E-resources
-
Bakail, May; Rodriguez‐Marin, Silvia; Hegedüs, Zsófia; Perrin, Marie E.; Ochsenbein, Françoise; Wilson, Andrew J.
Chembiochem : a European journal of chemical biology, April 1, 2019, Volume: 20, Issue: 7Journal Article
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 chemical 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. 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. Histones diss organisation: Inhibiting the histone H3–anti‐silencing function 1 (ASF1) interaction could potentially be used to treat numerous cancers. Biophysical analyses revealed that the binding affinity of hydrocarbon‐constrained histone H3 towards ASF1 protein is unaffected by pre‐organisation; instead enthalpy–entropy compensation occurs.
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|
Source: Personal bibliographies
and: SICRIS
The material is available in full text. If you wish to order the material anyway, click the Continue button.