Evaluation of pharmacokinetics/pharmacodynamics and efficacy of one-month depots of TAK-448 and TAK-683, investigational kisspeptin analogs, in male rats and an androgen-dependent prostate cancer model
Tanaka, Akira, Nakata, Daisuke, Masaki, Tsuneo, Kusaka, Masami, Watanabe, Tatsuya, Matsui, Hisanori
Published in European journal of pharmacology (05.03.2018)
Published in European journal of pharmacology (05.03.2018)
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Suppression of the hypothalamic–pituitary–gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: Studies in human GnRH receptor knock-in mice
Nakata, Daisuke, Masaki, Tsuneo, Tanaka, Akira, Yoshimatsu, Mie, Akinaga, Yumiko, Asada, Mari, Sasada, Reiko, Takeyama, Michiyasu, Miwa, Kazuhiro, Watanabe, Tatsuya, Kusaka, Masami
Published in European journal of pharmacology (15.01.2014)
Published in European journal of pharmacology (15.01.2014)
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Journal Article
Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
Miwa, Kazuhiro, Hitaka, Takenori, Imada, Takashi, Sasaki, Satoshi, Yoshimatsu, Mie, Kusaka, Masami, Tanaka, Akira, Nakata, Daisuke, Furuya, Shuichi, Endo, Satoshi, Hamamura, Kazumasa, Kitazaki, Tomoyuki
Published in Journal of medicinal chemistry (28.07.2011)
Published in Journal of medicinal chemistry (28.07.2011)
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Journal Article
Chronic Administration of the Metastin/Kisspeptin Analog KISS1-305 or the Investigational Agent TAK-448 Suppresses Hypothalamic Pituitary Gonadal Function and Depletes Plasma Testosterone in Adult Male Rats
Matsui, Hisanori, Tanaka, Akira, Yokoyama, Kotaro, Takatsu, Yoshihiro, Ishikawa, Kaori, Asami, Taiji, Nishizawa, Naoki, Suzuki, Atsuko, Kumano, Satoshi, Terada, Michiko, Kusaka, Masami, Kitada, Chieko, Ohtaki, Tetsuya
Published in Endocrinology (Philadelphia) (01.11.2012)
Published in Endocrinology (Philadelphia) (01.11.2012)
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Journal Article
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I
Aikawa, Katsuji, Miyawaki, Toshio, Hitaka, Takenori, Imai, Yumi N., Hara, Takahito, Miyazaki, Junichi, Yamaoka, Masuo, Kusaka, Masami, Kanzaki, Naoyuki, Tasaka, Akihiro, Shiraishi, Mitsuru, Yamamoto, Satoshi
Published in Bioorganic & medicinal chemistry (15.05.2015)
Published in Bioorganic & medicinal chemistry (15.05.2015)
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Journal Article
The Effects of Chronic Subcutaneous Administration of an Investigational Kisspeptin Analog, TAK-683, on Gonadotropin-Releasing Hormone Pulse Generator Activity in Goats
Yamamura, Takashi, Wakabayashi, Yoshihiro, Sakamoto, Kohei, Matsui, Hisanori, Kusaka, Masami, Tanaka, Tomomi, Ohkura, Satoshi, Okamura, Hiroaki
Published in Neuroendocrinology (01.01.2014)
Published in Neuroendocrinology (01.01.2014)
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Journal Article
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists
Yamamoto, Satoshi, Matsunaga, Nobuyuki, Hitaka, Takenori, Yamada, Masami, Hara, Takahito, Miyazaki, Junichi, Santou, Takashi, Kusaka, Masami, Yamaoka, Masuo, Kanzaki, Naoyuki, Furuya, Shuichi, Tasaka, Akihiro, Hamamura, Kazumasa, Ito, Mitsuhiro
Published in Bioorganic & medicinal chemistry (01.01.2012)
Published in Bioorganic & medicinal chemistry (01.01.2012)
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Journal Article
Differential Effects of Continuous Exposure to the Investigational Metastin/Kisspeptin Analog TAK-683 on Pulsatile and Surge Mode Secretion of Luteinizing Hormone in Ovariectomized Goats
