Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Tomoya Sameshima"'
Autor:
Akiko Oki, Katsunori Sasa, Hiroyuki Takada, Bunnai Saito, Kazumasa Miyamoto, Tomoko Nagino, Hidetoshi Sakurai, Ryuichi Tozawa, Tatsuo Oikawa, Makoto Miyamoto, Yuko Kokubu, Michiko Tawada, Tomoya Sameshima, Akira Kaieda
Publikováno v:
Journal of Medicinal Chemistry. 62:9175-9187
Dysferlinopathies, which are muscular diseases caused by mutations in the dysferlin gene, remain serious medical problems due to the lack of therapeutic agents. Herein, we report the design, synthesis, and structure-activity relationships of a 2,6-di
Autor:
Osamu Kurasawa, Yasutomi Asano, Ke Li, Hiroshi Banno, Jun Fujimoto, Georgia Kefala, Gyorgy Snell, Irena Levin, Takuto Kojima, Ryo Mizojiri, Bi-Ching Sang, Richard Tjhen, Michael G. Klein, Scott Weston Lane, Isaac Hoffman, Tsuyoshi Ishii, Douglas R. Cary, Xin Liu, Akito Hata, Tadahiro Nambu, Yasuyuki Debori, Tomoya Sameshima, Terufumi Takagi, Steve C. Ding, Akito Nakamura, Maki Miyamoto
Publikováno v:
ACS Med Chem Lett
[Image: see text] General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discover
Autor:
Taisuke Katoh, Tomoya Sameshima, Masato Yoshikawa, Tomoya Yukawa, Hideto Hara, Takatoshi Yogo, Russell Naven, Makoto Miyamoto, Ikuo Miyahisa, Yoshihiko Hirozane, Teruaki Okuda
Publikováno v:
Chemical Research in Toxicology. 33:154-161
Despite the recent advances in the life sciences and the remarkable investment in drug discovery research, the success rate of small-molecule drug development remains low. Safety is the second most influential factor of drug attrition in clinical stu
Autor:
Osamu Ujikawa, Takayuki Hattori, Nobumichi Ohoka, Nobuo Cho, Naoki Miyamoto, Norihito Shibata, Hiroshi Nara, Kenichiro Shimokawa, Katsunori Nagai, Tomoya Sameshima, Mikihiko Naito
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-12 (2018)
Scientific Reports
Scientific Reports
Chronic myelogenous leukemia (CML) is characterized by the oncogenic fusion protein, BCR-ABL protein kinase, against which clinically useful inhibitors have been developed. An alternative approach to treat CML is to degrade the BCR-ABL protein. Recen
Autor:
Osamu Ujikawa, Yoko Morita, Kenichiro Shimokawa, Takayuki Hattori, Masahiro Ito, Tomoya Sameshima, Keiichiro Okuhira, Katsunori Nagai, Ikuo Fujimori, Yasuhiro Imaeda, Hiroshi Nara, Ryokichi Koyama, Mikihiko Naito, Youji Hayase, Nobuo Cho, Nobumichi Ohoka, Norihito Shibata, Osamu Sano
Publikováno v:
Journal of Biological Chemistry. 293:6776-6790
Aberrant expression of proteins often underlies many diseases, including cancer. A recently developed approach in drug development is small molecule-mediated, selective degradation of dysregulated proteins. We have devised a protein-knockdown system
Autor:
Junichi Sakamoto, Seiji Yamasaki, Toshitake Kobayashi, Ikuo Miyahisa, Tomoya Sameshima, Gotou Mika
Publikováno v:
SLAS Discovery. 22:1168-1174
In a high-throughput screening (HTS) process, the chemical reactivity of test samples should be carefully examined because such reactive compounds may lead to false-positive results and adverse effects in vivo. Among all natural amino acids, the thio
Autor:
Shigekazu Sasaki, Masahiro Yaguchi, Kazuko Yonemori, Tomoya Sameshima, Taiji Asami, Kotaro Sakamoto, Masahiro Kamaura, Ayumu Niida
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2757-2761
A structure-activity relationship study of a K-Ras(G12D) selective inhibitory cyclic peptide, KRpep-2d was performed. Alanine scanning of KRpep-2d focusing on the cyclic moiety showed that Leu7, Ile9, and Asp12 are the key elements for K-Ras(G12D) se
Publikováno v:
Biochemistry. 56:2921-2927
Recently, there have been a limited number of new, validated targets for small-molecule drug discovery in the pharmaceutical industry. Although there are approximately 30 000 genes in the human genome, only 2% are targeted by currently approved small
Autor:
Satoshi Sogabe, Ayumu Niida, Tomoya Sameshima, Kazuko Yonemori, Junichi Sakamoto, Masanori Miwa, Shigekazu Sasaki, Kotaro Sakamoto, Yusuke Kamada, Masahiro Kamaura
Publikováno v:
ACS Medicinal Chemistry Letters. 8:732-736
The Ras proteins play roles in cell differentiation, proliferation, and survival. Aberrant signaling through Ras-mediated pathways in tumor cells occurs as a result of several types of mutational damage, which most frequently affects the amino acids
Autor:
Hiroyuki, Takada, Akira, Kaieda, Michiko, Tawada, Tomoko, Nagino, Katsunori, Sasa, Tatsuo, Oikawa, Akiko, Oki, Tomoya, Sameshima, Kazumasa, Miyamoto, Makoto, Miyamoto, Yuko, Kokubu, Ryuichi, Tozawa, Hidetoshi, Sakurai, Bunnai, Saito
Publikováno v:
Journal of medicinal chemistry. 62(20)
Dysferlinopathies, which are muscular diseases caused by mutations in the dysferlin gene, remain serious medical problems due to the lack of therapeutic agents. Herein, we report the design, synthesis, and structure-activity relationships of a 2,6-di