Reliably evaluate PROTAC interactions
involving small and large molecules
To develop effective PROTACs candidates, you need to characterize interactions
involving small ligands — like warheads and ligase ligands — and larger
molecules such as fully assembled PROTACs. If your affinity screening method
relies on significant mass changes upon binding, you'll spend a lot of time on
assay optimization before you see any results.
Measurements of molecular interactions with Dianthus are mass-independent,
so you don't need special tricks to successfully measure binding affinities with
small and large molecules.
Dianthus measured the two affinities between target protein BRD4 and
warhead JQ1(+): for the interaction with the warhead alone and when the
warhead is part of the fully assembled PROTAC dBET6.
Data collected from a collaboration with Aurelia Bioscience, a Charnwood Molecular company.
10
-10
10
-9
10
-8
10
-7
10
-6
10
-5
0.0
0.2
0.4
0.6
0.8
1.0
1.2
Binary complex BRD4 + Warhead JQ1 (+)
Binary complex BRD4 + PROTAC dBET6
Fraction
Bound
Concentration (M)
JQ1(+) dBET6
K
d
(nM)
Molecular weight (Da)
51.8
457.0
58.7
841.4
