Premium
Inside Cover: Modeling, Synthesis and Biological Evaluation of Potential Retinoid X Receptor‐Selective Agonists: Novel Halogenated Analogues of 4‐[1‐(3,5,5,8,8‐Pentamethyl‐5,6,7,8‐tetrahydro‐2‐naphthyl)ethynyl]benzoic Acid (Bexarotene) (ChemMedChem 9/2012)
Author(s) -
Furmick Julie K.,
Kaneko Ichiro,
Walsh Angela N.,
Yang Joanna,
Bhogal Jaskaran S.,
Gray Geoffrey M.,
Baso Juan C.,
Browder Drew O.,
Prentice Jessica L. S.,
Montano Luis A.,
Huynh Chanh C.,
Marcus Lisa M.,
Tsosie Dorian G.,
Kwon Jungeun S.,
Quezada Alexis,
Reyes Nicole M.,
Lemming Brittney,
Saini Puneet,
van der Vaart Arjan,
Groy Thomas L.,
Marshall Pamela A.,
Jurutka Peter W.,
Wagner Carl E.
Publication year - 2012
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.201290042
Subject(s) - bexarotene , retinoid x receptor , chemistry , nuclear receptor , halogenation , ring (chemistry) , stereochemistry , cover (algebra) , transcription factor , biochemistry , organic chemistry , gene , mechanical engineering , engineering
The inside cover picture shows how selective halogenation of bexarotene‐like ligands acts as a glue, helping to increase binding to and activation of retinoid X receptor (RXR), a nuclear receptor important for cancer and Alzheimer's disease. In search of better RXR agonists, a periodic trend of increased binding and homodimerization was found when introducing halogen atoms on the ortho position of the phenyl ring. For more details, see the Full Paper by Carl E. Wagner et al. on p. 1551 ff.