Kuniya Sakurai

Tu1864 A Novel Orally Active Phosphatidylinositol 3-Phosphate 5-Kinase (Pikfyve) Inhibitor Ameliorates Mouse Colitis by Inhibition of IL-12 and IL-23 Production From Macrophages

A Novel Orally Active Phosphatidylinositol 3-Phosphate 5-Kinase (Pikfyve) Inhibitor Ameliorates Mouse Colitis by Inhibition of IL-12 and IL-23 Production From Macrophages Ayatoshi Andou, Takashi Yamamoto, Eviryanti Agung, Yukie Seki, Hikaru Nishio, Manami Shuto, Misato Noguchi, Yoichiro Shima, Sen Takeshita, Ryohei Yokoyama, Nobuhiko Hayakawa, Masatsugu Noguchi, Shunsuke Kageyama, Hiroyuki Eda, Makoto Shiozaki, Itsuya Tanabe, Ryusuke Nakagawa, Kuniya Sakurai, Shoji Masataka

Pharmacophore Model of Endothelin Antagonists

Endothelin (ET) is a 21-amino acid peptide, and its receptor belongs to a family of Gprotein-coupled receptor. ET antagonist is expected to be a therapeutic agent for disease including myocardinal infarction, hypertension and restenosis. In an attempt to design new antagonists we have created a pharmacophore model using active antagonists with the consideration of conformational flexibility of molecules in which DISCO was applied. A new hydrogen bond donor site was identified in the model, and was utilized successfully in the design of highly active antagonists.