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NUCLEAR RECEPTORS: BIOLOGY, STRUCTURES, AND DRUG DISCOVERY
Nuclear receptors are DNA-binding and ligand-regulated transcriptional factors that play crucial roles in many aspects of human physiology and consist of an important family of drug targets. This year marked the 30th anniversary of the cloning of the first member of the nuclear receptor family and 25th year of the discovery of orphan nuclear receptors, for which no cognate ligands were known at the time of their cloning. Since then we have witnessed a tremendous expansion of our knowledge of this family of receptors. In this special issue, 11 review articles highlight our key understanding of structure, function, disease relevance, and drug discovery of nuclear receptors.
Original Articles
Development of β-amino-carbonyl compounds as androgen receptor antagonists
Zhi-yun Zhang, Yan-hui Zhu, Cai-hong Zhou, Qing Liu, Hui-li Lu, Yun-jun Ge & Ming-wei Wang
Acta Pharmacologica Sinica 35: 664–673; doi:10.1038/aps.2013.201
Tyrosine phosphorylation of estradiol receptor by Src regulates its hormone-dependent nuclear export and cell cycle progression in breast cancer cells
G Castoria, P Giovannelli, M Lombardi, C De Rosa, T Giraldi, A de Falco, M V Barone, C Abbondanza, A Migliaccio & F Auricchio
Oncogene 31: 4868–4877; doi:10.1038/onc.2011.642
A novel nuclear role for the Vav3 nucleotide exchange factor in androgen receptor coactivation in prostate cancer
S Rao, L S Lyons, C D Fahrenholtz, F Wu, A Farooq, W Balkan and K L Burnstein
Oncogene 31: 716–727; doi:10.1038/onc.2011.273
Reviews
Transcriptional integration of metabolism by the nuclear sterol-activated receptors LXR & FXR
Anna C. Calkin & Peter Tontonoz
Nature Reviews Molecular Cell Biology 13: 213–224; doi:10.1038/nrm3312
Nuclear receptor coregulators: modulators of pathology & therapeutic targets
David M. Lonard & Bert W. O'Malley
Nature Reviews Endocrinology 8: 598–604; doi:10.1038/nrendo.2012.100
REV-ERB & ROR nuclear receptors as drug targets
Douglas J. Kojetin & Thomas P. Burris
Nature Reviews Drug Discovery 13: 197–216; doi:10.1038/nrd4100
Nuclear hormone receptors in diabetic nephropathy
Xiaoxin X. Wang, Tao Jiang & Moshe Levi
Nature Reviews Nephrology 6: 342–351; doi:10.1038/nrneph.2010.56
Short communication
Differential recruitment of nuclear receptor coregulators in ligand-dependent transcriptional repression by estrogen receptor-α
K W Merrell, J D Crofts, R L Smith, J H Sin, K E Kmetzsch, A Merrlle, R O Migue, N R Candelaria & C-Y Lin
Oncogene 30: 1608–1614; doi:10.1038/onc.2010.528
Original paper
Nuclear receptors agonists exert opposing effects on the inflammation dependent survival of breast cancer stem cells
A Papi, T Guarnieri, G Storci, D Santini, C Ceccarelli, M Taffurelli, S De Carolis, N Avenia, A Sanguinetti, A Sidoni, M Orlandi & M Bonafé
Cell Death and Differentiation (2012) 19: 1208–1219; doi:10.1038/cdd.2011.207
Article
Antidiabetic phospholipid-nuclear receptor complex reveals the mechanism for phospholipid-driven gene regulation
Paul M Musille, Manish C Pathak, Janelle L Lauer, William H Hudson, Patrick R Griffin & Eric A Ortlund
Nature Structural & Molecular Biology 19: 532–537; doi:10.1038/nsmb.2279
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