Yasuo Kagawa (Kagawa Nutrition University)
in Japanese
1) Y@~gRhÃGlM[ӂƌNA̗͉ȊwA55: 175-180. 2006
2) Y@lqDL@ҁFQmr^~w@ 2008
3) Y@Kah@gV@@2000
4) Y@l{qYFl̂̕qw@ۑP@1997
5) Y@̖@gS0@1978
Barry Forman (The Beckman Research Institute at The City of Hope National Medical Center)
1) Wang YD, Yang F, Chen WD, Huang X, Lai L, Forman BM, Huang W., "Farnesoid X Receptor (FXR) Protects Liver Cells from Apoptosis Induced by Serum Deprivation in Vitro and Fasting in Vivo.", Mol Endocrinol., 2008
2) Patel NV, Forman BM., "Linking lipids, Alzheimer's and LXRs?", Nucl Recept Signal., 2, e001(2004).
3) Yuan X, Forman BM., "Detection of designer steroids." Nucl Recept Signal., 3, e002(2005)..
4) Yu DD, Forman BM., "Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma.", Bioorg Med Chem Lett., 15(5), 1311-3(2005).
5) Yu DD, Forman BM., "Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator.", J Org Chem., 68(24), 9489-91(2003)
Donald P. McDonnell (Duke University Medical Center)
1) Sathya, G., Chang, C.-Y., Kazmin, D., Cook, C.E. and McDonnell, D.P. (2003) Pharmacological uncoupling of androgen receptor-mediated prostate cancer cell proliferation and PSA secretion. Cancer Research 63: 8029-8036.
2) Chang, C.-Y., Abdo, J. Hartney, T. and McDonnell, D.P. (2005) Development of peptide antagonists for the androgen receptor using combinatorial peptide phage display. Mol. Endocrinol. 19: 2478-2490.
3) Chute, J.P., Muramoto, G.G., Whitesides, J., Colvin, M., Safi, R., Chao, N.J. and McDonnell, D.P. (2006) Inhibition of aldehyde dehydrogenase and retinoid signaling induces the expansion of human hematopoietic stem cells. Proc. Natl. Acad. Sci. USA 103: 11707-11712.
4) Kazmin, D., Prytkova, T., Cook, C.E., Wolfinger, R., Chu, T.-M., Beratan, D., Norris, J.D., Chang, C.-Y. and McDonnell, D.P. (2006) Linking ligand-induced alterations in androgen receptor structure to differential gene expression: A first step in the rational design of selective androgen receptor modulators. Mol. Endocrinol. 20: 1201-1217.
5) Gaillard, S., Grasfeder, L.L., Haeffele, C.L., Lobenhofer, E.K., Chu, T.-M., Wolfinger, R., Kazmin, D., Koves, T.R., Muoio, D.M., Chang, C.-Y. and McDonnell, D.P. (2006) Receptor-selective coactivators as tools to define the biology of specific receptor-coactivator pairs. Mol. Cell. 24: 797-803.
6) Hall, J.M. and McDonnell, D.P. (2007) The molecular mechanisms underlying the proinflammatory actions of thiazolidinediones in human macrophages. Mol. Endocrinol. 21: 1756-1768.
7) Wittmann, B.M., Sherk, A. and McDonnell, D.P. (2007) Definition of functionally important mechanistic differences among Selective Estrogen Receptor Downregulators (SERDs). Cancer Res. 67: 9549-9560.
8) Mettu, N.B., Stanley, T.B., Dwyer, M.A., Jansen, M.S., Allen, J.E., Hall, J.M. and McDonnell, D.P. (2007) The nuclear receptor-coactivator interaction surface as a target for peptide antagonists of the peroxisome proliferators activated receptors. Mol. Endocrinol. 21: 2361-2377.
9) DuSell, C.D., Umetani, M., Shaul, P.W., Mangelsdorf, D.J. and McDonnell, D.P. (2008) 27-hydroxycholesterol is an endogenous Selective Estrogen Receptor Modulator (SERM). Mol. Endocrinol. 22: 65-77.
10) Frigo, D.E. and McDonnell, D.P. (2008) Differential effects of prostate cancer therapeutics on neuroendocrine transdifferentiation. Mol. Cancer Ther. 7: 659-669.
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Heonjoong Kang (Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University)
Nuclear Receptor Biology
1) Grant D. Barish, Annette R. Atkins, Michael Downes, Peter Olson, Ling-Wa Chong, Mike Nelson, Yuhua Zou, Hoosang Hwang, Heonjoong Kang, Linda Curtiss, Ronald M. Evans, and Chih-Hao Lee. PPAR regulates multiple pro-inflammatory pathways to suppress atherosclerosis. Proceedings of National Academy of Science of USA, 2008, 105, 4271-4276.
2) Chih-Hao Lee, Peter Olson, Andrea Hevener, Ling-Wa Chong, Jerrold M. Olefsky, Frank J. Gonzalez, Jungyeob Ham, Heonjoong Kang, Jeffrey M. Peters and Ronald M. Evans. PPAR delta improves insulin sensitivity through a hepatomuscular fatty acid cycle. Proceedings of National Academy of Science of USA, 2006, 103, 3444-3449.
3) Yong-Xu Wang, Chun-Li Zhang, Ruth T. Yu, Helen K. Cho, Micheal C. Nelson, Corinne R. Bayuge-Ocampo, Jungyeob Ham, Heonjoong Kang, Ronald M. Evans. Regulation of Muscle Fiber Type and Running Endurance by PPAR. Public Library of Science Biology, 2004, 2, 1532-1539.
4) Yong-Xu Wang, Chih-Hao Lee, Sambath Tiep, Ruth T. Yu, Jungyeob Ham, Heonjoong Kang and Ronald M. Evans, Peroxisome-proliferator-activated receptor activates fat metabolism to prevent obesity. Cell, 2003, 113, 159-170.
Organic Synthesis
1) Young Hee Park, Hong Ryul Ahn, Belgin Canturk, Sang Il Jeon, Seokjoon Lee, Heonjoong Kang, Gary A. Molander and Jungyeob Ham. A Facile One-Pot Preparation of Potassium Hydroxyaryl- and (Hydroxyalkyl)aryltrifluoroborates. Organic Letters, 2008, 10, 1215-1218.
