2025

1

Kyoya T, Ishida H, Saitoh T, Itoh T*.

Preparation of ethynylsulfonamides and study of their reactivity with nucleophilic amino acids

Org. Biomol. Chem. 2025, 23, 1901−1908. [RSC]

 

2024

1

Yano T, Yamada T*, Ishida H, Ohashi N, Itoh T*.

2-cyanopyridine derivatives enable N-terminal cysteine bioconjugation and peptide bond cleavage of glutathione under aqueous and mild conditions

RSC Adv., 2024, 14, 6542-6547. [RSC]

 

2023

1

Kojima H, Yanagi R, Higuchi E, Yoshizawa M, Shimodaira T, Kumagai M, Kyoya T, Sekine M, Egawa D, Ohashi N, Ishida H, Yamamoto K, Itoh T.

Covalent Modifier Discovery using Hydrogen/Deuterium Exchange–Mass Spectrometry

J. Med. Chem. 2023, 66, 4827–4839. [ACS]

 

2

Sekine M, Ishida H, Itoh T.

Synthesis of triazolo[c]coumarins and differences in the fluorescence properties of their isomers

Asian J. Org. Chem. 2023, e202300013. [Wiley]

 

2022

1

Ito T, Miwa C, Haga Y, Kubo M, Itoh T, Yamamoto K, Mise S, Goto E, Tsuzuki T, Matsumura C,  Nakano T, Inui H.

Enantioselective metabolism of chiral polychlorinated biphenyl 2, 2′, 3, 4, 4′, 5′, 6-Heptachlorobiphenyl (CB183) by human and rat CYP2B subfamilies

Chemosphere 2022, 308, 136349. [ELSEVIER]

 

2

Differences in Enantioselective Hydroxylation of 2, 2′, 3, 6-Tetrachlorobiphenyl (CB45) and 2, 2′, 3, 4′, 6-Pentachlorobiphenyl (CB91) by Human and Rat CYP2B Subfamilies

Inui H, Ito T, Miwa C, Haga Y, Kubo M, Itoh T, Yamamoto K, Miyaoka M, Mori T, Tsuzuki H, Mise S, Goto E, Matsumura C, Nakano T

Environ. Sci. & Tec. 2022, 56, 10204-10215.[ACS]

 

3

Yoshizawa M, Aoyama T, Itoh T, Miyachi H.

Arylalkynyl amide-type peroxisome proliferator-activated receptor γ (PPARγ)-selective antagonists covalently bind to the PPARγ ligand binding domain with a unique binding mode

Bioorg. & Med. Chem. Lett. 2022, 64, 128676. [ELSEVIER]

 

4

Yabu M, Haga Y, Itoh T, Goto E, Suzuki M, Yamazaki K, Mise S, Yamamoto K, Matsumura C, Nakano T, Sakaki T, Inui H.

Hydroxylation and dechlorination of 3, 3′, 4, 4′-tetrachlorobiphenyl (CB77) by rat and human CYP1A1s and critical roles of amino acids composing their substrate-binding cavity

Sci. Total Environ. 2022, 155848. [ELSEVIER]

 

5

Ishida H*, Homma S, Kasuga R, Yamamoto K, Itoh T*.

Synthesis of Tetrahydrofuro[2,3-d]oxazoles and Oxazoles by Hypervalent Iodine (III)-Promoted [2 + 2 + 1] Annulation.

Chem. Pharm. Bull. 2022, 70, 192–194. DOI:10.1248/cpb.c21-01001 [CPB]

 

6

Takyo M, Sato Y, Hirata N, Tsuchiya K, Ishida H, Kurohara T, Yanase Y, Ito T, Kanda Y, Yamamoto K, Misawa T*, Demizu Y*.

Oligoarginine-conjugated peptide foldamers inhibiting vitamin D receptor-mediated transcription.

ACS Omega, 2022, 7, 46573–46582. DOI:10.1021/acsomega.2c05409 [ACS]

 

2021

1

Egawa D, Ogiso T, Nishikata K, Yamamoto K, Itoh T.

Structural Insights into the Loss-of-Function R288H Mutant of Human PPARγ

Biol. Pharm. Bull. 2021, 44, 1196-1201. DOI:10.1248/bpb.b21-00253 [BPB]

 

2

Yoshikawa C, Ishida H, Ohashi N, Itoh T.

Synthesis of a Coumarin-Based PPARγ Fluorescence Probe for Competitive Binding Assay.

Int. J. Mol. Sci. 2021, 22, 4034. DOI: 10.3390/ijms22084034 [IJMS]

 

3

Sasaki H, Masuno H, Kawasaki H, Yoshihara A, Numoto, N, Ito N, Ishida H, Yamamoto K, Hirata N, Kanda Y, Kawachi E, Kagechika H, and Tanatani A.

Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.

