Search Results - "Iwasawa, Yoshikazu"

Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents by Hirai, Hiroshi, Iwasawa, Yoshikazu, Okada, Megumu, Arai, Tsuyoshi, Nishibata, Toshihide, Kobayashi, Makiko, Kimura, Toshifumi, Kaneko, Naoki, Ohtani, Junko, Yamanaka, Kazunori, Itadani, Hiraku, Takahashi-Suzuki, Ikuko, Fukasawa, Kazuhiro, Oki, Hiroko, Nambu, Tadahiro, Jiang, Jian, Sakai, Takumi, Arakawa, Hiroharu, Sakamoto, Toshihiro, Sagara, Takeshi, Yoshizumi, Takashi, Mizuarai, Shinji, Kotani, Hidehito

“…Wee1 is a tyrosine kinase that phosphorylates and inactivates CDC2 and is involved in G 2 checkpoint signaling. Because p53 is a key regulator in the G 1…”
Get full text

p53-related protein kinase confers poor prognosis and represents a novel therapeutic target in multiple myeloma by Hideshima, Teru, Cottini, Francesca, Nozawa, Yoshihisa, Seo, Hyuk-Soo, Ohguchi, Hiroto, Samur, Mehmet K., Cirstea, Diana, Mimura, Naoya, Iwasawa, Yoshikazu, Richardson, Paul G., Munshi, Nikhil C., Chauhan, Dharminder, Massefski, Walter, Utsugi, Teruhiro, Dhe-Paganon, Sirano, Anderson, Kenneth C.

“…p53-related protein kinase (TP53RK, also known as PRPK) is an upstream kinase that phosphorylates (serine residue Ser15) and mediates p53 activity. Here we…”
Get full text

MK-5108, a Highly Selective Aurora-A Kinase Inhibitor, Shows Antitumor Activity Alone and in Combination with Docetaxel by Shimomura, Toshiyasu, Hasako, Shinichi, Nakatsuru, Yoko, Mita, Takashi, Ichikawa, Koji, Kodera, Tsutomu, Sakai, Takumi, Nambu, Tadahiro, Miyamoto, Mayu, Takahashi, Ikuko, Miki, Satomi, Kawanishi, Nobuhiko, Ohkubo, Mitsuru, Kotani, Hidehito, Iwasawa, Yoshikazu

“…Aurora-A kinase is a one of the key regulators during mitosis progression. Aurora-A kinase is a potential target for anticancer therapies because…”
Get full text

Establishment of a human hepatocellular cell line capable of maintaining long-term replication of hepatitis B virus by Yao, Wan-Ling, Ikeda, Sotaro, Tsukamoto, Yuta, Shindo, Keiko, Otakaki, Yukie, Qin, Mian, Iwasawa, Yoshikazu, Takeuchi, Fumihiko, Kaname, Yuki, Chou, Yu-Chi, Chang, Chungming, Watashi, Koichi, Wakita, Takaji, Noda, Takeshi, Kato, Hiroki, Fujita, Takashi

“…Hepatitis B virus (HBV) is a virus whose replication cycle cannot be completely reproduced using cultured cell lines. Here, we report an engineered cell line…”
Get full text

Screening for inhibitor of episomal DNA identified dicumarol as a hepatitis B virus inhibitor by Takeuchi, Fumihiko, Ikeda, Sotaro, Tsukamoto, Yuta, Iwasawa, Yoshikazu, Qihao, Chen, Otakaki, Yukie, Ryota, Ouda, Yao, Wan-Ling, Narita, Ryo, Makoto, Hijikata, Watashi, Koichi, Wakita, Takaji, Takeuchi, Koh, Chayama, Kazuaki, Kogure, Amane, Kato, Hiroki, Fujita, Takashi

“…Currently, there is no available therapy to eradicate hepatitis B virus (HBV) in chronically infected individuals. This is due to the difficulty in eliminating…”
Get full text

Structural Basis of Human p70 Ribosomal S6 Kinase-1 Regulation by Activation Loop Phosphorylation by Sunami, Tomoko, Byrne, Noel, Diehl, Ronald E., Funabashi, Kaoru, Hall, Dawn L., Ikuta, Mari, Patel, Sangita B., Shipman, Jennifer M., Smith, Robert F., Takahashi, Ikuko, Zugay-Murphy, Joan, Iwasawa, Yoshikazu, Lumb, Kevin J., Munshi, Sanjeev K., Sharma, Sujata