2) Jaeyoung Ko, Jungyeob Ham, Inho Yang, Jungwook Chin, Sang-Jip Nam and Heonjoong Kang. A Simple One-Pot Synthesis of Hydroxylated and Carboxylated Aryl Alkyl Sulfides from Various Bromobenzenes. Tetrahedron Letters, 2006, 47, 7101-7106.
3) 3. Jungyeob Ham, Sungjin-Cho, Jaeyoung Ko, Inho Yang and Heonjoong Kang. A Facile One-pot Preparation of Alkyl Aminoaryl Sulfides for the Synthesis of GW7647 as an Agonist of Peroxisome Proliferator-activated Receptor . Journal of Organic Chemistry, 2006, 71, 5781-5794.
4) Jungyeob Ham, Inho Yang, and Heonjoong Kang, A Facile One-Pot Synthesis of Alkyl Aryl Sulfides from Aryl Bromides. Journal of Organic Chemistry, 2004, 69, 3236-3239.
Marine Natural Product Chemistry
1) Hyukjae Choi, Sun Kwan Oh, Wonho Yih, Jungwook Chin, Heonjoong Kang and Jung-Rae Rho. Cyanopeptoline CB071: A cyclic depsipeptide isolated from the freshwater cyanobacterium Aphanocapsa sp. Chem. Pharm. Bull. 2008, in press.
2) Weihong Wang, Sang-Jip Nam, Byoung-Chan Lee, and Heonjoong Kang. - Carboline Alkaloids from a Korean Tunicate Eudistoma sp. Journal of Natural Products, 2008, 71, 163-166.
3) Sang-Jip Nam, Hyunsil Ko, Moon Kyeong Ju, Hoosang Hwang, Jungwook Chin, Jungyeob Ham, Byoungchan Lee, Jaehwan Lee, Dong Hwan Won, Hyukjae Choi, Jaeyoung Ko, Kyoungjin Shin, Taekyung Oh, Seokho Kim, Jung-Rae Rho, and Heonjoong Kang. Scalarane Sesterterpenes from a Marine Sponge of the Genus Spongia and Their FXR Antagonistic Activity. Journal of Natural Products, 2007, 70, 1691-1695.
4) Sang-Jip Nam, Hyunsil Ko, Mihee Shin, Jungyeob Ham, Jungwook Chin, Youngshin Kim, Heeyoung Kim, Kyoungjin Shin, Hyukjae Choi, and Heonjoong Kang. Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp., Bioorganic & Medicinal Chemistry Letters, 2006, 16, 5398-5402.
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Makoto Makishima (Nihon University)
1) Endo K, Uno S, Seki T, Ariga T, Kusumi Y, Mitsumata M, Yamada S, Makishima M. Inhibition of aryl hydrocarbon receptor transactivation and DNA adduct formation by CYP1 isoform-selective metabolic deactivation of benzo[a]pyrene. Toxicol Appl Pharmacol 230: 135-143, 2008
2) Ishizawa M, Matsunawa M, Adachi R, Uno S, Ikeda K, Masuno H, Shimizu M, Iwasaki K, Yamada S, Makishima M. Lithocholic acid derivatives act as selective vitamin D receptor modulators without inducing hypercalcemia. J Lipid Res 49: 763-772, 2008
3) Inaba Y, Yamamoto K, Yoshimoto N, Matsunawa M, Uno S, Yamada S, Makishima M. Vitamin D3 derivatives with adamantane or lactone ring side chains are cell type-selective vitamin D receptor modulators. Mol Pharmacol 71: 1298-1311, 2007
4) Koike T, Uno S, Ishizawa M, Takahashi H, Ikeda K, Yokota S, Makishima M. The heat shock protein inhibitor KNK437 induces neurite outgrowth in PC12 cells. Neurosci Lett 410: 212-217, 2006
5) Uno S, Makishima M. Regulation of xenobiotic metabolism by xenobiotic receptors and cytochrome P450 enzymes. Nihon Univ J Med 47: 69-79, 2005
6) Morita K, Kawana K, Sodeyama M, Shimomura I, Kagechika H, Makishima M. Selective allosteric ligand activation of the retinoid X receptor heterodimers of NGFI-B and Nurr1. Biochem Pharmacol 71: 98-107, 2005
7) Nakano H, Matsunawa M, Yasui A, Adachi R, Kawana K, Shimomura I, Makishima M. Enhancement of ligand-dependent vitamin D receptor transactivation by the cardiotonic steroid bufalin. Biochem Pharmacol 70: 1479-1486, 2005
8) Makishima M, Yamada S. Targeting the vitamin D receptor: advances in drug discovery. Expert Opin Ther Pat 15: 1133-1145, 2005
9) Makishima M. Regulation of cholesterol and bile acid metabolism by nuclear receptors. J Pharmacol Sci 97: 177-183, 2005
10) Adachi R, Honma Y, Masuno H, Kawana K, Shimomura I, Yamada S, Makishima M. Selective activation of vitamin D receptor by lithocholic acid acetate, a bile acid derivative. J Lipid Res 46: 46-57, 2005
11) Adachi R, Shulman AI, Yamamoto K, Shimomura I, Yamada S, Mangelsdorf DJ, Makishima M. Structural determinants for vitamin D receptor response to endocrine and xenobiotic signals. Mol Endocrinol 18: 43-52, 2004
12) Kaneko E, Matsuda M, Yamada Y, Tachibana Y, Shimomura I, Makishima M. Induction of intestinal ATP-binding cassette transporters by a phytosterol-derived liver X receptor agonist. J Biol Chem 278: 36091-36098, 2003
13) Makishima M, Lu TT, Xie W, Whitfield GK, Domoto H, Evans RM, Haussler MR, Mangelsdorf DJ. Vitamin D receptor as an intestinal bile acid sensor. Science 296: 1313-1316, 2002
14) Lu TT, Makishima M, Repa JJ, Schoonjans K, Kerr TA, Auwerx J, Mangelsdorf DJ. Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol Cell 6: 507-515, 2000
15) Makishima M, Okamoto AY, Repa JJ, Tu H, Learned RM, Luk A, Hull MV, Lustig KD, Mangelsdorf DJ, Shan B. Identification of a nuclear receptor for bile acids. Science 284: 1362-1365, 1999
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Sean Ekins (Collaborations in Chemistry and University of Maryland)
1) Ekins S, Kholodovych V, Ai N, Sinz M, Gal J, Gera L, Welsh WJ, Bachmann K and Mani S, Computational discovery of novel low micromolar human pregnane X receptor antagonists, Mol Pharmacol, In Press 2008.
