Search Results - "Tamura, Yunoshin"

Design and Synthesis of 2-(1-Alkylaminoalkyl)pyrazolo[1,5-a]pyrimidines as New Respiratory Syncytial Virus Fusion Protein Inhibitors by Yamaguchi-Sasaki, Toru, Tamura, Yunoshin, Ogata, Yuya, Kawaguchi, Takanori, Kurosaka, Jun, Sugaya, Yutaka, Iwakiri, Kanako, Busujima, Tsuyoshi, Takahashi, Ryo, Ueda-Yonemoto, Naoko, Tanigawa, Eiji, Abe-Kumasaka, Tomoko, Sugiyama, Hiroyuki, Kanuma, Kosuke

“…Respiratory syncytial virus (RSV) is one of the most common causes of lower respiratory tract infections and a significant pathogen for both adults and…”
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Unique structure of ozoralizumab, a trivalent anti-TNFα NANOBODY ® compound, offers the potential advantage of mitigating the risk of immune complex-induced inflammation by Kyuuma, Masanao, Kaku, Ayaka, Mishima-Tsumagari, Chiemi, Ogawa, Bunichiro, Endo, Mayumi, Tamura, Yunoshin, Ishikura, Kei-Ichiro, Mima, Masashi, Nakanishi, Yutaka, Fujii, Yasuyuki

“…Biologics have become an important component of treatment strategies for a variety of diseases, but the immunogenicity of large immune complexes (ICs) and…”
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Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide by Futamura, Aya, Nozawa, Dai, Araki, Yuko, Tamura, Yunoshin, Tokura, Seiken, Kawamoto, Hiroshi, Tokumaru, Yuichi, Kakihara, Sora, Aoki, Takeshi, Ohtake, Norikazu

“…[Display omitted] The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective…”
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Molecular Dynamics Unveils Multiple-Site Binding of Inhibitors with Reduced Activity on the Surface of Dihydrofolate Reductase by Araki, Mitsugu, Ekimoto, Toru, Takemura, Kazuhiro, Matsumoto, Shigeyuki, Tamura, Yunoshin, Kokubo, Hironori, Bekker, Gert-Jan, Yamane, Tsutomu, Isaka, Yuta, Sagae, Yukari, Kamiya, Narutoshi, Ikeguchi, Mitsunori, Okuno, Yasushi

“…The sensitivity to protein inhibitors is altered by modifications or protein mutations, as represented by drug resistance. The mode of stable drug binding to…”
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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 by Takeuchi, Tomoki, Nomura, Yusaku, Tamita, Tomoko, Nishikawa, Rie, Kakinuma, Hiroyuki, Kojima, Naoki, Hitaka, Kosuke, Tamura, Yunoshin, Kamitani, Masafumi, Mima, Masashi, Nozoe, Akiko, Hayashi, Masato

“…Matrix metalloproteinase-2 (MMP2) is a zinc-dependent endopeptidase and a promising target for various diseases, including cancer and fibrosis. Herein, we…”
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Discovery of Highly Potent and Selective Matrix Metalloproteinase‑7 Inhibitors by Hybridizing the S1′ Subsite Binder with Short Peptides by Tabuse, Hideaki, Abe-Sato, Kumi, Kanazawa, Harumi, Yashiro, Miyoko, Tamura, Yunoshin, Kamitani, Masafumi, Hitaka, Kosuke, Gunji, Emi, Mitani, Akiko, Kojima, Naoki, Oka, Yusuke

“…Matrix metalloproteinase-7 (MMP-7) has emerged as a protein playing important roles in both physiological and pathophysiological processes. Despite the growing…”
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Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia by Futamura, Aya, Suzuki, Ryo, Tamura, Yunoshin, Kawamoto, Hiroshi, Ohmichi, Mari, Hino, Noriko, Tokumaru, Yuichi, Kirinuki, Sora, Hiyoshi, Tetsuaki, Aoki, Takeshi, Kambe, Daiji, Nozawa, Dai

“…[Display omitted] Here, we present the design, synthesis, and SAR of dual orexin 1 and 2 receptor antagonists, which were optimized by balancing the…”
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Binding interaction of SGLT with sugar and thiosugar by the molecular dynamics simulation by Tamura, Yunoshin, Miyagawa, Hiroh, Yoshida, Tatsusada, Chuman, Hiroshi