J. Med. Chem. 2021, 64, 516–526. DOI: 10.1021/acs.jmedchem.0c01420 [ACS]

 

4

Kanamori S, Ohashi N, Ishida H, Yamamoto K, Itoh T.

HNF4α Is a Covalent Bond-Forming Receptor.

J. Nutr. Sci. Vitaminol., 2021, 67, 126–129. DOI: 10.3177/jnsv.67.126 [JNSV] 

 

5

Yoshikawa C, Ishida H, Ohashi N, Kojima H, Itoh T.

Construction of 7-diethylaminocoumarins promoted by an electro-withdrawing group.

Chem. Pharm. Bull. 2021, 69, 608–611. DOI:10.1248/cpb.c21-00228 [CPB]

Featured Article

 

2020

1

Montanari R,* Capelli D, Yamamoto K, Awaishima H, Nishikata K, Barendregt A, Heck AJR, Loiodice F, Altieri F, Paiardini A, Grotessi A, Pirone L, Pedone E. M, Peiretti F, Brunel JM, Itoh T,* Pochetti G.*

Insights into PPARγ phosphorylation and its inhibition mechanism.

J. Med. Chem. 2020, 63, 4811–4823. DOI: 10.1021/acs.jmedchem.0c00048 [ACS]

 

2

Kamata S, Oyama T, Saito K, Honda A, Yamamoto Y, Suda K, Ishikawa R, Itoh T, Watanabe Y, Shibata T, Uchida K, Suematsu M, Ishii I.

PPARα Ligand-Binding Domain Structures with Endogenous Fatty Acids and Fibrates.

iScience. 2020, 23, 101727. DOI:10.1016/j.isci.2020.101727 [Cell]

 

3

Teratani T, Tomita K, Toma-Fukai S, Nakamura Y, Itoh T, Shimizu H, Shiraishi Y, Sugihara N, Higashiyama M, Shimizu T, Inoue I, Takenaka Y, Hokari R, Adachi T, Shimizu T, Miura S, Kanai T.

Redox-dependent PPARγ/Tnpo1 complex formation enhances PPARγ nuclear localization and signaling.

Free Radic Biol Med. 2020, 156, 45-56. [ELSEVIER]

4

Kojima H,* Itoh T.

Preparation and use of turn-on fluorescent probe for detection and live cell imaging of vitamin D receptor as a target protein.

STAR Protocols, 2020, 1, 100036. DOI: 10.1016/j.xpro.2020.100036 [Cell Press]

 

5

Yoshikawa C, Ishida H, Itoh T.

Incorporation of a coumarin unit by nucleophilic addition reaction into a PPARγ ligand.

Tetrahedron Lett. 2020, 61, 151842. DOI:10.1016/j.tetlet.2020.151842 [ELSEVIER]

 

6

Kojima H, Fujita Y, Takeuchi R, Ohashi N, Yamamoto K, Itoh T.

Cyclization Reaction-Based Turn-on Probe for Covalent Labeling of Target Proteins.

Cell Chem. Biol. 2020, 27, 334-349.E11. DOI:10.1016/j.chembiol.2020.01.006 [Cell Press] 

Cover Art / Featured Article / Most Read as of 27th Mar 2020

 

7

Turcotte C, Archambault AS, Dumais É, Martin C, Blanchet MR, Bissonnette E, Ohashi N, Yamamoto K, Itoh T, Laviolette M, Veilleux A, Boulet LP, Marzo VD, Flamand N.

Endocannabinoid hydrolysis inhibition unmasks that unsaturated fatty acids induce a robust biosynthesis of 2-arachidonoylglycerol and its congeners in human myeloid leukocytes.

FASEB J.  2020, 34, 4253-4265. DOI: 10.1096/fj.201902916R [WILEY]

 

2019

1

Kubo M, Yamamoto K, Itoh T.

Design and synthesis of selective CYP1B1 inhibitor via dearomatization of α-naphthoflavone.

Bioorg. Med. Chem. 2019, 27, 285–304. doi.org/10.1016/j.bmc.2018.11.045. [BMC]

 

2018

1

Kanamori S, Ishida H, Yamamoto K, Itoh T.

Construction of a series of intermediates in the β-oxidation pathway from THA to EPA via DHA in free acid form.

Bioorg. Med. Chem. 2018, 26, 4390–4401. doi:10.1016/j.bmc.2018.07.004. [BMC]

 

2

Goto E, Haga Y, Kubo M, Itoh T, Kasai C, Shoji O, Yamamoto K, Matsumura C, Nakano T, Inui H.

Metabolic enhancement of 2,3´,4,4´,5-pentachlorobiphenyl (CB118) using cytochrome P450 monooxygenase isolated from soil bacterium under the presence of perfluorocarboxylic acids (PFCAs) and the structural basis of its metabolism.

Chemosphere, 2018, 210, 376–383. doi:10.1016/j.chemosphere.2018.07.026. [ELSEVIER]

 

3

Yoshizawa M, Itoh T, Hori T, Kato A, Anami Y, Yoshimoto N, Yamamoto K.