2) Krasowski MD, Reschly EJ and Ekins S, Intrinsic disorder in nuclear hormone receptors, J Proteome Res, In Press 2008.
3) Yasuda K, Ranade A, Venkataramanan R, Strom S, Chupka J, Ekins S, Schuetz E and Bachmann K, A comprehensive in vitro and in silico analysis of antibiotics that activate and induce CYP3A4 in liver and intestine, Drug Metab Dispos, 36:1689-97, 2008.
4) Khandelwal A, Krasowski MD, Reschly EJ, Sinz M, Peter W Swaan and Ekins S, Machine learning methods and docking for human Pregnane X Receptor activation, Chem Res Toxicol, 21:1457-67, 2008.
5) Reschly EJ, Ai N, Ekins S, Welsh WJ, Hagey LR, Hoffman AF, Krasowski MD, Evolution of the bile salt nuclear receptor FXR in vertebrates, J Lipid Res, 49:1577-1587, 2008.
6) Ekins S, Reschly EJ, Hagey LR and Krasowski MD, Evolution of pharmacologic specificity in the Pregane X Receptor, BMC Evolutionary Biology, 8:103, 2008.
7) Reschly EJ, Ai N, Welsh WJ, Ekins S, Hagey LR, Krasowski MD, Ligand specificity and evolution of liver X receptors, J Steroid Biochem Mol Biol, 110:83-94, 2008.
8) Ekins S, Chang C, Mani S, Krasowski MD, Reschly EJ, Iyer M, Kholodovych V, Ai N, Welsh WJ, Sinz M, Swaan PW, Patel R and Bachmann K, Human pregnane X receptor antagonists and agonists define molecular requirements for different binding sites, Mol Pharm, 72: 592-603, 2007.
9) Ekins S, Andreyev S, Ryabov A, Kirillov E, Rakhmatulin E, Sorokina S, Bugrim A and Nikolskaya T. A combined approach to drug metabolism and toxicity assessment. Drug Metab Dispos, 34:495-503, 2006.
10) Ekins S, Computational Toxicology: Risk Assessment For Pharmaceutical and Environmental Chemicals, Series Editor Ekins S. John Wiley and Sons, June 2007. ISBN 978-0-470-04962-4.
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Bruce Blumberg (University of California, Irvine)
1) Grun F, Blumberg, "Perturbed nuclear receptor signaling by environmental obesogens as emerging factors in the obesity crisis.", B.Rev Endocr Metab Disord., 8(2), 161-71(2007).
2) Kumagai J, Fujimura T, Takahashi S, Urano T, Ogushi T, Horie-Inoue K, Ouchi Y, Kitamura T, Muramatsu M, Blumberg B, Inoue S, "Cytochrome P450 2B6 is a growth-inhibitory and prognostic factor for prostate cancer.", Prostate, 67(10), 1029-37(2007)
3) Zhou C, Tabb MM, Nelson EL, Grun F, Verma S, Sadatrafiei A, Lin M, Mallick S, Forman BM, Thummel KE, Blumberg B, "Mutual repression between steroid and xenobiotic receptor and NF-kappaB signaling pathways links xenobiotic metabolism and inflammation.", J Clin Invest., 116(8), 2280-2289(2006)
4) Grun F, Blumberg B, "Environmental obesogens: organotins and endocrine disruption via nuclear receptor signaling.", Endocrinology, 147(6 Suppl), S50-5(2006).
5) Ichikawa T, Horie-Inoue K, Ikeda K, Blumberg B, Inoue S, "Steroid and xenobiotic receptor SXR mediates vitamin K2-activated transcription of extracellular matrix-related genes and collagen accumulation in osteoblastic cells.", Biol Chem.,281(25), 16927-34(2006).
Masahiko Negishi(The National Institute of Environmental Health Sciences)
1) Konno Y, Negishi M, Kodama S., gThe roles of nuclear receptors CAR and PXR in hepatic energy metabolism.h, Drug Metab Pharmacokinet,. 23(1), 8-13 (2008).
2) Inoue K, Negishi M., gNuclear receptor CAR requires early growth response 1 to activate the human cytochrome P450 2B6 gene.h, J Biol Chem., 283(16), 10425-32(2008).
3) Sueyoshi T, Moore R, Sugatani J, Matsumura Y, Negishi M., hPPP1R16A, the membrane subunit of protein phosphatase 1beta, signals nuclear translocation of the nuclear receptor constitutive active/androstane receptor.h, Mol Pharmacol., 73(4), 1113-21(2008).
4) Nakamura K., Moore R, Negishi M, Sueyoshi T., gThe nuclear pregnane X receptor cross-talk with FOXA2 to mediate drug-induced regulation of lipid metabolism.h J. Biol. Chem. 284, 9768-9776 (2007).
5) Koike C, Moore R, Negishi M., gMEK-ERK is an endogenous signal retaining the nuclear receptor CAR in the cytoplasm of mouse primary hepatocytes.h Mol. Pharmacol. 71, 1217-1221 (2007).
