Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 1, 2014, Pages 178-185

  Desphande, Anil ^a   Xia, Gang ^a   Boerma, Leeann J ^b   Vines, Kimberly K ^a   Atigadda, Venkatram R ^a   Lobo Ruppert, Susan ^c   Grubbs, Clinton J ^d   Moeinpour, Fariba L ^d   Smith, Craig D ^a   Christov, Konstantin ^e   Brouillette, Wayne J ^a   Muccio, Donald D ^a  

^a UNIVERSITY OF ALABAMA AT BIRMINGHAM   (United States)

^b UNIVERSITY OF ALABAMA AT BIRMINGHAM   (United States)

^c University of Alabama at Birmingham   (United States)

^d Kentucky   (United States)

^e UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

Author keywords

Cancer prevention; Conformationally constrained retinoids; Ligand protein crystal structures; Rexinoids

Indexed keywords

8 (3',4' DIHYDRO 1'(2H) NAPHTHALEN 10 YLIDENE) 3,7 DIMETHYL 2,3,6 OCTATRIENOINIC ACID; 8 [METHYL 3',4' DIHYDRO 1'(2'H) NAPHTHALEN 10 YLIDENE] 3,7 DIMETHYL 2,4,6 OCTATRIENOIC ACID; BEXAROTENE; NUCLEAR RECEPTOR COACTIVATOR 2; RETINOIC ACID; RETINOID; RETINOID X RECEPTOR; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; ARTICLE; BREAST CANCER; CANCER PREVENTION; CHIRALITY; CONFORMATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENANTIOMER; FEMALE; HEPATOMEGALY; HYPERLIPIDEMIA; LIGAND BINDING; LIPOGENESIS; NONHUMAN; PROTEIN DOMAIN; RAT; TRANSACTIVATION; TRIACYLGLYCEROL BLOOD LEVEL;

2-IODOXYBENZOIC ACID; CANCER PREVENTION; CONFORMATIONALLY CONSTRAINED RETINOIDS; DMEM; DULBECCO'S MODIFIED EAGLE MEDIUM; ER; ESTROGEN RECEPTOR; GLUCOCORTICOID RECEPTOR INTERACTING PROTEIN-1; GRIP-1; HEXAMETHYLPHOSPHORAMIDE; HMPA; IBX; KLF4; KRUPPEL-LIKE FACTOR 4; LBD; LBP; LIGAND BINDING DOMAIN; LIGAND BINDING POCKET; LIGAND-PROTEIN CRYSTAL STRUCTURES; LIVER X RECEPTORS; LXRS; NR; NUCLEAR RECEPTOR; PDB; PROTEIN DATA BANK; RA; RAR; RAT KIDNEY EPITHELIAL; RETINOIC ACID; RETINOIC ACID RECEPTOR; RETINOID X RECEPTOR; REXINOIDS; RKE; RMSD; ROOT MEAN SQUARE DEVIATION; RXR; SCC; SQUAMOUS CELL CARCINOMA; TETRAHYDROFURAN; TG; THF; THIN LAYER CHROMATOGRAPHY; TLC; TRIGLYCERIDES;

HUMANS; LIGANDS; MOLECULAR CONFORMATION; NEOPLASMS; RETINOID X RECEPTORS; RETINOIDS;

EID: 84891490295     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.11.039     Document Type: Article

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