Identification of single amino acid substitutions of Cys-736 that affect the steroid-binding affinity and specificity of the glucocorticoid receptor using phenotypic screening in yeast

Molecular Endocrinology

Volumn 10, Issue 11, 1996, Pages 1358-1370

  Lind, Ulrika ^a   Carlstedt Duke, Jan ^a   Gustafsson, Jan Åke ^a   Wright, Anthony P H ^a  

^a KAROLINSKA INSTITUTE   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

GLUCOCORTICOID RECEPTOR; STEROID HORMONE;

AMINO ACID SUBSTITUTION; ARTICLE; CONTROLLED STUDY; HORMONE RECEPTOR INTERACTION; MOLECULAR RECOGNITION; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; SACCHAROMYCES CEREVISIAE; STRUCTURE ACTIVITY RELATION;

AMINO ACIDS; ANIMALS; COS CELLS; CYSTEINE; HUMANS; MAMMALS; MUTAGENESIS; MUTATION; PHENOTYPE; PROTEIN ENGINEERING; RECEPTORS, GLUCOCORTICOID; RECOMBINANT PROTEINS; SENSITIVITY AND SPECIFICITY; STEROIDS; SUBSTRATE SPECIFICITY; TRANS-ACTIVATION (GENETICS); YEASTS;

MAMMALIA; SACCHAROMYCES CEREVISIAE;

EID: 0030471105     PISSN: 08888809     EISSN: None     Source Type: Journal    
DOI: 10.1210/me.10.11.1358     Document Type: Article

References (62)

