Bibliograpy( related to HMG-CoA reductase inhibitors and cholesterol metabolism )

1. Original Articles

1. 1. Endo A, Kuroda M. Citrinin, an inhibitor of cholesterol synthesis. J Antibiot 1976; 29: 841-843.
2. 2. Kuroda M, Tanzawa K, Endo A. Inhibition of lipid metabolism by mycotoxins. Proc Jap Assoc Mycotoxicol(in Japanese) 1976; 2: 41-42.
3. 3. Endo A, Kuroda M, Tsujita Y. ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinum. J Antibiot 1976; 29: 1346-1348.
4. 4. Endo A, Kuroda M, Tanzawa K. Competitive inhibition of 3-hydroxy-3-methyl-　glutaryl coenzyme A reductase by ML-236A and ML-236B fungal　metabolites,　having hypocholesterolemic activity. FEBS Lett 1976; 72: 323-326.
5. 5. Kuroda M, Endo A. Inhibition of in vitro cholesterol synthesis by fatty acids. Biochim Biophys Acta 1977; 486: 254-259.
6. 6. Kuroda,M, Hazama-Shimada Y, Endo A. Inhibition of cholesterol synthesis by citrinin in a cell-free system from rat liver and yeast. Biochim Biophys Acta 1977; 486: 254-259.
7. 7. Endo A, Tsujita T, Kuroda M, Tanzawa K. Inhibition of cholesterol synthesis in vitro and in vivo by ML-236A and ML-236B, competitive inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Eur J Biochem 1977; 77: 31-36.
8. 8. Tanzawa K, Kuroda M, Endo A. Time-dependent, irreversible inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A reductase by the antibiotic citrinin. Biochim Biophys Acta 1977; 488: 97-101.
9. 9. Kuroda M, Tanzawa K, Tsujita Y, Endo A. Mechansim for elevation of hepatic cholesterol synthesis and serum cholesterol levels in Trition WR-1339-induced hyperlipidemia. Biochim Biophys Acta 1977; 489: 119-125.
10. 10. Kaneko I, Hazama-Shimada Y, Endo A. Inhibition of 3-hydroxy-3- methyl- glutaryl-coenzyme A reductase in cultured L cells by the hypocholesterolemic drug clofibrate. Biochem Biophys Res Commun 1977; 76: 1207-1213.
11. 11. Kaneko I, Hazama-Shimada Y, Endo A. Inhibitory effects on lipid metabolism in cultured cells of ML-236B, a potent inhibitor of 3-hydroxy-3-methylglutaryl- coenzyme-A reductase. Eur J Biochem 1978; 87: 313-321.
12. 12. Brown MS, Faust JR, Goldstein JL, Kaneko I, Endo A. Induction of 3-hydroxy-3-methylglutaryl coenzyme A reductase activity in human fibroblasts incubated with compactin (ML-236B), a competitive inhibitor of the reductase. J Biol Chem 1978; 253:1121-1128.
13. 13. Yamamoto A, Endo A, Kitano Y, Okada A, Ishikawa K, Kuroshima T, Kaneko I. Two Japanese kindreds of familial hypercholesterolemia including homozygous cases : a report of cases, and studies on serum-lipoproteins and enzymes. Japanese J Med 1978; 17: 230-239.
14. 14. Doi O, Endo A. Specific inhibition of desmosterol synthesis by ML-236B in mouse LM cells grown in suspension in a lipid-free medium. J Med Sci Biol 1978; 31: 225-233.
15. 15. Tanzawa K, Endo, A. Kinetic analysis of the reaction catalyzed by rat-liver 3-hydroxy-3methylglutaryl coenzyme-A reductase using two specific inhibitors. Eur J Biochem 1978; 98: 195-201.
16. 16. Tsujita Y, Kuroda M, Tanzawa K, Kitano N, Endo A. Hypolipidemic effects in dogs of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Atherosclerosis 1979; 32: 307-313.
