The importance of vitamin A in nutritionM I Dawson
Department of Medicinal Chemistry, Molecular Medicine Research Institute, 325 East Middlefield Rd, Mountain View, CA 94943, USA
Curr Pharm Des 6:311-25. 2000
..In addition to serving as a metabolic source of retinol, beta-carotene, along with other dietary carotenoids, function as antioxidants that can prevent carcinogenesis by decreasing the levels of the free-radicals that cause DNA damage...
- sp2-bridged diaryl retinoids: effects of bridge-region substitution on retinoid X receptor (RXR) selectivity
M I Dawson
Medicinal Chemistry Department, Molecular Medicine Research Institute, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 10:1307-10. 2000
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- 4-[3-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and heterocyclic-bridged analogues are novel retinoic acid receptor subtype and retinoid X receptor alpha agonists
M I Dawson
Medicinal Chemistry Department, Molecular Medicine Research Institute, Mountain View, CA 94043, USA
Bioorg Med Chem Lett 10:1311-3. 2000
..Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth...
- Retinoic acid (RA) receptor transcriptional activation correlates with inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced ornithine decarboxylase (ODC) activity by retinoids: a potential role for trans-RA-induced ZBP-89 in ODC inhibition
M I Dawson
Molecular Medicine Research Institute, Mountain View, CA 94043, USA
Int J Cancer 91:8-21. 2001
..The natural retinoid all-trans-RA induced expression of transcription factor ZBP-89, which represses activation of the GC box in the ODC promoter by the transcription factor Sp1...
- Discovery and design of retinoic acid receptor and retinoid X receptor class- and subtype-selective synthetic analogs of all-trans-retinoic acid and 9-cis-retinoic acid
Marcia I Dawson
Department of Medicinal Chemistry, Molecular Medicine Research Institute, Mountain View, La Jolla, CA 94043, USA
Curr Med Chem 9:623-37. 2002
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- Apoptosis induction in cancer cells by a novel analogue of 6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalenecarboxylic acid lacking retinoid receptor transcriptional activation activity
M I Dawson
Department of Medicinal Chemistry, Molecular Medicine Research Institute, Mountain View, California 94043, USA
Cancer Res 61:4723-30. 2001
..These studies strongly suggest that AHPN exerts its cell cycle arrest and apoptotic activity by a signaling pathway independent of retinoid receptor activation...
- Regulation of Nur77 nuclear export by c-Jun N-terminal kinase and Akt
Y H Han
Burnham Institute for Medical Research, Cancer Center, La Jolla, CA 92037, USA
Oncogene 25:2974-86. 2006
..Together, our results demonstrate that both activation of JNK and inhibition of Akt play a role in translocation of Nur77 from the nucleus to the cytoplasm...
- Synthetic retinoids and their nuclear receptors
M I Dawson
Cancer Center, The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Curr Med Chem Anticancer Agents 4:199-230. 2004
..Emphasis is placed on the retinoid X receptors and their ligands...
- Cytochrome c release and apoptosis induced by mitochondrial targeting of nuclear orphan receptor TR3
H Li
The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Science 289:1159-64. 2000
..Our results reveal a mechanism by which a nuclear transcription factor translocates to mitochondria to initiate apoptosis...
- Antagonist analogue of 6-[3'-(1-adamantyl)-4'-hydroxyphenyl]-2-naphthalenecarboxylic acid (AHPN) family of apoptosis inducers that effectively blocks AHPN-induced apoptosis but not cell-cycle arrest
Marcia I Dawson
The Burnham Institute, Cancer Center, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
J Med Chem 47:3518-36. 2004
..As a result, the position of RARgamma helix H12 in forming the coactivator-binding site was impacted in a manner consistent with the experimental effect of each analogue on RARgamma transcriptional activation...
- Nicotine modulates the effects of retinoids on growth inhibition and RAR beta expression in lung cancer cells
Guo-quan Chen
The Burnham Institute, Cancer Center, La Jolla, CA 92037, USA
Int J Cancer 99:171-8. 2002
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- Determinants of retinoid X receptor transcriptional antagonism
Claudio N Cavasotto
Cancer Center, The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, USA
J Med Chem 47:4360-72. 2004
..The antagonist also blocked activation of RAR subtypes alpha and beta by 9-cis-RA but not that of RARgamma...
Derivation of a retinoid X receptor scaffold from peroxisome proliferator-activated receptor gamma ligand 1-Di(1H-indol-3-yl)methyl-4-trifluoromethylbenzeneMarcia I Dawson
Cancer Center, Burnham Institute for Medical Research, 10901 North Torrey Pines Rd, La Jolla, CA 92037, USA
ChemMedChem 4:1106-19. 2009
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- The peptidomimetic, 1-adamantyl-substituted, and flex-het classes of retinoid-derived molecules: structure-activity relationships and retinoid receptor-independent anticancer activities
Marcia I Dawson
Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Mini Rev Med Chem 10:455-91. 2010
..Structure-activity relationships and potential for clinical translation as anticancer therapeutics are presented...
- Regulation of retinoic acid receptor beta expression by peroxisome proliferator-activated receptor gamma ligands in cancer cells
Sharon Y James
Cancer Center, The Burnham Institute, La Jolla, California 92037, USA
Cancer Res 63:3531-8. 2003
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- Conversion of Bcl-2 from protector to killer by interaction with nuclear orphan receptor Nur77/TR3
Bingzhen Lin
The Burnham Institute, Cancer Center, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Cell 116:527-40. 2004
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Studies of cannabinoid-1 receptor antagonists for the treatment of obesity: hologram QSAR model for biarylpyrazolyl oxadiazole ligandsMao Ye
Burnham Institute for Medical Research, La Jolla, CA 92037, USA
Bioorg Med Chem Lett 19:3310-5. 2009
..Both the HQSAR model and analysis from the contribution map should be useful for the further design of novel structurally related CB(1) antagonists...
- Retinoid X receptor regulates Nur77/TR3-dependent apoptosis [corrected] by modulating its nuclear export and mitochondrial targeting
Xihua Cao
The Burnham Institute, Cancer Center, 10901 N Torrey Pines Rd, La Jolla, CA 92037, USA
Mol Cell Biol 24:9705-25. 2004
..Together, our results reveal a novel nongenotropic function of RXRalpha and its involvement in the regulation of the Nur77-dependent apoptotic pathway [corrected]..
- An adamantyl-substituted retinoid-derived molecule that inhibits cancer cell growth and angiogenesis by inducing apoptosis and binds to small heterodimer partner nuclear receptor: effects of modifying its carboxylate group on apoptosis, proliferation, and
Marcia I Dawson
Cancer Center, Burnham Institute for Medical Research, La Jolla, California 92037, USA
J Med Chem 50:2622-39. 2007
..3-Cl-AHPC at 1.0 microM induced human microvascular endothelial cell apoptosis but did not inhibit cell migration or tube formation...
- 3D-QSAR and QSSR studies of 3,8-diazabicyclo[4.2.0]octane derivatives as neuronal nicotinic acetylcholine receptors by comparative molecular field analysis (CoMFA)
Mao Ye
Burnham Institute for Medical Research, La Jolla, CA 92037, USA
Bioorg Med Chem Lett 19:127-31. 2009
..924, 0.935 and 0.875 for conventional r(2). Analyses indicated that both the steric and electrostatic factors should be considered in the rational design of more active and selective nAChR agonists...
- Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and
Marcia I Dawson
Cancer Center and Inflammatory and Infectious Disease Center, Burnham Institute for Medical Research, La Jolla, California 92037, USA
J Med Chem 51:5650-62. 2008
..Inhibitory activity against Src homology 2 domain-containing protein tyrosine phosphatase 2 (Shp-2) was also assessed. The most active Shp-2 inhibitor was found to be the 3'-(3,3-dimethylbutynyl) analogue of 3-Cl-AHPC...
- Mass-spectrometric analysis of agonist-induced retinoic acid receptor gamma conformational change
Valerie J Peterson
Laboratory of Molecular Pharmacology, Department of Pharmaceutical Sciences, College of Pharmacy, Oregon State University, Corvallis, OR 97331, U.S.A
Biochem J 362:173-81. 2002
..This technique should be generally applicable to other members of the nuclear receptor superfamily that undergo an induced structural alteration upon agonist or antagonist binding, DNA binding and/or protein-protein interaction...
- Retinoic acid (RA) regulates 17beta-hydroxysteroid dehydrogenase type 2 expression in endometrium: interaction of RA receptors with specificity protein (SP) 1/SP3 for estradiol metabolism
You Hong Cheng
Division of Reproductive Biology Research, Department of Obstetrics and Gynecology, Northwestern University, 303 E Superior Street, Chicago, IL 60611, USA
J Clin Endocrinol Metab 93:1915-23. 2008
..Retinoic acid (RA) induces HSD17B2 expression, but the underlying mechanism is not known...
- Induction of apoptosis of human B-CLL and ALL cells by a novel retinoid and its nonretinoidal analog
Yuxiang Zhang
Department of Medicine, Karmanos Cancer Institute, Wayne State University, and the John D Dingell VA Medical Center, Detroit, MI 48201, USA
Blood 100:2917-25. 2002
..These results suggest that CD437 and MM002 analogs may have a potential role in the treatment of B-CLL and ALL...
- Identification and characterization of a cell cycle and apoptosis regulatory protein-1 as a novel mediator of apoptosis signaling by retinoid CD437
Arun K Rishi
Veterans Affairs Medical Center, Department of Internal Medicine and Karmanos Cancer Institute, Wayne State University, Detroit, Michigan 48201, USA
J Biol Chem 278:33422-35. 2003
..Identification of CARP-1 as a key mediator of signaling by CD437 or adriamycin allows for delineation of pathways that, in turn, may prove beneficial for design and targeting of novel antitumor agents...
- Induction of apoptosis in retinoid-refractory acute myelogenous leukemia by a novel AHPN analog
Yuxiang Zhang
John D Dingell VA Medical Center, and Department of Medicine, Wayne State University, Detroit, MI 48201, USA
Blood 102:3743-52. 2003
..3-log kill in the leukemic blasts. While 3-Cl-AHPC does not activate retinoic nuclear receptors, it is a potent inducer of apoptosis in AML cells and may represent a novel therapy in the treatment of this disease...