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Masayuki Yamamoto (Tohoku University)
1) gStructural insights into the similar modes of Nrf2 transcription factor recognition by the cytoplasmic repressor Keap1. g[J Synchrotron Radiat,15(Pt 3),(2008),273-276] Padmanabhan Balasundaram, Tong Kit I, Kobayashi Akira, Yamamoto Masayuki, Yokoyama Shigeyuki
2) gDefining the functional boundaries of the gata2 locus by rescue with a linked bacterial artificial chromosome transgene. g[J Biol Chem,283(14),(2008),8976-8983] Brandt William, Khandekar Melin, Suzuki Norio, Yamamoto Masayuki, Lim Kim-Chew, Engel James Douglas
3) gAntioxidants and phase 2 enzymes in macrophages: regulation by nrf2 signaling and protection against oxidative and electrophilic stress. g[Exp Biol Med (Maywood),233(4),(2008),463-474] Zhu Hong, Jia Zhenquan, Zhang Li, Yamamoto Masayuki, Misra Hara P, Trush Michael A, Li Yunbo
4) gAblation of Gata1 in adult mice results in aplastic crisis, revealing its essential role in steady-state and stress erythropoiesis. g[Blood,111(8),(2008),4375-4385] Gutierrez Laura, Tsukamoto Saho, Suzuki Mikiko, Yamamoto-Mukai Harumi, Yamamoto Masayuki, Philipsen Sjaak, Ohneda Kinuko
5) gRunx1 is involved in primitive erythropoiesis in the mouse. g[Blood,111(8),(2008),4075-4080] Yokomizo Tomomasa, Hasegawa Kazuteru, Ishitobi Hiroyuki, Osato Motomi, Ema Masatsugu, Ito Yoshiaki, Yamamoto Masayuki, Takahashi Satoru
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Takashi Kadowaki (The University of Tokyo)
1) Kubota N, Kubota T, Itoh S, Kumagai H, Kozono H, Takamoto I, Mineyama H, Ogata H, Tokuyama K, Ohsugi M, Sasako T, Moroi M, Sugi K, Kakuta S, Iwakura Y, Noda T, Ohnishi S, Nagai R, Tobe K, Terauchi Y, Ueki K, Kadowaki T: Dynamic functional relay between insulin receptor substrate-1 and -2 in hepatic insulin signaling during fasting and feeding. Cell Metabolism 8: 49-64, 2008
2) Oishi Y, Manabe I, Tobe K, Ohsugi, M, Kubota, T, Fujiu K, Maemura K, Kubota N, Kadowaki T, Nagai R: SUMOylation of Kruppel-like transcription factor 5 acts as a molecular switch in transcriptional programs of lipid metabolism involving PPAR-d., Nature Medicine, 14: 656-665, 2008
3) Kubota N, Yano W, Kubota T, Yamauchi T, Itoh S, Kumagai H, Kozono H, Takamoto I, Okamoto S, Shiuchi T, Suzuki R, Satoh H, Tsuchida A, Moroi M, Sugi K, Noda T, Ebinuma H, Ueda Y, Kondo T, Araki E, Ezaki O, Nagai R, Tobe K, Terauchi Y, Ueki K, Minokoshi Y, Kadowaki T: Adiponectin stimulates AMP-activated protein kinase in the hypothalamus and increases food intake., Cell Metabolism 6: 55-68, 2007
4) Yamauchi T, Nio Y, Maki T, Kobayashi M, Takazawa T, Iwabu M, Okada-Iwabu M, Kawamoto S, Kubota N, Kubota T, Ito Y, Kamon J, Tsuchida A, Kumagai K, Kozono H, Hada Y, Ogata H, Tokuyama K, Tsunoda M, Ide T, Murakami K, Awazawa M, Takamoto I, Froguel P, Hara K, Tobe K, Nagai R, Ueki K, Kadowaki T: Targeted disruption of AdipoR1 and AdipoR2 causes abrogation of adiponectin binding and metabolic actions., Nature Medicine 13: 332-339, 2007
5) Kadowaki T, Yamauchi T, Kubota N, Hara K, Ueki K, Tobe K: Adiponectin and adiponectin receptors in insulin resistance, diabetes and metabolic syndrome-Adiponectin hypothesis-., J.Clin.Invest. 116: 1784-1792, 2006
6) Oishi Y, Manabe I, Tobe K, Tsushima K, Shindo T, Fujiu K, Nishimura, Maemura K, Yamauchi T, Kubota N, Suzuki R, Kitamura T, Akira S, Kadowaki T, Nagai R: Kruppel-like transcription factor KLF5 is a key regulator of adipocyte differentiation., Cell Metabolism 1: 27-39, 2005
7) Yamauchi T, Kamon J, Ito Y, Tsuchida A, Yokomizo T, Kita S, Sugiyama T, Miyagishi M, Hara K, Tsunoda M, Murakami K, Ohteki T, Uchida S, Waki H, Tsuno NH, Shibata Y, Terauchi Y, Froguel P, Tobe K, Koyasu S, Taira K, Kitamura T, Shimizu T, Nagai R, Kadowaki T: Molecular cloning of adiponectin / Acrp30 receptors that mediate antidiabetic metabolic effects., Nature 423: 762-769, 2003
8) Yamauchi T, Kamon J, Minokoshi Y, Ito Y, Waki H, Uchida S, Yamashita S, Noda M, Kita S, Ueki K, Eto K, Akanuma Y, Froguel P, Foufelle F, Ferre P, Carling D, Kimura S, Nagai R, Kahn BB, Kadowaki T: Adiponectin stimulates glucose utilization and fatty-acid oxidation by activating AMP-activated protein kinase., Nature Medicine 8: 1288-1295, 2002
9) Yamauchi T, Kamon J, Waki H, Terauchi Y, Kubota N, Hara K, Mori Y, Ide T, Murakami K, Tsuboyama-Kasaoka N, Ezaki O, Akanuma Y, Gavrilova O, Vinson C, Reitman ML, Kagechika H, Shudo K, Yoda M, Nakano Y, Tobe K, Nagai R, Kimura S, Tomita M, Froguel P, Kadowaki T: The fat-derived hormone adiponectin reverses insulin resistance associated with both lipoatrophy and obesity., Nature Medicine 7:941-946, 2001
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Yoshihide Hayashizaki (RIKEN Omics Science Center)
1) Hayashizaki Y., et al, Functional annotation of a full-length mouse cDNA collection, Nature 409: 685-690 (2001)
2) Hayashizaki Y., et al, Analysis of the mouse transcriptome based on functional annotation of 60,770 full-length cDNA,Nature 420: 563-573 (2002)
3) Hayashizaki Y., et al, The Transcriptional Landscape of the Mammalian Genome, Science, 309, 1559-1563 (2005)
4) Hayashizaki Y., et al, Antisense transcription in the mammalian transcriptome, Science, 309, 1564-1566 (2005)
5) Hayashizaki Y., et al, Rapid SNP diagnostics using asymmetric isothermal amplification and a new mismatch-suppression technology, Nat Methods 4, 257-262(2007).
