Mellini P, Itoh Y, Elboray EE, Tsumoto H, Li Y, Suzuki M, Takahashi Y, Tojo T, Kurohara T, Miyake Y, Miura Y, Kitao Y, Kotoku M, Iida T, Suzuki T. Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the “Selectivity Pocket”, Substrate-Binding Site, and NAD+-Binding Site. J. Med. Chem. 2019, 62, 5844-5862. Supplementary Cover.
Etani T, Naiki T, Naiki-Ito A, Suzuki T, Iida K, Nozaki S, Kato H, Nagayasu Y, Suzuki S, Kawai N, Yasui T, Takahashi S. NCL1, a highly selective lysine-specific demethylase 1 inhibitor, suppresses castration-resistant prostate cancer growth via regulation of apoptosis and autophagy. J. Clin. Med. 2019, 8, 442.
Jaikhan P, Buranrat B, Itoh Y, Chotitumnavee J, Kurohara T, Suzuki T. Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors. Bioorg. Med. Chem. Lett. 2019, 29, 1173-1176.
Kotoku M, Maeba T, Fujioka S, Yokota M, Seki N, Ito K, Suwa Y, Ikenogami T, Hirata K, Hase Y, Katsuda Y, Miyagawa N, Arita K, Asahina K, Noguchi M, Nomura A, Doi S, Adachi T, Crowe P, Tao H, Thacher S, Hashimoto H, Suzuki T, Shiozaki M. Discovery of the Second Generation RORg Inhibitors Composed of an Azole Scaffold. J. Med. Chem. 2019, 62, 2837-2842.
Miyake Y, Itoh Y, Hatanaka A,Suzuma Y, Suzuki M, Kodama H, Arai Y, Suzuki T. Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy. Bioorg. Med. Chem. 2019, 27, 1119-1129.
Itoh Y, Nakashima Y, Tsukamoto S, Kurohara T, Suzuki M, Sakae Y, Oda M, Okamoto Y, Suzuki T. N+-C-H…O Hydrogen bonds in protein-ligand complexes. Sci. Rep. 2019, 9, 767.Top 100 in Chemistry
Ota Y, Nakamura A, Elboray EE, Itoh Y, Suzuki T. Design, synthesis, and biological evaluation of a conjugate of 5-fluorouracil and an LSD1 inhibitor. Chem. Pharm. Bull. 2019, 192-195.
Qin R, Takayanagi S, Kondo Y, Li J, Shiga N, Nakajima M, Shinohara K, Yoda N, Suzuki T, Kaneda A, Nemoto T. Synthesis of LSD1 Inhibitor-Pyrrole Imidazole Polyamide Conjugates for Region-Specific Alterations of Histone Modification. Heterocycles 2019, 99, 891-905.
Yukihiro Itoh Identification of a KDM5C Inhibitor and Its Biological Evaluation. 10th Joint RSC-CSJ Symposium: Chemistry for Complex Biological Systems Sep 2019 (Kyoto)
Yuka Miyake, Yukihiro Itoh, Yoshinori Suzuma, Hidehiko Kodama, Shusaku, Uchida. In situ click reaction activated by a metal ion in targeted proteins: Identification of a triazole compound as a lysine demethylase 5C inhibitor The 27th International Society of Heterocyclic Chemistry Congress Sep 2019 (Kyoto)
Takayoshi Suzuki. Chemical Control of Epigenetics for the Treatment of Cancers and Neurological Disorders. The 27th French-Japanese Symposium on Medicinal and Fine Chemistry L4 Mar 2019 (Fukuoka)
Pattaporn Jaikhan, Yukihiro Itoh, Takayoshi Suzuki. Identification of ortho-substituted anilide as a new pharmacophore for KDM5 inhibitors. The 27th French-Japanese Symposium on Medicinal and Fine Chemistry Mar 2019 (Fukuoka)
原著論文
Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos-Morales E, Da Veiga C, Kalinin D, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce RJ, Jung M, Sippl W, Romier C. Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants. J. Med. Chem. 2018, 61, 10000-10016.
Matsui M, Terasawa K, Kajikuri J, Kito H, Endo K, Jaikhan P, Suzuki T, Ohya S. Histone Deacetylases Enhance Ca2+-Activated K+ Channel KCa3.1 Expression in Murine Inflammatory CD4+ T Cells. Int. J. Mol. Sci. 2018, 19, E2942.
Kozako T, Mellini P, Ohsugi T, Aikawa A, Uchida Y, Honda S, Suzuki T. Novel small molecule SIRT2 inhibitors induce cell death in leukemic cell lines. BMC Cancer. 2018, 18, 791.
