Results 11 to 20 of about 488 (104)

Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis [PDF]

iScience, 2019
Summary: The peptide hormone H2 relaxin has demonstrated promise as a therapeutic, but mimetic development has been hindered by the poorly understood relaxin receptor RXFP1 activation mechanism.
Bradley L. Hoare, Shoni Bruell, Ashish Sethi, Paul R. Gooley, Michael J. Lew, Mohammed A. Hossain, Asuka Inoue, Daniel J. Scott, Ross A.D. Bathgate   +8 more
doaj   +4 more sources

TGF-β receptor-specific NanoBRET Target Engagement in living cells for high-throughput kinase inhibitor screens [PDF]

SLAS Discovery
Targeting transforming growth factor-β (TGF-β) receptors is a promising pharmacological approach to normalize aberrant signaling in genetic and non-genetic TGF-β associated diseases including fibrosis, cancer, cardiovascular and musculoskeletal disorders.
Marius Wits, Nicole Haarmans, Gonzalo Sanchez-Duffhues, Marie-José Goumans   +3 more
doaj   +3 more sources

Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells [PDF]

Frontiers in Immunology, 2022
IntroductionThe Epidermal Growth Factor Receptor is a member of the Erb receptor tyrosine kinase family. It binds several ligands including EGF, betacellulin (BTC) and TGF-α, controls cellular proliferation and invasion and is overexpressed in various ...
Dehan Comez, Dehan Comez, Jacqueline Glenn, Jacqueline Glenn, Stephanie M. Anbuhl, Stephanie M. Anbuhl, Raimond Heukers, Raimond Heukers, Martine J. Smit, Stephen J. Hill, Stephen J. Hill, Laura E. Kilpatrick, Laura E. Kilpatrick   +12 more
doaj   +2 more sources

Development of a novel NanoBRET high-throughput drug screening assay for human GnRH receptor using sulfo-cyanine 5 fluorophore

Journal of Pharmaceutical Analysis
G protein-coupled receptors (GPCRs), the largest superfamily of cell surface receptors and targets for over 30% of current clinical drugs, remain crucial for future therapeutic development.
Li Shen, Xiaozhe Du, Yakai Yang, Ming Su, Rong Rong, Jia Meng, Lee Wei Lim, David G. Fernig, Zhi-Liang Lu   +8 more
doaj   +2 more sources

Systematic Assessment of Human CCR7 Signalling Using NanoBRET Biosensors Points towards the Importance of the Cellular Context

Biosensors
The human CC chemokine receptor 7 (CCR7) is activated by two natural ligands, CC chemokine ligand 19 (CCL19) and 21 (CCL21). The CCL19-CCL21-CCR7 axis has been extensively studied in vitro, but there is still debate over whether CCL21 is an overall ...
Nathan Vanalken, Katrijn Boon, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Tom Van Loy   +5 more
doaj   +2 more sources

A kinetic intra-cellular assay (KICA) to measure quantitative compound binding kinetics within living cells

STAR Protocols, 2022
Summary: The Kinetic Intra-Cellular Assay (KICA) is a recombinant cell-based technique that utilizes NanoBRET technology. KICA enables the measurement of intracellular binding kinetics.
Charles S. Lay, Daniel A. Thomas, John P. Evans, Emma J. Jones, Kelly M. Gatfield, Peter D. Craggs   +5 more
doaj   +1 more source

Agonist dependency of the second phase access of β-arrestin 2 to the heteromeric µ-V1b receptor

Scientific Reports, 2021
During the development of analgesic tolerance to morphine, the V1b vasopressin receptor has been proposed to bind to β-arrestin 2 and the µ-opioid receptor to enable their interaction.
Nuttawadee Ngamlertwong, Hiroyoshi Tsuchiya, Yuta Mochimaru, Morio Azuma, Takahiro Kuchimaru, Taka-aki Koshimizu   +5 more
doaj   +1 more source

NanoBRET in C. elegans illuminates functional receptor interactions in real time

BMC Molecular and Cell Biology, 2022
Background Protein-protein interactions form the basis of every organism and thus, investigating their dynamics, intracellular protein localization, trafficking and interactions of distinct proteins such as receptors and their ligand-binding are of ...
Victoria Elisabeth Groß, Miron Mikhailowitsch Gershkovich, Torsten Schöneberg, Anette Kaiser, Simone Prömel   +4 more
doaj   +1 more source

A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins

Frontiers in Cell and Developmental Biology, 2022
E3 ligases constitute a large and diverse family of proteins that play a central role in regulating protein homeostasis by recruiting substrate proteins via recruitment domains to the proteasomal degradation machinery. Small molecules can either inhibit,
Martin P. Schwalm, Martin P. Schwalm, Lena M. Berger, Lena M. Berger, Maximilian N. Meuter, James D. Vasta, Cesear R. Corona, Sandra Röhm, Sandra Röhm, Benedict-Tilman Berger, Benedict-Tilman Berger, Frederic Farges, Sebastian M. Beinert, Franziska Preuss, Franziska Preuss, Viktoria Morasch, Viktoria Morasch, Vladimir V. Rogov, Vladimir V. Rogov, Sebastian Mathea, Sebastian Mathea, Krishna Saxena, Krishna Saxena, Matthew B. Robers, Susanne Müller, Susanne Müller, Stefan Knapp, Stefan Knapp, Stefan Knapp   +28 more
doaj   +1 more source

Discovery of Environment-Sensitive Fluorescent Ligands of β‑Adrenergic Receptors for Cell Imaging and NanoBRET Assay

, 2022
By fusing several environment-sensitive fluorophores to the pharmacophore mirabegron, a series of new fluorescent ligands for β-adrenergic receptors (β-ARs) were produced with a turn-on mechanism and high binding affinity to β-ARs efficiently.
Gaopan Dong (6493922), Wenhua Li (426756), Lupei Du (1376673), Zhao Ma (655370), Minyong Li (69472), Jiwei Chen (413314)   +5 more
core   +4 more sources