Discovery of peroxisome proliferator–activated receptor α (PPARα) activators with a ligandscreening system using a human PPARα-expressing cell line.

Keisuke Tachibana, Tomohiro Yuzuriha, Ryotaro Tabata, Syohei Fukuda, Takashi Maegawa, Rika Takahashi, Keiichi Tanimoto, Hirofumi Tsujino, Kazuto Nunomura, Bangzhong Lin, Yoshiharu Matsuura, Toshiya Tanaka, Takao Hamakubo, Juro Sakai, Tatsuhiko Kodama, Tadayuki Kobayashi, Kenji Ishimoto, Hiroyuki Miyachi, and Takefumi Doi. Discovery of peroxisome proliferator–activated receptor α (PPARα) activators with a ligandscreening system using a human PPARα-expressing cell line. J. Biol. Chem., In press.

What consequence is anticipated by the emergence of novel SPPARMa agent developed so as to achieve an improved safety/efficacy balance?

Motonobu Anai, Toshiya Tanaka, Tatsuhiko Kodama. What consequence is anticipated by the emergence of novel SPPARMa agent developed so as to achieve an improved safety/efficacy balance? Jpn Pharmacol. Ther., 46: 471-480 (2018).

Overexpression of p54nrb/NONO induces differential EPHA6 splicing and contributes to castration-resistant prostate cancer growth.

Yamamoto R, Osawa T, Sasaki Y, Yamamoto S, Anai M, Izumi K, Matsumura Y, Sakai J, Aburatani H, Mizokami A, Kodama T, Tanaka T. Overexpression of p54nrb/NONO induces differential EPHA6 splicing and contributes to castration-resistant prostate cancer growth. Oncotarget. 2018 Jan 8;9(12):10510-10524. doi: 10.18632/oncotarget.24063.

The Influence of Pemafibrate (Parmodia Tablet) on Liver and Renal Function

Toshiya Tanaka, Motonobu Anai, and Tatsuhiko Kodama The Influence of Pemafibrate (Parmodia Tablet) on Liver and Renal Function J Pharmacol Ther. 2017 Nov 20; 45(11):1775-1785.

Aberrant DNA methylation of pregnane X receptor underlies metabolic gene alterations in the diabetic kidney.

Watanabe A, Marumo T, Kawarazaki W, Nishimoto M, Ayuzawa N, Ueda K, Hirohama D, Tanaka T, Yagi S, Ota S, Nagae G, Aburatani H, Kumagai H, Fujita T. Aberrant DNA methylation of pregnane X receptor underlies metabolic gene alterations in the diabetic kidney. Am J Physiol Renal Physiol. 2018 Apr 1;314(4):F551-F560. doi: 10.1152/ajprenal.00390.2017.

Degradation of human Lipin-1 by BTRC E3 ubiquitin ligase.

Ishimoto K, Hayase A, Kumagai F, Kawai M, Okuno H, Hino N, Okada Y, Kawamura T, Tanaka T, Hamakubo T, Sakai J, Kodama T, Tachibana K, Doi T. Degradation of human Lipin-1 by BTRC E3 ubiquitin ligase. Biochem Biophys Res Commun. 2017 Jun 17;488(1):159-164. doi: 10.1016/j.bbrc.2017.04.159. Epub 2017 May 5

Ubiquitination of Lysine 867 of the Human SETDB1 Protein Upregulates Its Histone H3 Lysine 9 (H3K9) Methyltransferase Activity.

Ishimoto K, Kawamata N, Uchihara Y, Okubo M, Fujimoto R, Gotoh E, Kakinouchi K, Mizohata E, Hino N, Okada Y, Mochizuki Y, Tanaka T, Hamakubo T, Sakai J, Kodama T, Inoue T, Tachibana K, Doi T. Ubiquitination of Lysine 867 of the Human SETDB1 Protein Upregulates Its Histone H3 Lysine 9 (H3K9) Methyltransferase Activity. PLoS One. 2016 Oct 31;11(10):e0165766. doi: 10.1371/journal.pone.0165766. eCollection 2016.

Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα))-Regulated Genes in Primary Human Hepatocytes and the Mouse Liver.

Raza-Iqbal S, Tanaka T, Anai M, Inagaki T, Matsumura Y, Ikeda K, Taguchi A, Gonzalez FJ, Sakai J, Kodama T. Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα))-Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb. 2015 Aug 26;22(8):754-72. doi: 10.5551/jat.28720. Epub 2015 Jun 4.

Analysis of the subcellular localization of the human histone methyltransferase SETDB1.

Tachibana K, Gotoh E, Kawamata N, Ishimoto K, Uchihara Y, Iwanari H, Sugiyama A, Kawamura T, Mochizuki Y, Tanaka T, Sakai J, Hamakubo T, Kodama T, Doi T. Analysis of the subcellular localization of the human histone methyltransferase SETDB1. Biochem Biophys Res Commun. 2015 Oct 2;465(4):725-31. doi: 10.1016/j.bbrc.2015.08.065. Epub 2015 Aug 18.

