Table 1 SPR and dissociation constants of drug binding to proteasomal DUBs and 26S proteasomes.

From: The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells

 

USP14(P) KD

UCHL5(P)) KD

USP14(U) KD

USP14(K) KD

26S(V) KD

26S(V) + USP14(K) KD

NTA chip

VLX1570

8.1 μM

14 μM

1.5 μM

18 μM

–

–

CM7 chip

VLX1570

–

–

–

35 μM

25 μM

35 μM

  1. Source of proteins in parenthesis: ProSpec (P), Ubiquigent (U), Karolinska Institute Protein Science Facility (K) and VIVA Bioscience (V).
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