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Article Dans Une Revue ChemBioChem Année : 2019

Recognition of ASF1 by Using Hydrocarbon-Constrained Peptides

Résumé

Inhibiting the histone H3-ASF1 (anti-silencing function 1) protein-protein interaction (PPI) represents a potential approach for treating numerous cancers. As an alpha-helix-mediated PPI, constraining the key histone H3 helix (residues 118-135) is a strategy through which chemical probes might be elaborated to test this hypothesis. In this work, variant H3(118-135) peptides bearing pentenylglycine residues at the i and i+4 positions were constrained by olefin metathesis. Biophysical 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.

Dates et versions

hal-02169570 , version 1 (01-07-2019)

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Citer

May Bakail, Silvia Rodriguez-Marin, Zsofia Hegedues, Marie E. Perrin, Françoise Ochsenbein, et al.. Recognition of ASF1 by Using Hydrocarbon-Constrained Peptides. ChemBioChem, 2019, 20 (7), pp.891--895. ⟨10.1002/cbic.201800633⟩. ⟨hal-02169570⟩
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