Results 21 to 30 of about 1,238 (123)

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
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(S)-3-(3-((7-Ethynyl-9H-pyrimido[4,5-b]indol-4-yl)amino)piperidin-1-yl)propanenitrile

Molbank, 2022
The title compound (S)-3-(3-((7-ethynyl-9H-pyrimido[4,5-b]indol-4-yl)amino)piperidin-1-yl)propanenitrile (2) was synthesized in five steps, starting from 4-chloro-7-iodo-9H-pyrimido[4,5-b]indole (3), and was characterized by 1H-NMR, 13C-NMR, MS and HPLC.
Stanislav Andreev, Nicole Plank, Dieter Schollmeyer, Pierre Koch   +3 more
doaj   +1 more source

Novel Pharmacology Following Heteromerization of the Angiotensin II Type 2 Receptor and the Bradykinin Type 2 Receptor

Frontiers in Endocrinology, 2022
The angiotensin type 2 (AT2) receptor and the bradykinin type 2 (B2) receptor are G protein-coupled receptors (GPCRs) that have major roles in the cardiovascular system. The two receptors are known to functionally interact at various levels, and there is
Elizabeth K. M. Johnstone, Elizabeth K. M. Johnstone, Elizabeth K. M. Johnstone, Mohammed Akli Ayoub, Mohammed Akli Ayoub, Rebecca J. Hertzman, Rebecca J. Hertzman, Heng B. See, Heng B. See, Rekhati S. Abhayawardana, Rekhati S. Abhayawardana, Ruth M. Seeber, Ruth M. Seeber, Kevin D. G. Pfleger, Kevin D. G. Pfleger, Kevin D. G. Pfleger   +15 more
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Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis

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   +1 more source

SGC-CAMKK2-1: A Chemical Probe for CAMKK2

Cells, 2023
The serine/threonine protein kinase calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) plays critical roles in a range of biological processes. Despite its importance, only a handful of inhibitors of CAMKK2 have been disclosed.
Carrow Wells, Yi Liang, Thomas L. Pulliam, Chenchu Lin, Dominik Awad, Benjamin Eduful, Sean O’Byrne, Mohammad Anwar Hossain, Carolina Moura Costa Catta-Preta, Priscila Zonzini Ramos, Opher Gileadi, Carina Gileadi, Rafael M. Couñago, Brittany Stork, Christopher G. Langendorf, Kevin Nay, Jonathan S. Oakhill, Debarati Mukherjee, Luigi Racioppi, Anthony R. Means, Brian York, Donald P. McDonnell, John W. Scott, Daniel E. Frigo, David H. Drewry   +24 more
doaj   +1 more source

Characterisation of IL-23 receptor antagonists and disease relevant mutants using fluorescent probes

Nature Communications, 2023
Association of single nucleotide polymorphisms in the IL-23 receptor with several auto-inflammatory diseases, led to the heterodimeric receptor and its cytokine-ligand IL-23, becoming important drug targets.
Charles S. Lay, Albert Isidro-Llobet, Laura E. Kilpatrick, Peter D. Craggs, Stephen J. Hill   +4 more
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Author Correction: NanoBRET binding assay for histamine H2 receptor ligands using live recombinant HEK293T cells

Scientific Reports, 2021
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
Lukas Grätz, Katharina Tropmann, Merlin Bresinsky, Christoph Müller, Günther Bernhardt, Steffen Pockes   +5 more
doaj   +2 more sources

NanoBRET: The Bright Future of Proximity-Based Assays

Frontiers in Bioengineering and Biotechnology, 2019
Bioluminescence resonance energy transfer (BRET) is a biophysical technique used to monitor proximity within live cells. BRET exploits the naturally occurring phenomenon of dipole-dipole energy transfer from a donor enzyme (luciferase) to an acceptor ...
Natasha C. Dale, Natasha C. Dale, Natasha C. Dale, Elizabeth K. M. Johnstone, Elizabeth K. M. Johnstone, Elizabeth K. M. Johnstone, Carl W. White, Carl W. White, Carl W. White, Kevin D. G. Pfleger, Kevin D. G. Pfleger, Kevin D. G. Pfleger, Kevin D. G. Pfleger   +12 more
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Development of a cell-based target engagement assay for pyruvate dehydrogenase kinase

SLAS Discovery
Pyruvate dehydrogenase kinases (PDHKs) are non-canonical serine/threonine kinases that regulate the pyruvate dehydrogenase complex. Given their central role in metabolism, dysregulation of PDHKs has been linked with a broad variety of pathological ...
Mya D. Gough, Matthew B. Robers, Cesear R. Corona, Ranjit K. Mehta, Mukesh K. Nyati, Peter L. Toogood   +5 more
doaj   +1 more source