Table 1 Affinity of Cyp inhibitors against CypA and CypB by SPR

From: Macrocycle-based PROTACs selectively degrade cyclophilin A and inhibit HIV-1 and HCV

  

TWH106

CG167

RJS308

CsA

CypA KD (nM)

 

53 ± 5

64 ± 12

108 ± 12

67 ± 1

CypB KD (nM)

 

139 ± 24

71 ± 13

320 ± 40

nd

  1. Affinities of TWH106 (non-PROTAC parental ligand), CG167 (Cyp-PROTAC) and RJS308 (Cyp-PROTAC) measured by SPR equilibrium analysis on an amide coupling CM5 chip derivatised with full-length CypA or N-truncated CypB. Kinetic analysis provided similar results. SPR curves and affinity plots for one representative experiment are shown in Supplementary Fig. 2 and Supplementary Fig. 3. Experiments were run in duplicate, and KDs are means from two independent experiments ± SD. The affinity of CsA against CypA was also determined (n = 2), but not against CypB due to slow dissociation and the lack of successful regeneration strategies.
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