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Characterization of a novel inhibitor of cytosolic phospholipase A2α, pyrrophenone

Autor: Takashi ONO, Katsutoshi YAMADA, Yukiko CHIKAZAWA, Masahiko UENO, Shozo NAKAMOTO, Takayuki OKUNO, Kaoru SENO

Publikováno v: Biochemical Journal. 363:727-735

Cytosolic phospholipase A2α (cPLA2α), one of the three subtypes of cPLA2 (α, β and γ), is thought to be a rate-limiting enzyme in eicosanoid biosynthesis. We developed a novel and potent cPLA2α inhibitor with an optically active pyrrolidine, te

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::67d4ec071b2a7070621e26542d645954
https://doi.org/10.1042/bj3630727

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Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2

Autor: Yasushi Murakami, Katsutoshi Yamada, Shozo Nakamoto, Takayuki Okuno, Takashi Ono, Koichi Nishi, Kaoru Seno

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:587-590

We synthesized a potent and crystallized human cytosolic phospholipase A 2 α inhibitor, pyrrophenone ( 6 ) which inhibits the isolated enzyme with an IC 50 value of 4.2 nM. Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a243f366da431c00413aa257cfb3ff27
https://doi.org/10.1016/s0960-894x(01)00003-8

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Hepatic Rupture Resulting from Seat-belt Trauma During Car Crash. The Machanism of Breaking Stress on the Liver

Autor: Kaoru Seno, Tsuneyuki Itano, Kouhei Akagi, Shuji Seki, Hidehisa Iwamoto

Publikováno v: Nihon Kyukyu Igakukai Zasshi. 10:98-103

肝破壊応力(肝を損傷する最小外力)を測定し,自動車正面衝突事故で前列左側座席(助手席)のシートベルト(ベルト)が同席搭乗者の肝を損傷する場合を考察した。まず,肝と体壁の接触面で�

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ad2c17cfcf34867779f74f87d291bd9a
https://doi.org/10.3893/jjaam.10.98

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Synthesis and pharmacological properties of ureidomethylcarbamoylphenylketone derivatives. A new potent and subtype-selective nonpeptide CCK-B/gastrin receptor antagonist, S-0509

Autor: Ryuichi Kiyama, Yasuhiko Kanda, Susumu Kamata, Yasunobu Ishihara, Takeshi Shiota, Michio Ishikawa, Mayumi Shimamura, Toshiro Konoike, Koji Yoshimura, Nobuhiro Haga, Sanji Hagishita, Yasushi Murakami, Koji Abe, Kaoru Seno

Publikováno v: Bioorganic & Medicinal Chemistry. 5:1695-1714

A novel series of CCK-B/gastrin receptor antagonists—ureidomethylcarbamoylphenylketone derivatives—were designed, synthesized, and evaluated for activity. Structure-activity relationship studies revealed the importance of a carboxylic acid at sub

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a562eb2802c04ac1e31aeab3dcb98315
https://doi.org/10.1016/s0968-0896(97)00104-1

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Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists

Autor: Yasuyuki Kawanishi, Shoichi Ishihara, Tadahiko Tsushima, Mayumi Shimamura, Kaoru Seno, Noriko Shima, Masanori Miyagoshi, Yasunobu Ishihara, Sanji Hagishita, Michio Ishikawa

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:1427-1430

The chemical modification of the dual histamine H2 and gastrin receptor antagonists described in our preceding paper, particularly the modification of spacers as well as the alteration of their connecting bonds at the gastrin receptor antagonist site

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::136654fc15a9e67c9eff0e47b5294eeb
https://doi.org/10.1016/s0960-894x(96)00249-1

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Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists

Autor: Yasuyuki Kawanishi, Sanji Hagishita, Masanori Miyagoshi, Mayumi Shimamura, Tadahiko Tsushima, Shoichi Ishihara, Michio Ishikawa, Noriko Shima, Yasunobu Ishihara, Kaoru Seno

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:1421-1426

The joint type of hybrid molecules composed of two pharmacophore moieties taken from histamine H2 and gastrin receptor antagonists have been designed and synthesized to exhibit dual histamine H2 and gastrin receptor antagonistic activities. Here we r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5c8f8d957f46cc67dba5c4a59798119b
https://doi.org/10.1016/s0960-894x(96)00248-x

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ChemInform Abstract: Pyrrolidine Inhibitors of Human Cytosolic Phospholipase A2. Part 2. Synthesis of Potent and Crystallized 4-Triphenylmethylthio Derivative 'Pyrrophenone'

Autor: Yasushi Murakami, Koichi Nishi, Takashi Ono, Takayuki Okuno, Kaoru Seno, Katsutoshi Yamada, Shozo Nakamoto

Publikováno v: ChemInform. 32

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::197662ce796f3e6589e904ef15735ef6
https://doi.org/10.1002/chin.200126103

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Characterization of a novel inhibitor of cytosolic phospholipase A2alpha, pyrrophenone

Autor: Takashi, Ono, Katsutoshi, Yamada, Yukiko, Chikazawa, Masahiko, Ueno, Shozo, Nakamoto, Takayuki, Okuno, Kaoru, Seno

Publikováno v: The Biochemical journal. 363(Pt 3)

Cytosolic phospholipase A(2)alpha (cPLA(2)alpha), one of the three subtypes of cPLA(2) (alpha, beta and gamma), is thought to be a rate-limiting enzyme in eicosanoid biosynthesis. We developed a novel and potent cPLA(2)alpha inhibitor with an optical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2fc1fa159ace4a7688f8c580daa3a680
https://pubmed.ncbi.nlm.nih.gov/11964173

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