Výsledky vyhledávání - "Kimiyuki Shibuya"

Akademický článek

Esterification of 24S-OHC induces formation of atypical lipid droplet-like structures, leading to neuronal cell death[S]

Autor: Wakako Takabe, Yasuomi Urano, Diep-Khanh Ho Vo, Kimiyuki Shibuya, Masaki Tanno, Hiroaki Kitagishi, Toyoshi Fujimoto, Noriko Noguchi

Publikováno v: Journal of Lipid Research, Vol 57, Iss 11, Pp 2005-2014 (2016)

The 24(S)-hydroxycholesterol (24S-OHC), which plays an important role in maintaining brain cholesterol homeostasis, has been shown to possess neurotoxicity. We have previously reported that 24S-OHC esterification by ACAT1 and the resulting lipid drop

Externí odkaz: https://doaj.org/article/075bdaece3af4c72994b229d9a656e72

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Akademický článek

Crystal structures of (S)-(+)-5-(3-bromo/chloro-4-isopropoxyphenyl)-5-methylimidazolidine-2,4-dione

Autor: Shigeru Ohba, Minoru Koura, Hisashi Sumida, Kimiyuki Shibuya

Publikováno v: Acta Crystallographica Section E: Crystallographic Communications, Vol 72, Iss 2, Pp 184-187 (2016)

In (S)-(+)-5-(3-bromo-4-isopropoxyphenyl)-5-methylimidazolidine-2,4-dione, C13H15BrN2O3, (I), the hydantoin groups are connected via intermolecular N—H...O hydrogen bonds, forming a terraced sheet structure. In the chloro analogue, (S)-(+)-5-(3-chl

Externí odkaz: https://doaj.org/article/b1ae37b9f06d4450b45b0ea0967ba8ee

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Brain Targeting of Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor K-604 via the Intranasal Route Using a Hydroxycarboxylic Acid Solution

Autor: Noriko Noguchi, Yasuomi Urano, Masayoshi Miyamoto, Yoshihiko Tsunenari, Shin-ichiro Ogawa, Kimiyuki Shibuya, Shigeru Morikawa

Publikováno v: ACS Omega
ACS Omega, Vol 4, Iss 16, Pp 16943-16955 (2019)

An acyl-CoA:cholesterol O-acyltransferase-1 (ACAT-1/SOAT-1) inhibitor, K-604 is a promising drug candidate for the treatment of Alzheimer's disease and glioblastoma; however, it exhibits poor solubility in neutral water and low permeability across th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fad4fe7cc5ca6aef1b49bda38aade33
http://europepmc.org/articles/PMC6796924

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Synthesis of oxidative metabolites of K-115, a novel Rho-kinase inhibitor

Autor: Noriaki Gomi, Kimiyuki Shibuya, Kiyoshi Kawamura, Mototsugu Kabeya

Publikováno v: Tetrahedron Letters. 91:153589

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b432f9a1be0f2dd4cbfacfd34312a4a7
https://doi.org/10.1016/j.tetlet.2021.153589

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Discovery of Clinical Candidate 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor

Autor: Tadaaki Ohgiya, Yasunobu Yoshinaka, Toshiyuki Kawagoe-shi Edano, Yoshihiko Tsunenari, Kimiyuki Shibuya, Chiyoka Ozaki, Katsumi Kawamine

Publikováno v: Journal of Medicinal Chemistry. 61:10635-10650

2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide hydrochloride (K-604, 2) has been identified as an aqueous-soluble potent inhibitor of human acyl-coenzyme A:cholesterol O-acyltransfe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3cebdb7358c6c0e4003540d4e19945b7
https://doi.org/10.1021/acs.jmedchem.8b01256

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Determination of the Absolute Configuration and a Practical Chiral Synthesis of 5-[5-(1-Methylethoxy)pyridin-2-yl]-5-methylimidazolidine-2,4-dione as a Novel Liver X Receptor β-Selective Agonist

Autor: Hisashi Sumida, Shigeru Ohba, Kimiyuki Shibuya, Minoru Koura

Publikováno v: Synthesis. 49:2074-2080

We determined that the absolute configuration of 5-[5-(1-methylethoxy)pyridin-2-yl]-5-methylimidazolidine-2,4-dione (hydantoin) is the (S)-form for the liver X receptor (LXR) β-selective agonist through X-ray crystal structure analysis of the hydant

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::53a0cd9c34a97fcd7b4613896a4aab28
https://doi.org/10.1055/s-0036-1588700

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Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist

Autor: Yuki Matsumoto, Tomoaki Koshizawa, Sayaka Kurobuchi, Takayuki Matsuda, Hisashi Sumida, Minoru Koura, Yuki Yamaguchi, Yuichiro Watanabe, Ayumu Okuda, Takashi Enomoto, Kimiyuki Shibuya

Publikováno v: Bioorganic & Medicinal Chemistry. 24:3436-3446

Our research found that the 2-hydroxyacetophenone derivative is an outstanding linker between the 1,1-bistrifluoromethylcarbinol moiety and the imidazolidine-2,4-dione moiety to enhance the potency and β-selectivity of liver X receptor (LXR) agonist

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8849ffcdf71bbe94714a6249e59732e
https://doi.org/10.1016/j.bmc.2016.05.048

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Synthesis of 24(S)-hydroxycholesterol esters responsible for the induction of neuronal cell death

Autor: Noriko Noguchi, Kimiyuki Shibuya, Toshiaki Watanabe, Yasuomi Urano, Wakako Takabe, Hiroaki Kitagishi

Publikováno v: Bioorganic & Medicinal Chemistry. 24:2559-2566

We synthesized several candidates of 24(S)-hydroxycholesterol (24S-OHC) esters, which are involved in neuronal cell death, through catalysis with acyl-CoA:cholesterol acyltransferase-1 (ACAT-1). We studied the regioselectivity of the acylation of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fb131ac4d9c08639e9cace0297db374
https://doi.org/10.1016/j.bmc.2016.04.024

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