Search Results - "Kurasawa, Osamu"

Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response by Nakamura, Akito, Nambu, Tadahiro, Ebara, Shunsuke, Hasegawa, Yuka, Toyoshima, Kosei, Tsuchiya, Yasuko, Tomita, Daisuke, Fujimoto, Jun, Kurasawa, Osamu, Takahara, Chisato, Ando, Ayumi, Nishigaki, Ryuichi, Satomi, Yoshinori, Hata, Akito, Hara, Takahito

“…General control nonderepressible 2 (GCN2) plays a major role in the cellular response to amino acid limitation. Although maintenance of amino acid homeostasis…”
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Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase by Tanaka, Yuta, Kurasawa, Osamu, Yokota, Akihiro, Klein, Michael G, Ono, Koji, Saito, Bunnai, Matsumoto, Shigemitsu, Okaniwa, Masanori, Ambrus-Aikelin, Geza, Morishita, Daisuke, Kitazawa, Satoshi, Uchiyama, Noriko, Ogawa, Kazumasa, Kimura, Hiromichi, Imamura, Shinichi

“…Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor…”
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Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine Fumarate (TAK-438) as a Potassium-Competitive Acid Blocker (P-CAB) by Arikawa, Yasuyoshi, Nishida, Haruyuki, Kurasawa, Osamu, Hasuoka, Atsushi, Hirase, Keizo, Inatomi, Nobuhiro, Hori, Yasunobu, Matsukawa, Jun, Imanishi, Akio, Kondo, Mitsuyo, Tarui, Naoki, Hamada, Teruki, Takagi, Terufumi, Takeuchi, Toshiyuki, Kajino, Masahiro

“…In our pursuit of developing a novel and potent potassium-competitive acid blocker (P-CAB), we synthesized pyrrole derivatives focusing on compounds with low…”
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Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones by Kurasawa, Osamu, Oguro, Yuya, Miyazaki, Tohru, Homma, Misaki, Mori, Kouji, Iwai, Kenichi, Hara, Hideto, Skene, Robert, Hoffman, Isaac, Ohashi, Akihiro, Yoshida, Sei, Ishikawa, Tomoyasu, Cho, Nobuo

“…[Display omitted] Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic…”
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Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor by Iwai, Kenichi, Nambu, Tadahiro, Dairiki, Ryo, Ohori, Momoko, Yu, Jie, Burke, Kristine, Gotou, Masamitsu, Yamamoto, Yukiko, Ebara, Shunsuke, Shibata, Sachio, Hibino, Ryosuke, Nishizawa, Satoru, Miyazaki, Tohru, Homma, Misaki, Oguro, Yuya, Imada, Takashi, Cho, Nobuo, Uchiyama, Noriko, Kogame, Akifumi, Takeuchi, Toshiyuki, Kurasawa, Osamu, Yamanaka, Kazunori, Niu, Huifeng, Ohashi, Akihiro

“…Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation…”
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Discovery, synthesis, and biological evaluation of novel pyrrole derivatives as highly selective potassium-competitive acid blockers by Nishida, Haruyuki, Hasuoka, Atsushi, Arikawa, Yasuyoshi, Kurasawa, Osamu, Hirase, Keizo, Inatomi, Nobuhiro, Hori, Yasunobu, Sato, Fumihiko, Tarui, Naoki, Imanishi, Akio, Kondo, Mitsuyo, Takagi, Terufumi, Kajino, Masahiro

“…To discover a gastric antisecretory agent more potent than existing proton pump inhibitors, novel pyrrole derivatives were synthesized, and their H+,K+-ATPase…”
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A CDC7 inhibitor sensitizes DNA-damaging chemotherapies by suppressing homologous recombination repair to delay DNA damage recovery by Iwai, Kenichi, Nambu, Tadahiro, Kashima, Yukie, Yu, Jie, Eng, Kurt, Miyamoto, Kazumasa, Kakoi, Kazuyo, Gotou, Masamitsu, Takeuchi, Toshiyuki, Kogame, Akifumi, Sappal, Jessica, Murai, Saomi, Haeno, Hiroshi, Kageyama, Shun-Ichiro, Kurasawa, Osamu, Niu, Huifeng, Kannan, Karuppiah, Ohashi, Akihiro

