Search Results - "KUSAKA, Masami"

Overcoming Persistent Dependency on Androgen Signaling after Progression to Castration-Resistant Prostate Cancer by YAMAOKA, Masuo, HARA, Takahito, KUSAKA, Masami

“…Prostate cancer is the most common form of cancer in males in the United States, and the second leading cause of cancer death. Initially, most cases of…”
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Selective androgen receptor modulator activity of a steroidal antiandrogen TSAA-291 and its cofactor recruitment profile by Hikichi, Yukiko, Yamaoka, Masuo, Kusaka, Masami, Hara, Takahito

“…Selective androgen receptor modulators (SARMs) specifically bind to the androgen receptor and exert agonistic or antagonistic effects on target organs. In this…”
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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 by Tanaka, Akira, Nakata, Daisuke, Masaki, Tsuneo, Kusaka, Masami, Watanabe, Tatsuya, Matsui, Hisanori

“…TAK-448 and TAK-683 are kisspeptin agonist analogs with improved in vivo stability and activity. Previous studies showed that continuous subcutaneous…”
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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 by Nakata, Daisuke, Masaki, Tsuneo, Tanaka, Akira, Yoshimatsu, Mie, Akinaga, Yumiko, Asada, Mari, Sasada, Reiko, Takeyama, Michiyasu, Miwa, Kazuhiro, Watanabe, Tatsuya, Kusaka, Masami

“…TAK-385 (relugolix) is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist, which builds on previous work with non-peptide…”
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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 by Miwa, Kazuhiro, Hitaka, Takenori, Imada, Takashi, Sasaki, Satoshi, Yoshimatsu, Mie, Kusaka, Masami, Tanaka, Akira, Nakata, Daisuke, Furuya, Shuichi, Endo, Satoshi, Hamamura, Kazumasa, Kitazaki, Tomoyuki

“…We previously discovered an orally active human gonadotropin-releasing hormone (GnRH) receptor antagonist, thieno[2,3-d]pyrimidine-2,4-dione derivative 1…”
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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 by 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

“…Metastin/kisspeptin, a hypothalamic peptide, plays a pivotal role in controlling GnRH neurons. Here we studied the effect of chronic sc administration of two…”
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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I by 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

“…[Display omitted] To develop effective drugs for hypogonadism, sarcopenia, and cachexia, we designed, synthesized, and evaluated selective androgen receptor…”
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The effects of chronic subcutaneous administration of an investigational kisspeptin analog, TAK-683, on gonadotropin-releasing hormone pulse generator activity in goats by Yamamura, Takashi, Wakabayashi, Yoshihiro, Sakamoto, Kohei, Matsui, Hisanori, Kusaka, Masami, Tanaka, Tomomi, Ohkura, Satoshi, Okamura, Hiroaki

“…The continuous activation of the kisspeptin receptor by its agonists causes the abrogation of kisspeptin signaling, leading to decreased pulsatile luteinizing…”
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Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists by 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

“…A series of 4-phenylpyrrole derivatives were designed, synthesized, and evaluated for their potential as novel orally available androgen receptor antagonists…”
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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 by TANAKA, Tomomi, OHKURA, Satoshi, WAKABAYASHI, Yoshihiro, KUROIWA, Takenobu, NAGAI, Kiyosuke, ENDO, Natsumi, TANAKA, Akira, MATSUI, Hisanori, KUSAKA, Masami, OKAMURA, Hiroaki

“…The aim of the present study was to determine if the estradiol-induced luteinizing hormone (LH) surge is influenced by the constant exposure to TAK-683, an…”
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A novel androgen-dependent prostate cancer xenograft model derived from skin metastasis of a Japanese patient by Kimura, Takahiro, Kiyota, Hiroshi, Nakata, Daisuke, Masaki, Tsuneo, Kusaka, Masami, Egawa, Shin

“…BACKGROUND The incidence of, and mortality from, prostate cancer (PCa) has increased in Asian countries over the past decades, partly due to a change in…”
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C17,20-Lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors by MATSUNAGA, Nobuyuki, KAKU, Tomohiro, TASAKA, Akihiro, ITOH, Fumio, TANAKA, Toshimasa, HARA, Takahito, MIKI, Hiroshi, IWASAKI, Masahiko, AONO, Tetsuya, YAMAOKA, Masuo, KUSAKA, Masami

“…Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds…”
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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 by Hara, Takahito, Araki, Hideo, Kusaka, Masami, Harada, Masataka, Cho, Nobuo, Suzuki, Nobuhiro, Furuya, Shuichi, Fujino, Masahiko

“…TAK-013 is a novel nonpeptide and orally active GnRH antagonist. We first examined the effect of TAK-013 on GnRH-stimulated LH release using primary-cultured…”
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Potent anti-angiogenic action of AGM-1470: comparison to the fumagillin parent by Kusaka, M, Sudo, K, Fujita, T, Marui, S, Itoh, F, Ingber, D, Folkman, J

“…The anti-angiogenic activity of AGM-1470, a new synthetic analog of fumagillin isolated from Aspergillus fumigatus, was extensively examined both in vitro and…”
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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 by 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

“…A novel naphthylmethylimidazole derivative 1 and its related compounds were identified as 17,20-lyase inhibitors. Based on the structure–activity relationship…”
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Growth Inhibition by Testosterone in an Androgen Receptor Splice Variant-Driven Prostate Cancer Model by Nakata, Daisuke, Nakayama, Kazuhide, Masaki, Tsuneo, Tanaka, Akira, Kusaka, Masami, Watanabe, Tatsuya

“…BACKGROUND Castration resistance creates a significant problem in the treatment of prostate cancer. Constitutively active splice variants of androgen receptor…”
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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 by 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

“…Metastin/kisspeptin is an endogenous ligand of KISS1 Receptor (KISS1R). Metastin and KISS1R are suggested to play crucial roles in regulating the secretion of…”
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Effect of a novel 17,20-lyase inhibitor, orteronel (TAK-700), on androgen synthesis in male rats by Hara, Takahito, Kouno, Jin, Kaku, Tomohiro, Takeuchi, Toshiyuki, Kusaka, Masami, Tasaka, Akihiro, Yamaoka, Masuo

“…► Orteronel specifically inhibited 17,20 lyase over 17-hydroxylase in a rat model. ► Inhibition by orteronel appeared reversible. ► Orteronel may therefore be…”
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Growth Inhibition by Testosterone in an Androgen Receptor Splice Variant-Driven Prostate Cancer Model: Growth Inhibition by Testosterone in CRPC by Nakata, Daisuke, Nakayama, Kazuhide, Masaki, Tsuneo, Tanaka, Akira, Kusaka, Masami, Watanabe, Tatsuya

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Novel mutations of androgen receptor: A possible mechanism of bicalutamide withdrawal syndrome by HARA, Takahito, MIYAZAKI, Jun-Ichi, ARAKI, Hideo, YAMAOKA, Masuo, KANZAKI, Naoyuki, KUSAKA, Masami, MIYAMOTO, Masaomi

“…Most prostate cancers (PCs) become resistant to combined androgen blockade therapy with surgical or medical castration and antiandrogens after several years…”
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