Tackle undruggable
targets by screening
for binary and ternary
PROTAC interactions
using Dianthus
PROTACs have huge therapeutic potential for
tackling "undruggable" protein targets. As they
start to populate your companies' pipeline,
there is a need to find a biophysical method
that efficiently evaluates the binary and ternary
complex formed by PROTACs, ubiquitin ligase,
and your protein of interest (POI). Dianthus helps
to solve common problems you will face when
characterizing these complex interactions.
948
947
946
945
944
943
942
1x10 1x10 1x10
+
1x10
+
Fnorm
[‰]
Ligand Concentration [µM]
964
960
956
952
948
Fnorm
[‰]
Ligand Concentration [nM]
1x10
+
1x10
+
1x10
+
964
962
960
958
956
954
952
950
1x10 1x10
+
1x10
+
1x10
+
Fnorm
[‰]
Ligand Concentration [nM]
VCB Complex:PROTAC
K
d
: 0.69 μM
Brd4BD2:PROTAC
K
d
: 28.8 nM
Brd4BD2:PROTAC:VCB
Complex
K
d
: 8.86 nM α: 77.9
QUICKLY MEASURE BINDING AFFINITIES AND
EASILY DETERMINE THE COOPERATIVITY FACTOR α
Characterize binary and ternary interactions
and calculate cooperativity values from
measurements done in solution under
carefully controlled equilibrium conditions
Measure interactions in the pM to mM range
Screen hundreds or thousands of PROTAC
candidates when you integrate Dianthus
into your automation workflow
Screen different ligases too, and find the
one that works best for your POI
Ligase
PROTAC
POI
PROTAC
Ligase
POI
PROTAC
*Cooperativity factor α calculated as the ratio of binary (Ligase-PROTAC)
and ternary (POI-PROTAC-Ligase) dissociation constants (K
d
)