Alagarswamy K, Shinohara K, Takayanagi S, Fukuyo M, Okabe A, Rahmutulla B, Yoda N, Qin R, Shiga N, Sugiura M, Sato H, Kita K, Suzuki T, Nemoto T, Kaneda A. “Region-specific alteration of histone modification by LSD1 inhibitor conjugated with pyrrole-imidazole polyamide” Oncotarget 2018,9,29316-29335.
Ota Y, Kakizawa T, Itoh Y, Suzuki T. “Design, Synthesis, and In Vitro Evaluation of Novel Histone H3 Peptide-Based LSD1 Inactivators Incorporating α,α-Disubstituted Amino Acids with γ-Turn-Inducing Structures” Molecules 2018, 23, 1099.
Yamamoto R, Kawahara M, Ito S, Satoh J, Tatsumi G, Hishizawa M, Suzuki T, Andoh A. “Selective dissociation between LSD1 and GFI1B by a LSD1 inhibitor NCD38 induces the activation of ERG super-enhancer in erythroleukemia cells” Oncotarget 2018, 9, 21007-21021.
Tsukamoto S, Sakae Y, Itoh Y, Suzuki T, Okamoto Y. Computational analysis for selectivity of histone deacetylase inhibitor by replica-exchange umbrella sampling molecular dynamics simulations. J. Chem. Phys. 2018, 148, 125102.
Katayama S, Morii A, Makanga JO, Suzuki T, Miyata N, Inazu T. HDAC8 regulates neural differentiation through embryoid body formation in P19 cells. Biochem. Biophys. Res. Commun. 2018, 498, 45-51.
Ota Y, Miyamura S, Araki M, Itoh Y, Yasuda S, Masuda M, Taniguchi T, Sowa Y, Sakai T, Itami K, Yamaguchi J, Suzuki T. Design, synthesis and evaluation of γ-turn mimetics as LSD1-selective inhibitors. Bioorg. Med. Chem. 2018, 26, 775-785.
Kakizawa T, Ota Y, Itoh Y, Suzuki T. Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors. Bioorg. Med. Chem. Lett. 2018, 28, 167-169.
Pattaporn Jaikhan、伊藤幸裕、鈴木孝禎 Identification of o-substituted anilide compounds as histone lysine demethylase inhibitors 日本薬学会第138年会 27PA-pm134 2018年3月 金沢
国際学会・海外での発表
Yosuke Ota, Yukihiro Itoh, Takayoshi Suzuki. Controlled Release of Anticancer Drugs by LSD1 Inhibition. 4th International Symposium for Medicinal Sciences 27O-ISMS10 Mar 2018 (Kanazawa)
原著論文
Mellini P, Itoh Y, Tsumoto H, Li Y, Suzuki M, Tokuda N, Kakizawa T, Miura Y, Takeuchi J, Lahtela-Kakkonene M, Suzuki T. Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, “selectivity pocket” and NAD+-binding site. Chem. Sci. 2017, 8, 6400-6408.
Sugino N, Kawahara M, Tatsumi G, Kanai A, Matsui H, Yamamoto R, Nagai Y, Fujii S, Shimazu Y, Hishizawa M, Inaba T, Andoh A, Suzuki T, Takaori-Kondo A. A novel LSD1 inhibitor NCD38 ameliorates MDS-related leukemia with complex karyotype by attenuating leukemia programs via activating super-enhancer. Leukemia 2017, 31, 2303-2314.
Erburu M, Munoz-Cobo I, Diaz T, Mellini P, Suzuki T, Puerta E, Tordera RM. SIRT2 inhibition modulate glutamate and serotonin systems in the prefrontal cortex and induces antidepressant-like action. Neuropharmacology 2017, 117, 195-208.
Uchida S, Teubner BJW, Hevi C, Hara K, Kobayashi A, Dave RM, Shintaku T, Jaikhan P, Yamagata H, Suzuki T, Watanabe Y, Zakharenko SS, Shumyatsky GP. CRTC1 Nuclear Translocation Following Learning Modulates Memory Strength via Exchange of Chromatin Remodeling Complexes on the Fgf1 Gene. Cell Rep. 2017, 18, 352-366.
Sareddy GR, Viswanadhapalli S, Surapaneni P, Suzuki T, Brenner A, Vadlamudi R. Novel KDM1A inhibitors induce differentiation and apoptosis of glioma stem cells via unfolded protein response (UPR) pathway. Oncogene 2017, 36,2423-2434.
Fujimoto M, Inoue T, Kito H, Niwa S, Suzuki T, Muraki K, Ohya S. Transcriptional repression of HER2 by ANO1 Cl- channel inhibition in human breast cancer cells with resistance to trastuzumab. Biochem. Biophys. Res. Commun. 2017, 482, 188-194.
