Výsledky vyhledávání - "Kosuke Hitaka"

Akademický článek

Lead Identification of 8‑(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation

Autor: Fumihito Ushiyama, Hideaki Amada, Tomoki Takeuchi, Nozomi Tanaka-Yamamoto, Harumi Kanazawa, Koichiro Nakano, Masashi Mima, Aiko Masuko, Iichiro Takata, Kosuke Hitaka, Kunihiko Iwamoto, Hiroyuki Sugiyama, Norikazu Ohtake

Publikováno v: ACS Omega, Vol 5, Iss 17, Pp 10145-10159 (2020)

Externí odkaz: https://doaj.org/article/17fa358e19ce435eaf8d3e740e6f6ab1

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Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase-2 Inhibitor with a Phenylbenzamide–Pentapeptide Hybrid Scaffold

Autor: Tomoki Takeuchi, Yusaku Nomura, Tomoko Tamita, Rie Nishikawa, Hiroyuki Kakinuma, Naoki Kojima, Kosuke Hitaka, Yunoshin Tamura, Masafumi Kamitani, Masashi Mima, Akiko Nozoe, Masato Hayashi

Publikováno v: Journal of Medicinal Chemistry. 66:822-836

Matrix metalloproteinase-2 (MMP2) is a zinc-dependent endopeptidase and a promising target for various diseases, including cancer and fibrosis. Herein, we report the discovery of a novel MMP2-selective inhibitor with high chemical stability and slow

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05ee2c823088d6fbc7258a75ecef0c88
https://doi.org/10.1021/acs.jmedchem.2c01698

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Discovery of Aryloxyphenyl–Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis

Autor: Tomoki Takeuchi, Masato Hayashi, Tomoko Tamita, Yusaku Nomura, Naoki Kojima, Akiko Mitani, Takuya Takeda, Kosuke Hitaka, Yuki Kato, Masafumi Kamitani, Masashi Mima, Hidetoh Toki, Masahiko Ohkubo, Akiko Nozoe, Hiroyuki Kakinuma

Publikováno v: Journal of Medicinal Chemistry. 65:8493-8510

Matrix metalloproteinase-2 (MMP2) is a zinc-dependent endopeptidase that plays important roles in the degradation of extracellular matrix proteins. MMP2 is considered to be an attractive target for the treatment of various diseases such as cancer, ar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c56fb1ec00ef8793d1de48786c789f9e
https://doi.org/10.1021/acs.jmedchem.2c00613

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Discovery of Highly Potent and Selective Matrix Metalloproteinase-7 Inhibitors by Hybridizing the S1' Subsite Binder with Short Peptides

Autor: Hideaki Tabuse, Kumi Abe-Sato, Harumi Kanazawa, Miyoko Yashiro, Yunoshin Tamura, Masafumi Kamitani, Kosuke Hitaka, Emi Gunji, Akiko Mitani, Naoki Kojima, Yusuke Oka

Publikováno v: Journal of medicinal chemistry. 65(19)

Matrix metalloproteinase-7 (MMP-7) has emerged as a protein playing important roles in both physiological and pathophysiological processes. Despite the growing interest in MMP-7 as a potential therapeutic target for diseases including cancer and fibr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2475dd8ba597803edce752b11c7feb1
https://pubmed.ncbi.nlm.nih.gov/36137271

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Lead Identification of 8-(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation

Autor: Aiko Masuko, Hiroyuki Sugiyama, Fumihito Ushiyama, Harumi Kanazawa, Koichiro Nakano, Norikazu Ohtake, Masashi Mima, Kosuke Hitaka, Hideaki Amada, Takeuchi Tomoki, Nozomi Tanaka-Yamamoto, Kunihiko Iwamoto, Iichiro Takata

Publikováno v: ACS Omega
ACS Omega, Vol 5, Iss 17, Pp 10145-10159 (2020)

DNA gyrase and topoisomerase IV are well-validated pharmacological targets, and quinolone antibacterial drugs are marketed as their representative inhibitors. However, in recent years, resistance to these existing drugs has become a problem, and new

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7ab8f6fd6bd3f2be8c5a152b9adb049
https://doi.org/10.1021/acsomega.0c00865

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Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity

Publikováno v: Journal of medicinal chemistry. 63(23)

UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes the first committed step in the biosynthesis of Lipid A, an essential component of the cell envelope of Gram-negative bacteria. The most advanced, disclosed Lp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::019ee8a95fea26f38a355f0054fb803d
https://pubmed.ncbi.nlm.nih.gov/33210531

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Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors

Autor: Mayumi Endo, Hideaki Amada, Masafumi Kamitani, Takeuchi Tomoki, Norikazu Ohtake, Yunoshin Tamura, Aiko Masuko, Nozomi Tanaka-Yamamoto, Hiroyuki Sugiyama, Fumihito Ushiyama, Yasuhiro Mihara, Kosuke Hitaka, Iichiro Takata, Reiko Wada, Masashi Mima

Publikováno v: Bioorganicmedicinal chemistry. 28(22)

The global increase in multidrug-resistant pathogens has caused severe problems in the treatment of infections. To overcome these difficulties, the advent of a new chemical class of antibacterial drug is eagerly desired. We aimed at creating novel an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c778902e9c7dd887132f2d7e97ce1d0
https://pubmed.ncbi.nlm.nih.gov/33032189

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