The 1,25-dihydroxyvitamin D3 (VD) analogues MC903, EB1089 and KH1060 activate the VD receptor: Homodimers show higher ligand sensitivity than heterodimers with retinoid X receptors

Carsten Carlberg1, Ida S. Mathiasen2, Jean-Hilaire Saurat1, Lise Binderup2
1Clinique de Dermatologie, Hôpital Cantonal Universitaire, 1211 Genève 14, Switzerland
2Biological Research and Development, LEO Pharmaceutical Products, 2750 Ballerup, Denmark

Tài liệu tham khảo

Bikle, 1992, Vitamin D: New actions, new analogues, new therapeutic potential, Endocrine Rev., 13, 765 Pike, 1991, Vitamin D3 receptors: structure and function in transcription, A. Rev. Nutr., 11, 189, 10.1146/annurev.nu.11.070191.001201 Evans, 1988, The steroid and thyroid hormone receptor superfamily, Science, 240, 889, 10.1126/science.3283939 Minghetti, 1988, 1,25(OH)2-vitamin D3 receptors: gene regulation and genetic circuitry, FASEB J., 2, 3043, 10.1096/fasebj.2.15.2847948 Yu, 1992, Transcriptional regulation by the nuclear receptor superfamily, Curr. Opin. Biotech., 3, 597, 10.1016/0958-1669(92)90002-Z Parker, 1993, Steroid and related receptors, Curr. Opin. Cell Biol., 5, 499, 10.1016/0955-0674(93)90016-J Sone, 1991, A 55-kilodalton accessory factor facilitates vitamin D receptor DNA binding of rat, Molec. Endocr., 5, 1578, 10.1210/mend-5-11-1578 Ross, 1992, A nuclear protein essential for binding of rat 1,25-dihydroxyvitamin D3 receptor to its response elements, 89, 256 Yu, 1991, RXRβ: a coregulator that enhances binding of retinoic acid, thyroid hormone, and vitamin D receptors to their cognate response elements, Cell, 67, 1251, 10.1016/0092-8674(91)90301-E Kliewer, 1992, Retinoid X receptors interacts with nuclear receptors in retinoic acid, thyroid hormone and vitamin D3 signalling, Nature, 355, 446, 10.1038/355446a0 Umesono, 1991, Direct repeats as selective response elements for the thyroid hormone, retinoic acid, and vitamin D3 receptors, Cell, 65, 1255, 10.1016/0092-8674(91)90020-Y Noda, 1990, Identification of a DNA sequence responsible for binding of the 1,25-dihydroxyvitamin D3 receptor and 1,25-dihydroxyvitamin D3 enhancement of mouse secreted phosphoprotein 1 (Spp-1 or osteopontin) gene expression, 87, 9995 Carlberg, 1993, Two nuclear signalling pathways for vitamin D, Nature, 361, 657, 10.1038/361657a0 Kerner, 1989, Sequence elements in the human osteocalcin gene confer basal activation and inducible response to hormonal vitamin D3, 86, 4455 Morrison, 1989, 1,25-dihydroxyvitamin D-responsive element and glucocorticoid repression in the osteocalcin gene, Science, 246, 1158, 10.1126/science.2588000 Carlberg, 1993, RXR-independent action of the receptors for thyroid hormone, retinoic acid, and vitamin D on inverted palindromes, Biochem. Biophys. Res. Commun., 195, 1345, 10.1006/bbrc.1993.2191 Green, 1993, Promiscuous liaisons, Nature, 361, 590, 10.1038/361590a0 Vieth, 1990, The mechanisms of vitamin D toxicity, Bone Mineral, 11, 267, 10.1016/0169-6009(90)90023-9 Binderup, 1992, Origin of the use of calcipotriol in psoriasis treatment, Rev. Contemp. Pharmacother., 3, 357 Binderup, 1992, Immunological properties of vitamin D analogues and metabolites, Biochem. Pharmac., 43, 1885, 10.1016/0006-2952(92)90630-2 Mathiasen, 1993, EB1089, a novel vitamin D analogue, has strong antiproliferative and differentiation inducing effects on cancer cells, J. Steroid Biochem. Molec. Biol., 46, 365, 10.1016/0960-0760(93)90226-M Luckow, 1987, CAT construction with multiple unique restriction sites for the functional analysis of eukaryotic promoters and regulatory elements, Nucleic Acids Res., 15, 5490, 10.1093/nar/15.13.5490 Schneider, 1972, Cell lines derived from late embryonic stages of Drosophila melanogaster, J. Embryl. Exp. Morph., 27, 353 Pothier, 1992, An improved CAT assay for promoter analysis in either transgenic mice or tissue culture cells, DNA Cell Biol., 11, 83, 10.1089/dna.1992.11.83 Carlberg, 1993, 9-cis retinoic acid is a natural antagonist for the retinoic acid receptor response pathway, Biochem. J., 295, 343, 10.1042/bj2950343 Schräder, 1993, Interaction between retinoic acid and vitamin D signalling pathways, J. Biol. Chem., 268, 17830, 10.1016/S0021-9258(17)46779-2 Schräder, 1993, RXR-dependent and RXR-independent transactivation by retinoic acid receptors, Nucleic Acids Res., 21, 1231, 10.1093/nar/21.5.1231 Binderup, 1991, 20-epi-vitamin D3 analogues: a novel class of potent regulators of cell growth and immune responses, Biochem. Pharmac., 42, 1569, 10.1016/0006-2952(91)90426-6 Schräder, 1994, Specificity and flexibility of vitamin D signaling, J. Biol. Chem., 269, 5501, 10.1016/S0021-9258(17)37487-2 Schräder, 1994, Vitamin D3-thyroid hormone receptor heterodimer polarity directs ligand sensitivity of transactivation, Nature, 370, 382, 10.1038/370382a0