17. 17. Kuroda M, Tsujita Y, Tanzawa K, Endo, A. Hypolipidemic effects in monkeys of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Lipids 1979; 14: 585-589.
18. 18. Endo A, Tsujita Y, Kuroda M, Tanzawa K. Effects of ML-236B on cholesterol metabolism in mice and rats: lack of hypocholesterolemic activity in normal animals. Biochim Biophys Acta 1979; 575: 266-276.
19. 19. Endo A. Monacolin K, a new hypocholesterolemic agent produced by a Monasus species. J Antibiot 1979; 32: 852-854.
20. 20. Yamamoto A, Sudo H, Endo A. Therapeutic effects of ML-236B in primary hypercholesterolemia. Atherosclerosis 1980; 35: 259-266.
21. 21. Endo A. Monacolin K, a new hypocholesterolmic agent that specifically inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase. J Antibiot 1980; 33: 334-336.
22. 22. Endo A. Hypocholesterolemic activity in several animal species of ML-236B, a potent inhibitors of cholesterol synthesis. J Japanese Atherosclerosis Soc (in Japanese) 1980; 7: 607-610.
23. 23. Ryan J, Hardeman EC, Endo A, Simoni RD. Isolation and characterization of cells resistant to ML-236B (compactin) with increased levels of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase. J Biol Chem 1981; 256: 6762-6769.
24. 24. Hashizume T, Matsubara S, Endo A. Compactin (ML-236B) as a new growth inhibitor of plant callus. Agric Biol Chem 1983; 47: 1401-1403.
25. 25. Hiruma K, Yagi S, Endo A. ML-236B (compactin) as an inhibitor of juvenile hormone biosynthesis. Appl Ent Zool 1983; 18: 111-115.
26. 26. Hardeman EC, Endo A, Simoni RD. Effects of compactin on the levels of 3-hydroxy-3-methylglutaryl coenzyme A reductaase in compaction-resistant C 100 and wild-type cells. Arch Biochem Biophys 1984; 232: 549-561.
27. 27. Hasumi K, Otsuki R, Endo A. Regulation of cholesterol synthesis in cultured mouse mammary carcinoma FM3A cells. J Biochem 1985; 98: 319-325.
28. 28. Endo A, Hasumi K, Nakamura T, Kunishima M, Masuda M. Dihydromonacolin L and monacolin X, new metabolites that inhibit cholesterol biosynthesis. J Antibiot 1985; 38: 321-327.
29. 29. Endo A, Yamashita H, Naoki H, Iwashita T, Mizukawa Y. Microbial phosphorylation of compactin (ML-236B) and related compounds. J Antibiot 1985; 38: 328-332.
30. 30. Endo A, Hasumi K, Negishi S. Monacolins J and L, new inhibitors of cholesterol biosynthesis produced by Monascus ruber. J Antibiot 1985; 38: 420-422.
31. 31. Endo A, Negishi Y, Iwashita T, Mizukawa K, Hirama M. Biosynthesis of ML-236B (compactin) and monacolin K. J Antibiot 1985; 38: 444-448.
32. 32. Yamashita H, Tsubokawa S, Endo A. Microbial hydroxylation of compactin (ML-236B) and monacolin K. J Antibiot 1985; 38: 605-609.
33. 33. Negishi S, Huang ZC, Hasumi K, Murakawa S, Endo A. Productivity of monacolin K (mevinolin) in the genus Monascus. Hakkokogaku (in Japanese) 1986; 64: 509- 512.
34. 34. Kikuchi K, Murakawa S, Endo A. Immobilization of the zygomycete Circinera muscae and phoshorylation of ML-236B (compactin) by the immobilized cells. Hakkokogaku (in Japanese) 1986; 64: 513-516.
35. 35. Komagata D, Yamashita H, Endo A. Microbial conversion of compactin (ML-236B) to ML-236A. J Antibiot 1986; 39: 1574-1577.
