Výsledky vyhledávání - "Akihiko Sumita"

Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives

Autor: Yoshitaka Inui, Masanori Okaniwa, Takeo Arita, Terufumi Takagi, Tomohiro Kawamoto, Bi-Ching Sang, Noriko Uchiyama, Jason Yano, Kathleen Aertgeerts, Shunichirou Tsutsumi, Sei Yoshida, Masato Yabuki, Masaaki Hirose, Akihiko Sumita, Tomoyasu Ishikawa, Tsuneaki Tottori, Akito Nakamura

Publikováno v: Journal of medicinal chemistry. 56(16)

With the aim of discovering a selective kinase inhibitor targeting pan-RAF kinase inhibition, we designed novel 1,3-benzothiazole derivatives based on our thiazolo[5,4-b]pyridine class RAF/VEGFR2 inhibitor 1 and developed a regioselective cyclization

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff96452604fde4c9446069da41abd82f
https://pubmed.ncbi.nlm.nih.gov/23906342

Zobrazit plný text záznamu

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives

Autor: Sei Yoshida, Takeo Arita, Masato Yabuki, Terufumi Takagi, Tomohiro Kawamoto, Shunichirou Tsutsumi, Tomoyasu Ishikawa, Masanori Okaniwa, Akihiko Sumita, Tomohiro Ohashi, Takashi Imada, Tohru Miyazaki, Bi-Ching Sang, Yuta Tanaka, Jason Yano, Masaaki Hirose, Kathleen Aertgeerts

Publikováno v: Bioorganicmedicinal chemistry. 20(18)

Our aim was to discover RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors that possess strong activity and sufficient oral absorption, and thus, we selected a 5-amino-linked thiazolo[5,4-d]pyrimidine derivative as the lead compoun

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13f447afe28dbc1a6b932475d9f6a1ac
https://pubmed.ncbi.nlm.nih.gov/22883026

Zobrazit plný text záznamu

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption

Autor: Tomohiro Ohashi, Shunichirou Tsutsumi, Masanori Okaniwa, Masato Yabuki, Tomoyasu Ishikawa, Akihiko Sumita, Terufumi Takagi, Takashi Imada, Takeo Arita, Tohru Miyazaki, Tomohiro Kawamoto, Keiko Higashikawa, Yoshitaka Inui, Sei Yoshida

Publikováno v: Bioorganicmedicinal chemistry. 20(15)

As an alternative to the previously reported solid dispersion formulation for enhancing the oral absorption of thiazolo[5,4-b]pyridine 1, we investigated novel N-acyl imide prodrugs of 1 as RAF/vascular endothelial growth factor receptor 2 (VEGFR2) i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3db82957611c316e8ca2f557017caa54
https://pubmed.ncbi.nlm.nih.gov/22763369

Zobrazit plný text záznamu

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds

Publikováno v: Journal of medicinal chemistry. 55(7)

To develop RAF/VEGFR2 inhibitors that bind to the inactive DFG-out conformation, we conducted structure-based drug design using the X-ray cocrystal structures of BRAF, starting from an imidazo[1,2-b]pyridazine derivative. We designed various [5,6]-fu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bda49aa850bbe5d095ba95eed52dd619
https://pubmed.ncbi.nlm.nih.gov/22376051

Zobrazit plný text záznamu

Modulation of Taurine on CYP3A4 Induction by Rifampicin in a HepG2 Cell Line

Autor: Hideyasu Matsuda, Norikazu Matsunaga, Kyoko Takahashi, Akihiko Sumita, Kayoko Kinoshita, Junichi Azuma, Koichi Takahashi, Takahisa Matsuda

Publikováno v: Advances in Experimental Medicine and Biology ISBN: 9781461349136

There has recently been an increased demand for nutritional supplements and health drinks containing taurine. The Japanese diet also provides high levels of taurine. In addition, 60% of the over-the-counter (OTC) drugs classified as vitamin-mixture m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a1658c7e2786d21aa6188b87f9cdfe49
https://doi.org/10.1007/978-1-4615-0077-3_30

Zobrazit plný text záznamu

Abstract C255: Discovery of TAK-632: A selective kinase inhibitor of pan-RAF with potent antitumor activity against BRAF and NRAS mutant melanomas

Autor: Masaaki Hirose, Kathleen Aertgeerts, Terufumi Takagi, Shunichirou Tsutsumi, Akihiko Sumita, Noriko Uchiyama, Tsuneaki Tottori, Takeo Arita, Yoshitaka Inui, Masanori Okaniwa, Bi-Ching Sang, Tomoyasu Ishikawa, Akito Nakamura, Tomohiro Kawamoto, Masato Yabuki, Sei Yoshida, Jason Yano

Publikováno v: Molecular Cancer Therapeutics. 12:C255-C255

The RAF family kinases play critical roles in cancer progression. Recently, BRAF selective inhibitors have shown significant clinical efficacy in melanoma patients bearing oncogenic BRAFV600E mutation. However, several studies reported that RAF inhib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a1e7fa48d2d68b8e155a068a66b3b8a2
https://doi.org/10.1158/1535-7163.targ-13-c255

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání