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Akademický článek

Inhibition of microRNA-33b specifically ameliorates abdominal aortic aneurysm formation via suppression of inflammatory pathways

Publikováno v: Scientific Reports, Vol 12, Iss 1, Pp 1-19 (2022)

Abstract Abdominal aortic aneurysm (AAA) is a lethal disease, but no beneficial therapeutic agents have been established to date. Previously, we found that AAA formation is suppressed in microRNA (miR)-33-deficient mice compared with wild-type mice.

Externí odkaz: https://doaj.org/article/445284dacf4046649dd1ebec40553f4f

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Altered Biodistribution and Hepatic Safety Profile of a Gapmer Antisense Oligonucleotide Bearing Guanidine-Bridged Nucleic Acids

Autor: Takashi Sasaki, Yoko Hirakawa, Fumiko Yamairi, Takashi Kurita, Karin Murahashi, Hirokazu Nishimura, Norihiko Iwazaki, Hidenori Yasuhara, Takashi Tateoka, Tetsuya Ohta, Satoshi Obika, Jun Kotera

Publikováno v: Nucleic acid therapeutics. 32(3)

Guanidine-bridged nucleic acid (GuNA) is a novel 2',4'-bridged nucleic acid/locked nucleic acid (2',4'-BNA/LNA) analog containing cations that exhibit strong affinity for target RNA and superior nuclease resistance. In this study

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b4d0cd122d69e3c02cbbee2d49e891be
https://pubmed.ncbi.nlm.nih.gov/35073217

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Discovery of 2-[(E)-2-(7-Fluoro-3-methylquinoxalin-2-yl)vinyl]-6-pyrrolidin-1-yl-N-(tetrahydro-2H-pyran-4-yl)pyrimidin-4-amine Hydrochloride as a Highly Selective PDE10A Inhibitor

Autor: Kei Takedomi, Eiji Kawanishi, Yumi Watanabe, Mayumi Kimura, Koki Kojima, Yoichi Kadoh, Yoshihito Tanaka, Takehiko Matsumura, Kenji Omori, Tamaki Kobayashi, Toshiaki Sakamoto, Haruko Miyoshi, Jun Kotera, Toshiyuki Himiyama, Mitsuya Hongu, Takashi Sasaki, Hiroyuki Taniguchi

Publikováno v: Chemical and Pharmaceutical Bulletin. 66:243-250

Phosphodiesterase (PDE) 10A is a dual hydrolase of cAMP and cGMP and highly expressed in striatal medium spiny neurons. Inhibition of PDE10A modulates the activity of medium spiny neurons (MSN) via the regulation of cAMP and cGMP. Signal control of M

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e6843e881235274aefe3a3c26a35ba5a
https://doi.org/10.1248/cpb.c17-00783

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Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety

Autor: Takehiko Matsumura, Hiroyuki Taniguchi, Takashi Sasaki, Misae Takakuwa, Haruko Miyoshi, Yoichi Kadoh, Eiji Kawanishi, Mitsuya Hongu, Yoshihito Tanaka, Yumi Watanabe, Kei Takedomi, Nobuyuki Baba, Yuuki Koizumi, Jun Kotera, Koki Kojima, Itsuko Nakamura

Publikováno v: Bioorganicmedicinal chemistry. 27(15)

We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene struct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bd08f7ec18e9eee0e29fcebbf425ca7
https://pubmed.ncbi.nlm.nih.gov/31235264

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12-oxo-phytodienoic acid, a plant-derived oxylipin, attenuates lipopolysaccharide-induced inflammation in microglia

Autor: Hiroyuki Ohta, Jun Kotera, Nozomi Taki-Nakano

Publikováno v: Biochemical and Biophysical Research Communications. 473(4):1288-1294

Jasmonates are plant lipid–derived oxylipins that act as key signaling compounds in plant immunity, germination, and development. Although some physiological activities of natural jasmonates in mammalian cells have been investigated, their anti-inf

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6343a48a8bf0ea8309ebcc3303b91c7

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Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: Scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation

Autor: Kenji Matsuki, Masataka Hikota, Toshiaki Sakamoto, Koichiro Yamada, Hiroshi Morimoto, Jun Kotera, Michino Murakami, Kenji Omori, Yuichi Koga, Kohei Kikkawa, Kotomi Fujishige

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:5175-5180

5-(3,4,5-Trimethoxybenzoyl)-4-amimopyrimidine derivatives were found as a novel chemical class of potent and highly selective phosphodiesterase 5 inhibitors. A pseudo-ring formed by an intramolecular hydrogen bond constrained the conformation of 3-ch

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d30b83a518dc8e25821e74f434afe84
https://doi.org/10.1016/j.bmcl.2014.09.082

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