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Toshimori Kitami (Broad Institute of MIT & Harvard)
1) Wagner BK, Kitami T, Gilbert TJ, Peck D, Ramanathan A, Schreiber SL, Golub TR, Mootha VK. Large-scale chemical dissection of mitochondrial function. Nat Biotechnol. 2008 Mar;26(3):343-51.
2) Mootha VK, Handschin C, Arlow D, Xie X, St Pierre J, Sihag S, Yang W, Altshuler D, Puigserver P, Patterson N, Willy PJ, Schulman IG, Heyman RA, Lander ES, Spiegelman BM., Erralpha and Gabpa/b specify PGC-1alpha-dependent oxidative phosphorylation gene expression that is altered in diabetic muscle. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6570-5.
3) Kitami T, Nadeau JH., Biochemical networking contributes more to genetic buffering in human and mouse metabolic pathways than does gene duplication., Nat Genet. 2002 Sep;32(1):191-4.
4) Kitami T, Ernest S, Gallaugher L, Friedman L, Frankel WN, Nadeau JH. Genetic and phenotypic analysis of seizure susceptibility in PL/J mice. Mamm Genome. 2004 Sep;15(9):698-703.
5) Dushay MS, Roethele JB, Chaverri JM, Dulek DE, Syed SK, Kitami T, Eldon ED. Two attacin antibacterial genes of Drosophila melanogaster. Gene. 2000 Apr 4;246(1-2):49-57.
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Vincent Laudet (Ecole Normale Superieure de Lyon, Institute of Functional Genomics)
1) Paris M, Escriva H, Schubert M, Brunet F, Brtko J, Ciesielski F, Roecklin D, Vivat-Hannah V, Jamin EL, Cravedi JP, Scanlan TS, Renaud JP, Holland ND, Laudet V., "Amphioxus postembryonic development reveals the homology of chordate metamorphosis." Curr Biol., 18(11), 825-30(2008).
2) Nishio S, Gibert Y, Bernard L, Brunet F, Triqueneaux G, Laudet V., "Adiponectin and adiponectin receptor genes are coexpressed during zebrafish embryogenesis and regulated by food deprivation.", Dev Dyn., 237(6), 1682-90(2008).
3) Bonneton F, Chaumot A, Laudet V., "Annotation of Tribolium nuclear receptors reveals an increase in evolutionary rate of a network controlling the ecdysone cascade.", Insect Biochem Mol Biol., 8(4), 416-29(2008).
4) Kakizawa T, Nishio S, Triqueneaux G, Bertrand S, Rambaud J, Laudet V., "Two differentially active alternative promoters control the expression of the zebrafish orphan nuclear receptor gene Rev-erbalpha.", J Mol Endocrinol., 38(5), 555-68(2007).
5) Ingraham H, Lazar M, Muscat G, Perlmann T, Renaud JP, Schwabe J, Sladek F, Tsai MJ, Laudet V, Benoit G, Cooney A, Giguere V, "International Union of Pharmacology. LXVI. Orphan nuclear receptors.", Pharmacol Rev., 58(4), 798-836(2006).
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Matthias Reuss (Institute for Biochemical, Engineering and Centre for Systems Biology, University of Stuttgart)
1) Buziol S, Warth L, Magario I, Freund A, Siemann-Herzberg M, Reuss M, "Dynamic response of the expression of hxt1, hxt5 and hxt7 transport proteins in Saccharomyces cerevisiae to perturbations in the extracellular glucose concentration.", J Biotechnol., 134(3-4), 203-10(2008).
2) Hofmann U, Maier K, Niebel A, Vacun G, Reuss M, Mauch K, "Identification of metabolic fluxes in hepatic cells from transient 13C-labeling experiments: Part I. Experimental observations.", Biotechnol Bioeng., 100(2), 344-54(2008).
3) Maier K, Hofmann U, Reuss M, Mauch K, "Identification of metabolic fluxes in hepatic cells from transient 13C-labeling experiments: Part II. Flux estimation.", Biotechnol Bioeng., 100(2), 355-70(2008).
4) Schaub J, Mauch K, Reuss M, "Metabolic flux analysis in Escherichia coli by integrating isotopic dynamic and isotopic stationary 13C labeling data.", Biotechnol Bioeng., 99(5), 1170-85(2008).
5) Hardiman T, Ewald JC, Lemuth K, Reuss M, Siemann-Herzberg M, "Quantification of rRNA in Escherichia coli using capillary gel electrophoresis with laser-induced fluorescence detection.", Anal Biochem., 374(1), 79-86(2008).
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Tatsuhiko Kodama (The University of Tokyo, Research Center for Advanced Science and Technology)
1) Takaoka A, Wang Z, Choi MK, Yanai H, Negishi H, Ban T, Lu Y, Miyagishi M, Kodama T, Honda K, Ohba Y, Taniguchi T. DAI (DLM-1/ZBP1) is a cytosolic DNA sensor and an activator of innate immune response. Nature. 2007 Jul 26;448(7152):501-5.
2) Watanabe M, Houten SM, Mataki C, Christoffolete MA, Kim BW, Sato H, Messaddeq N, Ezaki O, Kodama T, Bianco AC, Auwerx J, Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation, Nature 2006; 439: 484-9
3) Koga T, Inui M, Inoue K, Kin S, Suematsu A, Kobayashi E, Iwata T, Ohnishi H, Matozaki T, Kodama T, Tniguchi T, Takayanagi H, Takai T. ITAM-mediated costimulatory signals cooperate with RANKL for bone homeostasis., Nature 2004 428, 758-63.
4) 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 J-K, van Berkel T-J-C, Steinbrecher U-P, Ishibashi S, maeda N, Gordon S & Kodama T. Resistance to atherosclerosis and susceptibility to infection in scavenger receptor knockout mice, Nature, 1997, 386, 292-6
5) Kurihara, Y., Kurihara, H., Suzuki, H., Kodama, T., Maemura, K., Nagai, R., Oda, H., Kuwaki, T., Cao, W-H., Kamata, N., Jishage, K., Ouchi, Y., Azuma, S., Toyoda, Y., Ishikawa, T., Kumada, M.,& Yazaki, Y. Disruption of mouse endothelin-1 gene results in lethality and craniofacial anomaly in homozygotes and elevated blood pressure in heterozygotes. Nature, 1994, 368, 703-710
6) Rohrer, L., Freeman, M., Kodama, T., Penman, M., & Krieger, M. Coiled-coil fibrous domains mediate ligand binding by macrophage scavenger receptor type II., Nature, 1990, 343, 570-572.
