Structural basis for the glucocorticoid response in a mutant human androgen receptor (ARccr) derived from an androgen-independent prostate cancer

Journal of Medicinal Chemistry

Volumn 45, Issue 7, 2002, Pages 1439-1446

  Matias, Pedro M ^a   Carrondo, Maria Arménia ^a   Coelho, Ricardo ^a   Thomaz, Monica ^b   Zhao, Xiao Yan ^c   Wegg, Anja ^d   Crusius, Kerstin ^d   Egner, Ursula ^d   Donner, Peter ^d  

^a INSTITUTO DE TECNOLOGIA QUÍMICA E BIOLÓGICA   (Portugal)

^b INSTITUTO DE BIOLOGIA EXPERIMENTAL E TECNOLÓGICA   (Portugal)

^c BAYER AG   (Germany)

^d BAYER PHARMA AG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ANDROGEN RECEPTOR; CORTISONE; FLUDROCORTISONE; GLUCOCORTICOID; HYDROCORTISONE; MUTANT PROTEIN;

ALPHA HELIX; ARTICLE; CANCER CELL CULTURE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG RECEPTOR BINDING; DRUG RESPONSE; DRUG SCREENING; GENE MUTATION; HUMAN; HUMAN CELL; HYDROGEN BOND; PROSTATE CARCINOMA; PROTEIN TERTIARY STRUCTURE; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ALGORITHMS; ANTI-INFLAMMATORY AGENTS; CRYSTALLOGRAPHY, X-RAY; ELECTROPHORESIS, POLYACRYLAMIDE GEL; ESCHERICHIA COLI; FLUDROCORTISONE; GLUCOCORTICOIDS; HUMANS; HYDROGEN BONDING; LIGANDS; MALE; MODELS, CHEMICAL; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; MUTATION; PHENOTYPE; PROSTATIC NEOPLASMS; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, ANDROGEN; TUMOR CELLS, CULTURED;

EID: 0037187408     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm011072j     Document Type: Article

References (45)

1. In vivo amplification of the androgen receptor gene and progression of human prostate cancer
2. Prostate cancer schemes for androgen escape
3. Mutation of the androgen receptor gene in metastatic androgen independent prostate cancer
4. Two mutations identified in the androgen receptor of the new human prostate cancer cell line MDA PCa 2a
5. Glucocorticoids can promote androgen-independent growth of prostate cancer cells through a mutated androgen receptor
6. 1alpha,-25-dihydroxyvitamin D3 inhibits prostate cancer cell growth by androgen-dependent and androgen-independent mechanisms
7. Establishment of two human prostate cancer cell lines derived from a single bone metastasis
8. Frequent detection of codon 877 mutation in the androgen receptor gene in advanced prostate cancers
9. Unusual specificity of the androgen receptor in the human prostate tumor cell line LNCaP: High affinity for progestagenic and estrogenic steroids
10. Structural evidence for ligand specificity in the binding domain of the human Androgen receptor: Implications for pathogenic gene mutations
11. Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone
12. Dictionary of protein secondary structure: Pattern recognition of hydrogen-bonded and geometrical features
13. Atomic structure of progesterone complexed with its receptor
14. PROCHECK - A program to check the stereochemical quality of proteins
15. Conformation of polypeptides and proteins
16. A solution for the best rotation to relate two sets of vectors
17. 5F
18. Cortisone
19. Cortisol methanol solvate. (11β,17α,21-Trihydroxy-pregn-4-ene-3,20-di-one methanol solvate)
20. 5N
21. Cambridge structural database
22. IsoStar: A library of information about nonbonded interactions
23. Enantiomer discrimination illustrated by high-resolution crystal structures of the human nuclear receptor hRARγ
24. Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands
25. Ligand-protein interactions in nuclear receptors of hormones
26. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
27. Molecular basis of agonism and antagonism in the oestrogen receptor
28. Structural insights into the mode of action of a pure antiestrogen
29. Eukaryotic proteins expressed in Escherichia coli: An improved thrombin cleavage and purification procedure of fusion proteins with glutathione S-transferase
30. Processing of X-ray diffraction data collected in oscillation mode
31. AMoRe: An automated package for molecular replacement
32. Free R value: A novel statistical quantity for assessing the accuracy of crystal structures
33. Automated refinement for protein crystallography
34. wARP: Improvement and extension of crystallographic phases by weighted averaging of multiple refined dummy atomic models
35. Dictionaries for heteros
36. SHELXL: High-resolution refinement
37. The Protein Data Bank: A computer-based archival file for macromolecular structures
38. Protein Data Bank
39. The CCP4 suite: Programs for protein crystallography
40. Improved Fourier coefficients for maps using phases from partial structures with errors
41. MOLSCRIPT: A program to produce both detailed and schematic plots of protein structures
42. Raster3D version 2.0. A program for photorealistic molecular graphics
43. Further additions to MolScript version 1.4, including reading and contouring of electron-density maps