Identification of a small-molecule, nonpeptide macrophage scavenger receptor antagonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 289, Issue 3, 1999, Pages 1277-1285

  Lysko, Paul G ^a,b   Weinstock, Joseph ^a   Webb, Christine L ^a   Brawner, Mary E ^a   Elshourbagy, Nabil A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b UW2510 ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

LOW DENSITY LIPOPROTEIN; METHYL 4 CHLORO ALPHA [4 (4 CHLOROPHENYL) 1,5 DIHYDRO 3 HYDROXY 5 OXO 1 (2 THIAZOLYL) 2H PYRROL 2 YLIDENE]BENZENEACETATE; MONENSIN; POLYINOSINIC ACID; SCAVENGER RECEPTOR; SCAVENGER RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ARTICLE; ATHEROSCLEROSIS; CHOLESTEROL TRANSPORT; DOSE RESPONSE; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; HUMAN; HUMAN CELL; MACROPHAGE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR BINDING;

ANIMALS; BINDING, COMPETITIVE; BIOLOGICAL TRANSPORT; CELL LINE; CELLS, CULTURED; CLONING, MOLECULAR; DEXTRAN SULFATE; HUMANS; KINETICS; LIGANDS; LIPOPROTEINS, LDL; MACROPHAGES; MACROPHAGES, PERITONEAL; MICE; MICE, KNOCKOUT; PHENYLACETATES; POLY I; RATS; RECEPTORS, IMMUNOLOGIC; RECEPTORS, SCAVENGER; RECOMBINANT PROTEINS; SCAVENGER RECEPTORS, CLASS A; THIAZOLES; TRANSFECTION;

EID: 0032990319     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (42)