“…p70 ribosomal S6 kinase (p70S6K) is a downstream effector of the mTOR signaling pathway involved in cell proliferation, cell growth, cell-cycle progression,…”
Get full text

Recent advances in the development of selective small molecule inhibitors for cyclin-dependent kinases by Hirai, Hiroshi, Kawanishi, Nobuhiko, Iwasawa, Yoshikazu

“…Loss of normal cell cycle regulation is the hallmark of human cancers, and alteration of the components involved in cell cycle regulation occurs in most human…”
Get more information

Discovery of the First Potent and Selective Small Molecule Opioid Receptor-like (ORL1) Antagonist:  1-[(3R,4R)-1-Cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl- 1,3-dihydro-2H-benzimidazol-2-one (J-113397) by Kawamoto, Hiroshi, Ozaki, Satoshi, Itoh, Yoshiki, Miyaji, Mitsuru, Arai, Sachie, Nakashima, Hiroshi, Kato, Tetsuya, Ohta, Hisashi, Iwasawa, Yoshikazu

Get full text

In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist by Ozaki, Satoshi, Kawamoto, Hiroshi, Itoh, Yoshiki, Miyaji, Mitsuru, Azuma, Tomoko, Ichikawa, Daisuke, Nambu, Hirohide, Iguchi, Tomoko, Iwasawa, Yoshikazu, Ohta, Hisashi

“…1-[(3 R,4 R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2 H-benzimidazol-2-one (J-113397) was found to be the first potent nonpeptidyl…”
Get full text

Enhanced Spinal Nociceptin Receptor Expression Develops Morphine Tolerance and Dependence by Ueda, Hiroshi, Inoue, Makoto, Takeshima, Hiroshi, Iwasawa, Yoshikazu

“…The tolerance and dependence after chronic medication with morphine are thought to be representative models for studying the plasticity, including the…”
Get full text

Biological characterization of 2-aminothiazole-derived Cdk4/6 selective inhibitor in vitro and in vivo by Hirai, Hiroshi, Shimomura, Toshiyasu, Kobayashi, Makiko, Eguchi, Tomohiro, Taniguchi, Eri, Fukasawa, Kazuhiro, Machida, Takumitsu, Oki, Hiroko, Arai, Tsuyoshi, Ichikawa, Koji, Hasako, Shinichi, Haze, Kyosuke, Kodera, Tsutomu, Kawanishi, Nobuhiko, Takahashi-Suziki, Ikuko, Nakatsuru, Yoko, Kotani, Hidehito, Iwasawa, Yoshikazu

“…Abnormalities in the p16INK4a/ cyclin-dependent kinase (Cdk)4, 6/ Retinoblastoma (Rb) pathway frequently occur in various human cancers. Thus, Cdk4/6 is an…”
Get full text

Design, Synthesis, and Discovery of a Novel CCR1 Antagonist by Naya, Akira, Sagara, Yufu, Ohwaki, Kenji, Saeki, Toshihiko, Ichikawa, Daisuke, Iwasawa, Yoshikazu, Noguchi, Kazuhito, Ohtake, Norikazu

“…The CC chemokines may play an important role in the pathogenesis of chronic inflammatory diseases including rheumatoid arthritis, and their effects are thought…”
Get full text

Efficient and practical asymmetric synthesis of 1- tert-butyl 3-methyl (3 R,4 R)-4-(2-oxo-2,3-dihydro-1 H-benzimidazol-1-yl)piperidine-1,3-dicarboxylate, a useful intermediate for the synthesis of nociceptin antagonists by Jona, Hideki, Shibata, Jun, Asai, Masanori, Goto, Yasuhiro, Arai, Sachie, Nakajima, Shigeru, Okamoto, Osamu, Kawamoto, Hiroshi, Iwasawa, Yoshikazu

“…An efficient and practical asymmetric synthesis of 1- tert-butyl 3-methyl (3 R,4 R)-4-(2-oxo-2,3-dihydro-1 H-benzimidazol-1-yl)piperidine-1,3-dicarboxylate 1,…”
Get full text

MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil by Hirai, Hiroshi, Arai, Tsuyoshi, Okada, Megumu, Nishibata, Toshihide, Kobayashi, Makiko, Sakai, Naoko, Imagaki, Kazuhide, Ohtani, Junko, Sakai, Takumi, Yoshizumi, Takashi, Mizuarai, Shinji, Iwasawa, Yoshikazu, Kotani, Hidehito

“…MK-1775 is a potent and selective small molecule Wee1 inhibitor. Previously we have shown that it abrogated DNA damaged checkpoints induced by gemcitabine,…”
Get full text

Abstract P06-02: Discovery of TAS0953/HM06, a novel next generation RET-specific inhibitor capable of inhibiting RET solvent front mutations by Miyazaki, Isao, Ishida, Keiji, Kato, Masanori, Suzuki, Tatsuya, Fujita, Hidenori, Ohkubo, Shuichi, Iwasawa, Yoshikazu

“…Abstract RET gene fusions are oncogenic drivers in multiple tumor types and are estimated to be present in 1% to 2% of non-squamous non-small cell lung cancers…”
Get full text

TAS3681, a novel type of AR antagonist with AR downregulating activity, as a new targeted therapy for aberrant AR-driven prostate cancer by Seki, Masanao, Minamiguchi, Kazuhisa, Kajiwara, Daisuke, Mizutani, Hiroya, Yoshida, Shohei, Sasaki, Eiji, Utsugi, Teruhiro, Iwasawa, Yoshikazu

“…Abstract only 298 Background: Recent reports suggest that AR aberrations are involved in the development of metastatic castration-resistant prostate cancer and…”
Get full text

TAS4464, a Novel, Highly Potent NEDD8-Activating Enzyme Inhibitor Shows Antitumor Activity in Ibrutinib-Insensitive Mantle Cell Lymphoma Via Inactivation of the NF-κB Pathway by Muraoka, Hiromi, Yoshimura, Chihoko, Tsuji, Shingo, Hashimoto, Akihiro, Nakagawa, Fumio, Mizutani, Takashi, Ohkubo, Shuichi, Matsuo, Kenichi, Utsugi, Teruhiro, Iwasawa, Yoshikazu

“…Background: Although ibrutinib, a Bruton tyrosine kinase inhibitor, is becoming widely used to treat patients with mantle cell lymphoma (MCL), about one-third…”
Get full text

Abstract B180: TAS-115 attenuates tumor-associated macrophages and enhances sensitivity to anti-PD-1 monoclonal antibody in syngeneic mouse tumors by Haruma, Tomonori, Fujita, Hidenori, Yamada, Yukari, Fukaya, Satoshi, Hashimoto, Akihiro, Harada, Takafumi, Suzuki, Takamasa, Matsuo, Kenichi, Utsugi, Teruhiro, Iwasawa, Yoshikazu

“…Abstract Background: Clinical efficacy of anti-PD-1 monoclonal antibody (mAb) has been established in various types of cancers. On the other hand, many…”
Get full text

The impact of TAS3681, a new type of androgen receptor antagonist, on aberrant AR signaling that drives tumor resistance to AR-targeted therapies by down-regulating full length and splice variant AR by Kajiwara, Daisuke, Minamiguchi, Kazuhisa, Seki, Masanao, Mizutani, Hiroya, Yamamura, Keisuke, Okajima, Shigeo, Sasaki, Eiji, Utsugi, Teruhiro, Iwasawa, Yoshikazu

“…Abstract only 197 Background: The treatment of castration-resistant prostate cancer (CRPC) has changed dramatically with the use of two new therapies,…”
Get full text

Abstract A169: Combination of TPC-144, a reversible LSD1 inhibitor, and a hypomethylating agent resulted in synergistic antitumor efficacy in preclinical models of AML by Osada, Akiko, Kawagishi, Aki, Hatanaka, Ryo, Machida, Takumitsu, Ito, Kenjiro, Yamashita, Satoshi, Ogawa, Takahiro, Imaoka, Tadashi, Matsuo, Kenichi, Utsugi, Teruhiro, Iwasawa, Yoshikazu

“…Abstract Background: Lysine-specific demethylase 1A (LSD1/KDM1A) is a flavin adenine dinucleotide (FAD)-dependent histone demethylase that specifically…”
Get full text