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Article ; Online: Development of STING degrader with double covalent ligands.

Nakamura, Miki / Ohoka, Nobumichi / Shibata, Norihito / Inoue, Takao / Tsuji, Genichiro / Demizu, Yosuke

Bioorganic & medicinal chemistry letters

2024 Volume 102, Page(s) 129677

Abstract: Stimulator of interferon genes (STING), a homodimeric membrane receptor localized in the endoplasmic reticulum, plays a pivotal role in signaling innate immune responses. Inhibitors and proteolysis-targeting chimeras (PROTACs) targeting STING are ... ...

Abstract	Stimulator of interferon genes (STING), a homodimeric membrane receptor localized in the endoplasmic reticulum, plays a pivotal role in signaling innate immune responses. Inhibitors and proteolysis-targeting chimeras (PROTACs) targeting STING are promising compounds for addressing autoinflammatory and autoimmune disorders. In this study, we used a minimal covalent handle recently developed as the ligand portion of an E3 ligase. The engineered STING degrader with a low molecular weight compound covalently binds to STING and E3 ligase. Degrader 2 showed sustained STING degradation activity at lower concentrations (3 µM, 48 h, about 75 % degradation) compared to a reported STING PROTAC, SP23. This discovery holds significance for its potential in treating autoinflammatory and autoimmune diseases, offering promising avenues for developing more efficacious STING-targeted therapies.
MeSH term(s)	Proteolysis ; Ligands ; Ubiquitin-Protein Ligases/metabolism ; Signal Transduction
Chemical Substances	Ligands ; Ubiquitin-Protein Ligases (EC 2.3.2.27)
Language	English
Publishing date	2024-02-24
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2024.129677
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Article ; Online: CRBN ligand expansion for hematopoietic prostaglandin D

Osawa, Hinata / Kurohara, Takashi / Ito, Takahito / Shibata, Norihito / Demizu, Yosuke

Bioorganic & medicinal chemistry

2023 Volume 84, Page(s) 117259

Abstract: An increasing number of research reports are describing modifications of the E3 ligand, in particular, cereblon (CRBN) ligands, to improve the chemical and metabolic stabilities as well as the physical properties of PROTACs. In this study, phenyl- ... ...

Abstract	An increasing number of research reports are describing modifications of the E3 ligand, in particular, cereblon (CRBN) ligands, to improve the chemical and metabolic stabilities as well as the physical properties of PROTACs. In this study, phenyl-glutarimide (PG) and 6-fluoropomalidomide (6-F-POM), recently used as CRBN ligands for PROTAC design, were applied to hematopoietic prostaglandin D
MeSH term(s)	Ligands ; Prostaglandins/metabolism ; Proteolysis ; Ubiquitin-Protein Ligases/chemistry ; Ubiquitin-Protein Ligases/metabolism ; Proteolysis Targeting Chimera/chemistry ; Proteolysis Targeting Chimera/pharmacology
Chemical Substances	Ligands ; Prostaglandins ; Ubiquitin-Protein Ligases (EC 2.3.2.27) ; CRBN protein, human ; prostaglandin R2 D-isomerase (EC 5.3.99.2) ; Proteolysis Targeting Chimera
Language	English
Publishing date	2023-03-30
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1161284-8
ISSN	1464-3391 ; 0968-0896
ISSN (online)	1464-3391
ISSN	0968-0896
DOI	10.1016/j.bmc.2023.117259
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Zs.A 3815: Show issues

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Article ; Online: Development of a degrader against oncogenic fusion protein FGFR3-TACC3.

Shibata, Norihito / Cho, Nobuo / Koyama, Hiroo / Naito, Mikihiko

Bioorganic & medicinal chemistry letters

2022 Volume 60, Page(s) 128584

Abstract: Fibroblast growth factor receptor 3-transforming acidic coiled-coil containing protein 3 (FGFR3-TACC3), which has been identified in many cancers such as glioblastoma and bladder cancer, is a potent oncogenic fusion protein that induces constitutive ... ...

