Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Takeshi Shigenaga"'
Autor:
Yuzo Matsumoto, Yuji Koga, Norio Seki, Kenichi Mori, Tsukasa Ishihara, Yumiko Moritani, Ryouta Shiraki, Takeshi Kadokura, Yoshiyuki Iwatsuki, Shuichi Sakamoto, Takeshi Shigenaga, Hiroyuki Koshio, Keizo Sugasawa, Shunichiro Hachiya, Fukushi Hirayama, Shin-ichi Tsukamoto, Tomihisa Kawasaki
Publikováno v:
Journal of Medicinal Chemistry. 54:8051-8065
Inhibitors of factor Xa (FXa), a crucial serine protease in the coagulation cascade, have attracted a great deal of attention as a target for developing antithrombotic agents. We previously reported findings from our optimization study of a high-thro
Autor:
Tatsuya Niimi, Tsukasa Ishihara, Shuichi Sakamoto, Yumiko Sakai-Moritani, Fukushi Hirayama, Mitsuaki Ohta, Takeshi Shigenaga, Shin-ichi Tsukamoto, Masanori Miura, Norio Seki, Tomihisa Kawasaki, Takanori Koike, Minoru Okada
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:7688-7705
Inhibition of tissue factor/factor VIIa complex (TF/FVIIa) is an attractive strategy for antithrombotic therapies. We began with an investigation of a non-amidine TF/FVIIa inhibitor based on a modification of amidine compound 1. Optimization of the s
Autor:
Kazuo Sato, Naoko Katayama, Tsukasa Ishihara, Yuzo Matsumoto, Yumiko Moritani, Fukushi Hirayama, Shin-ichi Tsukamoto, Yoshiyuki Iwatsuki, Shuichi Sakamoto, Hiroyuki Koshio, Tomihisa Kawasaki, Takeshi Shigenaga, Seiji Kaku, Yuta Taniuchi, Ryouta Shiraki
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:1305-1323
Factor Xa (fXa) is a serine protease that plays a pivotal role in the coagulation cascade. High-throughput screening of the Yamanouchi compound library yielded lead compound 1 with the ability to inhibit fXa at micromolar concentrations. To improve i
Autor:
Koji Nagai, Kazumi Hayashi, Tomihisa Kawasaki, Masatoshi Taniguchi, Toshio Uemura, Jun Takasaki, Tetsu Saito, Yumiko Moritani, Takeshi Shigenaga, Hajime Takamatsu
Publikováno v:
Thrombosis and Haemostasis. 94:184-192
SummaryThe pharmacological properties of YM-254890,a specific Gαq/11 inhibitor, on acute thrombosis and chronic neointima formation after vascular injury have been investigated. FeCl3 was used to induce vascular injury in the carotid artery of mice.
Autor:
Shin-ichi Tsukamoto, Fukushi Hirayama, Yuta Taniuchi, Tomihisa Kawasaki, Tsukasa Ishihara, Yumiko Moritani, Shuichi Sakamoto, Yoshiyuki Iwatsuki, Yuzo Matsumoto, Seiji Kaku, Hiroyuki Koshio, Takeshi Shigenaga, Kazuo Sato, Toshio Uemura, Hiroyuki Kaizawa
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:5415-5426
Factor Xa (fXa) is a serine protease, which plays a pivotal role in the coagulation cascade. To improve the oral anticoagulant activity of fXa inhibitors containing a 1,4-diazepane moiety as the P4 part, a prodrug strategy was examined. Among the com
Autor:
Tomioka Kenichi, Takeshi Shigenaga, Nami Hisamichi, Tomoko Nii, Ken-ichi Suzuki, Tomihisa Kawasaki, Isao Yanagisawa, Osamu Inagaki, Seiji Kaku, Yuzo Matsumoto, Kazuo Sato, Masato Ichihara, Yumiko Moritani, Seijiro Akamatsu
Publikováno v:
European Journal of Pharmacology. 439:43-52
The pharmacological properties of YM-57029 ({4-[4-(4-carbamimidoylphenyl)-3-oxopiperazin-1-yl]piperidino}acetic acid monohydrochloride trihydrate), a novel glycoprotein IIb/IIIa antagonist were examined in this study. YM-57029 inhibited fibrinogen bi
Autor:
Tomihisa Kawasaki, Kazuo Sato, Yumiko Moritani, Seiji Kaku, Hiroshi Arai, Ken-ichi Suzuki, Yuta Taniuchi, Yuzo Matsumoto, Isao Yanagisawa, Takeshi Shigenaga, Seijiro Akamatsu, Masato Ichihara, Tomoko Nii, Nami Hisamichi, Hiroshi Matsushima, Osamu Inagaki, Tomioka Kenichi
Publikováno v:
Drug Development Research. 55:149-161
We examined the biochemical properties of YM-57029 ({4-[4-(4-Carbamimidoylphenyl)-3-oxopiperazin-1-yl]piperidino}acetic acid monohydrochloride trihydrate) and the pharmacodynamics and pharmacokinetics of its prodrug, YM128 (Ethyl (Z)-(4-{4-[4-(N 2 -h
Autor:
Takeshi Shigenaga, Toshio Takagi, Junko Cho, Shun Ichiro Kawabata, Hiroshi Nakajima, Ranko Nagayama, Kishan Lal Agarwala, Sadaaki Iwanaga, Michimasa Hirata, Tetsu Saito
Publikováno v:
Journal of Biochemistry. 120:1253-1260
Small granules of horseshoe crab hemocytes contain two known major antimicrobial substances, tachyplesin and big defensin (S5), and at least five protein components (S1 to S6), with unknown functions. In the present study, we examined the biological
Autor:
Sadaaki Iwanaga, Junko Cho, Michimasa Hirata, Shun Ichiro Kawabata, Hiroshi Nakajima, Tetsu Saito, Takeshi Shigenaga, Yoko Takayenoki
Publikováno v:
The Journal of Biochemistry. 117:1131-1137
Hemocytes of the horseshoe crab (limulus) contain a family of arthropodous peptide antibiotics, termed the tachyplesin family, and antibacterial protein, called anti-LPS factor, of which the former is located in the small (S) granules and the latter
Autor:
Takeshi Shigenaga, Toshiyuki Funatsu, Mami Suzuki, Yoshiyuki Iwatsuki, Yumiko Moritani, Takayuki Sato, Tomihisa Kawasaki, Seiji Kaku
Publikováno v:
European journal of pharmacology. 673(1-3)
Darexaban (YM150) is an oral factor Xa inhibitor developed for the prophylaxis of venous and arterial thromboembolic disease. This study was conducted to investigate the biochemical and pharmacological profiles of darexaban and its active metabolite