1. Evans RM 1988 The steroid and thyroid hormone receptor superfamily. Science 240:889-895
2. Carlstedt-Duke J, Strömstedt P-E, Wrange Ö, Bergman T, Gustafsson J-Å, Jörnvall H 1987 Domain structure of the glucocorticoid receptor protein. Proc Natl Acad Sci USA 84:4437-4440
3. Picard D, Yamamoto KR 1987 Two signals mediate hormone-dependent nuclear localization of the glucocorticoid receptor. EMBO J 6:3333-3340
4. Hollenberg SM, Evans RM 1988 Multiple and cooperative trans-activation domains of the human glucocorticoid receptor. Cell 55:899-906
5. Danielsen M, Northrop JP, Jonklaas J, Ringold GM 1987 Domains of the glucocorticoid receptor involved in specific and nonspecific deoxyribonucleic acid binding, hormone activation, and transcriptional enhancement. Mol Endocrinol 1:816-822
6. Godowski PJ, Picard D, Yamamoto KR 1988 Signal transduction and transcriptional regulation by glucocorticoid receptor-LexA fusion proteins. Science 241:812-816
7. Hollenberg SM, Giguere V, Segui P, Evans RM 1987 Colocalization of DNA-binding and transcriptional activation functions in the human glucocorticoid receptor. Cell 49:39-46
8. r = 90,000 heat shock protein with the steroid-binding domain of the glucocorticoid receptor. J Biol Chem 263:18520-18523
9. Howard KJ, Holley SJ, Yamamoto KR, Distelhorst CW 1990 Mapping the HSP90 binding region of the glucocorticoid receptor. J Biol Chem 265:11928-11935
10. Dalman FC, Scherrer LC, Taylor LP, Akil H, Pratt WB 1991 Localization of the 90-kDa heat shock protein-binding site within the hormone-binding domain of the glucocorticoid receptor by peptide competition. J Biol Chem 266:3482-3490
11. Cadepond F, Schweizer GG, Segard Ml, Jibard N, Hollenberg SM, Giguere V, Evans RM, Baulieu EE 1991 Heat shock protein 90 as a critical factor in maintaining glucocorticosteroid receptor in a nonfunctional state. J Biol Chem 266:5834-5841
12. Pratt WB, Hutchison KA, Scherrer LC 1992 Steroid receptor folding by heat shock proteins and composition of the receptor heterocomplex. Trends Endocrinol Metab 3:326-333
13. Bresnick EH, Dalman FC, Sanchez ER, Pratt WB 1989 Evidence that the 90-kDa heat shock protein is necessary for the steroid binding conformation of the L cell glucocorticoid receptor. J Biol Chem 264:4992-4997
14. Ohara-Nemoto Y, Strömstedt P-E, Dahlman-Wright K, Nemoto T, Gustafsson J-Å, Carlstedt-Duke J 1990 The steroid-binding properties of recombinant glucocorticoid receptor: a putative role for heat shock protein hsp90. J Steroid Biochem Mol Biol 37:481-490
15. Nemoto T, Ohara-Nemoto Y, Denis M, Gustafsson J-Å 1990 The transformed glucocorticoid receptor has a lower steroid-binding affinity than the nontransformed receptor. Biochemistry 29:1880-1886
16. Godowski PJ, Rusconi S, Miesfeld R, Yamamoto KR 1987 Glucocorticoid receptor mutants that are constitutive activators of transcriptional enhancement. Nature 325:365-368
17. Miesfeld R, Godowski PJ, Maler BA, Yamamoto KR 1987 Glucocorticoid receptor mutants that define a small region sufficient for enhancer activation. Science 236:423-427
18. Picard D, Salser SJ, Yamamoto KR 1988 A movable and regulable inactivation function within the steroid binding domain of the glucocorticoid receptor. Cell 54:1073-1080
19. Simons SS, Sistare FD, Chakraborti PK 1989 Steroid binding activity is retained in a 16-kDa fragment of the steroid binding domain of rat glucocorticoid receptors. J Biol Chem 264:14493-14497
20. Chakraborti PK, Garabedian MJ, Yamamoto KR, Simons SS 1992 Role of cysteines 640, 656, and 661 in steroid binding to rat glucocorticoid receptors. J Biol Chem 267:11366-11373
21. Rusconi S, Yamamoto KR 1987 Functional dissection of the hormone and DNA binding activities of the glucocorticoid receptor. EMBO J 6:1309-1315
22. 3H]promegestone. A comparison with the glucocorticoid receptor. J Biol Chem 265:12973-12977
23. Carlstedt-Duke J, Strömstedt P-E, Persson B, Cederlund E, Gustafsson J-Å, Jörnvall H 1988 Identification of hormone-interacting amino acid residues within the steroid-binding domain of the glucocorticoid receptor in relation to other steroid hormone receptors. J Biol Chem 263:6842-6846
24. Simons SS, Pumphrey JG, Rudikoff S, Eisen HJ 1987 Identification of cysteine 656 as the amino acid of hepatoma tissue culture cell glucocorticoid receptors that is covalently labeled by dexamethasone 21-mesylate. J Biol Chem 262:9676-9680
25. Smith LI, Bodwell JE, Mendel DB, Ciardelli T, North WG, Munck A 1988 Identification of cysteine-644 as the covalent site of attachment of dexamethasone 21-mesylate to murine glucocorticoid receptors in WEHI-7 cells. Biochemistry 27:3747-3753
26. Sweet F, Murdock GL 1987 Affinity labeling of hormone-specific proteins. Endocr Rev 8:154-184
27. Wrenn CK, Katzenellenbogen BS 1993 Structure-function analysis of the hormone binding domain of the human estrogen receptor by region-specific mutagenesis and phenotypic screening in yeast. J Biol Chem 268:24089-24098
28. Garabedian MJ, Yamamoto KR 1992 Genetic dissection of the signaling domain of a mammalian steroid receptor in yeast. Mol Biol Cell 3:1245-1257
29. Giguere V, Hollenberg SM, Rosenfeld MG, Evans RM 1986 Functional domains of the human glucocorticoid receptor. Cell 46:645-652
30. Patterson MN, McPhaul MJ, Hughes IA 1994 Androgen insensitivity syndrome. Baillieres Clin Endocrinol Metab 8:379-404
31. Chatterjee VK, Beck-Peccoz P 1994 Hormone-nuclear receptor interactions in health and disease. Thyroid hormone resistance. Baillieres Clin Endocrinol Metab 8:267-283