1. Acton S, Resnick D, Freeman M, Ekkel Y, Ashkenas J and Krieger M (1993) The collagenous domains of macrophage scavenger receptors and complement C1q mediate similar, but not identical, binding specificities for polyanionic ligands. J Biol Chem 268:3530-3537.
2. Acton S, Scherer P, Lodish H and Krieger M (1994) Expression cloning of SR-BI, a CD36-related class B scavenger receptor. J Biol Chem 269:21003-21009.
3. Andersson L and Freeman M (1998) Functional changes in scavenger receptor binding conformation are induced by charge mutants spanning the entire collagen domain. J Biol Chem 273:19592-19601.
4. Ashkenas J, Penman M, Vasile E, Acton S, Freeman M and Krieger M (1993) Structures and high and low affinity ligand binding properties of murine type I and type II macrophage scavenger receptors. J Lipid Res 34:983-1000.
5. Basu SK, Brown MS, Ho YK and Goldstein JL (1979) Degradation of low density lipoprotein-dextran sulfate complexes associated with deposition of cholesteryl esters in mouse macrophages. J Biol Chem 254:7141-7146.
6. Brown MS, Basu SK, Falck JR, Ho YK and Goldstein JL (1980) The scavenger receptor pathway for lipoprotein degradation: specificity of the binding site that mediates the uptake of negatively-charged LDL by macrophages. J Supramol Struct 13:67-81.
7. Brown MS and Goldstein JL (1983) Lipoprotein metabolism in the macrophage: Implications for cholesterol deposition in atherosclerosis. Annu Rev Biochem 52: 223-261.
8. Chappell DA, Fry GL, Waknitz MA and Berns JJ (1991) Ligand size as a determinant for catabolism by the low density lipoprotein (LDL) receptor pathway. A lattice model for LDL binding. J Biol Chem 266:19296-19302.
9. Colotta F, Peri G, Villa A and Mantovani A (1984) Rapid killing of actinomycin D-treated tumor cells by human mononuclear cells. I. Effectors belong to the monocyte-macrophage lineage. J Immunol 132:936-944.
10. Doi T, Higashino K, Kurihara Y, Wada Y, Miyazaki T, Nakamura H, Uesugi S, Imanishi T, Kawabe Y, Itakura H, Yazaki Y, Matsumoto A and Kodama T (1993) Charged collagen structure mediates the recognition of negatively charged macromolecules by macrophage scavenger receptors. J Biol Chem 268:2126-2133.
11. Doi T, Kurasawa M, Higashino K, Imanishi T, Mori T, Naito M, Takahashi K, Kawabe Y, Wada Y, Matsumoto A and Kodama T (1994) The histidine interruption of an α-helical coiled coil allosterically mediates a pH-dependent ligand dissociation from macrophage scavenger receptors, J Biol Chem 269:25598-25604.
12. Elshourbagy NA, Korman DR, Wu H-L, Sylvester DR, Lee JA, Nuthalaganti P, Bergsma DJ, Kumar CS and Nambi P (1993) Molecular characterization and regulation of the human endothelin receptors. J Biol Chem 268:3873-3879.
13. Endemann G, Stanton LW, Madden KS, Bryant CM, White RT and Protter AA (1993) CD36 is a receptor for oxidized low density lipoprotein. J Biol Chem 268:11811-11816.
14. Freeman M, Ekkel Y, Rohrer L, Penman M, Freedman NJ, Chisolm GM and Krieger M (1991) Expression of type I and type II bovine scavenger receptors in Chinese hamster ovary cells: Lipid droplet accumulation and nonreciprocal cross competition by acetylated and oxidized low density lipoprotein. Proc Natl Acad Sci USA 88:4931-4935.
15. Freeman MW (1997) Scavenger receptors in atherosclerosis. Curr Opin Hematol 4:41-47.
16. Gerrity RG (1981) The role of the monocyte in atherogenesis. I. Transition of blood-borne monocytes into foam cell lesions in fatty lesions. Am J Pathol 103:181-190.
17. Goldstein JL, Basu SK and Brown MS (1983) Receptor-mediated endocytosis of low-density lipoprotein in cultured cells. Methods Enzymol 98:241-260.
18. Goldstein JL, Ho YK, Basu SK and Brown MS (1979) Binding site on macrophages that mediates uptake and degradation of acetylated low density lipoprotein, producing massive cholesterol deposition. Proc Natl Acad Sci USA 76:333-337.
19. Gough PJ, Greaves DR and Gordon S (1998) A naturally occurring isoform of the human macrophage scavenger receptor (SR-A) gene generated by alternative splicing blocks modified LDL uptake. J Lipid Res 39:531-543.
20. Krieger M (1992) Molecular flypaper and atherosclerosis: structure of the macrophage scavenger receptor. Trends Biochem Sci 17:141-146.
21. Krieger M and Herz J (1994) Structures and functions of multiligand lipoprotein receptors: Macrophage scavenger receptors and LDL receptor-related protein (LRP). Annu Rev Biochem 63:601-637.
