Fig. 2: Optimization of a KLHDC2 targeting ligand. | Nature Communications

Fig. 2: Optimization of a KLHDC2 targeting ligand.

From: Principles of paralog-specific targeted protein degradation engaging the C-degron E3 KLHDC2

Fig. 2

a Electrostatic representation of KLHDC2SBD bound to the diGly substrate EPBH2 (chocolate, sticks, 8EBL.pdb). For clarity, only the C-terminal five residues of EPHB2 are shown. b As in (a), but with SJ10278 (orange, sticks). c Summary of SAR campaign surrounding SJ10278. d Chemical structure and biophysical characterization of SJ46411. Data are the average of n = 2 independent experiments. e As in (a) but with SJ46411 shown in surface representation. f LigPlot of SJ46411-KLHDC2SBD, hydrogen bonds between SJ46411 and KLHDC2 are show in black sticks with distances indicated. The water molecule involved in intramolecular hydrogen bonding with SJ46411 is shown as a gray sphere. Source data are provided as a Source Data file.

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