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Endo, A., Kuroda, M. & Tsujita, Y. ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinum. J. Antibiot. (Tokyo) 29, 1346–1348 (1976).
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. 72, 323–326 (1976).
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 575, 266–276 (1979).
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 32, 307–313 (1979).
Endo, A. The discovery and development of HMG-CoA reductase inhibitors. J. Lipid Res. 33, 1569–1582 (1992).
Steinberg, D. An interpretative history of the cholesterol controversy. V. The discovery of the statins and the end of the controversy. J. Lipid Res. 47, 1339–1351 (2006).
Yamamoto, A., Sudo, H. & Endo, A. Therapeutic effects of ML-236B in primary hypercholesterolemia. Atherosclerosis 35, 259–266 (1980).
Alberts, A.W. et al. Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proc. Natl. Acad. Sci. USA 77, 3957–3961 (1980).
Mabuchi, H. et al. Effects of an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase on serum lipoproteins and ubiquinone-10-levels in patients with familial hypercholesterolemia. N. Engl. J. Med. 305, 478–482 (1981).
There are too many friends and colleagues who have contributed to this work over the years to name them individually, but special thanks must go to M. Kuroda for his key role in searching for HMG-CoA reductase inhibitors, to N. Kitano for collaborating in evaluating compactin in hens, dogs and monkeys, and to A. Yamamoto, who first gave compactin to a patient with severe hypercholesterolemia. I am greatly indebted to J. Goldstein and M. Brown, whose friendship and expertise have proved so valuable during my career. And finally, I would like to express my deep gratitude to the Lasker Foundation for the honor of being distinguished with such a prestigious award, which I share with all the members of my laboratories at both Sankyo and Tokyo Noko University.
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Endo, A. A gift from nature: the birth of the statins. Nat Med 14, 1050–1052 (2008). https://doi.org/10.1038/nm1008-1050
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