5-Carboxyfluorescein tagged N-phenylanthranilamide as a tracer reagent for fluorescence polarization: a robust method to screen MAPK pathway allosteric inhibitors.
Fluorescence polarization using N(alpha)-(fluorescein-5-carbonyl)-N(epsilon)-(N-[2-fluoro-4-iodophenyl]-3,4-difluoroanthraniloyl)lysyl amide is capable of rapidly identifying inhibitor ligands that bind to an allosteric site in MEK1.
Rezvani
Z Nooshin
ZN
School of Biomedical Sciences, University of Nottingham Medical School, Queen's Medical Centre, Nottingham, UK NG7 2UH.
Mayer
R John
RJ
Chan
Weng C
WC
D000494:Allosteric Regulation; D000577:Amides / Q000737:chemistry*; D002460:Cell Line; D005452:Fluoresceins / Q000737:chemistry*; D005454:Fluorescence Polarization; D006801:Humans; D007202:Indicators and Reagents / Q000737:chemistry*; D020935:MAP Kinase Signaling System; D011485:Protein Binding; D062367:ortho-Aminobenzoates / Q000737:chemistry*
D000577:Amides; D005452:Fluoresceins; D007202:Indicators and Reagents; D062367:ortho-Aminobenzoates; C045132:4-carboxyfluorescein; C001209:fenamic acid