Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Kei Takedomi"'
Autor:
Daisuke Iijima, Hiroshi Sugama, Yoichi Takahashi, Miki Hirai, Yuko Togashi, Jianshu Xie, Jingkang Shen, Ying Ke, Hidenori Akatsuka, Takayuki Kawaguchi, Kei Takedomi, Akiko Kashima, Masashi Nishio, Yosuke Inui, Hikaru Yoneda, Guangxin Xia, Toru Iijima
Publikováno v:
Journal of Medicinal Chemistry. 65:10882-10897
Renin is the rate-limiting enzyme in the renin-angiotensin-aldosterone system (RAAS) which regulates blood pressure and renal function and hence is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. However, the
Autor:
Toru Iijima, Makoto Katoh, Kei Takedomi, Yasuo Yamamoto, Hidenori Akatsuka, Naritoshi Shirata, Akito Nishi, Misae Takakuwa, Yoshinori Watanabe, Hitomi Munakata, Naomi Koyama, Tomoko Ikeda, Taku Iguchi, Harutoshi Kato, Kohei Kikkawa, Takayuki Kawaguchi
Publikováno v:
Journal of Medicinal Chemistry. 65:8127-8143
Overactivation of the mineralocorticoid receptor (MR) is involved in many diseases, such as hypertension, kidney disease, and heart failure. Thus, MR antagonists (MRAs) are expected to be beneficial to patients with these diseases. In order to identi
Publikováno v:
Journal of Chemical Information and Modeling. 61:3583-3592
The mineralocorticoid receptor (MR) is a nuclear receptor whose endogenous ligands are mineralocorticoids, a type of steroid hormone. The activating S810L mutation is known to cause severe early-onset and pregnancy-related hypertension. Progesterone
Autor:
Daisuke Iijima, Hiroshi Sugama, Nobumasa Awai, Yoichi Takahashi, Yuko Togashi, Tohru Takebe, Jianshu Xie, Jingkang Shen, Ying Ke, Hidenori Akatsuka, Takayuki Kawaguchi, Kei Takedomi, Akiko Kashima, Masashi Nishio, Yosuke Inui, Hikaru Yoneda, Guangxin Xia, Toru Iijima
Publikováno v:
ACS medicinal chemistry letters. 13(8)
The renin-angiotensin-aldosterone system (RAAS) plays a key role in the regulation of blood pressure. Renin, the first and rate-limiting enzyme of the RAAS, is an attractive target for the treatment of hypertension and cardiovascular/renal diseases.
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
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
Autor:
Yoichi, Kadoh, Haruko, Miyoshi, Takehiko, Matsumura, Yoshihito, Tanaka, Mitsuya, Hongu, Mayumi, Kimura, Kei, Takedomi, Kenji, Omori, Jun, Kotera, Takashi, Sasaki, Tamaki, Kobayashi, Hiroyuki, Taniguchi, Yumi, Watanabe, Koki, Kojima, Toshiaki, Sakamoto, Toshiyuki, Himiyama, Eiji, Kawanishi
Publikováno v:
Chemicalpharmaceutical bulletin. 66(3)
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
Publikováno v:
Biophysical Chemistry. :119-126
Accurate methods to predict the binding affinities of compounds for target molecules are powerful tools in structure-based drug design (SBDD). A recently developed method called massively parallel computation of absolute binding free energy with a we
Autor:
Tsuyoshi Ogiku, James Zapf, Shao-Hui Zhang, Kui Xu, Kei Takedomi, Naoki Sakurai, Guang Yang, Rick Jack, Jie-Fei Cheng, Miguel Barbosa, Chiaki Fukushima
Publikováno v:
Journal of Medicinal Chemistry. 51:2057-2061
We conducted virtual docking studies using GLIDE with modified LXRbeta ligand-binding domain (LBD) on internal compound collection followed by the gene profiling with ArrayPlate mRNA assay. A total of 69 compounds were found to upregulate LXRalpha an
Autor:
Ila Sircar, Chiaki Fukushima, Lisa Schneider, James Zapf, Madhavi Pannala, Lisa Morera, Trang Nguyen, Jie-Fei Cheng, Rick Jack, Norma Wilson, Shao-Hui Zhang, Kui Xu, Farid Bakir, Juping Liu, Kei Takedomi, Naoki Sakurai, Sunil Kher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3473-3479
A structurally novel liver X receptor (LXR) agonist (1) was identified from internal compound collection utilizing the combination of structure-based virtual screening and high-throughput gene profiling. Compound 1 increased ABCA1 gene expression by