A vacuolar ATPase inhibitor, FR167356, prevents bone resorption in ovariectomized rats with high potency and specificity: Potential for clinical application

Journal of Bone and Mineral Research

Volumn 20, Issue 9, 2005, Pages 1579-1588

  Niikura, Kazuaki ^a,b   Takeshita, Nobuaki ^a   Takano, Mikiko ^a  

^a ASTELLAS PHARMA INC   (Japan)

^b NONE   (Japan)

Author keywords

Bone resorption; Lysosome; Osteoclast; Osteoporosis; Vacuolar ATPase

Indexed keywords

2,6 DICHLORO N [3 (1 HYDROXY 1 METHYLETHYL) 2 METHYL 7 BENZOFURANYL]BENZAMIDE; 5 (5,6 DICHLORO 2 INDOLYL) 2 METHOXY N (1,2,2,6,6 PENTAMETHYLPIPERIDIN 4 YL) 2,4 PENTADIENAMIDE; ADENOSINE TRIPHOSPHATASE INHIBITOR; BAFILOMYCIN A1; ENZYME INHIBITOR; FR 167356; PROTON TRANSPORTING ADENOSINE TRIPHOSPHATE SYNTHASE; RETINOIC ACID; SB 242784; UNCLASSIFIED DRUG;

ACID BASE BALANCE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD GAS ANALYSIS; BLOOD SAMPLING; BODY WEIGHT; CALCIUM TRANSPORT; CHEMICAL ANALYSIS; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; DRUG SPECIFICITY; ENZYME INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; HYPERCALCEMIA; LYSOSOME MEMBRANE; NONHUMAN; OSTEOCLAST; OSTEOLYSIS; OVARIECTOMY; RAT; WEIGHT GAIN;

ANIMALS; BENZAMIDES; BENZOFURANS; BIOLOGICAL TRANSPORT; BONE AND BONES; BONE DENSITY; BONE RESORPTION; CALCIUM; CELL MEMBRANE; DRUG EVALUATION, PRECLINICAL; ENZYME-LINKED IMMUNOSORBENT ASSAY; FEMALE; FEMUR; INHIBITORY CONCENTRATION 50; KIDNEY; LYSOSOMES; MACROLIDES; MALE; MICE; MODELS, CHEMICAL; OSTEOCLASTS; OSTEOPOROSIS; PROTONS; RABBITS; RATS; RATS, WISTAR; TIME FACTORS; VACUOLAR PROTON-TRANSLOCATING ATPASES;

EID: 24144489983     PISSN: 08840431     EISSN: None     Source Type: Journal    
DOI: 10.1359/JBMR.050517     Document Type: Article

References (39)

