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» Authors » Bunnai Saito

Bunnai Saito

Explore the profile of Bunnai Saito including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 23
Citations 200
Followers 0
Related Specialties
Chemistry
Biochemistry
Biology
Top 10 Co-Authors
Tsutomu Katsuki
Kazuhiro Matsumoto
Tomoyasu Ishikawa
Shinichi Imamura
Hiroyuki Sumi
Kentaro Hashimoto
Zenyu Shiokawa
Sei Yoshida
Masato Yabuki
Kazunobu Aoyama
Published In
Angew Chem Int Ed Engl
J Am Chem Soc
J Med Chem
Bioorg Med Chem
Chirality
Affiliations
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Recent Articles
1.
CDK8/19 inhibition plays an important role in pancreatic β-cell induction from human iPSCs
Sakuma K, Tsubooka-Yamazoe N, Hashimoto K, Sakai N, Asano S, Watanabe-Matsumoto S, et al.
Stem Cell Res Ther . 2023 Jan; 14(1):1. PMID: 36600289
Background: Transplantation of differentiated cells from human-induced pluripotent stem cells (hiPSCs) holds great promise for clinical treatments. Eliminating the risk factor of malignant cell transformation is essential for ensuring the...
2.
Ring-opening fluorination of bicyclic azaarenes
Komatsuda M, Suto A, Kondo Jr H, Takada H, Kato K, Saito B, et al.
Chem Sci . 2022 Feb; 13(3):665-670. PMID: 35173930
We have discovered a ring-opening fluorination of bicyclic azaarenes. Upon treatment of bicyclic azaarenes such as pyrazolo[1,5-]pyridines with electrophilic fluorinating agents, fluorination of the aromatic ring is followed by a...
3.
New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase
Tanaka Y, Kurasawa O, Yokota A, Klein M, Saito B, Matsumoto S, et al.
ACS Med Chem Lett . 2021 Aug; 11(8):1645-1652. PMID: 34345355
Deoxyhypusine synthase (DHPS) is the primary enzyme responsible for the hypusine modification and, thereby, activation of the eukaryotic translation initiation factor 5A (eIF5A), which is key in regulating the protein...
4.
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase
Tanaka Y, Kurasawa O, Yokota A, Klein M, Ono K, Saito B, et al.
J Med Chem . 2020 Mar; 63(6):3215-3226. PMID: 32142284
Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in...
5.
Identification of 2,6-Disubstituted 3-Imidazo[4,5-]pyridines as Therapeutic Agents for Dysferlinopathies through Phenotypic Screening on Patient-Derived Induced Pluripotent Stem Cells
Takada H, Kaieda A, Tawada M, Nagino T, Sasa K, Oikawa T, et al.
J Med Chem . 2019 Sep; 62(20):9175-9187. PMID: 31550153
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...
6.
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents
Kojima T, Asano Y, Kurasawa O, Hirata Y, Iwamura N, Wong T, et al.
Bioorg Med Chem . 2018 Apr; 26(9):2452-2465. PMID: 29669694
We pursued serine palmitoyltransferase (SPT) inhibitors as novel cancer therapeutic agents based on a correlation between SPT inhibition and growth suppression of cancer cells. High-throughput screening and medicinal chemistry efforts...
7.
Screening and Characterization of Hydrate Forms of T-3256336, a Novel Inhibitor of Apoptosis (IAP) Protein Antagonist
Takeuchi S, Kojima T, Hashimoto K, Saito B, Sumi H, Ishikawa T, et al.
Chem Pharm Bull (Tokyo) . 2015 Nov; 63(11):858-65. PMID: 26521850
Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability...
8.
Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells
Shiokawa Z, Hashimoto K, Saito B, Oguro Y, Sumi H, Yabuki M, et al.
Bioorg Med Chem . 2013 Oct; 21(24):7938-54. PMID: 24169315
We previously reported octahydropyrrolo[1,2-a]pyrazine derivative 2 (T-3256336) as a potent antagonist for inhibitors of apoptosis (IAP) proteins. Because compound 2 was susceptible to MDR1 mediated efflux, we developed another scaffold,...
9.
Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists
Asano M, Hashimoto K, Saito B, Shiokawa Z, Sumi H, Yabuki M, et al.
Bioorg Med Chem . 2013 Aug; 21(18):5725-37. PMID: 23928071
We recently reported the discovery of octahydropyrrolo[1,2-a]pyrazine A as a lead compound for an inhibitor of apoptosis proteins (IAP) antagonist. To develop IAP antagonists with favorable PK profiles, we designed...
10.
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic
Hashimoto K, Saito B, Miyamoto N, Oguro Y, Tomita D, Shiokawa Z, et al.
J Med Chem . 2013 Jan; 56(3):1228-46. PMID: 23298277
To develop novel inhibitor of apoptosis (IAP) proteins antagonists, we designed a bicyclic octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline bioisostere. This design was based on the X-ray co-crystal structure of...