22. Matsumoto A, Naito M, Itakura H, Ikemoto S, Asaoka H, Hayakawa I, Kanamori H, Aburatani H, Takaku F, Suzuki H, Kobari Y, Miyai T, Takahashi K, Cohen EH, Wydro R, Housman DE and Kodama T (1990) Human macrophage scavenger receptors: Primary structure, expression and localization in atherosclerotic lesions. Proc Natl Acad Sci USA 87:9133-9137.
23. Munson PJ and Rodbard D (1980) LIGAND: A versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220-239.
24. Pearson AM, Rich A and Krieger M (1993) Polynucleotide binding to macrophage scavenger receptors depends on the formation of base-quartet-stabilized four-stranded helices. J Biol Chem 268:3546-3554.
25. 83-disulfide-linked dimers. J Biol Chem 266:23985-23993.
26. Ramprasad MP, Fischer W, Witztum JL, Sambrano GR, Quehenberger O and Steinberg D (1995) The 94-to 97-kDa mouse macrophage membrane protein that recognizes oxidized low density lipoprotein and phosphatidylserine-rich liposomes is identical to macrosialin, the mouse homologue of human CD68. Proc Natl Acad Sci USA 92:9580-9584.
27. Resnick D, Chatterton JE, Schwartz K, Slayter H and Krieger K (1996) Structure of class A macrophage scavenger receptors. J Biol Chem 271:26924-26930.
28. Sakaguchi H, Takeya M, Suzuki H, Hakamata H, Kodama T, Horiuchi S, Gordon S, van der Laan LJW, Kraal G, Ishibashi S, Kitamura N and Takahashi K (1998) Role of macrophage scavenger receptors in diet-induced atherosclerosis in mice. Lab Invest 78:423-434.
29. Sawamura T, Kume N, Aoyama T, Moriwaki H, Hoshikawa H, Aiba Y, Tanaka T, Miwa S, Katsura Y, Kita T and Masaki T (1997) An endothelial receptor for oxidized low-density lipoprotein. Nature (London) 386:73-77.
30. Schwartz CJ, Valente AJ, Sprague EA, Kelley JL, Cayatte AJ and Mowery J (1992) Atherosclerosis. Potential targets for stabilization and regression. Circulation 86 (Suppl III):117-123.
31. Snyder ML, Hay RV, Whitington PF, Scanu AM and Fless GM (1994) Binding and degradation of lipoprotein (a) and LDL by primary cultures of human hepatocytes. Comparison with cultured human monocyte-macrophages and fibroblasts. Arterioscler Thromb 14:770-779.
32. Stanton LW, White RT, Bryant CM, Protter AA and Endemann G (1992) A macrophage Fc receptor for IgG is also a receptor for oxidized low density lipoprotein. J Biol Chem 267:2446-22451.
33. Stary HC (1987) Macrophages, macrophage foam cells and eccentric intimai thickening in the coronary arteries of young children. Atherosclerosis 64:91-108.
34. Stary HC, Chandler AB, Glagov S, Guyton JR, Insull W, Rosenfeld ME, Schaffer SA, Schwartz CJ, Wagner WD and Wissler RW (1994) A definition of initial, fatty streak, and intermediate lesions of atherosclerosis. A report from the Committee on Vascular Lesions of the Council on Arteriosclerosis, American Heart Association, Special report. Arterioscler Thromb 14:840-856.
35. Steinberg D, Parthasarathy S, Carew TE, Khoo JC and Witztum JL (1989) Beyond cholesterol. Modifications of low-density lipoprotein that increase its atherogenicity. N Engl J Med 320:915-924.
36. Suzuki H, Kurihara Y, Takeya M, Kamada N, Kataoka M, Jishage K, Ueda O, Sakaguchi H, Higashi T, Suzuki T, Takashima Y, Kawabe Y, Cynshi O, Wada Y, Honda M, Kurihara H, Aburatani H, Doi T, Matsumoto A, Azuma S, Noda T, Toyoda Y, Itakura H, Yazaki Y, Horiuchi S, Takahashi K, Kruijt JK, van Berkel TJC, Steinbrecher UP, Ishibashi S, Maeda N, Gordon S and Kodama T (1997) A role for macrophage scavenger receptors in atherosclerosis and susceptibility to infection. Nature (Lond) 386:292-296.
37. Suzuki K, Doi T, Imanishi T, Kodama T and Tanaka T (1997) The conformation of the α-helical coiled coil domain of macrophage scavenger receptor is pH dependent. Biochemistry 36:15140-15146.
38. Tanaka T, Nishikawa A, Tanaka Y, Nakamura H, Kodama T, Imanishi T and Doi T (1996) Synthetic collagen-like domain derived from the macrophage scavenger receptor binds acetylated low-density lipoprotein in vitro. Protein Eng 9:307-313.
39. van Berkel TJC, De Rijke YB and Kruijt JK (1991) Different fate in vivo of oxidatively modified low density lipoprotein and acetylated low density lipoprotein in rats. J Biol Chem 266:2282-2289.
40. 2+ and trifluoperazine on the processing of human acetylated low density lipoprotein by non-parenchymal liver cells. FEBS Lett 132:61-66.
41. van Berkel TJC, van Velzen A, Kruijt JK, Suzuki H and Kodama T (1998) Uptake and catabolism of modified LDL in scavenger-receptor class A type I/II knock-out mice. Biochem J 331:29-35.
42. Zhang H, Yang Y and Steinbrecher UP (1993) Structural requirements for the binding of modified proteins to the scavenger receptor of macrophages. J Biol Chem 268:5535-5542.