1. Aibe K, Yazawa H, Abe K, Teramura K, Kumegawa M, Kawashima H, Honda K 1996 Substrate specificity of recombinant osteoclast-specific cathepsin K from rabbits. Biol Pharm Bull 19:1026-1031.
2. Blair HC, Teitelbaum SL, Ghiselli R, Gluck S 1989 Osteoclastic bone resorption by a polarized vacuolar proton pump. Science 245:855-857.
3. Laitala T, Vaananen HK 1994 Inhibition of bone resorption in vitro by antisense RNA and DNA molecules targeted against carbonic anhydrase II or two subunits of vacuolar H(+)-ATPase. J Clin Invest 93:2311-2318.
4. Frattini A, Orchard PJ, Sobacchi C, Giliani S, Abinun M, Mattsson JP, Keeling DJ, Andersson AK, Wallbrandt P, Zecca L, Notarangelo LD, Vezzoni P, Villa A 2000 Defects in TCIRG1 subunit of the vacuolar proton pump are responsible for a subset of human autosomal recessive osteopetrosis. Nat Genet 25:343-346.
5. Forgac M 1989 Structure and function of vacuolar class of ATP-driven proton pumps. Physiol Rev 69:765-796.
6. Bowman EJ, Siebers A, Altendorf K 1988 Bafilomycins A class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells. Proc Natl Acad Sci USA 85:7972-7976.
7. +)-ATPases Nature's most versatile proton pumps. Nat Rev Mol Cell Biol 3:94-103.
8. Keeling DJ, Herslof M, Ryberg B, Sjogren S, Solvell L 1997 Vacuolar H(+)-ATPases. Targets for drug discovery? Ann N Y Acad Sci 834:600-608.
9. +-ATPase prevents bone loss in both thyroparathyroidectomized and ovariectomized rats. J Clin Invest 106:309-318.
10. Niikura K, Takano M, Sawada M 2004 A novel inhibitor of vacuolar ATPase, FR167356, which can discriminate between osteoclast vacuolar ATPase and lysosomal vacuolar ATPase. Br J Pharmacol 142:558-566.
11. Udagawa N, Takahashi N, Akatsu T, Sasaki T, Yamaguchi A, Kodama H, Martin TJ, Suda T 1989 The bone marrow-derived stromal cell lines MC3T3-G2/PA6 and ST2 support osteoclast-like cell differentiation in cocultures with mouse spleen cells. Endocrinology 125:1805-1813.
12. Koizumi K, Ito Y, Kojima K, Fujii T 1976 Isolation and characterization of the plasma membranes from rat ascites hepatomas and from normal rat livers, including newborn, regenerating, and adult livers. J Biochem 79:739-748.
13. Arai K, Shimaya A, Hiratani N, Ohkuma S 1993 Purification and characterization of lysosomal H(+)-ATPase. An anion-sensitive v-type H(+)-ATPase from rat liver lysosomes. J Biol Chem 268:5649-5660.
14. Biber J, Stieger B, Haase W, Murer H 1981 A high yield preparation for rat kidney brush border membranes Different behaviour of lysosomal markers. Biochim Biophys Acta 647:169-176.
15. Wlodawer P, Parsons DF, Williams GR, Wojtczak L 1966 Morphological changes in isolated rat-liver mitochondria during swelling and contraction. Biochim Biophys Acta 128:34-47.
16. +) ATPase and acid secretion in rabbit gastric glands. Folia Pharmacol Jpn 92:105-111.
17. 2+-ATPase acts as a proton pump. J Biochem 95:995-1007.
18. Villanueva AR, Lundin KD 1989 A versatile new mineralized bone stain for simultaneous assessment of tetracycline and osteoid seams. Stain Technol 64:129-138.
19. Teti A, Carano A, Santacroce G, Zambonin Zallone A 1987 Vitamin A directly stimulates bone resorption by isolated osteoclasts in vitro. Boll Soc Ital Biol Sper 63:1075-1080.
20. Trechsel U, Stutzer A, Fleisch H 1987 Hypercalcemia induced with an arotinoid in thyroparathyroidectomized rats. New model to study bone resorption in vivo. J Clin Invest 80:1679-1686.
21. Akiyama H, Nakamura N, Nagasaka S, Sakamaki H, Onozawa Y 1992 Hypercalcaemia due to all-trans retinoic acid. Lancet 339:308-309.
22. Baron R, Tross R, Vignery A 1984 Evidence of sequential remodeling in rat trabecular bone: Morphology, dynamic histomorphometry, and changes during skeletal maturation. Anat Rec 208:137-145.
23. Goldstein JL, Brown MS 1977 The low-density lipoprotein pathway and its relation to atherosclerosis. Annu Rev Biochem 46:897-930.
24. Woo JT, Shinohara C, Sakai K, Hasumi K, Endo A 1992 Inhibition of the acidification of endosomes and lysosomes by the antibiotic concanamycin B in macrophage J774. Eur J Biochem 207:383-389.
25. Gluck SL, Underbill DM, Iyori M, Holliday LS, Kostrominova TY, Lee BS 1996 Physiology and biochemistry of the kidney vacuolar H+-ATPase. Annu Rev Physiol 58:427-445.
26. Wang T, Giebisch G, Aronson PS 2002 Use of transgenic animals to study renal acid-base transport. J Nephrol 15:S151-S160.
27. Suda T, Takahashi N, Udagawa N, Jimi E, Gillespie MT, Martin TJ 1999 Modulation of osteoclast differentiation and function by the new members of the tumor necrosis factor receptor and ligand families. Endocr Rev 20:345-357.
28. Simonet WS, Lacey DL, Dunstan CR, Kelley M, Chang MS, Luthy R, Nguyen HQ, Wooden S, Bennett L, Boone T, Shimamoto G, DeRose M, Elliott R, Colombero A, Tan HL, Trail G, Sullivan J, Davy E, Bucay N, Renshaw-Gegg L, Hughes TM, Hill D, Pattison W, Campbell P, Sander S, Van G, Tarpley J, Derby P, Lee R, Boyle WJ for the Amgen EST Program 1997 Osteoprotegerin, a novel secreted protein involved in the regulation of bone density. Cell 89:309-319.
29. Campagnuolo G, Bolon B, Feige U 2002 Kinetics of bone protection by recombinant osteoprotegerin therapy in Lewis rats with adjuvant arthritis. Arthritis Rheum 46:1926-1936.
30. Oyajobi BO, Anderson DM, Traianedes K, Williams PJ, Yoneda T, Mundy GR 2001 Therapeutic efficacy of a soluble receptor activator of nuclear factor kappaB-IgG Fc fusion protein in suppressing bone resorption and hypercalcemia in a model of humoral hypercalcemia of malignancy. Cancer Res 61:2572-2578.
31. Zhang J, Dai J, Yao Z, Lu Y, Dougall W, Keller ET 2003 Soluble receptor activator of nuclear factor kappaB Fc diminishes prostate cancer progression in bone. Cancer Res 63:7883-7890.
32. McClung MR, Lewiecki EM, Bolognese MA, Woodson G, Moffett A, Peacock M, Miller PD, Lederman S, Chestnut CH, Murphy R, Holloway DL, Bekker PJ 2004 AMG 162 increases bone mineral density (BMD) within 1 month in postmenopausal women with low BMD. J Bone Miner Res 19:820.
33. Jimi E, Nakamura I, Duong LT, Ikebe T, Takahashi N, Rodan GA, Suda T 1999 Interleukin 1 induces multinucleation and bone-resorbing activity of osteoclasts in the absence of osteoblasts/stromal cells. Exp Cell Res 247:84-93.
34. Miedlich S, Krohn K, Paschke R 2003 Update on genetic and clinical aspects of primary hyperparathyroidism. Clin Endocrinol 59:539-554.
35. Moseley JM 1990 Parathyroid hormone-related protein of humoral hypercalcemia of malignancy. Adv Clin Chem 28:219-242.
36. Romas E, Martin TJ 1997 Cytokines in the pathogenesis of osteoporosis. Osteoporos Int 7:S47-S53.
37. Breedveld FC 1999 Future trends in the treatment of rheumatoid arthritis: Cytokine targets. Rheumatology 38:11-13.
38. Seymour GJ, Gemmell E 2001 Cytokines in periodontal disease: Where to from here? Acta Odontol Scand 59:167-173.
39. Suda T, Udagawa N, Nakamura I, Miyaura C, Takahashi N 1995 Modulation of osteoclast differentiation by local factors. Bone 17:87S-91S.