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Ruben Abagyan (The Scripps Research Institute, Molecular Biology)
1) Nicola G, Smith CA, Abagyan R, "New method for the assessment of all drug-like pockets across a structural genome.", J Comput Biol., 15(3), 231-40(2008).
2) Bottegoni G, Kufareva I, Totrov M, Abagyan R, "A new method for ligand docking to flexible receptors by dual alanine scanning and refinement (SCARE).", J Comput Aided Mol Des., 22(5), 311-25(2008).
3) J. Chrencik JE, Brooun A, Recht MI, Nicola G, Davis LK, Abagyan R, Widmer H, Pasquale EB, Kuhn P, "Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition.", Biol Chem., 282(50), 36505-13(2007).
4) Totrov M, Abagyan R, "Flexible ligand docking to multiple receptor conformations: a practical alternative.", Curr Opin Struct Biol., 18(2), 178-84(2008).
5) Kovacs JA, Baker KA, Altenberg GA, Abagyan R, Yeager M, "Molecular modeling and mutagenesis of gap junction channels.", Prog Biophys Mol Biol.,. 94(1-2), 15-28(2007).
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Geoffrey L. Greene (The University of Chicago)
1) Nettles KW, Bruning JB, Gil G, Nowak J, Sharma SK, Hahm JB, Kulp K, Hochberg RB, Zhou H, Katzenellenbogen JA, Katzenellenbogen BS, Kim Y, Joachmiak A, Greene GL 2008 NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses. Nature chemical biology 4:241-247
2) Nettles KW, Gil G, Nowak J, Metivier R, Sharma VB, Greene GL 2008 CBP Is a dosage-dependent regulator of nuclear factor-kappaB suppression by the estrogen receptor. Molecular endocrinology 22:263-272
3) Hsieh RW, Rajan SS, Sharma SK, Greene GL 2008 Molecular characterization of a B-ring unsaturated estrogen: Implications for conjugated equine estrogen components of Premarin. Steroids 73:59-68
4) Nettles KW, Bruning JB, Gil G, O'Neill EE, Nowak J, Hughs A, Kim Y, DeSombre ER, Dilis R, Hanson RN, Joachimiak A, Greene GL 2007 Structural plasticity in the oestrogen receptor ligand-binding domain. EMBO Rep 8:563-568
5) Huang J, Koide A, Nettle KW, Greene GL, Koide S 2006 Conformation-specific affinity purification of proteins using engineered binding proteins: application to the estrogen receptor. Protein Expr Purif 47:348-354
6) Hsieh RW, Rajan SS, Sharma SK, Guo Y, DeSombre ER, Mrksich M, Greene GL 2006 Identification of ligands with bicyclic scaffolds provides insights into mechanisms of estrogen receptor subtype selectivity. J Biol Chem 281:17909-17919
7) Wu YL, Yang X, Ren Z, McDonnell DP, Norris JD, Willson TM, Greene GL 2005 Structural basis for an unexpected mode of SERM-mediated ER antagonism. Mol Cell 18:413-424
8) Nettles KW, Greene GL 2005 Ligand control of coregulator recruitment to nuclear receptors. Annu Rev Physiol 67:309-333
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Sunil Nagpal (Wyeth Research)
1) Transcriptional profiling of keratinocytes reveals a vitamin D-regulated differentiation network. (2005) Jianfen Lu, Keith Goldstein, Peining Chen, Shuguang Huang, Larry Gelbert and Sunil Nagpal. J. Invest. Dermatol. 124, 778-785, 2005.
2) Non-calcemic actions of vitamin D receptor ligands. Sunil Nagpal, Songqing Na and Radhakrishnan Rathnachalam. Endocr. Rev. 26, 662-687, 2005.
3) Vitamin D receptor modulators for inflammation and cancer. Ying K. Yee, Subba R. Chintalacharuvu, Jianfen Lu and Sunil Nagpal. Mini Rev. Med. Chem. 5, 761-778, 2005.
4) Nuclear receptors as drug discovery targets. Editorial Sunil Nagpal. Mini Rev. Med. Chem. 5, 699-700, 2005
5) Coactivation of the human vitamin D receptor by the peroxisome proliferator-activated receptor g coactivator-1a (PGC-1a). (2005) Rajesh S. Savkur, Kelli S. Bramlett, Sunil Nagpal and Thomas P. Burris. Mol. Pharmacol. 68, 511-517, 2005.
6) Identification and characterization of noncalcemic, tissue-selective, nonsecosteroidal vitamin D receptor modulators. Linda Ma, Berket Khalifa, Ying Y. Yee, Jianfen Lu, Ai Memezawa, Rajesh S. Savkur, Yoko Yamamoto, Subba R. Chintalacharuvu. Kazuyoshi Yamaoka, Keith R. Stayrook, Kelli S. Bramlett, Qing Q. Zeng, Srinivasan Chandrasekhar, Xiao-Peng Yu, Jared Linebarger, Stephen J. Iturria, Thomas P. Burris, Shigeaki Kato, William W. Chin and Sunil Nagpal. J. Clin. Invest. 116, 892-904, 2006.
7) Vitamin D receptor ligands for osteoporosis. Boris J. Cheskis, Leonard P. Freedman and Sunil Nagpal. Curr. Opin. Investig. Drugs 7, 906-911, 2006.
8) Liver X receptor is a therapeutic target for rheumatoid arthritis. Subba R. Chintalacharuvu, George E. Sandusky, Thomas P. Burris, Glenna C. Burmer and Sunil Nagpal. Arthritis & Rheumatism 56, 1365-1367, 2007.
9) Signaling by estrogens. Boris J. Cheskis, James G. Greger, Sunil Nagpal and Leonard P. Freedman. J. Cell. Physiol. 213, 610-617, 2007.
10) Selective androgen receptor modulators for frailty and osteoporosis. (2007) Edward J. Kilbourne, William J. Moore, Leonard P. Freedman and Sunil Nagpal. Curr. Opin. Investig. Drugs 8, 821-829, 2007.