Abstract	Fibroblast growth factor receptor 3-transforming acidic coiled-coil containing protein 3 (FGFR3-TACC3), which has been identified in many cancers such as glioblastoma and bladder cancer, is a potent oncogenic fusion protein that induces constitutive activation of FGFR signaling, resulting in uncontrolled cell proliferation. Although several tyrosine kinase inhibitors against FGFR are currently under development, resistance to such types of inhibitors in patients has become a concern. In this study, a chimeric molecule SNIPER(TACC3)-11 (5a) was developed and found to reduce FGFR3-TACC3 levels effectively. Compound 5a conjugated KHS108 (a TACC3 ligand) to an LCL161 derivative (11) (an inhibitor of apoptosis protein [IAP] ligand) with a PEG linker (n = 2). Mechanistical analysis showed that cellular IAP1 was required for the reduction of FGFR3-TACC3 levels. Consistent with the decrease in FGFR3-TACC3 levels, compound 5a suppressed the growth of FGFR3-TACC3 positive cells. Thus, compound 5a is a candidate therapeutic with a novel drug modality against cancers that exhibit FGFR3-TACC3-dependent proliferation and exerts pharmacological effects distinct from FGFR3 kinase inhibitors because it lacks substructures crucial for kinase inhibition.
MeSH term(s)	Humans ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Development ; Drug Screening Assays, Antitumor ; Microtubule-Associated Proteins/antagonists & inhibitors ; Microtubule-Associated Proteins/metabolism ; Molecular Structure ; Receptor, Fibroblast Growth Factor, Type 3/antagonists & inhibitors ; Receptor, Fibroblast Growth Factor, Type 3/metabolism ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; FGFR3 protein, human (EC 2.7.10.1) ; Microtubule-Associated Proteins ; Receptor, Fibroblast Growth Factor, Type 3 (EC 2.7.10.1) ; TACC3 protein, human ; Sniper(tacc3)-2
Language	English
Publishing date	2022-01-24
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2022.128584
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Article: [Comparison of DNA Extraction Methods for Processed Foods Containing Soybean or Maize].

Egi, Tomohiro / Takabatake, Reona / Kishine, Masahiro / Soga, Keisuke / Yoshiba, Satoko / Shibata, Norihito / Kondo, Kazunari / Takashima, Yasuharu

Shokuhin eiseigaku zasshi. Journal of the Food Hygienic Society of Japan

2024 Volume 65, Issue 2, Page(s) 25–30

Abstract: Processed foods containing soybean or maize are subject to labeling regulations pertinent to genetically modified (GM) foods in Japan. To confirm the reliability of the labeling procedure of GM foods, the Japanese standard analytical methods (standard ... ...

Abstract	Processed foods containing soybean or maize are subject to labeling regulations pertinent to genetically modified (GM) foods in Japan. To confirm the reliability of the labeling procedure of GM foods, the Japanese standard analytical methods (standard methods) using real-time PCR technique have been established. Although certain DNA extraction protocols are stipulated as standard in these methods, the use of other protocols confirmed to be equivalent to the existing ones was permitted. In this study, the equivalence testing of the techniques employed for DNA extraction from processed foods containing soybean or corn was conducted. In this study, the equivalence testing of the techniques employed for DNA extraction from processed foods containing soybean or maize was conducted. The silica membrane-based DNA extraction kits, GM quicker 4 and DNeasy Plant Maxi Kit (Maxi Kit), as an existing method were compared. GM quicker 4 was considered to be equivalent to or better than Maxi Kit.
MeSH term(s)	DNA, Plant/isolation & purification ; DNA, Plant/genetics ; Food Analysis/methods ; Food Labeling ; Food, Genetically Modified ; Food, Processed ; Glycine max/chemistry ; Glycine max/genetics ; Japan ; Plants, Genetically Modified/genetics ; Plants, Genetically Modified/chemistry ; Real-Time Polymerase Chain Reaction ; Zea mays/chemistry ; Zea mays/genetics
Chemical Substances	DNA, Plant
Language	Japanese
Publishing date	2024-04-24
Publishing country	Japan
Document type	Journal Article ; Comparative Study ; English Abstract
ZDB-ID	604314-8
ISSN	1882-1006 ; 0015-6426
ISSN (online)	1882-1006
ISSN	0015-6426
DOI	10.3358/shokueishi.65.25
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Article ; Online: Control of STING Agonistic/Antagonistic Activity Using Amine-Skeleton-Based c-di-GMP Analogues.

Yanase, Yuta / Tsuji, Genichiro / Nakamura, Miki / Shibata, Norihito / Demizu, Yosuke

International journal of molecular sciences

2022 Volume 23, Issue 12

Abstract: Stimulator of Interferon Genes (STING) is a type of endoplasmic reticulum (ER)-membrane receptor. STING is activated by a ligand binding, which leads to an enhancement of the immune-system response. Therefore, a STING ligand can be used to regulate the ... ...