TANAKA, Tomomi, OHKURA, Satoshi, WAKABAYASHI, Yoshihiro, KUROIWA, Takenobu, NAGAI, Kiyosuke, ENDO, Natsumi, TANAKA, Akira, MATSUI, Hisanori, KUSAKA, Masami, OKAMURA, Hiroaki
Published in Journal of Reproduction and Development (2013)
Published in Journal of Reproduction and Development (2013)
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C17,20-Lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors
MATSUNAGA, Nobuyuki, KAKU, Tomohiro, TASAKA, Akihiro, ITOH, Fumio, TANAKA, Toshimasa, HARA, Takahito, MIKI, Hiroshi, IWASAKI, Masahiko, AONO, Tetsuya, YAMAOKA, Masuo, KUSAKA, Masami
Published in Bioorganic & medicinal chemistry (01.05.2004)
Published in Bioorganic & medicinal chemistry (01.05.2004)
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Suppression of a Pituitary-Ovarian Axis by Chronic Oral Administration of a Novel Nonpeptide Gonadotropin-Releasing Hormone Antagonist, TAK-013, in Cynomolgus Monkeys
Hara, Takahito, Araki, Hideo, Kusaka, Masami, Harada, Masataka, Cho, Nobuo, Suzuki, Nobuhiro, Furuya, Shuichi, Fujino, Masahiko
Published in The journal of clinical endocrinology and metabolism (01.04.2003)
Published in The journal of clinical endocrinology and metabolism (01.04.2003)
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Journal Article
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer
Kaku, Tomohiro, Hitaka, Takenori, Ojida, Akio, Matsunaga, Nobuyuki, Adachi, Mari, Tanaka, Toshimasa, Hara, Takahito, Yamaoka, Masuo, Kusaka, Masami, Okuda, Teruaki, Asahi, Satoru, Furuya, Shuichi, Tasaka, Akihiro
Published in Bioorganic & medicinal chemistry (01.11.2011)
Published in Bioorganic & medicinal chemistry (01.11.2011)
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Journal Article
Discovery of 1-{4[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
Miwa, Kazuhiro, Hitaka, Takenori, Imada, Takashi, Sasaki, Satoshi, Yoshimatsu, Mie, Kusaka, Masami, Tanaka, Akira, Nakata, Daisuke, Furuya, Shuichi, Endo, Satoshi, Hamamura, Kazumasa, Kitazaki, Tomoyuki
Published in Journal of medicinal chemistry (28.07.2011)
Published in Journal of medicinal chemistry (28.07.2011)
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Journal Article
Effect of a novel 17,20-lyase inhibitor, orteronel (TAK-700), on androgen synthesis in male rats
Hara, Takahito, Kouno, Jin, Kaku, Tomohiro, Takeuchi, Toshiyuki, Kusaka, Masami, Tasaka, Akihiro, Yamaoka, Masuo
Published in The Journal of steroid biochemistry and molecular biology (01.03.2013)
Published in The Journal of steroid biochemistry and molecular biology (01.03.2013)
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Journal Article
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac‑d‑Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility
Nishizawa, Naoki, Takatsu, Yoshihiro, Kumano, Satoshi, Kiba, Atsushi, Ban, Junko, Tsutsumi, Shunichirou, Matsui, Hisanori, Matsumoto, Shin-ichi, Yamaguchi, Masashi, Ikeda, Yukihiro, Kusaka, Masami, Ohtaki, Tetsuya, Itoh, Fumio, Asami, Taiji
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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Growth Inhibition by Testosterone in an Androgen Receptor Splice Variant-Driven Prostate Cancer Model: Growth Inhibition by Testosterone in CRPC
Nakata, Daisuke, Nakayama, Kazuhide, Masaki, Tsuneo, Tanaka, Akira, Kusaka, Masami, Watanabe, Tatsuya
Published in The Prostate (01.12.2016)
Published in The Prostate (01.12.2016)
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