Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Hiroyuki Miyachi"'
Autor:
Kazuto Nunomura, Kenji Ishimoto, Syohei Fukuda, Takefumi Doi, Keisuke Tachibana, Ryotaro Tabata, Hiroyuki Miyachi, Tomohiro Yuzuriha, Bangzhong Lin, Tadayuki Kobayashi
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(16)
We previously reported that 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid derivative 6 is an agonist of human peroxisome proliferator-activated receptor alpha (hPPARα). Here, we prepared a series of 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid deri
Autor:
Erika Noro, Kyoko Shimizu, Akiko Saito-Hakoda, Hiroyuki Miyachi, Hiroki Shimada, Atsushi Yokoyama, Susumu Suzuki, Rehana Parvin, Akira Sugawara
Publikováno v:
PPAR Research, Vol 2018 (2018)
Although therapeutic effects of the peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists rosiglitazone and pioglitazone against Cushing’s disease have been reported, their effects are still controversial and inconsistent. We therefor
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2639-2644
We designed and synthesized acylsulfonamide derivative (3) as a human peroxisome proliferator-activated receptor gamma (hPPARγ) partial agonist by structural modification of hPPARγ full agonist 1. Co-crystallization of 3 with hPPARγ LBD afforded a
Autor:
Minoru Waki, Takuji Oyama, Masao Ohashi, Hiroyuki Miyachi, Yuta Tanaka, Nobuyasu Matsuura, Kenji Matsuno, Hiroaki Tokiwa, Kanae Gamo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4001-4005
We previously reported that a α-benzylphenylpropanoic acid-type hPPARγ-selective agonist with a piperidine ring as the hydrophobic tail part (3) exhibited sub-micromolar-order hPPARγ agonistic activity. In order to enhance the activity, we planned
Autor:
Nobuyasu Matsuura, Yukihiro Akao, Nobuyuki Takahashi, Teruo Kawada, Hiroyuki Miyachi, Kanae Gamo, Munekazu Iinuma, Hideki Tosa
Publikováno v:
Bioscience, Biotechnology, and Biochemistry. 77:2430-2435
We tested the peroxisome proliferator-activated receptor (PPAR)δ agonistic activity of a Garcinia mangostana pericarp extract to develop a treatment for the metabolic syndrome, and demonstrated γ-mangostin to be an active compound on the basis of a
Autor:
Takuji Oyama, Ken Kataoka, Masao Ohashi, Nam Ho Huh, Masakazu Yashiro, Hiromi Nobusada, Kenji Matsuno, Hiroyuki Miyachi, Tsuyoshi Waku, Kosuke Morikawa, Endy Widya Putranto
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:2319-2332
In the continuing study directed toward the development of peroxisome proliferator-activated receptor gamma (hPPARγ) agonist, we attempted to improve the water solubility of our previously developed hPPARγ-selective agonist 3, which is insufficient
Autor:
Makoto Makishima, Hiromi Nobusada, Izumi Nakagome, Shuichi Hirono, Yuichi Hashimoto, Kenji Matsuno, Jun Ichi Kasuga, Hiroyuki Miyachi, Masao Ohashi
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:6375-6383
We previously demonstrated that the α-benzylphenylpropanoic acid-type PPARγ-selective agonist 6 exhibited a reversed stereochemistry-activity relationship, that is, the (R)-enantiomer is a more potent PPARγ agonist than the (S)-enantiomer, compare
Autor:
Tomomi Noguchi-Yachide, Yusuke Mita, Minoru Ishikawa, Hiroyuki Miyachi, Yuichi Hashimoto, Kosuke Dodo, Makoto Makishima
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1712-1717
Suppression of vitamin D receptor (VDR)-mediated transcription is expected be of therapeutic value in Paget's disease. Once an agonist activates VDR, recruitment of additional coactivator proteins is essential for transcription. Neither non-secostero
Autor:
Kenji Toyota, Hiroyuki Miyachi, Naoko Nagasawa, Takuji Oyama, Yuko Hirakawa, Yuichi Hashimoto, Kosuke Morikawa, Jun Ichi Kasuga, Tsuyoshi Waku
Publikováno v:
Acta Crystallographica Section D: Biological Crystallography
The structures of the ligand-binding domains (LBDs) of human peroxisome proliferator-activated receptors (PPARα, PPARγ and PPARδ) in complexes with a pan agonist, an α/δ dual agonist and a PPARδ-specific agonist were determined. The results exp
Autor:
Shuichi Hirono, Makoto Makishima, Atsushi Aoyama, Hiroyuki Miyachi, Takuji Oyama, Yuichi Hashimoto, Kosuke Morikawa, Jun Ichi Kasuga, Kumiko Sako, Izumi Nakagome
Publikováno v:
YAKUGAKU ZASSHI. 129:709-718
A series of 3-(4-alkoxypheny)propanoic acid derivatives was prepared as candidate peroxisome proliferator-activated receptor (PPAR) delta-selective agonists, based on our previously discovered potent human PPARalpha/delta dual agonist TIPP-401 as a l