“…Cell division cycle 7 (CDC7), a serine/threonine kinase, plays important roles in DNA replication. We developed a highly specific CDC7 inhibitor, TAK-931, as a…”
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Using a biologically annotated library to analyze the anticancer mechanism of serine palmitoyl transferase (SPT) inhibitors by Sano, Osamu, Kazetani, Ken‐ichi, Adachi, Ryutaro, Kurasawa, Osamu, Kawamoto, Tomohiro, Iwata, Hidehisa

“…Mechanistic understanding is crucial to anticancer drug discovery. Here, we reveal that inhibition of serine palmitoyl transferase (SPT), the rate‐limiting…”
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CCR5 Antagonists as Anti-HIV-1 Agents. 1. Synthesis and Biological Evaluation of 5-Oxopyrrolidine-3-carboxamide Derivatives by Imamura, Shinichi, Ishihara, Yuji, Hattori, Taeko, Kurasawa, Osamu, Matsushita, Yoshihiro, Sugihara, Yoshihiro, Kanzaki, Naoyuki, Iizawa, Yuji, Baba, Masanori, Hashiguchi, Shohei

“…A novel lead compound, N-{3-[4-(4-fluorobenzoyl)piperidin-1-yl]propyl}-1-methyl-5-oxo-N-phenylpyrrolidine-3-carboxamide (1), was identified as a CCR5…”
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CCR5 antagonists as anti-HIV-1 agents. Part 2: Synthesis and biological evaluation of N-[3-(4-benzylpiperidin-1-yl)propyl]- N, N′-diphenylureas by Imamura, Shinichi, Kurasawa, Osamu, Nara, Yoshi, Ichikawa, Takashi, Nishikawa, Youichi, Iida, Takehiro, Hashiguchi, Shohei, Kanzaki, Naoyuki, Iizawa, Yuji, Baba, Masanori, Sugihara, Yoshihiro

“…Graphic We have previously reported the novel lead compound 1a as a CCR5 antagonist for treatment of HIV-1 infection. SAR studies on incorporating various acyl…”
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Synthesis and Properties of Oligonucleotides Having a Phosphorus Chiral Center by Incorporation of Conformationally Rigid 5‘-Cyclouridylic Acid Derivatives by Sekine, Mitsuo, Kurasawa, Osamu, Shohda, Koh-ichiroh, Seio, Kohji, Wada, Takeshi

“…This paper describes the design and synthesis of a conformationally rigid dimer building block Umpc3Um as a chiral center at the phosphate group with the S/N…”
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Discovery of a Novel, Highly Potent, and Selective Thieno[3,2‑d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent by Kurasawa, Osamu, Miyazaki, Tohru, Homma, Misaki, Oguro, Yuya, Imada, Takashi, Uchiyama, Noriko, Iwai, Kenichi, Yamamoto, Yukiko, Ohori, Momoko, Hara, Hideto, Sugimoto, Hiroshi, Iwata, Kentaro, Skene, Robert, Hoffman, Isaac, Ohashi, Akihiro, Nomura, Toshiyuki, Cho, Nobuo

“…In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported…”
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Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents by Kojima, Takuto, Asano, Yasutomi, Kurasawa, Osamu, Hirata, Yasuhiro, Iwamura, Naoki, Wong, Tzu-Tshin, Saito, Bunnai, Tanaka, Yuta, Arai, Ryosuke, Yonemori, Kazuko, Miyamoto, Yasufumi, Sagiya, Yoji, Yaguchi, Masahiro, Shibata, Sachio, Mizutani, Akio, Sano, Osamu, Adachi, Ryutaro, Satomi, Yoshinori, Hirayama, Megumi, Aoyama, Kazunobu, Hiura, Yuto, Kiba, Atsushi, Kitamura, Shuji, Imamura, Shinichi

