The RXR agonists PA024 and HX630 have different abilities to activate LXR/RXR and to induce ABCA1 expression in macrophage cell lines

Biochemical Pharmacology

Volumn 76, Issue 8, 2008, Pages 1006-1013

  Nishimaki Mogami, Tomoko ^a   Tamehiro, Norimasa ^a   Sato, Yoji ^a   Okuhira, Kei ichiro ^a   Sai, Kimie ^a   Kagechika, Hiroyuki ^b   Shudo, Koichi ^d   Abe Dohmae, Sumiko ^c   Yokoyama, Shinji ^c   Ohno, Yasuo ^a   Inoue, Kazuhide ^a   Sawada, Jun ichi ^a  

^a NATIONAL INSTITUTE OF HEALTH SCIENCES   (Japan)

^b TOKYO MEDICAL AND DENTAL UNIVERSITY   (Japan)

^c NAGOYA CITY UNIVERSITY GRADUATE SCHOOL OF MEDICAL SCIENCES   (Japan)

^d Itsu Research Institute   (Japan)

Author keywords

ABCA1; HDL; Liver X receptor; Peroxisome proliferator activated receptor ; Retinoid X receptor modulator

Indexed keywords

ABC TRANSPORTER A1; APOLIPOPROTEIN A1; CHOLESTEROL; HX 630; IMMUNOMODULATING AGENT; LIVER X RECEPTOR; LIVER X RECEPTOR ALPHA; MESSENGER RNA; PA 024; RETINOID X RECEPTOR; RETINOID X RECEPTOR AGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GENE; GENE EXPRESSION; GENETIC TRANSFECTION; LIVER X RECEPTOR RESPONSIVE ELEMENT; MACROPHAGE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN EXPRESSION; RECEPTOR UPREGULATION; TRANSACTIVATION; TRANSCRIPTION INITIATION;

ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; CELL DIFFERENTIATION; CELL LINE; DNA-BINDING PROTEINS; HUMANS; MACROPHAGES; MICE; MONOCYTES; PPAR GAMMA; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, RETINOIC ACID; RNA, MESSENGER; RNA, RIBOSOMAL, 18S; TETRADECANOYLPHORBOL ACETATE; TRANSFECTION;

EID: 52949119173     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2008.08.005     Document Type: Article

References (34)

