Asymmetry in the PPARγ/RXRα crystal structure reveals the molecular basis of heterodimerization among nuclear receptors

Molecular Cell

Volumn 5, Issue 3, 2000, Pages 545-555

  Gampe Jr , Robert T ^a   Montana, Valerie G ^a   Lambert, Millard H ^a   Miller, Aaron B ^a   Bledsoe, Randy K ^a   Milburn, Michael V ^a   Kliewer, Steven A ^a   Willson, Timothy M ^a   Xu, H Eric ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALITRETINOIN; ANTIDIABETIC AGENT; FARGLITAZAR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PROTEIN TYROSINE KINASE; RETINOID X RECEPTOR; ROSIGLITAZONE; THIAZOLIDINE DERIVATIVE; 2,4 THIAZOLIDINEDIONE DERIVATIVE; CELL RECEPTOR; HISTONE ACETYLTRANSFERASE; LIGAND; NUCLEAR PROTEIN; RETINOIC ACID; RETINOIC ACID RECEPTOR; STEROID RECEPTOR COACTIVATOR 1; THIAZOLE DERIVATIVE; TRANSCRIPTION FACTOR;

ARTICLE; CRYSTAL STRUCTURE; DIMERIZATION; DRUG CONFORMATION; DRUG RECEPTOR BINDING; GLUCOSE HOMEOSTASIS; LIGAND BINDING; LIPID METABOLISM; METABOLIC REGULATION; MOLECULAR INTERACTION; NON INSULIN DEPENDENT DIABETES MELLITUS; PROTEIN DOMAIN; RECEPTOR UPREGULATION; AMINO ACID SEQUENCE; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; CRYSTALLOGRAPHY; DRUG DESIGN; DRUG POTENTIATION; HUMAN; MOLECULAR GENETICS; SEQUENCE HOMOLOGY; SURFACE PROPERTY;

AMINO ACID SEQUENCE; BINDING SITES; CRYSTALLOGRAPHY; DIABETES MELLITUS, TYPE 2; DIMERIZATION; DRUG DESIGN; HISTONE ACETYLTRANSFERASES; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; NUCLEAR PROTEINS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, RETINOIC ACID; RETINOID X RECEPTORS; SEQUENCE HOMOLOGY, AMINO ACID; SURFACE PROPERTIES; THIAZOLES; THIAZOLIDINEDIONES; TRANSCRIPTION FACTORS; TRETINOIN;

EID: 0033681001     PISSN: 10972765     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1097-2765(00)80448-7     Document Type: Article

References (40)

1. Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α
2. Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains
3. A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat
4. Crystallography and NMR system: A new software suite for macromolecular structure determination
5. Molecular basis of agonism and antagonism in the oestrogen receptor
6. The CCP4 suite: Programs for protein crystallography
7. Solvent-accessible surfaces of proteins and nucleic acids
8. Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors α and δ
9. Increasing the complexity of coactivation in nuclear receptor signaling
10. N-(2-Benzoylphenyl)-L-tyrosine PPARγ agonists. I. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents
11. 9-cis retinoic acid is a high affinity ligand for the retinoid X receptor
12. Conformational adaptation of agonists to the human nuclear receptor RARγ
13. Differential expression and activation of a family of murine peroxisome proliferator-activated receptors
14. The nuclear receptor PPARγ - Bigger than fat
15. 9-cis retinoic acid stereoisomer binds and activates the nuclear receptor RXRα
16. The RXR heterodimers and orphan receptors
17. Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists
18. AmoRe: An automated package for molecular replacement
19. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-γ
20. A unified nomenclature system for the nuclear receptor superfamily
21. Oscillation data reduction program
22. Engineering novel specificities for ligand-activated transcription in the nuclear hormone receptor RXR
23. Crystal structure of the RAR-γ ligand-binding domain bound to all-trans retinoic acid
24. Peroxisome proliferator-activated receptors, orphans with ligands and functions
25. Transactivation by retinoid X receptor-peroxisome proliferator-activated receptor γ (PPARγ) heterodimers: Intermolecular synergy requires only the PPARγ hormone-dependent activation function
26. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
27. PPAR-γ: Adipogenic regulator and thiazolidinedione receptor
28. Heterodimerization of the Drosophila ecdysone receptor with retinoid X receptor and ultraspiracle
29. Adipocyte-specific transcription factor ARF6 is a heterodimeric complex of two nuclear hormone receptors, PPARgamma and RXRalpha
30. Crystal structure of the ligand binding domain of the human nuclear receptor PPARγ
31. A structural role for hormone in the thyroid hormone receptor
32. Nuclear-receptor ligands and ligand-binding domains
33. Atomic structure of progesterone complexed with its receptor
34. Peroxisome proliferator-activated receptor agonists
35. The PPARs: From orphan receptors to drug discovery
36. A canonical structure for the ligand-binding domain of nuclear receptors
37. Molecular recognition of fatty acids by peroxisome proliferator-activated receptors
38. Thyroid hormone receptor variant alpha2. Role of the ninth heptad in DNA binding, heterodimerization with retinoid X receptors, and dominant negative activity
39. Drosophila ultraspiracle modulates ecdysone receptor function via heterodimer formation
40. Mutations that alter ligand-induced switches and dimerization activities in the retinoid X receptor