Results 31 to 40 of about 1,298 (145)

(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
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

NanoBRET—A Novel BRET Platform for the Analysis of Protein–Protein Interactions

ACS Chemical Biology, 2015
Dynamic interactions between proteins comprise a key mechanism for temporal control of cellular function and thus hold promise for development of novel drug therapies. It remains technically challenging, however, to quantitatively characterize these interactions within the biologically relevant context of living cells.
Thomas, Machleidt, Carolyn C, Woodroofe, Marie K, Schwinn, Jacqui, Méndez, Matthew B, Robers, Kris, Zimmerman, Paul, Otto, Danette L, Daniels, Thomas A, Kirkland, Keith V, Wood   +9 more
openaire   +2 more sources

Characterisation of tyrosine kinase inhibitor-receptor interactions at VEGFR2 using sunitinib-red and nanoBRET

Biochemical Pharmacology, 2023
Vascular endothelial growth factor (VEGF) is an important mediator of angiogenesis, proliferation and migration of vascular endothelial cells. It is well known that cardiovascular safety liability for a wide range of small molecule tyrosine kinase inhibitors (TKIs) can result from interference with the VEGFR2 signalling system.
Van Daele, Marieke, Kilpatrick, Laura E., Woolard, Jeanette, Hill, Stephen J.   +3 more
openaire   +2 more sources

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
doaj   +1 more source

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

Protocol for Measuring Drug–Target Engagement in Mouse Colorectal Cancer Organoids Using NanoBRET Assay

Bio-Protocol
Organoids as a drug discovery platform represent an emerging field that continues to refine its tools. NanoBRET (bioluminescence resonance energy transfer) has emerged as a proximity-based and highly sensitive assay to measure protein–protein and protein–
Hammed Badmos, Colin Steele, Ross Cagan
doaj   +1 more source

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

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

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   +1 more source