Paolo MELLINI、 伊藤幸裕、津元裕樹、李頴、鈴木美紀、徳田奈津子、柿澤多恵子、三浦ゆり、竹内淳、Maija LAHTELA-KAKKONEN、鈴木孝禎 Potent Mechanism-Based Sirtuin 2-Selective Inhibition by an in Situ Generated Occupant of Selectivity Pocket, Substrate-Binding Site, and NAD+-Bindig Pocket. 日本薬学会第137年会 26R-pm16 2017年3月 仙台
Pattaporn JAIKHAN、伊藤幸裕、鈴木孝禎 Design and Screening of an o-Substituted Anilide Library for Histone Lysine Demethylase Inhibitors. 日本薬学会第137年会 27PA-am032 2017年3月 仙台
Khatun A, Fujimoto M, Kito H, Niwa S, Suzuki T, Ohya S. Down-regulation of the Ca2+-activated K+ channel KCa1.1 in human breast cancer cells treated with vitamin D receptor agonists. Int. J. Mol. Sci. 2016, 17, 2083.
Ota Y, Itoh Y, Kaise A, Ohta K, Endo Y, Masuda M, Sowa Y, Sakai T, Suzuki T. Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen. Angew. Chem. Int. Ed. 2016, 55, 16115-16118.
Miyamura S, Araki M, Ota Y, Itoh Y, Yasuda S, Masuda M, Taniguchi T, Sowa Y, Sakai T, Suzuki T, Itami K, Yamaguchi J. C-H Activation Enables Rapid Structure-Activity Relationship Study of Arylcylclopropyl Amines for Potent and Selective LSD1 Inhibitors. Org. Biomol. Chem. 2016, 14, 8576-8585.
Higuchi F, Uchida S, Yamagata H, Abe-Higuchi N, Hobara T, Hara K, Kobayashi A, Shintaku T, Itoh Y, Suzuki T, Watanabe Y. Hippocampal microRNA-124 enhances chronic stress resilience in mice. J. Neurosci. 2016, 36, 7253-7267.
Men TT, van Thanh DN, Yamaguchi M, Suzuki T, Hattori G, Arii M, Huy NT, Kamei K. A Drosophila model for screening anti-obesity agents. BioMed Res. Int. 2016, 2016:6293163.
Wu X, Fang Z, Yang B, Zhong L, Yang Q, Zhang C, Huang S, Xiang R, Suzuki T, Li LL, Yang SY. Discovery of KDM5A Inhibitors: Homology Modeling, Virtual Screening and Structure-Activity Relationship Analysis. Bioorg. Med. Chem. Lett. 2016, 26, 2284-2288.
Kanatsuka S, Hatano N, Matsuba S, Fujimoto M, Niwa S, Kito H, Zhan P, Suzuki T, Muraki K, Ohya S. Downregulation of the Ca2+-activated K+ channel KCa3.1 by histone deacetylase inhibition in human breast cancer cells. Pharmacol. Res. Perspect. 2016, 4, e00228.
Kakizawa T, Mizukami T, Itoh Y, Hasegawa M, Sasaki R, Suzuki T. Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide. Bioorg. Med. Chem. Lett. 2016, 26, 1193-1195.
Itoh Y, Aihara K, Mellini P, Tojo T, Ota Y, Tsumoto H, Solomon VR, Zhan P, Suzuki M, Ogasawara D, Shigenaga A, Inokuma T, Nakagawa H, Miyata N, Mizukami T, Otaka A, Suzuki T. Identification of SNAIL1 Peptide-Based Irreversible Lysine Specific Demethylase 1-Selective Inactivators. J. Med. Chem. 2016, 59, 1531-1544.
Hoshino I, Akutsu Y, Murakami K, Akanuma N, Isozaki Y, Maruyama T, Toyozumi T, Matsumoto Y, Suito H, Takahashi M, Sekino N, Komatsu A, Suzuki T, Matsubara H. Histone Demethylase LSD1 Inhibitors Prevent Cell Growth by Regulating Gene Expression in Esophageal Squamous Cell Carcinoma Cells. Ann. Surg. Oncol. 2016, 23, 312-320.
総説
Itoh Y, Suzuki T. Molecular Technology for Controlling Epigenetics: Regulation of Histone Acetylation and Methylation by Small Molecules. J. Syn. Org. Chem. Jpn. 2016, 74, 441-452.
Sakae Y, Nishikawa N, Tsukamoto S, Suzuki T, Okamoto Y. Molecular simulations of protein systems toward drug discovery. Yakugaku Zasshi 2016, 136, 113-120.