“…The human sodium–glucose co-transporter 2 (hSGLT2) is a transporter responsible for reabsorption of glucose in the proximal convoluted tubule of the kidney…”
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Discovery of novel indole derivatives as potent and selective inhibitors of proMMP-9 activation by Nishikawa-Shimono, Rie, Kuwabara, Motoi, Fujisaki, Sho, Matsuda, Daisuke, Endo, Mayumi, Kamitani, Masafumi, Futamura, Aya, Nomura, Yusaku, Yamaguchi-Sasaki, Toru, Yabuuchi, Tetsuya, Yamaguchi, Chitose, Tanaka-Yamamoto, Nozomi, Satake, Shunya, Abe-Sato, Kumi, Funayama, Kosuke, Sakata, Mayumi, Takahashi, Shinji, Hirano, Koga, Fukunaga, Takuya, Uozumi, Yoriko, Kato, Sayaka, Tamura, Yunoshin, Nakamori, Tomoaki, Mima, Masashi, Mishima-Tsumagari, Chiemi, Nozawa, Dai, Imai, Yudai, Asami, Taiji

“…[Display omitted] •HTS of our internal compound library led to the discovery of two hit compounds.•The two hit compounds were merged to provide a lead with…”
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Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors by Ushiyama, Fumihito, Amada, Hideaki, Mihara, Yasuhiro, Takeuchi, Tomoki, Tanaka-Yamamoto, Nozomi, Mima, Masashi, Kamitani, Masafumi, Wada, Reiko, Tamura, Yunoshin, Endo, Mayumi, Masuko, Aiko, Takata, Iichiro, Hitaka, Kosuke, Sugiyama, Hiroyuki, Ohtake, Norikazu

“…[Display omitted] The global increase in multidrug-resistant pathogens has caused severe problems in the treatment of infections. To overcome these…”
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Binding Free-Energy Calculation Is a Powerful Tool for Drug Optimization: Calculation and Measurement of Binding Free Energy for 7‑Azaindole Derivatives to Glycogen Synthase Kinase-3β by Kitamura, Kunihiro, Tamura, Yunoshin, Ueki, Tomokazu, Ogata, Koji, Noda, Shigeho, Himeno, Ryutaro, Chuman, Hiroshi

“…Present computational lead (drug)-optimization is lacking in thermodynamic tactics. To examine whether calculation of binding free-energy change (ΔG) is…”
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Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors by Oka, Yusuke, Yabuuchi, Tetsuya, Fujii, Yasuyuki, Ohtake, Hidenori, Wakahara, Shunichi, Matsumoto, Kayo, Endo, Mayumi, Tamura, Yunoshin, Sekiguchi, Yoshinori

“…Novel 2-aminothiazole-oxazoles were synthesized and evaluated as phosphoinositide 3-kinase γ (PI3Kγ) inhibitors. A novel series of 2-aminothiazole-oxazoles was…”
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Binding Free-Energy Calculation Is a Powerful Tool for Drug Optimization: Calculation and Measurement of Binding Free Energy for 7-Azaindole Derivatives to Glycogen Synthase Kinase-3[Beta] by Kitamura, Kunihiro, Tamura, Yunoshin, Ueki, Tomokazu, Ogata, Koji, Noda, Shigeho, Himeno, Ryutaro, Chuman, Hiroshi

“…Present computational lead (drug)-optimization is lacking in thermodynamic tactics. To examine whether calculation of binding free-energy change (...G) is…”
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Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase [gamma] inhibitors by Oka, Yusuke, Yabuuchi, Tetsuya, Fujii, Yasuyuki, Ohtake, Hidenori, Wakahara, Shunichi, Matsumoto, Kayo, Endo, Mayumi, Tamura, Yunoshin, Sekiguchi, Yoshinori

“…A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase [gamma] (PI3K[gamma])…”
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Thermoreversible gelation with hydrogen-bonded zipper-like crosslink junctions by Tamura, Yunoshin, Tanaka, Fumihiko

“…Thermoreversible gelation of polymer chains bearing hydrogen‐bonding functional groups is studied by off‐lattice Monte Carlo simulation with semiflexible…”
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