Results 31 to 40 of about 488 (104)

From biochemical time–resolved fluorescence resonance energy transfer assay to live cell nanobio-luminescence resonance energy transfer assay: A case study with the bromodomain-containing protein 4 protein

ASPET Discovery
Fluorescent probe–based time-resolved fluorescence resonance energy transfer (TR-FRET) biochemical assays are widely used in characterizing ligands’ binding activities, whereas fluorescent probe–based nanobio-luminescence resonance energy transfer ...
Wenwei Lin, Young-Hwan Jung, Yongtao Li, Lei Yang, Taosheng Chen   +4 more
doaj   +1 more source

Determining whether bespoke nanoBRET tracers work with ALK5

, 2019
I have always wanted to establish nanoBRET target engagement assay for ALK5. Relative to dual luciferase promoter assay and immunofluorescent staining, nanoBRET is many times faster. With a robust ALK5 nanoBRET assay, I will be able to rapidly screen for
Alex Bullock, Jong Fu Wong, Alex Bullock (4949548), Jong Fu Wong (4949545)   +3 more
core   +1 more source

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

Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H3 and H4 Receptors on Living Cells [PDF]

, 2018
Receptor-binding affinity and ligand-receptor residence time are key parameters for the selection of drug candidates and are routinely determined using radioligand competition-binding assays.
Leurs, Rob, Mocking, Tamara A.M., Verweij, Eléonore W.E., Vischer, Henry F.   +3 more
core   +2 more sources

Development of a NanoBRET assay to validate inhibitors of Sirt2-mediated lysine deacetylation and defatty-acylation that block prostate cancer cell migration [PDF]

, 2022
Sirtuin2 (Sirt2) with its NAD+-dependent deacetylase and defatty-acylase activities plays a central role in the regulation of specific cellular functions.
Sum, M., Vogelmann, Anja, Jung, Manfred, Hong, JY., Hammelmann, Sören, Neuwirt, E., Colcerasa, Arianna, Schüle, Roland, Herp, Daniel, Komaniecki, G., Sippl, Wolfgang, Metzger, Eric, Wössner, Nathalie, Merz, Annika, Groß, O., Lin, Hening, Einsle, Oliver, Zhang, L., Schiedel, Matthias   +18 more
core   +4 more sources

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

Differential Water Networks Guide Selectivity Optimization of a Cell Active BPTF Inhibitor in Neuroblastoma

Angewandte Chemie International Edition, EarlyView.
BZ2 is a second‐generation Bromodomain PHD finger Transcription Factor (BPTF) inhibitor with improved selectivity over Class I and Class IV BRD off‐targets identified in our previously reported inhibitor, BZ1. Structural analyses reveal that water network engagement is key to this selectivity.
Kesavan Babu, Chun‐Ju Tsou, Sourav Das, Liying Fan, Anasuya Pal, Molly Sneddon, Timothy R. Stachowski, Priyanka Samanta, Stanley Nithianantham, Caroline Buchholz, Shi Zhang, Xiang Fu, Rahul S. Kathayat, Wenwei Lin, Yongtao Li, Lei Yang, Taosheng Chen, Marcus Fischer, Anang A. Shelat, William C. K. Pomerantz   +19 more
wiley   +1 more source

Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands

, 2019
A critical part of the development of CXCR4 modulators is to have a simple and sensitive assay system to complement the search by screening and evaluating the binding affinity.
Hirokazu Tamamura (1490866), Wataru Nomura, Takuya Kobayakawa, Maxwell M. Sakyiamah (6580064), Maxwell M. Sakyiamah, Hirokazu Tamamura, Wataru Nomura (1490860), Takuya Kobayakawa (1674325)   +7 more
core   +1 more source

From anthelmintic to neuro‐oncology: A systematic review of mebendazole repurposing for brain tumour therapy

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aim Mebendazole (MBZ), a benzimidazole anthelmintic with established clinical use, has emerged as a repurposing candidate for primary brain tumours due to its multimodal anticancer actions and central nervous system penetrance. This systematic review synthesizes preclinical and clinical evidence evaluating MBZ's efficacy, mechanisms of action ...
Ciara B. Blum, Milli McMenamin, Tessa Khoo, John M. Edwin, Prathibha Jose, Liam A. O’Callaghan   +5 more
wiley   +1 more source

BRET‐Based Approaches for Ion Channels: Emerging Applications and Future Directions

Archiv der Pharmazie, Volume 359, Issue 9, September 2026.
Bioluminescence resonance energy transfer (BRET) is a versatile method for studying ligand–protein interactions. Its compatibility with high‐throughput screening and real‐time kinetics has made it widely used in drug discovery. Here, we summarize recent applications of BRET‐based methods for studying ligand binding to ion channels, highlighting key ...
Nadine Kock, Laura Heitzer, Joana Massa, Marvin Taterra, Marcel Bermúdez, Oliver Koch, Matthias Schiedel   +6 more
wiley   +1 more source