Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Iichiro Kawahara"'
Publikováno v:
Pharmacology Research & Perspectives, Vol 8, Iss 1, Pp n/a-n/a (2020)
Abstract Prediction of the intestinal absorption of new chemical entities (NCEs) is still difficult, in part because drug efflux transporters, including breast cancer resistance protein (BCRP) and P‐glycoprotein (P‐gp), restrict their intestinal
Externí odkaz:
https://doaj.org/article/5ca6eb1b36c54e3cac1de9de03d207de
Autor:
Yusuke Kono, Iichiro Kawahara, Kohei Shinozaki, Ikuo Nomura, Honoka Marutani, Akira Yamamoto, Takuya Fujita
Publikováno v:
Pharmaceutics, Vol 13, Iss 3, p 388 (2021)
For developing oral drugs, it is necessary to predict the oral absorption of new chemical entities accurately. However, it is difficult because of the involvement of efflux transporters, including P-glycoprotein (P-gp), in their absorption process. I
Externí odkaz:
https://doaj.org/article/080201cf63014f8e9324f5c73e7659e5
Publikováno v:
Drug Metabolism and Disposition. 48:491-498
Breast cancer resistance protein (BCRP) is expressed on the apical membrane of small intestinal epithelial cells and functions as an efflux pump with broad substrate recognition. Therefore, quantitative evaluation of the contribution of BCRP to the i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc902ce21539197b186277680e916537
https://doi.org/10.1124/dmd.119.088674
https://doi.org/10.1124/dmd.119.088674
Autor:
Yasunori Hase, Kazutaka Ikegashira, Hiromasa Hashimoto, Takayuki Yamasaki, Iichiro Kawahara, Taku Ikenogami, Yoshihisa Koga, Koji Inagaki, Naoki Miyagawa, Takahiro Oka
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:873-877
Optimization of novel azetidine compounds, which we had found as colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors, provided JTE-952 as a clinical candidate with high cellular activity (IC50 = 20 nM) and good pharmacokinetics profile.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f442336db72895a98e9e75673b64cf0
https://doi.org/10.1016/j.bmcl.2019.02.006
https://doi.org/10.1016/j.bmcl.2019.02.006
Autor:
Takuya Fujita, Kohei Shinozaki, Iichiro Kawahara, Honoka Marutani, Yusuke Kono, Ikuo Nomura, Akira Yamamoto
Publikováno v:
Pharmaceutics
Pharmaceutics, Vol 13, Iss 388, p 388 (2021)
Volume 13
Issue 3
Pharmaceutics, Vol 13, Iss 388, p 388 (2021)
Volume 13
Issue 3
For developing oral drugs, it is necessary to predict the oral absorption of new chemical entities accurately. However, it is difficult because of the involvement of efflux transporters, including P-glycoprotein (P-gp), in their absorption process. I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::434c586f201b4561b134cbe32bd35ccd
https://doi.org/10.3390/pharmaceutics13030388
https://doi.org/10.3390/pharmaceutics13030388
Autor:
Hiroshi, Komura, Yukie, Shigemoto, Iichiro, Kawahara, Kenichi, Matsuda, Rieko, Ano, Yoko, Murayama, Toshiya, Moriwaki, Nagahiro H, Yoshida
Publikováno v:
YAKUGAKU ZASSHI. 125:141-147
Pharmacokinetic and metabolic screening plays an important role in the optimization of a lead compound in drug discovery. Since those screening methods are time-consuming and labor intensive, in silico models would be effective to select compounds an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17b974cf7019413e7d1e9feba13b76ff
https://doi.org/10.1248/yakushi.125.141
https://doi.org/10.1248/yakushi.125.141
Autor:
Hiroshi Komura, Toshiya Moriwaki, Rieko Ano, Yoko Murayama, Iichiro Kawahara, Yukie Shigemoto, Nagahiro Yoshida, Kenichi Matsuda
Publikováno v:
YAKUGAKU ZASSHI. 125:131-139
Metabolic screening using liver microsomes of rats and humans is an indispensable tool to optimize a lead structure and to select compounds for in vivo study. Elucidating the relationship between in vitro intrinsic clearance (CL(int, app)) and in viv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::312e1315b40dfe188a11569db6769241
https://doi.org/10.1248/yakushi.125.131
https://doi.org/10.1248/yakushi.125.131
Autor:
Shin-ichi Kanamitsu, Jun Aoki, Motohiro Kato, Yuko Tsukamoto, Yasumasa Gotoh, Kaoru Ueda, Takafumi Iwatsubo, Masato Horikawa, Michi Ishigami, Kiyomi Ito, Norihito Sato, Tomoo Itoh, Kayoko Niinuma, Yuichi Sugiyama, Akiko Nishino, Naomi Mizuno, Koji Chiba, Iichiro Kawahara
Publikováno v:
AAPS PharmSci. 4:53-60
When the metabolism of a drug is competitively or noncompetitively inhibited by another drug, the degree of in vivo interaction can be evaluated from the [I]u/Ki ratio, where [I]u is the unbound concentration around the enzyme and Ki is the inhibitio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df781e7d2272a32482e49ae4cad6fc27
https://doi.org/10.1208/ps040425
https://doi.org/10.1208/ps040425
Autor:
Kayo Takenaka, Akira Yamamoto, Takuya Fujita, Ying-Shu Quan, Koji Hattori, Iichiro Kawahara, Shozo Muranishi
Publikováno v:
Pharmaceutical Research. 15:1387-1392
Purpose. Three types of acyl tetragastrin (TG), acetyl-TG (C2-TG), butyryl-TG (C4-TG) and caproyl-TG (C6-TG) were synthesized and their in vitro intestinal permeability characteristics were examined using Caco-2 monolayers.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3af2e8e6717fbee46cb3d6c7fcef4c15
https://doi.org/10.1023/a:1011997404306
https://doi.org/10.1023/a:1011997404306
Autor:
Kono, Yusuke1 (AUTHOR) y-kono@fc.ritsumei.ac.jp, Kawahara, Iichiro2 (AUTHOR) iichiro.kawahara@jt.com, Shinozaki, Kohei2 (AUTHOR) ky02315@poppy.kyoto-phu.ac.jp, Nomura, Ikuo2 (AUTHOR) ky03243@poppy.kyoto-phu.ac.jp, Marutani, Honoka1 (AUTHOR) ph0107ih@ed.ritsumei.ac.jp, Yamamoto, Akira2 (AUTHOR) yamamoto@mb.kyoto-phu.ac.jp, Fujita, Takuya1 (AUTHOR) fujita-t@ph.ritsumei.ac.jp, Song, Im-Sook (AUTHOR)
Publikováno v:
Pharmaceutics. Mar2021, Vol. 13 Issue 3, p388-388. 1p.