11) Regulation of human 3a-hydroxysteroid dehydrogenase (AKR1C4) expression by the liver X receptor a. Keith R. Stayrook, Pamle M. Rogers, Rajesh S. Savkur, Yongjun Wang, Chen Su, Gabor Varga, Xin Bu, Tao Wei, Sunil Nagpal, Xiaole Shirley Liu and Thomas P. Burris. Mol. Pharmacol. 73, 607-612, 2008
12) MNAR Plays an Important Role in ERa Activation of Src/MAPK and PI3K/Akt Signaling Pathways. Boris J. Cheskis, James Greger, Neil Cooch, Chris McNally, Sean Mclarney, Ho-Sun Lam, Su Rutledge, Belew Mekonnen, Diane Hauze, Sunil Nagpal and Leonard P. Freedman. Steroids 2007 (In Press).
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Shigeaki Kato (The University of Tokyo, Institute of Molecular and Cellular Biosciences)
1) Ohtake, F., Baba, A., Takada, I., Okada, M., Iwasaki, K., Miki, H., Takahashi, S., Kouzmenko, A., Nohara, K., Chiba, T., Fujii-Kuriyama, Y., Kato, S.: Dioxin receptor is a ligand-dependent E3 ubiquitin ligase. Nature, 446, 562-566, 2007.
2) Nakamura, T., Imai, Y., Matsumoto, T., Sato, S., Takeuchi, K., Igarashi, K., Harada,Y., Azuma, Y., Krust, A., Yamamoto, Y., Nishina, H., Takeda, S., Takayanagi, H., Metzger, D., Kanno, J., Takaoka, K., Martin, T. J., Chambon, P., Kato, S.: Estrogen prevents bone loss via estrogen receptor alpha and induction of Fas ligand in osteoclasts. Cell, 130, 811-823, 2007
3) Kitagawa, H., Fujiki, R., Yoshimura, K., Mezaki, Y., Uematus, Y., Matsui, D., Ogawa, S., Unno, K., Okubo, M., Tokita, A., Nakagawa, T., Ito, T., Ishimi, Y., Nagasawa, H., Matsumoto, T., Yanagisawa, J., Kato, S.: The chromatin remodeling complex WINAC targets a nuclear receptor to promoters and is impaired in Williams Syndrome. Cell, 113, 905-917, 2003.
4) Ohtake, F., Takeyama, K., Matsumoto, T., Kitagawa H., Yamamoto Y., Nohara K., Tohyama, C., Krust, A., Mimura, J., Chambon, P., Yanagisawa, J., Fujii-Kuriyama, Y., Kato, S.: Modulation of oestrogen receptor signalling by association with the activated dioxin receptor. Nature, 423, 545-550, 2003.
5) Yanagisawa, J., Yanagi, Y., Masuhiro, Y., Suzawa, M., Toriyabe, T., Kashiwagi, K., Watanabe, M., Kawabata, M., Miyazono, K., Kato, S.: Convergence of transforming growth factor-b and vitamin D signaling pathways on SMAD transcriptional coactivators. Science, 283, 1317-1321, 1999.
6) Takeyama, K., Kitanaka, S., Sato, T., Kobori, M., Yanagisawa, J., Kato, S.: 25-Hydroxyvitamin D3 1a-hydroxylase and vitamin D synthesis. Science, 277, 1827-1830, 1997.
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Johan Auwerx (Institute of Genetics and Molecular and Cellular Biology)
1) Feige JN, Auwerx J, gTranscriptional targets of sirtuins in the coordination of mammalian physiology.h Curr Opin Cell Biol., 20(3), 303-9(2008).
2) Canto C, Auwerx J, gGlucose restriction: longevity SIRTainly, but without building muscle?h, Dev Cell., 14(5), 642-4(2008).
3) Sato H, Macchiarulo A, Thomas C, Gioiello A, Une M, Hofmann AF, Saladin R, Schoonjans K, Pellicciari R, Auwerx J, gNovel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.h, J Med Chem., 51(6), 1831-41(2008) .
4) Gofflot F, Chartoire N, Vasseur L, Heikkinen S, Dembele D, Le Merrer J, Auwerx J, "Systematic gene expression mapping clusters nuclear receptors according to their function in the brain" Cell, 131, 405-418(2007).
5) Watanabe M, Houten SM, Mataki C, Christoffolete MA, Kim BW, Sato H, Messaddeq N, Harney JW, Ezaki O, Kodama T, Schoonjans K, Bianco AC, Auwerx J, "Bile acid induce energy expenditure by promoting intracellular thyroid hormone activation", Nature, 439, 484-489(2006).
6) Lagouge M, Argmann C, Gerhart-Hines Z, Meziane H, Lerin C, Daussin F, Mesadeq N, Milne J, Lambert P, Elliott P, Geny B, Laakso M, Puigserver P, Auwerx J, "Resveratrol improves mitochondrial function and protects against metabolic disease by activating SIRT1 and PGC1alpha", Cell, 127, 1109-1122(2006).
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Peter Tontonoz (University of California, Los Angeles)
1) Bensinger, S.J., Bradley, M.N., Joseph, S.B., Zelcer, N., Janssen, E.M., Hausner, M.A., Shih, R., Parks, J., Edwards, P.A., Jamieson, B.D., and Tontonoz, P. (2008). LXR signaling couples sterol metabolism to proliferation in the acquired immune response. Cell. In press.
2) Bensinger, S.J. and Tontonoz, P. (2008). Integration of metabolism and inflammation by lipid-activated nuclear receptors. Nature. In press.
3) Tontonoz, P. and Spiegelman, B.M. (2008). Beyond fat: the diverse biology of PPARg. Ann Rev. Biochem. 77:289-312.
4) Waki, H., Park, K.W., Mitro, N., Pei, L., Damoiseaux, R., Wilpitz, D., Reue, K., Saez, E., Tontonoz, P. (2007). The small molecule harmine is an anti-diabetic cell-type-specific regulator of PPARg expression. Cell Metabolism. 5:357-370.
