Skip to main content
. 2019 May 29;2019(22):3581–3590. doi: 10.1002/ejoc.201900327

Table 1.

Protein‐templated DCC studies reported over the past five years, in which a target was used as a template to influence the equilibrium. Therefore, only articles using an adaptive approach are listed, pre‐equilibrated DCC examples are omitted29, 30, 31 The table is adapted from Frei et al. and complemented32 a

Target Reversible reaction Analysis Library size Equilibration time Method applied for affinity measurement Best affinity Ref.
Wt Tau RNA Disulfide HPLC‐MS and NMR 21 2 days Fluorescence titration EC 50 = 70 nm Artigas et al. 201533
HIV FSS RNA Disulfide MS 12 4 days n.a. n.a. McAnany et al. 201634
Vascular endothelial growth factor receptor (VEGFR) 2 Imine HRMS 297 24 h In vitro activity against cancer cell lines IC 50 = 2.4 µm Yang et al. 201635
Endothiapepsin Acylhydrazone HPLC‐MS 90 20 h Inhibition assay IC 50 = 54.5 nm K i = 25.4 nm Mondal et al. 201636
FimH Acylhydrazone HPLC 8 3 days SPR K D = 273 nm Frei et al. 201737
UDP‐galacto‐pyranose mutase Acylhydrazone HPLC 11 24 h Fluorescence‐based assay and MIC K D = 3 µm mic = 26 µg mL–1 Fu et al. 201738
Myeloperoxidase (MPO) Hydrazone Activity assay 6 n.a. in vivo activity assay IC 50 = 79 nm Soubhye et al. 201739
ecFabH Acylhydrazone 19F‐NMR 5 12 h Enzymatic assay IC 50 = 3 mm Ektström et al. 201840
Multi‐protein strategy on AlkB oxygenases: FTO, ALKBH3 and ALKBH5 Acylhydrazone DSF and HPLC 10 5 h HPLC‐based demethylase and DSF assays IC 50 = 2.6 µm Das et al. 201841
Trypanosoma cruzi bromodomain‐containing (TcBDF3) Acylhydrazone HPLC‐MS 30 n.a. DSF IC 50 = 13–23 µm García et al. 201842
G‐Quadruplex DNA Imine formation HPLC and ESI‐MS 10 24 h n.a. n.a. Jana et al. 201943
a

DSF = differential scanning fluorimetry, HPLC = high‐pressure liquid chromatography, IC 50 = half maximal inhibitory concentration, ITC = isothermal titration calorimetry, K D = dissociation constant, K i = inhibition constant, MIC = minimum inhibitory concentration, MS = mass spectrometry, n.a. = not available, NMR = nuclear magnetic resonance, SPR = surface plasmon resonance.