Takayoshi Suzuki Histone Lysine Demethylase Inhibitors for Cancer Therapy” The 75th Annual Meeting of the Japanese Cancer Association ~Epigenetic therapeutic targets: Discovery and utilization~ Oct 2016, Yokohama
Takayoshi Suzuki. Chemical Control of Epigenetics for Cancer Therapy ~Discovery of Histone Lysine Demethylase Inhibitors with Anticancer Activity~” Chung-Ang University Center for Metareceptome Research 2016 International Symposium; Oct 17, 2016 (Seoul)
Takayoshi Suzuki. Targeting Lysine Demethylases for Cancer Therapy. The 35th Sapporo International Cancer Symposium 2016~Cancer epigenome: from discovery to translation~; Jun 24, 2016 (Sappaoro)
Takayoshi Suzuki. Discovery of Histone Lysine Demethylase Inhibitors with Anticancer Activity Eleventh Drug Discovery Chemistry~Epigenetic Inhibitor Discovery~; Apr 20, 2016 (San Diego)
Takayoshi Suzuki. Targeting Histone Demethylases for Cancer Therapy. Regulatory Mechanisms of Epigenetic Information and Their Clinical Applications: Kick-Off Symposium in Nagoya City University in 2016; Mar. 1, 2016 (Nagoya)
Yosuke Ota, Yukihiro Itoh, Takayoshi Suzuki. Discovery of LSD1-inhibition triggered drug delivery molecules. Regulatory Mechanisms of Epigenetic Information and Their Clinical Applications: Kick-Off Symposium in Nagoya City University in 2016; Mar. 1, 2016 (Nagoya)
Paolo Mellini, Sergio Valente, Yukihiro Itoh, Taeko Kakizawa, Maija Lahtela-Kakkonen, Clemens Steegborn, Roberta Budriesi, Marco Tafani, Donatella Del Bufalo Lucia Altucci Carlo Gaetanoi, Antonello Mai, Takayoshi Suzuki, 1,4-dihydropyridines Active on the SIRT1/AMPK Pathway and SIRT2 Inhibitors Design: New Insight on Sirtuin Modulators. International Symposium for RIKEN Epigenetics Program 2016, P52; Feb. 15, 2016 (Wako)
Toshifumi Tojo, Yukihiro Itoh, Yosuke Ota, Zi Hui, Miki Suzuki Shusaku Uchida, Takayoshi Suzuki, Identification of histone deacetylase 1/2-selective inhibitors using click chemistry. International Symposium for RIKEN Epigenetics Program 2016, P56; Feb. 15, 2016 (Wako)
原著論文
Nakagawa H, Seike S, Sugimoto M, Ieda N, Kawaguchi M, Suzuki T, Miyata N. Peptidyl prolyl isomerase Pin1-inhibitory activity of D-glutamic and D-aspartic acid derivatives bearing a cyclic aliphatic amine moiety. Bioorg. Med. Chem. Lett. 2015, 25, 5619-5624.
Erburu M, Munoz-Cobo I, Dominguez J, Beltran E, Suzuki T, Mai A, Valente S, Puerta E, Tordera RM. Chronic stress and antidepressant induced changes in Hdac5 and Sirt2 affect synaptic plasticity. Eur. Neuropsychopharmacol. 2015, 25, 2036-2048.
Ye Q, Holowatyj A, Wu J, Liu H, Zhang L, Suzuki T, Yang ZQ. Genetic alterations of KDM4 subfamily and therapeutic effect of novel demethylase inhibitor in breast cancer. Am. J. Cancer Res. 2015, 5, 1519-1530.
Ieda N, Hishikawa K, Eto K, Kitamura K, Mori S, Maeno M, Kawaguchi M, Suzuki T, Fukuhara K, Miyata N, Furuta T, Nabekura J, Nakagawa H. A double bond-conjugated dimethylnitrobenzene-type photolabile nitric oxide donor with improved two-photon cross section. Bioorg. Med. Chem. Lett. 2015, 25, 3172-3175.
Kozako T, Suzuki T, Yoshimitsu M, Uchida Y, Kuroki A, Aikawa A, Honda S, Arima N, Soeda S. Novel small-molecule SIRT1 inhibitors induce cell death in adult T-cell leukemia cells. Sci. Rep. 2015, 5, 11345.
Tsumoto H, Ogasawara D, Hashii N, Suzuki T, Akimoto Y, Endo T, Miura Y. Enrichment of O-GlcNAc-modified peptides using novel thiol-alkyne and thiol-disulfide exchange. Bioorg. Med. Chem. Lett. 2015, 25, 2645-2649.
