Nuclear receptor ligand-binding domains: Three-dimensional structures, molecular interactions and pharmacological implications

Trends in Pharmacological Sciences

Volumn 21, Issue 10, 2000, Pages 381-388

  Bourguet, William ^a   Germain, Pierre ^a   Gronemeyer, Hinrich ^a  

^a INSERM   (France)

Author keywords

[No Author keywords available]

Indexed keywords

9 CIS RETINOIC ACID; CELL NUCLEUS RECEPTOR; DIETHYLSTILBESTROL; ESTRADIOL; ESTROGEN RECEPTOR; GENISTEIN; HYDROXYTAMOXIFEN; LIOTHYRONINE; MEMBRANE RECEPTOR; N BUTYL 11 (3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; OLEIC ACID; RALOXIFENE; RETINOIC ACID; RETINOIC ACID RECEPTOR; RETINOID X RECEPTOR; ROSIGLITAZONE; THYROID HORMONE RECEPTOR;

AGONIST; ALLOSTERISM; CRYSTAL STRUCTURE; DRUG ANTAGONISM; DRUG DEVELOPMENT; LIGAND BINDING; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION;

ANDROGEN ANTAGONISTS; ANIMAL; BINDING SITES; ESTROGEN ANTAGONISTS; GLUCOCORTICOIDS; HUMAN; LIGANDS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; SUPPORT, NON-U.S. GOV'T;

EID: 0034306499     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0165-6147(00)01548-0     Document Type: Review

References (60)

1. Transcription factors 3; nuclear receptors
2. Nuclear receptor coregulators; cellular and molecular biology
3. The coregulator exchange intranscriptional functions of nuclear receptors
4. Increasing the complexity of coactivation in nuclear receptor signaling
5. Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α
6. A canonical structure for the ligand-binding domain of nuclear receptors
7. Asymmetry in the PPARγ/RXRα crystal structure reveals the molecular basis of heterodimerization among nuclear receptors
8. Crystal structure of the human RXRα ligand-binding domain bound to its natural ligand 9-cis retinoic acid
9. Ligand binding and co-activator assembly ofthe peroxisome proliferator-activated receptor-γ
10. Crystal structure of the ligand-binding domain of the human nuclear receptor PPARγ
11. Molecular recognition of fatty acids by peroxisome proliferator-activated receptors
12. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
13. Structure and specificity of nuclear receptor-coactivator interactions
14. A signature motif in transcriptional co-activators mediates binding to nuclear receptors
15. Determinants of coactivator LxxLL motif specificity in nuclear receptor transcriptional activation
16. Molecular basis of agonism and antagonism in the oestrogen receptor
17. Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains
18. Crystal structure of the RAR-γ ligand-binding domain bound to all-trans retinoic acid
19. Structure of the ligand-binding domain of oestrogen receptor β in the presence of a partial agonist and a full antagonist
20. Differential response of estrogen receptor α and estrogen receptor β to partial estrogen agonists/antagonists
21. A peroxisome proliferator-activated receptor γ ligand inhibits adipocyte differentiation
22. The RXR heterodimers and orphan receptors
23. Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators
24. Terminal differentiation of human liposarcoma cells induced by ligands for peroxisome proliferator-activated receptor γ and the retinoid X receptor
25. Terminal differentiation of human breast cancer through PPARγ
26. Peroxisome proliferator-activated receptors; nuclear control of metabolism
27. Nuclear receptor regulation ofcholesterol and bile acid metabolism
28. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway
29. SXR, a novel steroid and xenobiotic-sensing nuclear receptor
30. Conformational adaptation of agonists to the human nuclear receptor RARγ
31. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists
32. Enantiomer discrimination illustrated by high resolution crystal structures of the human nuclear receptor hRARγ
33. Cloning of a novel estrogen receptor expressed in rat prostate and ovary
34. Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-α or estrogen receptor-β
35. Two distinct actions of retinoid-receptor ligands
36. Sensitization of diabetic and obese mice to insulin by retinoic X receptor agonists
37. Ligand-independent recruitment of SRC-1 to estrogen receptor β through phosphorylation of activation function AF-1
38. Basic guide to the mechanisms of antiestrogen action
39. Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-estrogen 4-hydroxytamoxifen
40. Transcriptional cross-talk, the second mode of steroid hormone receptor action
41. Therapeutic potential of selective modulators of nuclear receptor action
42. RAR-specific agonist/antagonists which dissociate transactivation and AP1 transrepression inhibit anchorage-independent cell proliferation
43. Synthetic glucocorticoids that dissociate transactivation and AP-1 transrepression exhibit anti-inflammatory activity in vivo
44. Nuclear receptor cofactors as chromatin remodelers
45. AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer
46. A cold-inducible coactivator of nuclear receptors linked to adaptive thermogenesis
47. Cloning and characterization of a specific coactivator, ARA70, for the androgen receptor in human prostate cells
48. Interaction of the putative androgen receptor-specific coactivator ARA70/ELE1α with multiple steroid receptors and identification of an internally deleted ELE1β isoform
49. The CoRNR motif controls the recruitment of corepressors by nuclear hormone receptors
50. Mechanism of corepressor binding and release from nuclear hormone receptors
51. Molecular determinants of nuclear receptor-corepressor interaction
52. Dissection of the LxxLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries; discovery of peptide antagonists of estrogen receptors α and β
53. Estrogen receptor (ER) modulators each induce distinct conformational changes in ERα and ERβ
54. HATs; selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF
55. 20-epi analogues of 1,25-dihydroxyvitamin D3 are highly potent inducers of DRIP coactivator complex binding to the vitamin D3 receptor
56. A structural role for hormone in the thyroid hormone receptor
57. The crystal structure of the nuclear receptor for vitamin D bound to its natural ligand
58. Atomic structure of progesterone complexed with its receptor
59. Crystallographic comparison of the estrogen and progesterone receptor's ligand-binding domains
60. Structural aspects of agonism and antagonism in the oestrogen receptor