Results 11 to 20 of about 1,238 (123)

BRET measurement on CCD camera-based microtiter plate readers

SLAS Discovery, 2022
NanoBRET assays, which utilize bioluminescence energy resonance transfer (BRET), have been widely adopted in drug discovery for measuring both protein-protein interactions and drug target engagement. While the EnVision and other traditional well-scanning
Kelvin F. Cho, Noelle Javier, Kaylee Choi   +2 more
doaj   +1 more source

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells

Molecules, 2023
PLK1 is a protein kinase that regulates mitosis and is both an important oncology drug target and a potential antitarget of drugs for the DNA damage response pathway or anti-infective host kinases.
Xuan Yang, Jeffery L. Smith, Michael T. Beck, Jennifer M. Wilkinson, Ani Michaud, James D. Vasta, Matthew B. Robers, Timothy M. Willson   +7 more
doaj   +1 more source

Single tracer-based protocol for broad-spectrum kinase profiling in live cells with NanoBRET

STAR Protocols, 2021
Summary: This protocol is used to profile the engagement of kinase inhibitors across nearly 200 kinases in a live-cell context. This protocol utilizes one single kinase tracer (NanoBRET(TM) Tracer K10) that operates quantitatively at four different ...
Matthew B. Robers, Jennifer M. Wilkinson, James D. Vasta, Lena M. Berger, Benedict-Tilman Berger, Stefan Knapp   +5 more
doaj   +1 more source

Protocol for measuring BRAF autoinhibition in live cells using a proximity-based NanoBRET assay

STAR Protocols, 2023
Summary: BRAF is frequently activated via mutation in human cancer and the RASopathy syndromes; however, for BRAF activation to occur, autoinhibitory interactions between the regulatory and catalytic domains must be relieved. Here, we present a proximity-
Russell Spencer-Smith, Deborah K. Morrison   +1 more
doaj   +1 more source

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

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   +1 more source

Development of a Lysine-Reactive Targeted Covalent Inhibitor for the P300/CBP-Associated Factor Bromodomain Through Structure-Based Design. [PDF]

ChemMedChem
We developed a targeted covalent inhibitor for the p300/CBP‐associated factor (PCAF) bromodomain. Our lead molecule, 10, labeled a unique lysine residue in the PCAF bromodomain, demonstrated potent inhibition in biophysical/biochemical assays, and engaged the PCAF bromodomain in cells.
Ede RR, Peterson KE, Begyinah RK, Tom IP, Ochoada JM, Sneddon MS, Tiu AKY, Fischer M, Shelat AA, Pomerantz WCK.   +9 more
europepmc   +2 more sources

A Live-Cell NanoBRET Assay to Monitor RNA–Protein Interactions and Their Inhibition by Small Molecules [PDF]

ACS Central Science
Jingsong Shan, Amirhossein Taghavi, Elizabeth A. Caine, Ryuichi Sekioka, Veronika Rajchin, James M. Burke, J. Monty Watkins, Jessica L. Childs-Disney, Matthew D. Disney   +8 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

One Tracer, Dual Platforms: Unlocking Versatility of Fluorescent Probes in TR-FRET and NanoBRET Target Engagement Assays [PDF]

ACS Medicinal Chemistry Letters
Dong Lu, Xiaoli Qi, Jin Wang
exaly   +2 more sources

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