Chemistry:BPPSA
From HandWiki
BPPSA (N‐(2‐bromophenyl)pyrrolidine‐1‐sulfonamide) is a small molecular chaperone that helps partially stabilize the P187S variant of NQO1, recovering part of its lost catalytic activity.[1]
Isothermal titration calorimetry shows that it binds the P187S variant at 20.0 uM, as compared to 7.95 uM for wildtype NQO1.
It is contrasted to dicoumarol, which binds the enzyme and acts as a competitive inhibitor.
An X-ray crystal structure of wild-type human NQO1 in complex with BPPSA is in the Protein Data Bank under the code PDB: 6FY4.
References
- ↑ Strandback, Emilia; Lienhart, Wolf-Dieter; Hromic-Jahjefendic, Altijana; Bourgeois, Benjamin; Högler, Anja; Waltenstorfer, Daniel; Winkler, Andreas; Zangger, Klaus et al. (2020). "A small molecule chaperone rescues the stability and activity of a cancer-associated variant of NAD(P)H:quinone oxidoreductase 1 in vitro". FEBS Letters 594 (3): 424–438. doi:10.1002/1873-3468.13636. PMID 31605637.
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