32. Hurley DM, Accili D, Stratakis CA, Karl M, Vamvakopoulos N, Rorer E, Constantine K, Taylor SI, Chrousos GP 1991 Point mutation causing a single amino acid substitution in the hormone binding domain of the glucocorticoid receptor in familial glucocorticoid resistance. J Clin Invest 87:680-686
33. Malchoff DM, Brufsky A, Reardon G, McDermott P, Javier EC, Bergh CH, Rowe D, Malchoff CD 1993 A mutation of the glucocorticoid receptor in primary cortisol resistance. J Clin Invest 91:1918-1925
34. Karl M, Lamberts SW, Detera WS, Encio IJ, Stratakis CA, Hurley DM, Accili D, Chrousos GP 1993 Familial glucocorticoid resistance caused by a splice site deletion in the human glucocorticoid receptor gene. J Clin Endocrinol Metab 76:683-689
35. Lee S, Duncan LK, Cou H, Chen D, Kohli K, Huang C-F, Stallcup MR 1995 A somatic cell genetic method for identification of untargeted mutations in the glucocorticoid receptor that cause hormone binding deficiencies. Mol Endocrinol 9:826-837
36. Bourguet W, Ruff M, Chambon P, Gronemeyer H, Moras D 1995 Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α. Nature 375:377-382
37. Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronemeyer H, Moras D 1995 Crystal structure of the RARγ ligand-binding domain bound to all-trans retinoic acid. Nature 378:681-689
38. Wagner RL, Apriletti JW, Mcgrath ME, West BL, Baxter JD, Fletterick RJ 1995 A structural role for hormone in the thyroid hormone receptor. Nature 378:690-697
39. Wurtz JM, Bourguet W, Renaud JP, Vivat V, Chambon P, Moras D, Gronemeyer H 1996 A canonical structure for the ligand-binding domain of nuclear receptors. Nature Struct Biol 3:87-94
40. Danielian PS, White R, Lees JA, Parker MG 1992 Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors. EMBO J 11:1025-1033
41. Chen D, Stallcup MR 1994 The hormone-binding role of 2 cysteines near the C terminus of the mouse glucocorticoid receptor. J Biol Chem 269:7914-8
42. Chothia C 1975 Structural invariants in protein folding. Nature 254:304-308
43. Danielsen M, Northrop JP, Ringold GM 1986 The mouse glucocorticoid receptor: mapping of functional domains by cloning, sequencing and expression of wild-type and mutant receptor proteins. EMBO J 5:2513-2522
44. Byravan S, Milhon J, Rabindran SK, Olinger B, Garabedian MJ, Danielsen M, Stallcup MR 1991 Two point mutations in the hormone-binding domain of the mouse glucocorticoid receptor that dramatically reduce its function. Mol Endocrinol 5:752-758
45. Benhamou B, Garcia T, Lerouge T, Vergezac A, Gofflo D, Bigogne C, Chambon P, Gronemeyer H 1992 A single amino acid that determines the sensitivity of progesterone receptors to RU486. J Steroid Biochem 255:206-209
46. Chen D, Kohli K, Zhang S, Danielsen M, Stallcup MR 1994 Phenylalanine-780 near the C-terminus of the mouse glucocorticoid receptor is important for ligand binding affinity and specificity. Mol Endocrinol 8:422-430
47. Milhon J, Kohli K, Stallcup MR 1994 Genetic analysis of the N-terminal end of the glucocorticoid receptor hormone binding domain. J Steroid Biochem Mol Biol 51:11-19
48. Chakraborti PK, Garabedian MJ, Yamamoto KR, Simons SJ 1991 Creation of "super" glucocorticoid receptors by point mutations in the steroid binding domain. J Biol Chem 266:22075-22078
49. Warriar N, Yu C, Govindan MV 1994 Hormone binding domain of human glucocorticoid receptor. Enhancement of transactivation function by substitution mutants M565R and A573Q. J Biol Chem 269:29010-29015
50. Zhang S, Liang X, Danielsen M 1996 Role of the C terminus of the glucocorticoid receptor in hormone binding and agonist/antagonist discrimination. Mol Endocrinol 10:24-34
51. Schena M, Yamamoto KR 1988 Mammalian glucocorticoid receptor derivatives enhance transcription in yeast. Science 241:965-967
52. Wright AP, Gustafsson J-Å 1992 Glucocorticoid-specific gene activation by the intact human glucocorticoid receptor expressed in yeast. Glucocorticoid specificity depends on low level receptor expression. J Biol Chem 267:11191-11195
53. Kralli A, Bohen SP, Yamamoto KR 1995 LEM1, an ATP-binding-cassette transporter, selectively modulates the biological potency of steroid hormones. Proc Natl Acad Sci USA 92:4701-4705
54. Sikorski RS, Hieter P 1989 A system of shuttle vectors and yeast host strains designed for efficient manipulation of DNA in Saccharomyces cerevisiae. Genetics 122: 19-27
55. Wright AP, Carlstedt-Duke J, Gustafsson J-Å 1990 Ligand-specific transactivation of gene expression by a derivative of the human glucocorticoid receptor expressed in yeast. J Biol Chem 265:14763-14769
56. Andersson S, Davis DL, Dahlback H, Jörnvall H, Russell DW 1989 Cloning, structure, and expression of the mitochondrial cytochrome P-450 sterol 26-hydroxylase, a bile acid biosynthetic enzyme. J Biol Chem 264:8222-8229
57. Schule R, Muller M, Kaltschmidt C, Renkawitz R 1988 Many transcription factors interact synergistically with steroid receptors. Science 242:1418-1420
58. Kunkel TA, Roberts JD, Zakour RA 1987 Rapid and efficient site-specific mutagenesis without phenotypic selection. Methods Enzymol 154:367-382
59. McClary JA, Witney F, Geisselsoder J 1989 Efficient site-directed in vitro mutagenesis using phagemid vectors. Biotechniques 7:282-289
60. Gietz RD, Schiestl RH 1991 Applications of high efficiency lithium acetate transformation of intact yeast cells using single-stranded nucleic acids as carrier. Yeast 7:253-263
61. Schiestl RH, Gietz RD 1989 Hrgh efficiency transformation of intact yeast cells using single stranded nucleic acids as a carrier. Curr Genet 16:339-346
62. Kaiser P, Auer B 1993 Rapid shuttle plasmid preparation from yeast cells by transfer to E. coli. Biotechniques 14:552