Abstract	Stimulator of Interferon Genes (STING) is a type of endoplasmic reticulum (ER)-membrane receptor. STING is activated by a ligand binding, which leads to an enhancement of the immune-system response. Therefore, a STING ligand can be used to regulate the immune system in therapeutic strategies. However, the natural (or native) STING ligand, cyclic-di-nucleotide (CDN), is unsuitable for pharmaceutical use because of its susceptibility to degradation by enzymes and its low cell-membrane permeability. In this study, we designed and synthesized CDN derivatives by replacing the sugar-phosphodiester moiety, which is responsible for various problems of natural CDNs, with an amine skeleton. As a result, we identified novel STING ligands that activate or inhibit STING. The cyclic ligand
MeSH term(s)	Amines ; Cyclic GMP/analogs & derivatives ; Ligands ; Membrane Proteins/metabolism ; Nucleotides, Cyclic/metabolism ; Skeleton/metabolism
Chemical Substances	Amines ; Ligands ; Membrane Proteins ; Nucleotides, Cyclic ; bis(3',5')-cyclic diguanylic acid (61093-23-0) ; Cyclic GMP (H2D2X058MU)
Language	English
Publishing date	2022-06-20
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms23126847
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Article ; Online: Providing appropriate information to consumers boosts the acceptability of genome-edited foods in Japan.

Taguchi, Chie / Shibata, Norihito / Soga, Keisuke / Yoshiba, Satoko / Narushima, Jumpei / Sugino, Miyu / Kondo, Kazunari

GM crops & food

2023 Volume 14, Issue 1, Page(s) 1–14

Abstract: The Japanese Health Ministry recently granted permission for the market distribution of genome-edited (GE) foods, yet there remains a lack of full understanding among consumers regarding this technology. In this study, we conducted a survey to assess the ...

Abstract	The Japanese Health Ministry recently granted permission for the market distribution of genome-edited (GE) foods, yet there remains a lack of full understanding among consumers regarding this technology. In this study, we conducted a survey to assess the acceptability of GE foods among Japanese consumers and examined the impact of providing information about GE foods on their acceptability. We conducted a web-based survey among 3,408 consumers aged 20-69 years, focusing on three aspects: (1) the commercial availability of GE foods, (2) the consumption of GE foods by others, and (3) your own consumption of GE foods. The survey findings revealed that participants were most accepting of the consumption of GE foods by others, followed by their acceptance of GE foods being commercially available. Notably, participants' acceptance of GE foods increased in all three aspects after they viewed an informative video. The video had a particularly strong impact on participants who fully or partially understood its content, compared to those who did not. Furthermore, regression analyses showed that participants' understanding of two key areas, namely "Why are GE foods important" and "What procedures are in place to ensure the safety of GE foods," played a crucial role in increasing acceptability. Overall, these results indicate that providing information about GE foods to Japanese consumers can effectively enhance their acceptance of such foods. The findings highlight the importance of understanding the benefits and safety measures associated with GE foods in influencing consumer attitudes.
MeSH term(s)	Japan ; Dietary Supplements ; Surveys and Questionnaires ; Consumer Behavior
Language	English
Publishing date	2023-07-31
Publishing country	United States
Document type	Journal Article
ZDB-ID	2706099-8
ISSN	2164-5701 ; 2164-5701
ISSN (online)	2164-5701
ISSN	2164-5701
DOI	10.1080/21645698.2023.2239539
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Rapid Screening Detection of Genetically Modified Papaya by Loop-Mediated Isothermal Amplification.

Takabatake, Reona / Kagiya, Yukari / Futo, Satoshi / Minegishi, Yasutaka / Soga, Keisuke / Shibata, Norihito / Kondo, Kazunari

Biological & pharmaceutical bulletin

2023 Volume 46, Issue 5, Page(s) 713–717

Abstract: A loop-mediated isothermal amplification (LAMP)-mediated screening detection method for genetically modified (GM) papaya was developed targeting the 35S promoter (P35S) of the cauliflower mosaic virus. LAMP products were detected using a Genie II real- ... ...

Abstract	A loop-mediated isothermal amplification (LAMP)-mediated screening detection method for genetically modified (GM) papaya was developed targeting the 35S promoter (P35S) of the cauliflower mosaic virus. LAMP products were detected using a Genie II real-time fluorometer. The limit of detection (LOD) was evaluated and found to be ≤0.05% for papaya seeds. We also designed a primer set for the detection of the papaya endogenous reference sequence, chymopapain, and the species-specificity was confirmed. To improve cost-effectiveness, single-stranded tag hybridization (STH) on a chromatography printed-array strip (C-PAS) system, which is a lateral flow DNA chromatography technology, was applied. LAMP amplification was clearly detected by the system at the LOD level, and a duplex detection of P35S and chymopapain was successfully applied. This simple and quick method for the screening of GM papaya will be useful for the prevention of environmental contamination of unauthorized GM crops.
MeSH term(s)	Carica/genetics ; Chymopapain ; Plants, Genetically Modified/genetics ; Nucleic Acid Amplification Techniques/methods ; Vegetables ; Sensitivity and Specificity
Chemical Substances	Chymopapain (EC 3.4.22.6)
Language	English
Publishing date	2023-04-15
Publishing country	Japan
Document type	Journal Article
ZDB-ID	1150271-x
ISSN	1347-5215 ; 0918-6158
ISSN (online)	1347-5215
ISSN	0918-6158
DOI	10.1248/bpb.b22-00874
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Zs.A 1474: Show issues

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Article ; Online: Surgical treatment of tracheocutaneous fistula and tracheostomy scars using a hinged flap and local myocutaneous flap.