JMJD1A is a signal-sensing scaffold that regulates acute chromatin dynamics via SWI/SNF association for thermogenesis.

Abe Y, Rozqie R, Matsumura Y, Kawamura T, Nakaki R, Tsurutani Y, Tanimura-Inagaki K, Shiono A, Magoori K, Nakamura K, Ogi S, Kajimura S, Kimura H, Tanaka T, Fukami K, Osborne TF, Kodama T, Aburatani H, Inagaki T, Sakai J. JMJD1A is a signal-sensing scaffold that regulates acute chromatin dynamics via SWI/SNF association for thermogenesis. Nat Commun. 2015 May 7;6:7052. doi: 10.1038/ncomms8052.

The FBXL10/KDM2B scaffolding protein associates with novel polycomb repressive complex-1 to regulate adipogenesis.

Inagaki T, Iwasaki S, Matsumura Y, Kawamura T, Tanaka T, Abe Y, Yamasaki A, Tsurutani Y, Yoshida A, Chikaoka Y, Nakamura K, Magoori K, Nakaki R, Osborne TF, Fukami K, Aburatani H, Kodama T, Sakai J. The FBXL10/KDM2B scaffolding protein associates with novel polycomb repressive complex-1 to regulate adipogenesis. J Biol Chem. 2015 Feb 13;290(7):4163-77. doi: 10.1074/jbc.M114.626929. Epub 2014 Dec 22.

PPARβ/δ activation of CD300a controls intestinal immunity.

Tanaka T, Tahara-Hanaoka S, Nabekura T, Ikeda K, Jiang S, Tsutsumi S, Inagaki T, Magoori K, Higurashi T, Takahashi H, Tachibana K, Tsurutani Y, Raza S, Anai M, Minami T, Wada Y, Yokote K, Doi T, Hamakubo T, Auwerx J, Gonzalez FJ, Nakajima A, Aburatani H, Naito M, Shibuya A, Kodama T, Sakai J. PPARβ/δ activation of CD300a controls intestinal immunity. Sci Rep. 2014 Jun 24;4:5412. doi: 10.1038/srep05412.

Cross-enhancement of ANGPTL4 transcription by HIF1 alpha and PPAR beta/delta is the result of the conformational proximity of two response elements.

Inoue T, Kohro T, Tanaka T, Kanki Y, Li G, Poh HM, Mimura I, Kobayashi M, Taguchi A, Maejima T, Suehiro J, Sugiyama A, Kaneki K, Aruga H, Dong S, Stevens JF, Yamamoto S, Tsutsumi S, Fujita T, Ruan X, Aburatani H, Nangaku M, et al. Cross-enhancement of ANGPTL4 transcription by HIF1 alpha and PPAR beta/delta is the result of the conformational proximity of two response elements. Genome Biol. 2014 Apr 10;15(4):R63. doi: 10.1186/gb-2014-15-4-r63.

Human mannose-binding lectin 2 is directly regulated by peroxisome proliferator-activated receptors via a peroxisome proliferator responsive element.

Tachibana K, Takeuchi K, Inada H, Sugimoto K, Ishimoto K, Yamashita M, Maegawa T, Yamasaki D, Osada S, Tanaka T, Rakugi H, Hamakubo T, Sakai J, Kodama T, Doi T. Human mannose-binding lectin 2 is directly regulated by peroxisome proliferator-activated receptors via a peroxisome proliferator responsive element. J Biochem. 2013 Sep;154(3):265-73. doi: 10.1093/jb/mvt050. Epub 2013 May 27.

Dynamic change of chromatin conformation in response to hypoxia enhances the expression of GLUT3 (SLC2A3) by cooperative interaction of hypoxia-inducible factor 1 and KDM3A.

Mimura I, Nangaku M, Kanki Y, Tsutsumi S, Inoue T, Kohro T, Yamamoto S, Fujita T, Shimamura T, Suehiro J, Taguchi A, Kobayashi M, Tanimura K, Inagaki T, Tanaka T, Hamakubo T, Sakai J, Aburatani H, Kodama T, Wada Y. Dynamic change of chromatin conformation in response to hypoxia enhances the expression of GLUT3 (SLC2A3) by cooperative interaction of hypoxia-inducible factor 1 and KDM3A. Mol Cell Biol. 2012 Aug;32(15):3018-32. doi: 10.1128/MCB.06643-11. Epub 2012 May 29.

Novel repressor regulates insulin sensitivity through interaction with Foxo1.

Nakae J, Cao Y, Hakuno F, Takemori H, Kawano Y, Sekioka R, Abe T, Kiyonari H, Tanaka T, Sakai J, Takahashi S, Itoh H. Novel repressor regulates insulin sensitivity through interaction with Foxo1. EMBO J. 2012 May 16;31(10):2275-95. doi: 10.1038/emboj.2012.97. Epub 2012 Apr 17.

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