Search Results - "YAMAOKA, Masuo"

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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Amelioration of sexual behavior and motor activity deficits in a castrated rodent model with a selective androgen receptor modulator SARM-2f by Morimoto, Megumi, Amano, Yuichiro, Oka, Masahiro, Harada, Ayako, Fujita, Hisashi, Hikichi, Yukiko, Tozawa, Ryuichi, Yamaoka, Masuo, Hara, Takahito

“…Sarcopenia and cachexia present characteristic features of a decrease in skeletal muscle mass and strength, anorexia, and lack of motivation. Treatments for…”
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A selective androgen receptor modulator SARM‐2f activates androgen receptor, increases lean body mass, and suppresses blood lipid levels in cynomolgus monkeys by Morimoto, Megumi, Yamaoka, Masuo, Hara, Takahito

“…SARM‐2f a selective androgen receptor (AR) modulator, increases skeletal muscle mass and locomotor activity in rats. This study aimed to clarify its…”
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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate by Aikawa, Katsuji, Asano, Moriteru, Ono, Koji, Habuka, Noriyuki, Yano, Jason, Wilson, Keith, Fujita, Hisashi, Kandori, Hitoshi, Hara, Takahito, Morimoto, Megumi, Santou, Takashi, Yamaoka, Masuo, Nakayama, Masaharu, Hasuoka, Atsushi

“…[Display omitted] We previously reported that 4-(pyrrolidin-1-yl)benzonitrile derivative 1b was a selective androgen receptor modulator (SARM) that exhibited…”
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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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Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists by Yamamoto, Satoshi, Tomita, Naoki, Suzuki, Yuri, Suzaki, Tomohiko, Kaku, Tomohiro, Hara, Takahito, Yamaoka, Masuo, Kanzaki, Naoyuki, Hasuoka, Atsushi, Baba, Atsuo, Ito, Mitsuhiro

“…A series of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole compounds were designed, synthesized, and evaluated for their potential as novel…”
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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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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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Prevention of body weight loss and sarcopenia by a novel selective androgen receptor modulator in cancer cachexia models by Morimoto, Megumi, Aikawa, Katsuji, Hara, Takahito, Yamaoka, Masuo

“…Cancer cachexia is a syndrome that impairs the quality of life and overall survival of patients, and thus the effectiveness of anticancer agents. There are no…”
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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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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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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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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives by Asano, Moriteru, Hitaka, Takenori, Imada, Takashi, Yamada, Masami, Morimoto, Megumi, Shinohara, Hiromi, Hara, Takahito, Yamaoka, Masuo, Santou, Takashi, Nakayama, Masaharu, Imai, Yumi, Habuka, Noriyuki, Yano, Jason, Wilson, Keith, Fujita, Hisashi, Hasuoka, Atsushi

“…[Display omitted] We recently reported a class of novel tissue-selective androgen receptor modulators (SARMs), represented by a naphthalene derivative A…”
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Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: Effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys by Yamaoka, Masuo, Hara, Takahito, Hitaka, Takenori, Kaku, Tomohiro, Takeuchi, Toshiyuki, Takahashi, Junzo, Asahi, Satoru, Miki, Hiroshi, Tasaka, Akihiro, Kusaka, Masami

“…[Display omitted] ► Orteronel is a novel, selective, and potent inhibitor of 17,20-lyase. ► Orteronel potently suppressed androgen production in vitro in…”
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Effect of an investigational CYP17A1 inhibitor, orteronel (TAK-700), on estrogen- and corticoid-synthesis pathways in hypophysectomized female rats and on the serum estradiol levels in female cynomolgus monkeys by Yamaoka, Masuo, Hara, Takahito, Araki, Hideo, Kaku, Tomohiro, Hitaka, Takenori, Tasaka, Akihiro, Kusaka, Masami

“…•Orteronel does not directly inhibit aromatase activity.•At ≥3mg/kg, orteronel significantly suppresses serum estradiol in female rats.•In female cynomolgus…”
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Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists by Yamamoto, Satoshi, Kobayashi, Hiromi, Kaku, Tomohiro, Aikawa, Katsuji, Hara, Takahito, Yamaoka, Masuo, Kanzaki, Naoyuki, Hasuoka, Atsushi, Baba, Atsuo, Ito, Mitsuhiro

“…A series of 3-aryl-3-hydroxy-1-phenylpyrrolidine compounds were designed, synthesized, and evaluated for their potential as novel orally available androgen…”
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17,20-Lyase inhibitors. Part 4: Design, synthesis and structure–activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors by Kaku, Tomohiro, Matsunaga, Nobuyuki, Ojida, Akio, Tanaka, Toshimasa, Hara, Takahito, Yamaoka, Masuo, Kusaka, Masami, Tasaka, Akihiro

“…A novel series of naphthylmethylimidazole derivatives and related compounds have been investigated as selective 17,20-lyase inhibitors. A novel series of…”
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17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure–activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors by Kaku, Tomohiro, Tsujimoto, Saori, Matsunaga, Nobuyuki, Tanaka, Toshimasa, Hara, Takahito, Yamaoka, Masuo, Kusaka, Masami, Tasaka, Akihiro

“…A novel series of biphenylylmethylimidazole derivatives were synthesized as inhibitors of 17,20-lyase, and their biological activities were evaluated. A novel…”
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A mutation in β-tubulin and a sustained dependence on androgen receptor signalling in a newly established docetaxel-resistant prostate cancer cell line by Hara, Takahito, Ushio, Kazutaka, Nishiwaki, Mayumi, Kouno, Jin, Araki, Hideo, Hikichi, Yukiko, Hattori, Masahiko, Imai, Yumi, Yamaoka, Masuo

“…The mechanisms of docetaxel resistance in PC (prostate cancer) are unclear because of the lack of suitable experimental models, and no effective treatment…”
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