Itoh Y, Sawada H, Suzuki M, Tojo T, Sasaki R, Hasegawa M, Mizukami T, Suzuki T. Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells. ACS Med. Chem. Lett. 2015, 6, 665-670.
Krishnan SR, Nair BC, Sareddy GR, Roy SS, Natarajan M, Suzuki T, Peng Y, Raj G, Vadlamudi RK. Novel role of PELP1 in regulating chemotherapy response in mutant p53-expressing triple negative breast cancer cells. Breast. Cancer Res. Treat. 2015, 150, 487-99.
Hoshino I, Akutsu Y, Murakami K, Akanuma N, Isozaki Y, Maruyama T, Toyozumi T, Matsumoto Y, Suito H, Takahashi M, Sekino N, Komatsu A, Suzuki T, Matsubara H. Histone Demethylase LSD1 Inhibitors Prevent Cell Growth by Regulating Gene Expression in Esophageal Squamous Cell Carcinoma Cells. Ann. Surg. Oncol. 2015 in press.
Etani T, Suzuki T, Naiki T, Naiki-Ito A, Ando R, Iida K, Kawai N, Tozawa K, Miyata N, Kohri K, Takahashi S. NCL1, a highly selective lysine-specific demethylase 1 inhibitor, suppresses prostate cancer without adverse effect. Oncotarget 2015, 6, 2865-2878.
Khan MNA, Tsumoto H, Itoh Y, Ota Y, Suzuki M, Ogasawara D, Nakagawa H, Mizukami T, Miyata N, Suzuki T. Design, synthesis, and biological activity of N-alkylated analogue of NCL1, a selective inhibitor of lysine-specific demethylase 1. MedChemComm 2015, 6, 407-412.
Miyamura S, Araki M, Suzuki T, Yamaguchi J, Itami K. Stereodivergent Synthesis of Arylcyclopropylamines by Sequential C-H Borylation and Suzuki-Miyaura Coupling. Angew. Chem. Int. Ed. 2015, 54, 846-851.
Wang X, Huang B, Suzuki T, Liu X, Zhan P. Medicinal chemistry insights in the discovery of novel lysine-specific demethylase 1 inhibitors. Epigenomics 2015, 7, 1379-1396.
Zhan P, Itoh Y, Suzuki T, Liu X. Strategies for the Discovery of Target-specific or Isoform-selective Modulators. J. Med. Chem. 2015, 58, 7611-7633. Most Read Articles.
Zi Hui, Peng Zhan, Toshifumi Tojo, Yukihiro Itoh, Takayoshi Suzuki, Identification of histone deacetylase 1/2-selective inhibitors using click chemistry-based combinatorial fragment assembly, acifichem 2015 (7) Biological: 296; Dec. 16, 2015 (Honolulu)
Paolo Mellini, Yukihiro Itoh, Taeko Kakizawa, Maija Lahtela-Kakkonen, Elina M. Jarho, Sergio Valente, Dante Rotili, Antonello Mai, Takayoshi Suzuki, Toward SIRT7 inhibitors: From screening of known SIRT1-3 modulators to de novo-design, Pacifichem 2015 (7) Biological: 286; Dec. 16, 2015 (Honolulu)
Yosuke Ota, Yukihiro Itoh, Takayoshi Suzuki, Discovery of dual-functional anticancer drugs using LSD1 inhibition as a trigger, Pacifichem 2015 (7) Biological: 278; Dec. 16, 2015 (Honolulu)
Yukihiro Itoh, Hideyuki Sawada, Miki Suzuki, Tamio Mizukami, Takayoshi Suzuki, Identification of lysine demethylase 5A inhibitors and their effect on cancer cells, Pacifichem 2015 (7) Biological: 274; Dec. 16, 2015 (Honolulu)
“Chemical Control of Epigenetics ~Discovery of Histone Lysine Demethylase Inhibitors~” The 10th Asian Epigenomics Meeting 2015; Sep 9, 2015 (Seoul)
原著論文
Singh RK, Suzuki T, Mandal T, Balsubramanian N, Haldar M, Mueller DJ, Strode JA, Cook G, Mallik S, Srivastava DK. Binding Thermodynamics of Structurally Similar Ligands to Histone Deacetylase 8 Sheds Light on Challenges in Rational Design of Potent and Isozyme-selective Inhibitors of the Enzyme. Biochemistry 2014, 53, 7445-7458.
