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Items: 20

1.

GPR40 full agonism exerts feeding suppression and weight loss through afferent vagal nerve.

Ueno H, Ito R, Abe SI, Ogino H, Maruyama M, Miyashita H, Miyamoto Y, Moritoh Y, Tsujihata Y, Takeuchi K, Nishigaki N.

PLoS One. 2019 Sep 16;14(9):e0222653. doi: 10.1371/journal.pone.0222653. eCollection 2019.

2.

SCO-267, a GPR40 Full Agonist, Improves Glycemic and Body Weight Control in Rat Models of Diabetes and Obesity.

Ueno H, Ito R, Abe SI, Ookawara M, Miyashita H, Ogino H, Miyamoto Y, Yoshihara T, Kobayashi A, Tsujihata Y, Takeuchi K, Watanabe M, Yamada Y, Maekawa T, Nishigaki N, Moritoh Y.

J Pharmacol Exp Ther. 2019 Aug;370(2):172-181. doi: 10.1124/jpet.118.255885. Epub 2019 Jun 10.

PMID:
31182471
3.

Antihypertrophic Effects of Small Molecules that Maintain Mitochondrial ATP Levels Under Hypoxia.

Nagai H, Satomi T, Abiru A, Miyamoto K, Nagasawa K, Maruyama M, Yamamoto S, Kikuchi K, Fuse H, Noda M, Tsujihata Y.

EBioMedicine. 2017 Oct;24:147-158. doi: 10.1016/j.ebiom.2017.09.022. Epub 2017 Sep 19.

4.

Fasiglifam (TAK-875) has dual potentiating mechanisms via Gαq-GPR40/FFAR1 signaling branches on glucose-dependent insulin secretion.

Sakuma K, Yabuki C, Maruyama M, Abiru A, Komatsu H, Negoro N, Tsujihata Y, Takeuchi K, Habata Y, Mori M.

Pharmacol Res Perspect. 2016 Apr 27;4(3):e00237. doi: 10.1002/prp2.237. eCollection 2016 Jun.

5.

Fasiglifam/TAK-875, a Selective GPR40 Agonist, Improves Hyperglycemia in Rats Unresponsive to Sulfonylureas and Acts Additively with Sulfonylureas.

Ito R, Tsujihata Y, Suzuki M, Miyawaki K, Matsuda K, Takeuchi K.

J Pharmacol Exp Ther. 2016 Apr;357(1):217-27. doi: 10.1124/jpet.115.230730. Epub 2016 Jan 26.

PMID:
26813930
6.

[Discovery and development of a selective GPR40/FFAR1 agonist, fasiglifam, for treatment of type 2 diabetes mellitus].

Tsujihata Y.

Nihon Yakurigaku Zasshi. 2014 Aug;144(2):59-63. Japanese. No abstract available.

PMID:
25109517
7.

Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists.

Sato K, Sugimoto H, Rikimaru K, Imoto H, Kamaura M, Negoro N, Tsujihata Y, Miyashita H, Odani T, Murata T.

Bioorg Med Chem. 2014 Mar 1;22(5):1649-66. doi: 10.1016/j.bmc.2014.01.028. Epub 2014 Jan 28.

PMID:
24508142
8.

A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.

Yabuki C, Komatsu H, Tsujihata Y, Maeda R, Ito R, Matsuda-Nagasumi K, Sakuma K, Miyawaki K, Kikuchi N, Takeuchi K, Habata Y, Mori M.

PLoS One. 2013 Oct 10;8(10):e76280. doi: 10.1371/journal.pone.0076280. eCollection 2013.

9.

TAK-875, a GPR40/FFAR1 agonist, in combination with metformin prevents progression of diabetes and β-cell dysfunction in Zucker diabetic fatty rats.

Ito R, Tsujihata Y, Matsuda-Nagasumi K, Mori I, Negoro N, Takeuchi K.

Br J Pharmacol. 2013 Oct;170(3):568-80. doi: 10.1111/bph.12297.

10.

Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.

Negoro N, Sasaki S, Mikami S, Ito M, Tsujihata Y, Ito R, Suzuki M, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Morohashi A, Nonaka M, Matsunaga S, Yasuma T, Momose Y.

J Med Chem. 2012 Apr 26;55(8):3960-74. doi: 10.1021/jm300170m. Epub 2012 Apr 18.

PMID:
22490067
11.

Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.

Mikami S, Kitamura S, Negoro N, Sasaki S, Suzuki M, Tsujihata Y, Miyazaki T, Ito R, Suzuki N, Miyazaki J, Santou T, Kanzaki N, Funami M, Tanaka T, Yasuma T, Momose Y.

J Med Chem. 2012 Apr 26;55(8):3756-76. doi: 10.1021/jm2016123. Epub 2012 Apr 11.

PMID:
22428944
12.

Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists.

Negoro N, Sasaki S, Ito M, Kitamura S, Tsujihata Y, Ito R, Suzuki M, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T, Yasuma T, Momose Y.

J Med Chem. 2012 Feb 23;55(4):1538-52. doi: 10.1021/jm2012968. Epub 2012 Feb 10.

PMID:
22242551
13.

The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets.

Yashiro H, Tsujihata Y, Takeuchi K, Hazama M, Johnson PR, Rorsman P.

J Pharmacol Exp Ther. 2012 Feb;340(2):483-9. doi: 10.1124/jpet.111.187708. Epub 2011 Nov 21.

PMID:
22106100
14.

TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.

Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, Momose Y, Takeuchi K.

J Pharmacol Exp Ther. 2011 Oct;339(1):228-37. doi: 10.1124/jpet.111.183772. Epub 2011 Jul 13.

PMID:
21752941
15.

Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists.

Sasaki S, Kitamura S, Negoro N, Suzuki M, Tsujihata Y, Suzuki N, Santou T, Kanzaki N, Harada M, Tanaka Y, Kobayashi M, Tada N, Funami M, Tanaka T, Yamamoto Y, Fukatsu K, Yasuma T, Momose Y.

J Med Chem. 2011 Mar 10;54(5):1365-78. doi: 10.1021/jm101405t. Epub 2011 Feb 14.

PMID:
21319751
16.

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

Negoro N, Sasaki S, Mikami S, Ito M, Suzuki M, Tsujihata Y, Ito R, Harada A, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T, Kogame A, Matsunaga S, Yasuma T, Momose Y.

ACS Med Chem Lett. 2010 Jun 18;1(6):290-4. doi: 10.1021/ml1000855. eCollection 2010 Sep 9.

17.
18.

A single amino acid substitution in a self protein is sufficient to trigger autoantibody response.

Tsujihata Y, So T, Hashimoto Y, Ueda T, Imoto T.

Mol Immunol. 2001 Sep;38(5):375-81.

PMID:
11684293
19.

Mutant mouse lysozyme carrying a minimal T cell epitope of hen egg lysozyme evokes high autoantibody response.

Tsujihata Y, So T, Chijiiwa Y, Hashimoto Y, Hirata M, Ueda T, Imoto T.

J Immunol. 2000 Oct 1;165(7):3606-11.

20.

The molecular weight ratio of monomethoxypolyethylene glycol (mPEG) to protein determines the immunotolerogenicity of mPEG proteins.

So T, Ito HO, Tsujihata Y, Hirata M, Ueda T, Imoto T.

Protein Eng. 1999 Aug;12(8):701-5.

PMID:
10469832

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