Identification of the histidine residue in vitamin D receptor that covalently binds to electrophilic ligands.

J. Med. Chem. 2018, 61, 6339–6349. doi:10.1021/acs.jmedchem.8b00774. [ACS]

 

4

Itoh T,* Yoshimoto N, Hirano Y, Yamamoto K.*

Structural basis for the selective inhibition of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) by a selenium-containing inhibitor with chloro-aminopyridine as a basic group.

Bioorg. Med. Chem. Lett. 2018, 28, 2256–2260. doi: 10.1016/j.bmcl.2018.05.042. [BMCL]

Cover Art

 

2017

1

Kojima H, Itoh T, Yamamoto K.

On-site reaction for PPARγ modification using a specific bifunctional ligand.

Bioorg. Med. Chem. 2017, 25, 6492–6500. DOI: 10.1016/j.bmc.2017.10.024. [BMC]

 

2

Kato A, Yamao M, Hashihara Y, Ishida H, Itoh T, Yamamoto K.

Vitamin D analogues with a p-hydroxyphenyl group at the C25 position: crystal structure of vitamin D receptor ligand-binding domain complexed with the ligand explains the mechanism underlying full antagonistic action. 

J. Med. Chem. 2017, 60, 8394–8406. DOI: 10.1021/acs.jmedchem.7b00819. [ACS].

 

3

Yamamoto Y, Itoh T, Yamamoto K.

A study of synthetic approaches to 2-acyl DHA lysophosphatidic acid.

Org. Biomol. Chem. 2017, 15, 8186–8192. DOI: 10.1039/c7ob01771e. [RSC]

 

4

Ohura A, Itoh T, Ishida H, Saito A, Yamamoto K.

Three-Component Regioselective Synthesis of Tetrahydrofuro[2,3-d]oxazoles and their Efficient Conversion to Oxazoles.

Asian J. Org. Chem. 2017, 6, 673–676. DOI: 10.1002/ajoc.201700074 [ACES]

 

5

Egawa D, Itoh T, Kato A, Kataoka S, Anami Y, Yamamoto K.

SRC2-3 binds to vitamin D receptor with high sensitivity and strong affinity.

Bioorg. Med. Chem.  2017, 25, 568–574. DOI: 10.1016/j.bmc.2016.11.020 [BMC]

 

2016

1

Anami Y, Shimizu N, Ekimoto T,  Egawa D,  Itoh T,  Ikeguchi M,  Yamamoto K.

Apo- and Antagonist-Binding Structures of Vitamin D Receptor Ligand-Binding Domain Revealed by Hybrid Approach Combining Small-Angle X?ray Scattering and Molecular Dynamics.

J. Med. Chem. 2016, 59, 7888−7900. DOI: 10.1021/acs.jmedchem.6b00682. [ACS]

 

2

Egawa D, Itoh T, Akiyama Y, Saito T, Yamamoto K.

17-oxoDHA is a PPARα/γ dual covalent modifier and agonist.

ACS Chem. Biol. 2016, 11, 2447−2455. DOI: 10.1021/acschembio.6b00338 [ACS]

 

3

Kato A, Anami Y, Egawa D, Itoh T, Yamamoto K.

Helix12-stabilization antagonist of vitamin D receptor.

Bioconjugate Chem. 2016, 27, 1750−1761. DOI: 10.1021/acs.bioconjchem.6b00246[ACS]

 

4

Mise S, Haga Y, Itoh T, Kato A, Fukuda I, Goto E, Yamamoto K, Yabu M, Matsumura C, Nakano T, Sakaki T, Inui H.

Structural determinants of the position of 2,3’,4,4’,5-pentachlorobiphenyl (CB118) hydroxylation by mammalian cytochrome P450 monooxygenases.

Toxicol. Sci. 2016, 152, 340−348. doi: 10.1093/toxsci/kfw086 [PubMed]

 

5

Itoh T, Saito T, Yamamoto Y, Ishida H, Yamamoto K.

Gram scale synthesis of specialized pro-resolving mediator 17(S)-HDHA using lipoxygenase enhanced by water-soluble reducing agent TCEP.

Bioorg. Med. Chem. Lett. 2016, 26, 343-345. Doi:10.1016/j.bmcl.2015.12.011.  [BMCL]

 

2015

1

Anami Y, Sakamaki Y, Itoh T, Inaba Y, Nakabayashi M, Ikura T, Ito N, Yamamoto K.

Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.

Bioorganic. Med. Chem. 2015, 23, 7274–81. doi:10.1016/j.bmc.2015.10.026. [BMC]

 

2

Yamamoto Y, Itoh T, Yamamoto K.

Chemical Synthesis of a Very Long Chain Fatty Acid, Hexacosanoic Acid (C26:0), and the Ceramide Containing Hexacosanoic Acid.

J. Nutr. Sci. Vitaminol. 2015, 61<