Kitamura K, Ieda N, Hishikawa K, Suzuki T, Miyata N, Fukuhara K, Nakagawa H. Visible light-induced nitric oxide release from a novel nitrobenzene derivative cross-conjugated with a coumarin fluorophore. Bioorg. Med. Chem. Lett. 2014, 24, 5660-5562.
Mano T, Suzuki T, Tsuji S, Iwata A. Differential effect of HDAC3 on cytoplasmic and nuclear Huntingtin aggregates. PLoS ONE 2014, 9, e111277.
Matsuba S, Niwa S, Muraki K, Kanatsuka S, Nakazono Y, Hatano N, Fujii M, Zhan P, Suzuki T, Ohya S. Downregulation of Ca2+-activated Cl- channel TMEM16A by the inhibition of histone deacetylase in TMEM16A-expressing cancer cells. J. Pharmacol. Exp. Ther. 2014, 351, 510-518.
Kondo Y, Iwao T, Yoshihashi S, Mimori K, Ogihara R, Nagata K, Kurose K, Saito M, Niwa T, Suzuki T, Miyata N, Ohmori S, Nakamura K, Matsunaga T. Histone Deacetylase Inhibitor Valproic Acid Promotes the Differentiation of Human Induced Pluripotent Stem Cells into Hepatocyte-Like Cells. PLoS ONE 2014, 9, e104010.
Tatum PR, Sawada H, Ota Y, Itoh Y, Zhan P, Ieda N, Nakagawa H, Miyata N, Suzuki T. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorg. Med. Chem. Lett. 2014, 24, 1871-1874. Most Downloaded Article.
Sekizawa H, Amaike K, Itoh Y, Suzuki T, Itami K, Yamaguchi J. Late-Stage C-H Coupling Enables Rapid Identification of HDAC Inhibitors: Synthesis and Evaluation of NCH-31 Analogues. ACS Med. Chem. Lett. 2014, 5, 582-586. Most Read Articles.
Shirai T, Saito M, Kobayashi A, Asano M, Hizume M, Ikeda S, Teruya K, Morita M, Kitamoto T. Evaluating Prion Models Based on Comprehensive Mutation Data of Mouse PrP. Structure 2014, 22, 560-571.
Itoh Y, Ogasawara D, Ota Y, Mizukami T, Suzuki T. Synthesis, LSD1 Inhibitory Activity, and LSD1 Binding Model of Optically Pure Lysine-PCPA Conjugates. Comput. Struct. Biotechnol. J. 2014, 9, e201402002.
Tee A, Ling D, Nelson C, Atmadibrata B, Dinger M, Xu N, Mizukami T, Liu PY, Liu B, Cheung B, Pasquier E, Haber M, Norris MD, Suzuki T, Marshall GM, Liu T. The histone demethylase JMJD1A induces cell migration and invasion by up-regulating the expression of the long noncoding RNA MALAT1. Oncotarget 2014, 5, 1793-1804.
Mino K, Nishimura S, Ninomiya S, Tujii H, Matsumori Y, Tsuchida M, Hosoi M, Koseki K, Wada S, Hasegawa M, Sasaki R, Murakami-Yamaguchi Y, Narita H, Suzuki T, Miyata N, Mizukami T. Regulation of Tissue Factor Pathway Inhibitor-2 (TFPI-2) Expression by Lysine-Specific Demethylase 1 and 2 (LSD1 and LSD2). Biosci. Biotech. Bioch. 2014, 78, 1010-1017.
Nishizawa K, Oguma A, Kawata M, Sakasegawa Y, Teruya K, Doh-Ura K. Efficacy and mechanism of a glycoside compound inhibiting abnormal prion protein formation in prion-infected cells: implications of interferon and phosphodiesterase 4D interacting protein. J. Virol. 2014, 88, 4083-4099.
Suzuki T, Muto N, Bando M, Itoh Y, Masaki A, Ri M, Ota Y, Nakagawa H, Iida S, Shirahige K, Miyata N. Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylase 8-selective inhibitors. ChemMedChem 2014, 9 657-664.
Fukushima N, Ieda N, Sasakura K, Nagano T, Hanaoka K, Suzuki T, Miyata N, Nakagawa H. Synthesis of a photocontrollable hydrogen sulfide donor using ketoprofenate photocages. Chem. Commun. 2014, 50, 587-589.
Zhan P, Song Y, Itoh Y, Suzuki T, Liu X. Recent Advances in the Structure-based Rational Design of TNKSIs. Mol. Biosyst. 2014, 10, 2783-2799.
Itoh Y, Miyata N, Suzuki T. Target-guided Synthesis: Medicinal Chemistry Strategy to Allow Target Enzymes Themselves to Synthesize their Own Inhibitors. J. Syn. Org. Chem. Jpn. 2014, 72, 702-716.
