High-affinity nuclear receptor binding of 20-epi analogues of 1,25- dihydroxyvitamin D3 correlates well with gene activation

Journal of Cellular Biochemistry

Volumn 62, Issue 3, 1996, Pages 325-333

  Nayeri, Sepideh ^a   Mathiasen, Ida S ^b   Binderup, Lise ^b   Carlberg, Carsten ^a  

^a GENEVA UNIVERSITY HOSPITALS   (Switzerland)

^b LEO PHARMA A S   (Denmark)

Author keywords

limited protease digestion assay; receptor binding; regulation of transcription; structure activity relationships; vitamin D3 analogues; vitamin D3 receptor

Indexed keywords

CALCITRIOL DERIVATIVE; CALCITRIOL RECEPTOR; LEXACALCITOL;

ARTICLE; BINDING AFFINITY; CANCER CELL; DRUG RECEPTOR BINDING; GENE ACTIVATION; HUMAN; HUMAN CELL; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TRANSCRIPTION REGULATION;

BINDING SITES; BREAST NEOPLASMS; CALCITRIOL; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOPEPTIDASES; GENE EXPRESSION; HUMANS; PROTEIN CONFORMATION; RECEPTORS, CALCITRIOL; RECEPTORS, RETINOIC ACID; RECOMBINANT PROTEINS; RETINOID X RECEPTORS; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS; TRANSFECTION; TUMOR CELLS, CULTURED;

EID: 0029741914     PISSN: 07302312     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-4644(199609)62:3<325::AID-JCB3>3.3.CO;2-O     Document Type: Article

References (34)

1. Bikle DD, Pillai S (1993): Vitamin D, calcium, and epidermal differentiation. Endocr Rev 14:3-19.
2. Binderup L, Kragballe K (1992): Origin of the use of calcipotriol in psoriasis treatment. Rev Contemp Pharmacother 3:357-365.
3. 3 analogues: A novel class of potent regulators of cell growth and immune responses. Biochem Pharmacol 42:1569-1575.
4. 3: Interplay with retinoid and thyroid hormone signalling. Eur J Biochem 231:517-527.
5. Carlberg C, Bendik I, Wyss A, Meier E, Sturzenbecker LJ, Grippo JF, Hunziker W (1993): Two nuclear signalling pathways for vitamin D. Nature 361:657-660.
6. 3 analogues MC903, EB1089 and KH1060 function as transcriptional activators: vitamin D receptor homodimers show higher ligand sensitivity than heterodimers with retinoid X receptors. J Steroid Biochem Mol Biol 51:137-142.
7. 3 receptor (VDR) homodimers into VDR-retinoid X receptor heterodimers. Mol Cell Biol 14:3329-3338.
8. Colston KW, Chander SK, Mackay AG, Coombes RC (1992): Effects of synthetic vitamin D analogues on breast cancer cell proliferation in vivo and in vitro. Biochem Pharmacol 44:693-702.
9. Evans RM (1988): The steroid and thyroid hormone receptor superfamily. Science 240:889-895.
10. Green S, Chambon P (1988): Nuclear receptors enhance our understanding of transcriptional regulation. Trends Genet 4:309-314.
11. Jones G, Calverley MJ (1993): A dialogue on analogues. Trends Endocrinol Metab 4:297-303.
12. 3 receptor binding site found in the rat natriuretic factor promoter. Biochem Biophys Res Commun 218:882-886.
13. Keidel S, LeMotte P, Apfel C (1994): Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping. Mol Cell Biol 14:287-298.
14. Kissmeyer A-M, Mathiasen IS, Latini S, Binderup L (1995): Pharmacokinetic studies of vitamin D analogues: Relationship to vitamin D binding protein (DBP). Endocrine 3:263-266.
15. Leng X, Tsai S, O'Malley BW, Tsai M-J (1993): Ligand-dependent conformational changes in thyroid hormone and retinoic acid receptors are potentially enhanced by heterodimerization with retinoid X receptor. J Steroid Biochem Mol Biol 46:643-661.
16. Li Q, Gardner DG (1994): Negative regulation of the human atrial natriuretic peptide gene by 1,25-dihydroxyvitamin D3. J Biol Chem 269:4934-4939.
17. Luckow B, Schütz G (1987): CAT constructions with multiple unique restriction sites for the functional analysis of eukaryotic promoters and regulatory elements. Nucleic Acids Res 15:5490.
18. 3 induced differentiation in a human promyelocytic leukemia cell line HL-60: receptor-mediated maturation to macrophagelike cells. J Cell Biol 98:391-398.
19. Mathiasen IS, Colston KW, Binderup L (1993): EB 1089, a novel vitamin D analogue, has strong antiproliferative and differentiation inducing effects on cancer cells. J Steroid Biochem Mol Biol 46:365-371.
20. McDonnell DP, Clemm DL, Hermann T, Goldman ME, Pike JW (1995): Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol Endocrinol 9:659-669.
21. Mørk Hansen C, Mathiasen IS, Binderup L (1996): The antiproliferative and differentiation-inducing effects of vitamin D analogues are not determined by the binding affinity for the vitamin D receptor alone. J Invest Dermatol 106: (in press).
22. Morrison NA, Shine J, Fragonas J-C, Verkest V, McMenemey ML, Eisman JA (1989): 1,25-Dihydroxyvitamin D-responsive element and glucocorticoid repression in the osteocalcin gene. Science 246:1158-1161.
23. 3 analogues is not related to the AP-1 pathway, but related to promoter selectivity. Oncogene 11:1853-1858.
24. 3 enhancement of mouse secreted phosphoprotein 1 (Spp-1 or osteopontin) gene expression. Proc Natl Acad Sci USA 87:9995-9999.
25. 3 are associated with enhanced activation of the vitamin D receptor. J Biol Chem 270:10551-10558.
26. Pike JW (1991): Vitamin DS receptors: Structure and function in transcription. Annu Rev Nutr 11:189-216.
27. Pothier F, Quellet M, Julien J-P, Guérin SL (1992): An improved CAT assay for promoter analysis in either transgenic mice or tissue culture cells. DNA Cell Biol 11:83-90.
28. 3R heterodimer polarity directs ligand sensitivity of transactivation. Nature 370:382-386.
29. 3 response elements formed by inverted palindromes: Polarity-directed ligand sensitivity of VDR-RXR heterodimer-mediated transactivation. Mol Cell Biol 15:1154-1161.
30. Stern P (1981): A monolog on analogs. Calcif Tissue Int 33:1-4.
31. 3 receptors. Cell 65:1255-1266.
32. Vieth R (1990): The mechanisms of vitamin D toxicity. Bone Miner 11:267-272.
33. Walters MR (1992): Newly identified actions of the vitamin D endocrine system. Endocrine Rev 13:719-764.
34. Wiberg K, Ljunghall S, Binderup L, Ljunggren O (1995): Studies on two new vitamin D analogs, EB1089 and KH1060: Effects on bone resorption and osteoclast recruitment in vitro. Bone 17:391-395.