Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Mitsuyuki, Shimada"'
Autor:
Taisuke, Tawaraishi, Atsuko, Ochida, Yuichiro, Akao, Sachiko, Itono, Masahiro, Kamaura, Thamina, Akther, Mitsuyuki, Shimada, Stacie, Canan, Sanjoy, Chowdhury, Yafeng, Cao, Kevin, Condroski, Ola, Engkvist, Amanda, Francisco, Sunil, Ghosh, Rina, Kaki, John M, Kelly, Chiaki, Kimura, Thierry, Kogej, Kazuya, Nagaoka, Akira, Naito, Garry, Pairaudeau, Constantin, Radu, Ieuan, Roberts, David, Shum, Nao-Aki, Watanabe, Huanxu, Xie, Shuji, Yonezawa, Osamu, Yoshida, Ryu, Yoshida, Charles, Mowbray, Benjamin, Perry
Publikováno v:
Journal of medicinal chemistry.
Probing multiple proprietary pharmaceutical libraries in parallel via virtual screening allowed rapid expansion of the structure-activity relationship (SAR) around hit compounds with moderate efficacy against
Publikováno v:
Pharmacological Reports. 70:172-177
The effects of farnesoid X receptor (FXR) antagonists on plasma lipid profile in mice have not been investigated thus far. The aim of this study was to investigate the antidyslipidemic effects of an FXR antagonist in dyslipidemic mice, and to clarify
Publikováno v:
European Journal of Pharmacology. 723:108-115
We aimed to elucidate the mechanism underlying the anti-dyslipidemic effect of compound-T3, a farnesoid X receptor antagonist, by investigating its effects on hepatic lipid metabolism in non-human primates. We administered lipid-lowering drugs for 7
Autor:
Mitsuyuki Shimada, Hiroshi Miki, Kouhei Asano, Masaki Ogino, Yoshihisa Nakada, Toshihiro Yamamoto, Hiroshi Yamaguchi, Minori Masago, Norikazu Tamura, Kazuko Aoki, Koki Kato
Publikováno v:
European Journal of Pharmacology. 640:243-249
Coenzyme A (CoA):diacylglycerol acyltransferase 1 (DGAT1) is 1 of the 2 known DGAT enzymes that catalyze the final and only committed step in triacylglycerol synthesis; this enzyme is considered to be a potential therapeutic target in metabolic disor
Autor:
Emiko Shinozawa, Hiroko Yamakawa, Ryuichi Tozawa, Yuichiro Amano, Megumi Haba, Mitsuyuki Shimada
Publikováno v:
Pharmacology Research & Perspectives
We attempted to clarify the therapeutic capability of antagonists of the farnesoid X receptor (FXR), a nuclear receptor that regulates lipid and bile acid metabolism. Herein, we report the antidyslipidemic effects of a novel synthesized FXR antagonis
Autor:
Yoshihisa Nakada, Minori Masago, Mitsuyuki Shimada, Toshihiro Yamamoto, Kouhei Asano, Kazuko Aoki, Hiroshi Miki, Norikazu Tamura, Koki Kato, Masaki Ogino
Publikováno v:
Chemical and Pharmaceutical Bulletin. 58:673-679
In a program to discover new small molecule diacylglycerol acyltransferase (DGAT)-1 inhibitors, screening of our in-house chemical library was carried out using recombinant human DGAT-1 enzyme. From this library, the lead compound 1a was identified a
Autor:
Kevin Bacon, Keiko Fukushima, Koriyama Yuji, Yamauchi Megumi, Nunami Noriko, Mitsuyuki Shimada, Yoshino Takashi, Karl Ziegelbauer, Akihiko Watanabe, Tsutomu Masuda, Hiroki Sato, Toshiki Murata, Timothy B. Lowinger, Kinji Fuchikami, Sachiko Sakakibara, Hiroshi Komura, Takuya Shintani
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4019-4022
A series of 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl)pyridine derivatives was synthesized and evaluated as I kappaB kinase beta (IKK-beta) inhibitors. Modification of a novel IKK-beta inhibitor 1 (IKK-beta IC(50)=1500 nM, Cell IC(50)=8000 nM) at th
Autor:
Yoshino Takashi, Keisuke Takeshita, Hiroshi Kadono, Sachiko Sakakibara, Kevin Bacon, Makoto Shimazaki, Mitsuyuki Shimada, Takuya Shintani, Katsuya Sakai, Toshiro Niki, Toshiki Murata, Tsutomu Masuda, Masaomi Umeda, Timothy B. Lowinger, Hisayo Inbe, Karl Ziegelbauer, Kinji Fuchikami
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:913-918
IkappaB kinase beta (IKK-beta) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-kappaB) in response to various inflammatory stimuli. We have identified a small molecule
Autor:
Mitsuyuki Shimada, Shotaro Miura, Eiichiro Ishikawa, Emiko Shinozawa, Ryuichi Tozawa, Ryutaro Adachi, Yuichiro Amano
Publikováno v:
Life sciences. 108(1)
Aims We previously reported anti-dyslipidemic effects of a farnesoid X receptor antagonist in monkeys. In this study, we compared the cholesterol-lowering effects of single and combined administration of a farnesoid X receptor antagonist, compound-T8
Publikováno v:
Life sciences. 106(1-2)
Aims We investigated antidyslipidemic effects of a farnesoid X receptor antagonist compound-T3 in non-human primates as a novel treatment approach for dyslipidemia. Main methods Cynomolgus monkeys were fed a high-fat diet over 3 weeks. Drugs were adm