Suzuki T, Itoh Y, Ogasawara D, Miyata N, Mizukami T, Sasaki R, Takaori A, Kawahara M. Lsd1-selective inhibitor having lysine structure. PCT Int. Appl. (2014), WO 2014084298.
Takayoshi Suzuki “Chemical Control of Histone Lysine Methylation” Sino-Japan Workshop on Chemical Biology; Oct 12, 2014, Beijing (招待講演)
Takayoshi Suzuki “Chemical Control of Epigenetics” Asian Chemical Biology Initiative-Sponsored Lectures; Jul 1, 2014, Hanoi (招待講演).
Takayoshi Suzuki “Discovery of Histone Lysine Demethylase Inhibitors” Ninth Drug Discovery Chemistry~Epigenetic Inhibitor Discovery~; Apr 23, 2014, San Diego (招待講演).
Takayoshi Suzuki “Design, synthesis, and biological activity of lysine-specific demethylase 1 inhibitors” 2014 Queenstown Molecular Biology Meetings; Mar 13, 2014, Shanghai (招待講演).
Nakagawa H, Hishikawa K, Eto K, Ieda N, Namikawa T, Kamada K, Suzuki T, Miyata N, Nabekura J. Fine spatiotemporal control of nitric oxide release by infrared pulse-laser irradiation of a photo-labile donor. ACS Chem. Biol. 2013, 8, 2493-2500.
Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N. Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity. J. Med. Chem. 2013, 56, 7222-7231. Most Read Articles
Kawai K, Ieda N, Aizawa K, Suzuki T, Miyata N, Nakagawa H. A Reductant-Resistant and Metal-Free Fluorescent Probe for Nitroxyl Applicable to Living Cells. J. Am. Chem. Soc. 2013, 135, 12690-12696.
Matsuya Y, Kobayashia Y, Uchida S, Itoh Y, Sawada H, Suzuki T, Miyata N, Sugimoto K, Toyooka N. Search for a Novel SIRT1 Activator: Structural Modification of SRT1720 and Biological Evaluation. Bioorg. Med. Chem. Lett. 2013, 23, 4907-4910.
Ogasawara D, Itoh Y, Tsumoto H, Kakizawa T, Mino K, Fukuhara K, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N, Suzuki T. Lysine-Specific Demethylase 1-Selective Inactivators Based on Protein-Targeted Drug Delivery Mechanism. Angew. Chem. Int. Ed. 2013, 52, 8620-8624.
Suzuki T, Kasuya Y, Itoh Y, Ota Y, Zhan P, Asamitsu K, Nakagawa H, Okamoto T, Miyata N. Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly. PLoS ONE 2013, 8, e68669.
Pajtler KW, Weingarten C, Thor T, Kuenkele A, Heukamp LC, Buttner R, Suzuki T, Miyata N, Grotzer M, Rieb A, Sprussel A, Eggert A, Schramm A, Schulte JH. Lysin-specific histone demethylase 1 (LSD1/KDM1A) qualifies as promising new epigenetic therapy target in medulloblastoma. Acta Neuropathologica Communications 2013, 1, 19.
Sareddy GR, Nair BC, Krishnan SK, Gonugunta VK, Zhang QG, Suzuki T, Miyata N, Brenner AJ, Brann DW, Vadlamudi RK. KDM1 is a novel therapeutic target for the treatment of gliomas. Oncotarget 2013, 4, 18-28.
Takeuchi M, Hirasawa A, Hara T, Kimura I, Hirano T, Suzuki T, Miyata N, Awaji T, Ishiguro M, Tsujimoto G. FFA1-selective agonistic activity based on docking simulation using FFA1 and GPR120 homology models. Br. J. Pharmacol. 2013, 168, 1570-1583.
Hattori Y, Kinami G, Teruya K, Nosaka K, Kobayashi K, Akaji K. A Practical Synthesis of a Hydroxylated Sesquiterpene Coumarin 10’R-acetoxy-11’-hydroxyumbelliprenin by the regioselective dihydroxylation. HETEROCYCLES, 87, 423-428, 2013.
Khan MNA, Suzuki T, Miyata N. An overview of phenylcyclopropylamine derivatives: biochemical and biological significance and recent developments. Med. Res. Rev. 2013, 33, 873-910.
Itoh Y, Suzuki T, Miyata N. Small-molecular modulators of cancer-related epigenetic mechanisms. Mol. Biosyst. 2013, 9, 873-896.
Hideyuki Sawada, Discovery of SIRT2-selective Inhibitors by Structure-based Drug Design. 2nd Annual Conference ICBS2013, Oct. 8, Kyoto.
