Results 61 to 70 of about 488 (104)

Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time

Scientific Reports, 2017
Bioluminescence resonance energy transfer (BRET) has been a vital tool for understanding G protein-coupled receptor (GPCR) function. It has been used to investigate GPCR-protein and/or -ligand interactions as well as GPCR oligomerisation.
Carl W. White, Hannah K. Vanyai, Heng B. See, Elizabeth K. M. Johnstone, Kevin D. G. Pfleger   +4 more
doaj   +1 more source

Fluorescent ligands for dopamine D2/D3 receptors

Scientific Reports, 2020
Fluorescent ligands are versatile tools for the study of G protein-coupled receptors. Depending on the fluorophore, they can be used for a range of different applications, including fluorescence microscopy and bioluminescence or fluorescence resonance ...
Anni Allikalt, Nirupam Purkayastha, Khajidmaa Flad, Maximilian F. Schmidt, Alina Tabor, Peter Gmeiner, Harald Hübner, Dorothee Weikert   +7 more
doaj   +1 more source

tracerDB: a crowdsourced fluorescent tracer database for target engagement analysis

Nature Communications
Investigating ligand-protein complexes is essential in the areas of chemical biology and drug discovery. However, detailed information on key reagents such as fluorescent tracers and associated data for the development of widely used bioluminescence ...
Johannes Dopfer, James D. Vasta, Susanne Müller, Stefan Knapp, Matthew B. Robers, Martin P. Schwalm   +5 more
doaj   +1 more source

Agonist efficacy at the β2AR is driven by the faster association rate of the Gs protein

Frontiers in Pharmacology
IntroductionThe β2-adrenoceptor (β2AR) is a class A G protein-coupled receptor (GPCR). It is therapeutically relevant in asthma and chronic obstructive pulmonary disease (COPD), where β2AR agonists relieve bronchoconstriction.
Clare R. Harwood, Clare R. Harwood, David A. Sykes, David A. Sykes, David A. Sykes, Theo Redfern-Nichols, Owen Underwood, Colin Nicholson, Colin Nicholson, Armin N. Khoshgrudi, Armin N. Khoshgrudi, Eline J. Koers, Eline J. Koers, Graham Ladds, Graham Ladds, Stephen J. Briddon, Stephen J. Briddon, Dmitry B. Veprintsev, Dmitry B. Veprintsev, Dmitry B. Veprintsev   +19 more
doaj   +1 more source

Virtual screening and experimental validation of a METTL3-targeting peptide with in vitro antiproliferative activity against non-small cell lung cancer cells

Journal of Enzyme Inhibition and Medicinal Chemistry
The METTL3–METTL14 protein–protein interaction (PPI) plays an important role in tumour progression, and disruption of this interaction has been explored as a potential strategy. In this study, four peptides were identified from a peptide database through
Ying Dai, Hanying Wu, Yahui Shen, Fan Yang, Xiaohao Liu, Ting Zhuang   +5 more
doaj   +1 more source

Use of a new proximity assay (NanoBRET) to investigate the ligand binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells [PDF]

, 2016
Previous research has indicated that allosteric interactions across the dimer interface of β1-adrenoceptors may be responsible for a secondary low affinity binding conformation.
Hill, Stephen J., Brown, Alastair, Alastair Brown, Stoddart, Leigh A., Mark Soave, Woolard, Jeanette, Soave, Mark, Leigh A. Stoddart, Jeanette Woolard, Stephen J. Hill   +9 more
core   +1 more source

A versatile sub-nanomolar fluorescent ligand enables NanoBRET binding studies and single-molecule microscopy at the histamine H(3) receptor

, 2021
The histamine H(3) receptor (H(3)R) is considered an attractive drug target for various neurological diseases. We here report the synthesis of UR-NR266, a novel fluorescent H(3)R ligand.
Rosier, N., Schihada, H,, Işbilir, Ali, Nagl, M., Seibel, Ulla, Moeller, J, Rosier, N, Lohse, M.J., Lohse, MJ, Pockes, S., Humphrys, Laura J., Grätz, L., Möller, Jan, Seibel, U, Möller, J., Pockes, S, Işbilir, A., Nagl, Martin, Grätz, Lukas, Nagl, M, Lohse, Martin J., Humphrys, LJ, Isbilir, A, Seibel, U., Schihada, Hannes, Graetz, L,, Rosier, Niklas, Schihada, H., Humphrys, L.J., Pockes, Steffen   +29 more
core   +1 more source

Probe dependence of allosteric enhancers on the binding affinity of adenosine A1‐receptor agonists at rat and human A1‐receptors measured using NanoBRET [PDF]

, 2019
Background and Purpose: Adenosine is a local mediator that regulates a number of physiological and pathological processes via activation of adenosine A1‐receptors.
Samantha L. Cooper, Scammells, Peter J., Hill, Stephen J., Manuela Jörg, Jörg, Manuela, Cooper, Samantha L., Mark Soave, Woolard, Jeanette, Soave, Mark, Jeanette Woolard, Peter J. Scammells, Stephen J. Hill   +11 more
core   +1 more source

Development of an intracellular quantitative assay to measure compound binding kinetics

, 2022
Contemporary drug discovery typically quantifies the effect of a molecule on a biological target using the equilibrium-derived measurements of IC50, EC50, or KD.
Evans, John, Mahnoor Mahmood, Charles S. Lay, Carver, Charlotte, John P. Evans, Kelly M. Gatfield, Emma J. Jones, Thomas, Daniel, Cassie Messenger, Campbell, Matthew, Matthew Campbell, Peter D. Craggs, Lay, Charles, Gordon, Laurie, Phillipou, Alexander, Gatfield, Kelly, Laurie J. Gordon, Riching, Kristin, Charlotte E. Carver, Jones, Emma, Alexander N. Phillipou, Daniel A. Thomas, McCombe, Kristopher, Messanger, Cassie, Craggs, Peter, Kristin Riching, Mahmood, Mahnoor, Kristopher McCombe   +27 more
core   +1 more source

Discovery of a novel and potent KRASG12V-targeting peptide with antiproliferative activity against colorectal cancer cells

Journal of Enzyme Inhibition and Medicinal Chemistry
Despite the clinical relevance of KRASG12V in colorectal cancer, KRASG12V-specific inhibitors remain limited. Through structure-based virtual screening of a 59,319-member peptide library, we identified four KRASG12V-targeting peptides, among which ...
Hai Zhang, Shudan Yang, Yuting Wang, Miao-Miao Niu, Jingjiang She   +4 more
doaj   +1 more source