1. Yokoyama S. Assembly of high-density lipoprotein. Arterioscler Thromb Vasc Biol 26 (2006) 20-27
2. Bodzioch M., Orso E., Klucken J., Langmann T., Bottcher A., Diederich W., et al. The gene encoding ATP-binding cassette transporter 1 is mutated in Tangier disease. Nat Genet 22 (1999) 347-351
3. Brooks-Wilson A., Marcil M., Clee S.M., Zhang L.H., Roomp K., van Dam M., et al. Mutations in ABC1 in Tangier disease and familial high-density lipoprotein deficiency. Nat Genet 22 (1999) 336-345
4. Rust S., Rosier M., Funke H., Real J., Amoura Z., Piette J.C., et al. Tangier disease is caused by mutations in the gene encoding ATP-binding cassette transporter 1. Nat Genet 22 (1999) 352-355
5. Singaraja R.R., Bocher V., James E.R., Clee S.M., Zhang L.H., Leavitt B.R., et al. Human ABCA1 BAC transgenic mice show increased high density lipoprotein cholesterol and apoAI-dependent efflux stimulated by an internal promoter containing liver X receptor response elements in intron 1. J Biol Chem 276 (2001) 33969-33979
6. Vaisman B.L., Lambert G., Amar M., Joyce C., Ito T., Shamburek R.D., et al. ABCA1 overexpression leads to hyperalphalipoproteinemia and increased biliary cholesterol excretion in transgenic mice. J Clin Invest 108 (2001) 303-309
7. Joyce C.W., Amar M.J., Lambert G., Vaisman B.L., Paigen B., Najib-Fruchart J., et al. The ATP binding cassette transporter A1 (ABCA1) modulates the development of aortic atherosclerosis in C57BL/6 and apoE-knockout mice. Proc Natl Acad Sci USA 99 (2002) 407-412
8. Singaraja R.R., Fievet C., Castro G., James E.R., Hennuyer N., Clee S.M., et al. Increased ABCA1 activity protects against atherosclerosis. J Clin Invest 110 (2002) 35-42
9. Gordon T., Castelli W.P., Hjortland M.C., Kannel W.B., and Dawber T.R. High density lipoprotein as a protective factor against coronary heart disease. The Framingham study. Am J Med 62 (1977) 707-714
10. Fielding C.J., and Fielding P.E. Molecular physiology of reverse cholesterol transport. J Lipid Res 36 (1995) 211-228
11. Costet P., Luo Y., Wang N., and Tall A.R. Sterol-dependent transactivation of the ABC1 promoter by the liver X receptor/retinoid X receptor. J Biol Chem 275 (2000) 28240-28245
12. Langmann T., Klucken J., Reil M., Liebisch G., Luciani M.F., Chimini G., et al. Molecular cloning of the human ATP-binding cassette transporter 1 (hABC1): evidence for sterol-dependent regulation in macrophages. Biochem Biophys Res Commun 257 (1999) 29-33
13. Schwartz K., Lawn R.M., and Wade D.P. ABC1 gene expression and apoA-I-mediated cholesterol efflux are regulated by LXR. Biochem Biophys Res Commun 274 (2000) 794-802
14. Venkateswaran A., Laffitte B.A., Joseph S.B., Mak P.A., Wilpitz D.C., Edwards P.A., et al. Control of cellular cholesterol efflux by the nuclear oxysterol receptor LXR alpha. Proc Natl Acad Sci USA 97 (2000) 12097-12102
15. Chinetti G., Lestavel S., Bocher V., Remaley A.T., Neve B., Torra I.P., et al. PPAR-alpha and PPAR-gamma activators induce cholesterol removal from human macrophage foam cells through stimulation of the ABCA1 pathway. Nat Med 7 (2001) 53-58
16. Chawla A., Repa J.J., Evans R.M., and Mangelsdorf D.J. Nuclear receptors and lipid physiology: opening the X-files. Science 294 (2001) 1866-1870
17. Mangelsdorf D.J., and Evans R.M. The RXR heterodimers and orphan receptors. Cell 83 (1995) 841-850
18. Mukherjee R., Davies P.J., Crombie D.L., Bischoff E.D., Cesario R.M., Jow L., et al. Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists. Nature 386 (1997) 407-410
19. Claudel T., Leibowitz M.D., Fievet C., Tailleux A., Wagner B., Repa J.J., et al. Reduction of atherosclerosis in apolipoprotein E knockout mice by activation of the retinoid X receptor. Proc Natl Acad Sci USA 98 (2001) 2610-2615
20. Repa J.J., Turley S.D., Lobaccaro J.A., Medina J., Li L., Lustig K., et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 (2000) 1524-1529
21. Kagechika H., and Shudo K. Synthetic retinoids: recent developments concerning structure and clinical utility. J Med Chem 48 (2005) 5875-5883
22. Ohta K., Kawachi E., Inoue N., Fukasawa H., Hashimoto Y., Itai A., et al. Retinoidal pyrimidinecarboxylic acids. Unexpected diaza-substituent effects in retinobenzoic acids. Chem Pharm Bull (Tokyo) 48 (2000) 1504-1513
23. Umemiya H., Fukasawa H., Ebisawa M., Eyrolles L., Kawachi E., Eisenmann G., et al. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem 40 (1997) 4222-4234
24. Suzuki S., Nishimaki-Mogami T., Tamehiro N., Inoue K., Arakawa R., Abe-Dohmae S., et al. Verapamil increases the apolipoprotein-mediated release of cellular cholesterol by induction of ABCA1 expression via Liver X receptor-independent mechanism. Arterioscler Thromb Vasc Biol 24 (2004) 519-525
25. Fu X., Menke J.G., Chen Y., Zhou G., MacNaul K.L., Wright S.D., et al. 27-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. J Biol Chem 276 (2001) 38378-38387
26. Tamehiro N., Shigemoto-Mogami Y., Kakeya T., Okuhira K., Suzuki K., Sato R., et al. Sterol regulatory element-binding protein-2- and liver X receptor-driven dual promoter regulation of hepatic ABC transporter A1 gene expression: mechanism underlying the unique response to cellular cholesterol status. J Biol Chem 282 (2007) 21090-21099
27. Nishimaki-Mogami T., Une M., Fujino T., Sato Y., Tamehiro N., Kawahara Y., et al. Identification of intermediates in the bile acid synthetic pathway as ligands for the farnesoid X receptor. J Lipid Res 45 (2004) 1538-1545
28. Abe-Dohmae S., Suzuki S., Wada Y., Aburatani H., Vance D.E., and Yokoyama S. Characterization of apolipoprotein-mediated HDL generation induced by cAMP in a murine macrophage cell line. Biochemistry 39 (2000) 11092-11099
29. Umemiya H., Kagechika H., Fukasawa H., Kawachi E., Ebisawa M., Hashimoto Y., et al. Action mechanism of retinoid-synergistic dibenzodiazepines. Biochem Biophys Res Commun 233 (1997) 121-125
30. Chawla A., Boisvert W.A., Lee C.H., Laffitte B.A., Barak Y., Joseph S.B., et al. A PPAR gamma-LXR-ABCA1 pathway in macrophages is involved in cholesterol efflux and atherogenesis. Mol Cell 7 (2001) 161-171
31. Costet P., Lalanne F., Gerbod-Giannone M.C., Molina J.R., Fu X., Lund E.G., et al. Retinoic acid receptor-mediated induction of ABCA1 in macrophages. Mol Cell Biol 23 (2003) 7756-7766
32. Altucci L., Leibowitz M.D., Ogilvie K.M., de Lera A.R., and Gronemeyer H. RAR and RXR modulation in cancer and metabolic disease. Nat Rev Drug Discov 6 (2007) 793-810
33. Schultz J.R., Tu H., Luk A., Repa J.J., Medina J.C., Li L., et al. Role of LXRs in control of lipogenesis. Genes Dev 14 (2000) 2831-2838
34. Michellys P.Y., Ardecky R.J., Chen J.H., Crombie D.L., Etgen G.J., Faul M.M., et al. Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes. J Med Chem 46 (2003) 2683-2696