36. 36. Endo A, Hasumi K, Yamada A, Shimada R, Takeshima H. The synthesis of compactin (ML-236B) and monacolin K in fungi. J Antibiot 1986; 39: 1609-1610.
37. 37. Endo A, Komagata D, Shimada H. Monacolin M, a new inhibitor of cholesterol biosynthesis. J Antibiot 1986; 39: 1670-1673.
38. 38. Hasumi K, Arahira M, Sakai K, Endo A. Irreversible inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase by phenicin (phoenicine). J Antibiot 1987; 40: 224-226.
39. 39. Hasumi K, Yamada A, Shimizu Y, Endo A. Overaccumulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase in a compactin (ML-236B)-resistant mouse cell line with defects in the regulation of its activity. Eur J Biochem 1987; 164: 547-552.
40. 40. Murakawa S, Nakamura T, Komagata D, Sunagawa E, Endo A. Purification and properties of carboxyl-esterase from Emericella unguis that catalyzes the conversion of ML-236B (compactin) to ML-236A. Agric Biol Chem 1987; 51: 1879-1884.
41. 41. Ikeura R, Murakawa S, Endo A. Growth inhibition of yeast by compactin (ML-236B) analogues. J Antibiot 1988; 41: 1148-1150.
42. 42. Komagata D, Shimada H, Murakawa S, Endo A. Biosynthesis of monacolins: conversion of monacolin L to monacolin J by a monooxygenase of Monascus ruber. J Antibiot 1989; 42: 407-412.
43. 43. Koike S, Murakawa S, Endo A. Fermentation of mevalonate by Saccharomycopsis fibrigera IFO 0107. J Ferment Bioeng 1989; 68: 58-59.
44. 44. Nakamura T, Komagata D, Murakawa S, Sakai K, Endo A. Isolation and biosynthesis of 3α-hydroxy-3,5-dihydromonacolin L. J Antibiot 1990; 43: 1597-1600.
45. 45. Kimura K, Komagata D, Murakawa S, Endo A. Biosynthesis of monacolins: conversion of monacolin J to monacolin K (mevinolin). J Antibiot 1990; 43: 1621-1622.
46. 46. Sviridov DD, Endo A, Pavlov MY, Repin VS, Simirnov VN. Comparison of the effect of six compactin-related compounds on cholesterol synthesis in five human cell types. Lipids 1990; 25: 685-690.
47. 47. Hasumi K, Naganuma S, Sato Y, Endo A. Unstable amplification of the chromosomal gene for 3-hydroxy-3-methylglutaryl coenzyme A reductase in compactin-resistant CR200 cells. Biochim Biophys Acta 1991; 1083: 289-297.
48. 48. Ogawa H, Hasumi K, Sakai K, Murakawa S, Endo A. Pannorin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor produced by Chrysosporium pannorum. J Antibibiot 1991; 44: 762-767.
49. 49. Hasumi K, Shinohara C, Naganuma S, Endo A. Inhibition of the uptake of oxidized low density lipoprotein in macrophage J774 by the antibiotic ikarugamycin. Eur J Biochem 1992; 205: 841-846.
50. 50. Naganuma S, Kuzuya N, Sakai K, Hasumi K, Endo A. Inhibition of the accumulation of lipid droplets in macrophage J774 by bafilomycin B1 and destruxin E. Biochim Biophys Acta 1992; 1126: 41-48.
51. 51. Woo JT, Shinohara C, Sakai K, Hasumi K, Endo A. Inhibition of the acidificatio of endosomes and lysosomes by the antibiotic concanamycin B in macrophage J774. Eur J Biochem 1992; 207: 383-389.
52. 52. Woo JT, Shinohara C, Sakai K, Hasumi K, Endo A. Isolation, characterization and biological activities of concanamycins as inhibitors of lysosomal acidification. J Antibiot 1992; 45: 1108-1116.
