Výsledky vyhledávání - "Shigeru Igaki"

T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice

Autor: Shigeru Igaki, Ryosuke Hibino, Ken Tsuchida, Shinji Iwasaki, Satoru Matsuda, Ryujiro Hara, Hiroko Kamada, Masashi Toyofuku, Haruhide Kimura, Misa Iwatani, Rina Baba, Mitsuhiro Ito, Kota Matsumiya, Hideyuki Oki, Yusuke Kamada, Takeshi Hirakawa, Shinji Morimoto

Publikováno v: Neuropsychopharmacology

Dysregulation of histone H3 lysine 4 (H3K4) methylation has been implicated in the pathogenesis of several neurodevelopmental disorders. Targeting lysine-specific demethylase 1 (LSD1), an H3K4 demethylase, is therefore a promising approach to treat t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c6a412d79e9c823a65878035790b06f0
https://doi.org/10.1038/s41386-018-0300-9

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LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models

Autor: Ryuji Yamada, Mitsuhiro Ito, Hideyuki Oki, Yasushi Hattori, Yuuichi Arakawa, Matsumoto Shigemitsu, Satoru Matsuda, Atsushi Nakatani, Masaki Daini, Shigeru Igaki, Noriko Suzuki, Haruhide Kimura, Tatsuya Ando, Rina Baba

Publikováno v: Science Advances

LSD1 inhibitor TAK-418 could be a therapeutic option for neurodevelopmental disorders via normalization of gene expression.
Persistent epigenetic dysregulation may underlie the pathophysiology of neurodevelopmental disorders, such as autism spec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::226b60276736066095731de4a03ae505
https://doi.org/10.1126/sciadv.aba1187

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Cryo-EM Structure of K

Autor: Tatsuki, Asai, Naruhiko, Adachi, Toshio, Moriya, Hideyuki, Oki, Takamitsu, Maru, Masato, Kawasaki, Kano, Suzuki, Sisi, Chen, Ryohei, Ishii, Kazuko, Yonemori, Shigeru, Igaki, Satoshi, Yasuda, Satoshi, Ogasawara, Toshiya, Senda, Takeshi, Murata

Publikováno v: Structure (London, England : 1993). 29(3)

The hERG channel is a voltage-gated potassium channel involved in cardiac repolarization. Off-target hERG inhibition by drugs has become a critical issue in the pharmaceutical industry. The three-dimensional structure of the hERG channel was recently

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::0c5c71ba40770276671cc88c93110a4e
https://pubmed.ncbi.nlm.nih.gov/33450182

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Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole

Autor: Toshio Moriya, Shigeru Igaki, Satoshi Ogasawara, Satoshi Yasuda, Tatsuki Asai, Hideyuki Oki, Sisi Chen, Ryohei Ishii, Kazuko Yonemori, Takeshi Murata, Toshiya Senda, Naruhiko Adachi, Masato Kawasaki, Takamitsu Maru, Kano Suzuki

Publikováno v: Structure. 29:203-212.e4

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b709062c508cc32bed8c1cd6593d80b9
https://doi.org/10.1016/j.str.2020.12.007

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Discovery of an Irreversible and Cell-Active BCL6 Inhibitor Selectively Targeting Cys53 Located at the Protein-Protein Interaction Interface

Autor: Satoshi Sogabe, Tomoya Sameshima, Kotaro Sakamoto, Takeshi Yamamoto, Junichi Sakamoto, Gotou Mika, Osamu Sano, Koh Ida, Ikuo Miyahisa, Yasuhiro Imaeda, Shigeru Igaki

Publikováno v: Biochemistry. 57(8)

B-cell lymphoma 6 (BCL6) is the most frequently involved oncogene in diffuse large B-cell lymphomas (DLBCLs). BCL6 shows potent transcriptional repressor activity through interactions with its corepressors, such as BCL6 corepressor (BCOR). The inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7bf75482c9aab39025500267ab0e2c9
https://pubmed.ncbi.nlm.nih.gov/29293322

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Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors

Autor: Yoshihiro Kiyota, Craig A. Behnke, Takahiro Matsumoto, Junichi Miyazaki, Shigeru Igaki, Toru Kawamura, Mitsunori Kono, Masakuni Kori, Hideyuki Oki, Atsushi Nishimura, Masato Shimojo

Publikováno v: Bioorganic & Medicinal Chemistry. 21:28-41

A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02fe0e6423f9c80cdc30c75070da14d9
https://doi.org/10.1016/j.bmc.2012.11.006

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Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors

Autor: Tomoyasu Ishikawa, Youichi Kawakita, Douglas R. Cary, Takagi Shinji, Hiroshi Miki, Yoshikazu Ohta, Satoshi Sogabe, Terufumi Takagi, Hidehisa Iwata, Shigeru Igaki

Publikováno v: ACS Medicinal Chemistry Letters. 4:201-205

The epidermal growth factor receptor (EGFR) family plays a critical role in vital cellular processes and in various cancers. Known EGFR inhibitors exhibit distinct antitumor responses against the various EGFR mutants associated with nonsmall-cell lun

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a2b950088667d820c4194eae6980932
https://doi.org/10.1021/ml300327z

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Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins

Autor: Yasuhiro Imaeda, Yuta Tanaka, Tomohiro Kawamoto, Ikuo Miyahisa, Katsuji Aikawa, Michiko Tawada, Nobuo Cho, Tomoyasu Ishikawa, Satoshi Sogabe, Tomoya Sameshima, Yumi Imai, Yumi Hayano, Goushi Nishida, Masakazu Inazuka, Misaki Homma, Shigeru Igaki

Publikováno v: Journal of medicinal chemistry. 56(23)

Mcl-1 and Bcl-xL are crucial regulators of apoptosis, therefore dual inhibitors of both proteins could serve as promising new anticancer drugs. To design Mcl-1/Bcl-xL dual inhibitors, we performed structure-guided analyses of the corresponding select

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::371e05ea4b94af36e0b541c5a6c0decd
https://pubmed.ncbi.nlm.nih.gov/24215352

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