“…[Display omitted] We pursued serine palmitoyltransferase (SPT) inhibitors as novel cancer therapeutic agents based on a correlation between SPT inhibition and…”
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New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase by Tanaka, Yuta, Kurasawa, Osamu, Yokota, Akihiro, Klein, Michael G, Saito, Bunnai, Matsumoto, Shigemitsu, Okaniwa, Masanori, Ambrus-Aikelin, Geza, Uchiyama, Noriko, Morishita, Daisuke, Kimura, Hiromichi, Imamura, Shinichi

“…Deoxyhypusine synthase (DHPS) is the primary enzyme responsible for the hypusine modification and, thereby, activation of the eukaryotic translation initiation…”
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Abstract 3073: Potential predictive biomarkers of clinical responses for a novel CDC7-selective inhibitor TAK-931 by Iwai, Kenichi, Nambu, Tadahiro, Kurasawa, Osamu, Uchiyama, Noriko, Dairiki, Ryo, Yamamoto, Yukiko, Nishizawa, Satoru, Zhang, Mengkun, Ishii, Yuko, Niu, Huifeng, Ohashi, Akihiro

“…Abstract Cell division cycle 7 (CDC7) is a serine/threonine kinase, which plays important roles in initiation of DNA replication by phosphorylating MCM2…”
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Abstract 3847: Inhibition of GCN2 sensitizes ASNS-downregulated cancer cells to asparaginase by disrupting amino acid response by Nakamura, Akito, Nambu, Tadahiro, Ebara, Shunsuke, Hasegawa, Yuka, Toyoshima, Kosei, Tsuchiya, Yasuko, Tomita, Daisuke, Fujimoto, Jun, Kurasawa, Osamu, Takahara, Chisato, Kawamura, Ayumi, Nishigaki, Ryuichi, Satomi, Yoshinori, Hata, Akito, Hara, Takahito

“…Abstract General control nonderepressible 2 (GCN2) plays a major role in cellular response to amino acid limitation. Although maintenance of amino acid…”
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Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode by Fujimoto, Jun, Kurasawa, Osamu, Takagi, Terufumi, Liu, Xin, Banno, Hiroshi, Kojima, Takuto, Asano, Yasutomi, Nakamura, Akito, Nambu, Tadahiro, Hata, Akito, Ishii, Tsuyoshi, Sameshima, Tomoya, Debori, Yasuyuki, Miyamoto, Maki, Klein, Michael G, Tjhen, Richard, Sang, Bi-Ching, Levin, Irena, Lane, Scott Weston, Snell, Gyorgy P, Li, Ke, Kefala, Georgia, Hoffman, Isaac D, Ding, Steve C, Cary, Douglas R, Mizojiri, Ryo

“…General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor…”
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2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase by Kurasawa, Osamu, Homma, Misaki, Oguro, Yuya, Miyazaki, Tohru, Mori, Kouji, Uchiyama, Noriko, Iwai, Kenichi, Ohashi, Akihiro, Hara, Hideto, Yoshida, Sei, Cho, Nobuo

“…[Display omitted] In order to increase the success rate for developing new Cdc7 inhibitors for cancer therapy, we explored a new chemotype which can comply…”
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Synthesis and Properties of Oligodeoxynucleotides Incorporating a Conformationally Rigid Uridine Unit Having a Cyclic Structure at the 5‘-Terminal Site by Sekine, Mitsuo, Kurasawa, Osamu, Shohda, Koh-ichiroh, Seio, Kohji, Wada, Takeshi

“…A 2‘-O-methyluridylic acid derivative 3 having a cyclic structure linked between the 5-position of the uracil residue and the 5‘-phosphate group was…”
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Essential Factors for Stabilization of the Predominant C3′-endo Conformation in Dinucleoside Phosphotriester Derivatives with Cyclonucleotide Bridge Structures at the Downstream 3′-Position by Sekine, Mitsuo, Kurasawa, Osamu, Shohda, Koh-ichiroh, Seio, Kohji, Wada, Takeshi

“…This paper describes the synthesis of conformationally constrained dinucleoside cyclic phosphotriester derivatives and related compounds, such as Tpc3Um (2),…”
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