53. 53. Naganuma S, Sakai K, Hasumi K, Endo A. Acaterin, a novel inhibitor of acyl-CoA: cholesterol acyltransferase produced by Pseudomonas sp. A92. J Antibiot 1992; 45: 1216-1221.
54. 54. Shinohara C, Hasumi K, Endo, A. Inhibition of oxidized low density lipoprotein metabolism in macrophage J774 by helvolic acid. Biochim Biophys Acta 1993: 1167: 303-306.
55. 55. Hasumi K, Naganuma S, Koshizawa J, Mogi H, Endo, A. Stimulation of acyl-CoA:cholesterol acyltransferase activity by brefeldin A in macrophage J774 cells. Biochim Biophys Acta 1993; 1167: 155-158.
56. 56. Hasumi K, Tachikawa K, Sakai K, Murakawa S, Yoshikawa N, Kumazawa S, Endo A. Competitive inhibition of squalene synthetase by squalestatin 1. J Antibiot 1993; 46: 689-691.
57. 57. Park JK, Sakai K, Ogawa H, Hasumi K, Endo A. Chrysosporin, a new inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase produced by Chrysosporium pannorum. J Antibiot 1993; 46: 1170-1172.
58. 58. Park JK, Hasumi K, Endo A. Inhibition of acyl-CoA : cholesterol acyltransferase by helminthosporol and its related compounds. J Antibiot 1993; 46: 1303-1305.
59. 59. Hasumi K, Shinohara C, Iwanaga T, Endo A. Lateritin, a new inhibitor of acyl-CoA : cholesterol acyltransferase produced by Gibberella lateritium IFO 7188. J Antibiot 1993; 46: 1782-1787.
60. 60. Sviridov DD, Endo A, Pavlov MY, Repin VS. Time response of cholesterol synthesis inhibition by compactin-related compounds. In vitro quantitation of the “escape phenomenon". Lipids 1993; 28: 569-571.
61. 61. Murakawa S, Sakai K, Endo A. Isolation of 3a-hydroxy-3.5-dihydro ML-236C (sodium salt) from Paecilomyces viridis L-68. J Antibiot 1994; 47: 108-109.
62. 62. Shinohara C, Hasumi K, Takei Y, Endo A. Gypsetin, a new inhibitor of acyl-CoA: cholesterol acyltransferase produced by Nannizzia gypsea var. incurvata IFO 9228. I. Fermentation, isolation, physicochemical properties and biological activity. J Antibiot 1994; 47: 163-167.
63. 63. Nuber B, Hansske F, Shinohara C, Miura S, Hasumi K, Endo A. Gypsetin, a new inhibitor of acyl-CoA: cholesterol acyltransferase produced by Nannizzia gypsea var. incurvata IFO 9228. II. Structure determination. J Antibiotics 1994; 47: 168-172.
64. 64. Matsuda M, Kageyama S, Endo A, Umezawa, K. Induction of normal phenotypes and potentiation of 5-fluorouracil by an HMG-CoA reductase inhibitor, compactin, in ras-transformed cells. Cellular Pharmacol 1994; 1: 219-223.
65. 65. Park JK, Hasumi K, Endo A. Inhibition of the binding of oxidized low density lipoprotein to the macrophages by iturin C-related compounds. J Antibiot 1995; 48: 226-232.
66. 66. Sakai K, Watanabe K, Masuda K, Tsuji M, Hasumi K, Endo A. Isolation, characterization and biological activities of novel triprenyl phenols as pancreatic cholesterol esterase inhibitors produced by Stachybotrys sp. F-1839. J Antibiot 1995; 48: 447-456.
67. 67. Takahashi F, Hasumi K, Endo A. Modulation of the plasma cholesteryl ester transfer by stachybotramide. Biochim Biophys Acta 1995; 1258: 70-74.
