AGC kinase, medicine.disease, SAR, structure activity relationship, 0104 chemical sciences, Abl, Abelson murine leukemia viral oncogene, 010404 medicinal & biomolecular chemistry, CV, column volumes, Benzimidazoles, MeOH, methanol, PKN, protein kinase N
Abstract

Graphical abstract, Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases (

Published
2021
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2. Binding kinetics of ligands acting at GPCRs

Author

Sykes, David A., Stoddart, Leigh A., Kilpatrick, Laura E., and Hill, Stephen J.

Subjects
Models, Molecular, Kd, equilibrium dissociation constant, koff, dissociation rate constant, Ligands, Article, Receptors, G-Protein-Coupled, Association, GPCR, TR-FRET, time resolved fluorescence resonance energy transfer, Allosteric Regulation, PD, pharmacodynamics, HAC, heavy atom count, SKR, structure kinetic relationship, Humans, β2AR, β2 adrenoceptor, BRET, bioluminescence resonance energy transfer, GPCR, G protein-coupled receptor, RET, resonance energy transfer, kon(obs), observed rate of drug association, Cell Membrane, kon, association rate constant, 5HT2B, serotonin receptor 2B, kr, reverse rate coefficient, Kinetics, kf, forward rate coefficient, Binding kinetics, Dissociation, Protein Binding
Abstract

The influence of drug-receptor binding kinetics has often been overlooked during the development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the last decade there has been a growing understanding that an in-depth knowledge of binding kinetics at GPCRs is required to successfully target this class of proteins. Ligand binding to a GPCR is often not a simple single step process with ligand freely diffusing in solution. This review will discuss the experiments and equations that are commonly used to measure binding kinetics and how factors such as allosteric regulation, rebinding and ligand interaction with the plasma membrane may influence these measurements. We will then consider the molecular characteristics of a ligand and if these can be linked to association and dissociation rates., Highlights • Ligand binding kinetics can be measured using a variety of methods. • Kinetics can be influenced by the local environment surrounding the receptor. • The molecular determinants of kinetics rates are beginning to be understood. • Both kon and koff should be considered during drug discovery.

Published
2019

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