TY  - JOUR
AU  - Bakail, May
AU  - Rodriguez-Marin, Silvia
AU  - Hegedüs, Zsófia
AU  - Perrin, Marie E.
AU  - Ochsenbein, Francoise
AU  - Wilson, Andrew J.
TI  - Recognition of ASF1 by Using Hydrocarbon-Constrained Peptides.
JF  - CHEMBIOCHEM
J2  - CHEMBIOCHEM
VL  - 20
PY  - 2019
IS  - 7
SP  - 891
EP  - 895
PG  - 5
SN  - 1439-4227
DO  - 10.1002/cbic.201800633
UR  - https://m2.mtmt.hu/api/publication/30609649
ID  - 30609649
N1  - CAPLUS AN 2019:290706(Journal)
AB  - 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)]
LA  - English
DB  - MTMT
ER  -