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Inside Cover: Binding Mode and Structure–Activity Relationships around Direct Inhibitors of the Nrf2–Keap1 Complex (ChemMedChem 4/2014)
Author(s) -
Jnoff Eric,
Albrecht Claudia,
Barker John J.,
Barker Oliver,
Beaumont Edward,
Bromidge Steven,
Brookfield Frederick,
Brooks Mark,
Bubert Christian,
Ceska Tom,
Corden Vincent,
Dawson Graham,
Duclos Stephanie,
Fryatt Tara,
Genicot Christophe,
Jigorel Emilie,
Kwong Jason,
Maghames Rosemary,
Mushi Innocent,
Pike Richard,
Sands Zara A.,
Smith Myron A.,
Stimson Christopher C.,
Courade JeanPhilippe
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490011
Subject(s) - cover (algebra) , keap1 , chemistry , non covalent interactions , mode (computer interface) , small molecule , stereochemistry , molecule , nanotechnology , crystallography , computer science , materials science , biochemistry , human–computer interaction , engineering , transcription factor , organic chemistry , mechanical engineering , hydrogen bond , gene
The inside cover picture shows the activation of the Nrf2 pathway induced by a small molecule (NCE) disrupting the Keap1–Nrf2 interaction in a noncovalent manner. Crystallographic elucidation of its binding mode helped to focus and drive the drug design process more effectively and efficiently. For further details, see the Communication by Eric Jnoff et al. on p. 699 ff. Artwork by Réjane Leporcq.