Recognition of ASF1 by Using Hydrocarbon-Constrained Peptides.

Bakail, May; Rodriguez-Marin, Silvia; Hegedues, Zsofia [Hegedüs, Zsófia (gyógyszerkémia), szerző]; Perrin, Marie E.; Ochsenbein, Francoise; Wilson, Andrew J.

Angol nyelvű Tudományos Szakcikk (Folyóiratcikk)
Megjelent: CHEMBIOCHEM 1439-4227 1439-7633 p. Ahead of Print 2019
  • SJR Scopus - Organic Chemistry: Q1
Azonosítók
Inhibiting the histone H3-ASF1 (anti-silencing function 1) protein-protein interaction (PPI) represents a potential approach for treating numerous cancers. As an α-helix-mediated PPI, constraining the key histone H3 helix (residues 118-135) is a strategy through which chem. probes might be elaborated to test this hypothesis. In this work, variant H3118-135 peptides bearing pentenylglycine residues at the i and i+4 positions were constrained by olefin metathesis. Biophys. analyses revealed that promotion of a bioactive helical conformation depends on the position at which the constraint is introduced, but that the potency of binding towards ASF1 is unaffected by the constraint and instead that enthalpy-entropy compensation occurs. [on SciFinder(R)]
Hivatkozás stílusok: IEEEACMAPAChicagoHarvardCSL
2019-09-18 07:14