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Flexibility is important for inhibition of the MDM2/p53 protein-protein interaction by cyclic β-hairpins

Artikel i vetenskaplig tidskrift
Författare Emma Danelius
Mariell Pettersson
Matilda Bred
Jaeki Min
M. Brett Waddell
R. Kiplin Guy
Morten Grøtli
Mate Erdelyi
Publicerad i Organic and Biomolecular Chemistry
Volym 14
Sidor 10386-10393
ISSN 1477-0520
Publiceringsår 2016
Publicerad vid Svenskt NMR-centrum vid Göteborgs universitet
Institutionen för kemi och molekylärbiologi
Sidor 10386-10393
Språk en
Länkar pubs.rsc.org/en/content/articlepdf/...
Ämnesord peptide, hairpin, NMR, ppi
Ämneskategorier Bioorganisk kemi, Fysikalisk organisk kemi, Farmaceutisk kemi, Kemi, Spektroskopi, Kemi, Organisk kemi, Organisk syntes, Läkemedelskemi

Sammanfattning

© 2016 The Royal Society of Chemistry.Protein-protein interactions that have large, flat and featureless binding sites are difficult drug targets. In the development of their modulators conventional drug discovery strategies are often unsuccessful. Gaining a detailed understanding of the binding mode of protein-protein interaction inhibitors is therefore of vast importance for their future pharmaceutical use. The MDM2/p53 protein pair is a highly promising target for cancer treatment. Disruption of the protein complex using p53 α-helix mimetics has been shown to be a successful strategy to control p53 activity. To gain further insight into the binding of inhibitors to MDM2, the flexibility of four cyclic β-hairpins that act as α-helical mimetics and potential MDM2/p53 interaction inhibitors was investigated in relation to their inhibitory activity. MDM2-binding of the mimetics was determined using fluorescence polarization and surface plasmon resonance assays, whereas their conformation and dynamics in solution was described by the combined experimental and computational NAMFIS analysis. Molecular flexibility was shown to be important for the activity of the cyclic β-hairpin based MDM2 inhibitors.

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