68. 68. Hasumi K, Takizawa K, Takahashi F, Park JK, Endo A. Inhibition of acyl-CoA : cholesterol acyltransferase by isohalobacillin, a complex of novel cyclic acylpeptides produced by Bacillus sp. A1238. J Antibiiot 1995; 48: 1419-1424.
69. 69. Kawabe Y, Honda M, Wada Y, Yazaki Y, Suzuki T, Ohba Y, Nabata H, Endo A, Matsumoto A, Itakura H, Kodama T. Sterol mediated regulation of SREBP-1a, 1b, 1c, and SREBP-2 in cultured human cells. Biochem Biophys Res Commun 1995; 202: 1460-1467.
70. 70. Kawabe Y, Shimokawa T, Matsumoto A, Honda M, Wada Y, Yazaki Y, Endo A, Itakura H, Kodama T. The molecular mechanism of the induction of the low density lipoprotein receptor by chenodeoxycholic acid in cultured human cells. Biochem Biophys Res Commun 1995; 208: 405-411.
71. 71. Kawabe Y, Sato R, Matsumoto A, Honda M, Wada Y, Yazaki Y, Endo A, Takano T, Itakura H, Kodama T. Regulation of fatty acid synthase expression by cholesterol in human cultured cells. Biochem Biophys Res Commun 1996; .219: 515-520.
72. 72. Sekiyama Y, Araya H, Hasumi K, Endo A, Fujimoto Y. Biosynthesis of acaterin: isolation of 4.5-didehydroacaterin and its conversion into acaterin. Natural Prod Lett 1997; 11: 61-66.
73. 73. Miura S, Hasumi K, Takayasu R, Sugimoto M, Endo A. Enhancement of low density lipoprotein binding to both low density lipoprotein receptor-positive and -negative cells by tetracycline antibiotics. Lipids 1998; 33: 33-38.
74. 74. Harada T, Hasumi K, Endo A. Induction of low density lipoprotein catabolism in Hep G2 cells by a fungal sesquiterpene ester, FR 111142. Biochem Biophys Res Commun 1998; 251: 830-834.

2. Reviews and Other Publications

1. 1. Endo A. Biological and pharmacological activity of inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Trends Biochem Sci 1981; 6: 10-13.
2. 2. Endo A. 3-Hydroxy-3-methylglutaryl CoA reductase inhibitors from Penicilliumand Monascus species. In:“Methods in Enzymology" Vol 72. Lowenstein JM(ed), Academic Press, New York, 1981. pp.684-689.
3. 3. Endo A. HMG-CoA reductase inhibitors. In: “Advances in Experimental Medicine and Biology" Vol 183. Kritchevsky D et al (eds), Plenum Press, New York, 1985. pp.295-310.
4. 4. Endo A. Specific non-sterol inhibitors of HMG-CoA reductase. In: "Regulation of HMG-CoA reductase". Preiss B (ed), Academic Press, New York, 1985. pp.49-78.
5. 5. Endo A. Compactin (ML-236B) and related compounds as potential cholesterol- lowering agents that inhibit HMG-CoA reductase. J Med Chem 1985; 28: 401-405.
6. 6. Endo A. Drug inhibiting HMG-CoA reductase. Pharm Ther 1987; 31: 257-267.
7. 7. Endo A. Chemistry, biochemistry and pharmacology of HMG-CoA reductase inhibitors. Klin Wochenschr 1988; 66: 421-427.
8. 8. Endo A. Biochemistry and pharmacology of HMG-CoA reductase inhibitors. In: “Atherosclerosis" VIII. Crepaldi G et al (eds), Excerpta Medica, New York, 1989. pp.775-780.
9. 9. Endo A, Hasumi K. Biochemical aspects of HMG-CoA reductase inhibitors. In: “Advances in Enzyme Regulation" Vol 28. Weber G(ed), Pergamon Press, New York, 1989. pp.53-64.
