Zobrazeno 1 - 9 of 9 pro vyhledávání: '"Misaki, Homma"'
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Akademický článek
Novel beta-glucocerebrosidase chaperone compounds identified from cell-based screening reduce pathologically accumulated glucosylsphingosine in iPS-derived neuronal cells
Autor: Yusuke Naito, Sou Sakamoto, Takuto Kojima, Misaki Homma, Maiko Tanaka, Hideki Matsui
Publikováno v: SLAS Discovery, Vol 28, Iss 7, Pp 344-349 (2023)
The beta-glucocerebrosidase (GBA1) gene encodes the lysosomal beta-glucocerebrosidase (GCase) that metabolizes the lipids glucosylceramide (GlcCer) and glucosylsphingosine (GlcSph). Biallelic loss-of-function mutations in GBA1 such as L444P cause Gau
Externí odkaz: https://doaj.org/article/6fa5022fc3904bd99b6d9e7cc05d8004
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2
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent
Autor: Toshiyuki Nomura, Hiroshi Sugimoto, Noriko Uchiyama, Akihiro Ohashi, Hideto Hara, Takashi Imada, Yukiko Yamamoto, Isaac Hoffman, Kenichi Iwai, Momoko Ohori, Misaki Homma, Osamu Kurasawa, Nobuo Cho, Tohru Miyazaki, Yuya Oguro, Kentaro Iwata, Robert J. Skene
Publikováno v: Journal of Medicinal Chemistry. 63:1084-1104
In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analogue I showing time-dependent Cdc7 kinase inhibition and slow dissociation kinetics
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::302cc8787b4b0af51ff2d819e10565ac
https://doi.org/10.1021/acs.jmedchem.9b01427
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4
2-Aminomethylthieno[3,2- d ]pyrimidin-4(3 H )-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase
Autor: Hideto Hara, Misaki Homma, Akihiro Ohashi, Yuya Oguro, Kouji Mori, Osamu Kurasawa, Nobuo Cho, Tohru Miyazaki, Sei Yoshida, Kenichi Iwai, Noriko Uchiyama
Publikováno v: Bioorganic & Medicinal Chemistry. 25:3658-3670
In order to increase the success rate for developing new Cdc7 inhibitors for cancer therapy, we explored a new chemotype which can comply with the previously-constructed pharmacophore model. Substitution of a pyridine ring of a serendipitously-identi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbf0cb711b3289b52763b9b0437e281f
https://doi.org/10.1016/j.bmc.2017.04.044
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6
Visualizing and Modulating Mitophagy for Therapeutic Studies of Neurodegeneration
Autor: Hiroshi Hama, Yoko Ishida, Mayu Sugiyama, Hiroyuki Hioki, Hiroyuki Katayama, Yoshiyuki Tsujihata, Masaaki Funata, Koji Nagasawa, Megumu Takahashi, Ryoko Ando, Takanori Nishimura, Nobuyo Yoshida, Misaki Homma, Hiroshi Kurokawa, Atsushi Miyawaki
Publikováno v: Cell. 181:1176-1187.e16
Dysfunctional mitochondria accumulate in many human diseases. Accordingly, mitophagy, which removes these mitochondria through lysosomal degradation, is attracting broad attention. Due to uncertainties in the operational principles of conventional mi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c258af75e08b3dfd27a0e9c6d67ec936
https://doi.org/10.1016/j.cell.2020.04.025
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7
A simple and widely applicable hit validation strategy for protein–protein interaction inhibitors based on a quantitative ligand displacement assay
Autor: Katsuji Aikawa, Ikuo Miyahisa, Tomoya Sameshima, Mark S. Hixon, Misaki Homma, Junji Matsui
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:5836-5839
Identification of inhibitors for protein-protein interactions (PPIs) from high-throughput screening (HTS) is challenging due to the weak affinity of primary hits. We present a hit validation strategy of PPI inhibitors using quantitative ligand displa
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c6c8198f992a3f28f8f5a27f65a6582
https://doi.org/10.1016/j.bmcl.2014.09.073
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8
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones
Autor: Isaac Hoffman, Sei Yoshida, Osamu Kurasawa, Kenichi Iwai, Tomoyasu Ishikawa, Kouji Mori, Akihiro Ohashi, Hideto Hara, Nobuo Cho, Tohru Miyazaki, Robert J. Skene, Yuya Oguro, Misaki Homma
Publikováno v: Bioorganicmedicinal chemistry. 25(7)
Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective tumor-cell death in a p53-dependent manner, suggest
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f0f9a7ca7899e8598f82eecd7960b9a
https://pubmed.ncbi.nlm.nih.gov/28284870
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9
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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