5) Park, K.W., Waki, H., Villanueva, C.J., Monticelli, L., Hong, C., Kang, S., MacDougald, O.A., Goldrath, A.W., and Tontonoz, P. (2008). Id2 is a small molecule-inducible modulator of PPARg expression and adipocyte differentiation. Molecular Endocrinology. In press.
6) Bradley, M.N., Hong, C., Joseph, S.B., Chen, M., Wang. X., Lusis, J., Collins, A., Hseuh, W.A. Collins, J.L., Tangirala, R. and Tontonoz, P. (2007). Ligand activation of LXRb reverses whole body cholesterol overload and atherosclerosis in LXRa-/-apoE-/- mice. J. Clin. Invest. 117:2337-2346.
7) Zelcer, N., Khanlou, N., Clare, R., Jiang, Q., Reed-Geaghan, E.G., Landreth, G.E., Vinters, H.V.V., and Tontonoz, P. (2007). Attenuation of neuroinflammation and Alzehimer's disease pathology by LXRs. Proc. Natl. Acad. Sci. U.S.A. 104:10601-10606.
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Yoshihiro Ogawa (Tokyo Medical and Dental University)
1) Y. Ogawa, H. Masuzaki, N. Isse, T. Okazaki, K. Mori, M. Shigemoto, N. Satoh, N. Tamura, K. Hosoda, Y. Yoshimasa, H. Jingami, T. Kawada, and K. Nakao. Molecular cloning of rat obese cDNA and augmented gene expression in genetically obese Zucker fatty (fa/fa) rats. J. Clin. Invest. 96: 1647-1652, 1995.
2) K. Takaya, Y. Ogawa, J. Hiraoka, K. Hosoda, R. J. Koletsky, Y. Yamori, and K. Nakao.@Nonsense mutation of leptin receptor in the obese spontaneously hypertensive Koletsky rat.@Nat. Genet. 14: 130-131, 1996.
3) H. Masuzaki, Y. Ogawa, N. Sagawa, K. Hosoda, T. Matsumoto, H. Mise, H. Nishimura, Y. Yoshimasa, I. Tanaka, T. Mori, and K. Nakao. Nonadipose tissue production of leptin: leptin as a novel placenta-derived hormone in humans. Nat. Med. 3: 1029-1033, 1997.
4) Y. Ogawa, H. Masuzaki, K. Hosoda, M. Aizawa-Abe, J. Suga, M. Suda, K. Ebihara, H. Iwai, N. Matsuoka, N. Satoh, H. Odaka, H. Kasuga, Y. Fujisawa, G. Inoue, H. Nishimura, Y. Yoshimasa, and K. Nakao. Increased glucose metabolism and insulin sensitivity in transgenic skinny mice overexpressing leptin. Diabetes 48: 1822-1829, 1999.
5) S. Yura, Y. Ogawa, N. Sagawa, H. Masuzaki, H. Itoh, K. Ebihara, M. Aizawa-Abe, S. Fujii, and K. Nakao. Accelerated puberty and late-onset hypothalamic hypogonadism in female transgenic skinny mice overexpressing leptin. J. Clin. Invest. 105: 749-755, 2000.
6) M. Aizawa-Abe, Y. Ogawa, H. Masuzaki, K. Ebihara, N. Satoh, H. Iwai, N. Matsuoka, T. Hayashi, K. Hosoda, G. Inoue, Y. Yoshimasa, and K. Nakao. Pathophysiological role of leptin in obesity-related hypertension. J. Clin. Invest. 105: 1243-1252, 2000.
7) Y. Oike, M. Akao, K. Yasunaga, T. Yamauchi, T. Morisada, Y. Ito, T. Urano, Y. Kimura, Y. Kubota, H. Maekawa, T. Miyamoto, K. Miyata, S. Matsumoto, J. Sakai, N. Nakagata, M. Takeya, H. Koseki, Y. Ogawa, T. Kadowaki, and T. Suda. Angiopoietin-related growth factor antagonizes obesity and insulin resistance. Nat. Med. 11: 400-408, 2005.
8) S. Yura, H. Itoh, N. Sagawa, H. Yamamoto, H. Masuzaki, K. Nakao, M. Kawamura, M. Takemura, K. Kakui, Y. Ogawa, and S. Fujii. Role of premature leptin surge in obesity resulting from intrauterine undernutrition. Cell Metabolism 1: 371-378, 2005.
9) T. Suganami, J. Nishida, and Y. Ogawa. A paracrine loop between adipocytes and macrophages aggravates inflammatory changes: role of free fatty acids and tumor necrosis factor a. Arterioscler. Thromb. Vasc. Biol. 25: 2062-2068, 2005.
10) J. Park, S. S. Choe, A. H. Choi, K. H. Kim, M. J. Yoon, N. Houstis, E. D. Rogen, T. Suganami, Y. Ogawa, and J. B. Kim. Increase in glucose-6-phosphate dehydrogenase in adipocytes stimulates oxidative stress and inflammatory signal. Diabetes 55: 2939-2949, 2006.
11) T. Suganami, K. Tanimoto-Koyama, J. Nishida, M. Ito, X. Yuan, S. Mizuarai, H. Kotani, S. Yamaoka, K. Miyake, S. Aoe, Y. Kamei, and Y. Ogawa. Role of the Toll-like receptor 4/NF-kB pathway in saturated fatty acid-induced inflammatory changes in the interaction between adipocytes and macrophages. Arterioscler. Thromb. Vasc. Biol. 27: 84-91, 2007.
12) M. Itoh, T. Suganami, N. Satoh, K. Tanimoto-Koyama, X. Yuan, M. Tanaka, H. Kawano, T. Yano, S. Aoe, M. Takeya, A. Shimatsu, H. Kuzuya, Y. Kamei, and Y. Ogawa. Increased adiponectin secretion by highly purified eicosapentaenoic acid in rodent models of obesity and human obese subjects. Arterioscler. Thromb. Vasc. Biol. 27: 1918-1925, 2007.
13) A. Ito, T. Suganami, Y. Miyamoto, Y. Yoshimasa, M. Takeya, Y. Kamei, and Y. Ogawa. Role of mitogen-activated protein kinase phosphatase-1 in the induction of monocyte chemoattractant protein-1 during the course of adipocyte hypertrophy. J. Biol. Chem. 282: 25445-25452, 2007.
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