10. 10. Endo A. The discovery and development of HMG-CoA reductase inhibitors. J Lipid Res 1992; 33: 1569-1582.
11. 11. Endo A. HMG-CoA reductase inhibitors story. In: “Cellular Metabolism of the Arterial Wall and Central Nervous System". Schettler G et al (eds), Springer- Verlag, Berlin, 1993. pp.159-166.
12. 12. Endo A, Hasumi K. HMG-CoA reductase inhibitors. Natural Product Reports 1993; 10: 541-550.
13. 13. Endo A. Hypocholesterolemic agents. In: “ The Discovery of Natural Product with Therapeutic Potential". Gullo VP(ed), Butterworth-Heinemann, Boston, 1994. pp.301-320.
14. 14. Endo A, Hasumi K. Mevinic acids. In: “Fungal Biotechnology". Anke T (ed), Chapman & Hall, Weinhein, 1997. pp.162-172.
15. 15. Nakajima N, Endo A. Cholesterol-lowering effects of red koji. In: “Functional Foods for Disease Prevention II. Medicinal Plants and Other Foods". ACS Symposium Series. Shimamoto T et al (eds), American Chemical Society, 1998. pp.83-87.
16. 16. Endo A. Discovery and development of the statins. In:"Statins: The HMG-CoA Reductase Inhibitors in Perspective“. Gaw A et al (eds), Martin Dunitz, London, 1999. pp.35-47.
17. 17. Endo A. The origin of the statins,. In “Atherosclerosis XIII". International Congress Series (2003). Matsuzawa, Kita T et al (eds), Elsevier BV, The Netherlands, 2004. pp.3-8.
18. 18. Endo A. I finally tested a statin on myself! Atherosclerosis Suppl 2004; 5: 31.
19. 19. Endo A. A gift from nature: the birth of the statins. Nature Medicine 2008; 14: 1050-1052.
20. 20. Endo A. A historical perspective on the discovery of statins. Proc Jap Acad, Ser B 2010; 86: 488 493.

3. Selected Publications

1. 1. Endo A, Kuroda M, Tanzawa K. Competitive inhibition of 3-hydroxy- 3-methylglutaryl coenzyme A reductase by ML-236A and ML-236B fungal metabolites, having hypocholesterolemic activity. FEBS Lett 1976; 72: 323-326.
2. 2. Endo A, Kuroda M, Tsujita Y. ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinium. J Antibiot (Tokyo) 1976; 29: 1346-1348.
3. 3. Endo A, Tsujita Y, Kuroda M, Tanzawa K. Inhibition of cholesterol synthesis in vitro and in vivo by ML-236A and ML-236B, competitive inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Eur J Biochem 1977; 77: 31-36.
4. 4. Tsujita Y, Kuroda M, Tanzawa K, Kitano N, Endo A. Hypolipidemic effects in dogs of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Atherosclerosis 1979; 32: 307-313.
5. 5. Endo A, Tsujita Y, Kuroda M, Tanzawa K. Effects of ML-236B on cholesterol metabolism in mice and rats: lack of hypocholesterolemic activity in normal animals. Biochim Biophys Acta 1979; 575: 266-276.
6. 6. Endo A. Monacolin K, a new hypocholesterolmic agent that specifically inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase. J. Antibiot (Tokyo) 1979; 33: 334-336.
7. 7. Yamamoto A, Sudo H, Endo A. Therapeutic effects of ML-236B in primary hypercholesterolemia. Atherosclerosis 1980; 35: 259-266.
8. 8. Endo A. The discovery and development of HMG-CoA reductase inhibitors. J Lipid Res 1992; 33: 1569-1582.
9. 9. Endo A. A gift from nature: the birth of the statins. Nature Medicine 2008;14: 1050-1052.
10. 10. Endo A. A historical perspective on the discovery of statins. Proc Jap Acad, Ser B 2010; 86: 488 493.