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SHR Neuro Krebs Kardio Lipid Stoffw Microb

Strandback, E; Lienhart, WD; Hromic-Jahjefendic, A; Bourgeois, B; Högler, A; Waltenstorfer, D; Winkler, A; Zangger, K; Madl, T; Gruber, K; Macheroux, P.
A small molecule chaperone rescues the stability and activity of a cancer-associated variant of NAD(P)H:quinone oxidoreductase 1 in vitro.
FEBS Lett. 2020; 594(3):424-438 Doi: 10.1002/1873-3468.13636 [OPEN ACCESS]
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Co-Autor*innen der Med Uni Graz
Bourgeois Benjamin Michel Rene
Madl Tobias

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NAD(P)H:quinone oxidoreductase 1 (NQO1) is a human FAD-dependent enzyme that plays a crucial role in the antioxidant defense system. A naturally occurring single-nucleotide polymorphism (NQO1*2) in the NQO1 gene leads to an amino acid substitution (P187S), which severely compromises the activity and stability of the enzyme. The NQO1*2 genotype has been linked to a higher risk for several types of cancer and poor survival rate after anthracycline-based chemotherapy. In this study, we show that a small molecular chaperone (N-(2-bromophenyl)pyrrolidine-1-sulfonamide) repopulates the native wild-type conformation. As a consequence of the stabilizing effect, the enzymatic activity of the P187S variant protein is strongly improved in the presence of the molecular chaperone in vitro. © 2019 The Authors. FEBS Letters published by John Wiley & Sons Ltd on behalf of Federation of European Biochemical Societies.
Find related publications in this database (using NLM MeSH Indexing)
Amino Acid Sequence -
Drug Evaluation, Preclinical -
Enzyme Activation - drug effects
Enzyme Stability - drug effects
Ligands -
Molecular Docking Simulation -
Mutant Proteins - antagonists & inhibitors
Mutant Proteins - chemistry
Mutant Proteins - genetics
Mutant Proteins - metabolism
Mutation -
NAD(P)H Dehydrogenase (Quinone) - antagonists & inhibitors
NAD(P)H Dehydrogenase (Quinone) - chemistry
NAD(P)H Dehydrogenase (Quinone) - genetics
NAD(P)H Dehydrogenase (Quinone) - metabolism
Neoplasms - genetics
Protein Conformation -

Find related publications in this database (Keywords)
chemical chaperone
single-nucleotide polymorphism
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