Shimada, Kazuki / Komiya, Takako / Ito, Norihito / Sato, Munenori / Ida, Yukiko / Shibata, Dai / Matsumura, Hajime

International wound journal

2023 Volume 20, Issue 7, Page(s) 2499–2504

Abstract: Tracheocutaneous fistula and tracheostomy scar are complications associated with the prolonged use of tracheostomy tubes. They have functional and cosmetic problems owing to tracheal tugging during swallowing and easily visible scars. Although many ... ...

Abstract	Tracheocutaneous fistula and tracheostomy scar are complications associated with the prolonged use of tracheostomy tubes. They have functional and cosmetic problems owing to tracheal tugging during swallowing and easily visible scars. Although many procedures exist to correct this issue, there is no consensus on the optimal surgical technique. Therefore, an ideal surgical procedure was devised. The study was performed on 12 patients between September 2016 and May 2021. All patients had persistent tracheocutaneous fistulas or hypertrophic scars on the neck after tracheostomy. All procedures were performed using a hinged flap and two myocutaneous local flaps. All patients had no complications, and their aesthetics were excellent in postoperative photographs. The scar was better on the straight scar when the flap's skin is denuded than on the VY advancement flap. It should be noted, however, that this procedure can cause the flap to become congested in a short period after head and neck surgery. This procedure is safe, reliable and simple for surgical closure. This was found to produce excellent cosmetic results with no major complications.
MeSH term(s)	Humans ; Tracheostomy/adverse effects ; Tracheostomy/methods ; Myocutaneous Flap ; Cutaneous Fistula/complications ; Tracheal Diseases/etiology ; Tracheal Diseases/surgery ; Cicatrix, Hypertrophic
Language	English
Publishing date	2023-02-02
Publishing country	England
Document type	Journal Article
ZDB-ID	2170920-8
ISSN	1742-481X ; 1742-4801
ISSN (online)	1742-481X
ISSN	1742-4801
DOI	10.1111/iwj.14110
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Zs.A 6006: Show issues

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Article ; Online: Control of STING Agonistic/Antagonistic Activity Using Amine-Skeleton-Based c-di-GMP Analogues

Yuta Yanase / Genichiro Tsuji / Miki Nakamura / Norihito Shibata / Yosuke Demizu

International Journal of Molecular Sciences, Vol 23, Iss 6847, p

2022 Volume 6847

Abstract	Stimulator of Interferon Genes (STING) is a type of endoplasmic reticulum (ER)-membrane receptor. STING is activated by a ligand binding, which leads to an enhancement of the immune-system response. Therefore, a STING ligand can be used to regulate the immune system in therapeutic strategies. However, the natural (or native) STING ligand, cyclic-di-nucleotide (CDN), is unsuitable for pharmaceutical use because of its susceptibility to degradation by enzymes and its low cell-membrane permeability. In this study, we designed and synthesized CDN derivatives by replacing the sugar-phosphodiester moiety, which is responsible for various problems of natural CDNs, with an amine skeleton. As a result, we identified novel STING ligands that activate or inhibit STING. The cyclic ligand 7 , with a cyclic amine structure containing two guanines, was found to have agonistic activity, whereas the linear ligand 12 showed antagonistic activity. In addition, these synthetic ligands were more chemically stable than the natural ligands.
Keywords	STING ; cyclic dinucleotide ; amines ; drug design ; agonist ; antagonist ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2022-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D

Murakami, Yuki / Osawa, Hinata / Kurohara, Takashi / Yanase, Yuta / Ito, Takahito / Yokoo, Hidetomo / Shibata, Norihito / Naito, Mikihiko / Aritake, Kosuke / Demizu, Yosuke

RSC medicinal chemistry

2022 Volume 13, Issue 12, Page(s) 1495–1503

Abstract: Degradation of hematopoietic prostaglandin ... ...

Abstract	Degradation of hematopoietic prostaglandin D
Language	English
Publishing date	2022-09-23
Publishing country	England
Document type	Journal Article
ISSN	2632-8682
ISSN (online)	2632-8682
DOI	10.1039/d2md00284a
Database	MEDical Literature Analysis and Retrieval System OnLINE

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