A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton’s Tyrosine Kinase:

L. L. Ong,James D. Vasta,L. Monereau,G. Locke,H. Ribeiro,Mark A. Pattoli,Stacey Skala,James R. Burke,Scott H. Watterson,Joseph A. Tino,Poncho Meisenheimer,B. Arey,Jonathan Lippy,Lisa Zhang,Matthew B. Robers,Andrew J. Tebben,Charu Chaudhry

A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical to Cellular Activity for Bruton’s Tyrosine Kinase:

2019

L. L. Ong
James D. Vasta
L. Monereau
G. Locke
H. Ribeiro
Mark A. Pattoli
Stacey Skala
James R. Burke
Scott H. Watterson
Joseph A. Tino
Poncho Meisenheimer
B. Arey
Jonathan Lippy
Lisa Zhang
Matthew B. Robers
Andrew J. Tebben
Charu Chaudhry

Protein kinases are intensely studied mediators of cellular signaling. While traditional biochemical screens are capable of identifying compounds that modulate kinase activity, these assays are lim...

Keywords:

Cell signaling
Residence time
Structure–activity relationship
Bruton's tyrosine kinase
Cell biology
Kinase
Chemistry
cellular activity
kinase activity
target engagement

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