Yusuke Ota, Identification of HDAC3-Selective Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly. 2nd Annual Conference ICBS2013, Oct. 8, Kyoto. Poster Awards.
Yukihiro Itoh, Design and Synthesis of LSD1 inactivators Based on Enzyme-targeted Drug Delivery Mechanism. 2nd Annual Conference ICBS2013, Oct. 7, Kyoto.
Takayoshi Suzuki Discovery of Histone Lysine Demethylase Inhibitors. XXII National Meeting on Medicinal Chemistry (NMMC2013); Sep. 11, 2013, Rome (招待講演).
Suzuki T, Ota Y, Ri M, Bando M, Gotoh A, Itoh Y, Tsumoto H, Tatum PR, Mizukami T, Nakagawa H, Iida S, Ueda R, Shirahige K, Miyata N. Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries. J. Med. Chem. 2012, 55, 9562-9575.Most Read Articles
Teruya K, Tanaka T, Kawakami T, Akaji K, Aimoto S. Epimerization in Peptide Thioester Condensation. J. Pept. Sci. 2012, 18, 669-677.
Cortez V, Mann M, Tekmal S, Suzuki T, Miyata N, Rodriguez-Aguayo C, Lopez-Berestein G, Sood AK, Vadlamudi RK. Targeting PELP1-KDM1 axis as a potential therapeutic strategy for breast cancer. Breast Cancer Res. 2012, 14, R108.
Suzuki T, Khan MN, Sawada H, Imai E, Itoh Y, Yamatsuta K, Tokuda N, Takeuchi J, Seko T, Nakagawa H, Miyata N. Design, Synthesis, and Biological Activity of a Novel Series of Human Sirtuin 2-selective Inhibitors. J. Med. Chem. 2012, 55, 5760-5773.Most Read Articles
Kawahara I, Haruta K, Ashihara Y, Yamanaka D, Kuriyama M, Toki N, Kondo Y, Teruya K, Ishikawa J, Furuta H, Ikawa Y, Kojima C, Tanaka Y. Site-specific isotope labeling of long RNA for structural and mechanistic studies. Nucleic Acids Research 2012, 40, e7.
Fukada M, Hanai A, Nakayama A, Suzuki T, Miyata N, Rodriguiz RM, Wetsel WC, Yao TP, Kawaguchi Y. Loss of deacetylation activity of Hdac6 affects emotional behavior in mice. PLoS One. 7, e30924, 2012.
総説
Suzuki T. Drug Discovery Research towards Next-generation Epigenetic Drugs. Kyoto-furitsu Ika Daigaku Zasshi 2012, 121, 461-467.
Takayoshi Suzuki, Yosuke Ota, Yuki Kasuya, Hidehiko Nakagawa, Naoki Miyata Discovery of isozyme-selective histone deacetylase inhibitors by click chemistry. 243rd American Chemical Society National Meeting & Exposition, San Diego, U.S.A. March 2012.
Daisuke Ogasawara, Takayoshi Suzuki, Rie Ueda, Mohammed Naseer Ahmad Khan, Takuya Matsubara, Koshiki Mino, Hidehiko Nakagawa, Naoki Miyata Design, synthesis and biological evaluation of cyclopropylamine-based LSD1 inhibitors. 243rd American Chemical Society National Meeting & Exposition, San Diego, U.S.A. March 2012.
Hiroki Ozasa, Takayoshi Suzuki, Shohei Hamada, Koshiki MIno, Hidehiko Nakagawa, Tamio Mizukami, Naoki Miyata Design, synthesis and biological evaluation of JMJD2 histone demethylase inhibitors. 243rd American Chemical Society National Meeting & Exposition, San Diego, U.S.A. March 2012.
Hideyuki Sawada, Takayoshi Suzuki, Erica Imai, Mohammed Naseer Ahmad Khan, Hidehiko Nakagawa, Naoki Miyata Discovery of SIRT2-selective inhibitors. 243rd American Chemical Society National Meeting & Exposition, San Diego, U.S.A. March 2012.
国内の発表
一般講演
澤田英之、鈴木孝禎、今井英里佳、Mohammed Naseer Ahmed Khan、中川秀彦、宮田直樹 新規SIRT2 選択的阻害薬の創製 ～Structure-based Drug Design によるSIRT1 阻害からSIRT2 阻害へのアイソザイム選択性転換～ 第30回メディシナルケミストリーシンポジウム 2012年11月、東京
Unno M, Shinohara M, Takayama K, Tanaka H, Teruya K, Doh-Ura K, Sakai R,Sasaki M, Ikeda-Saito M. Binding and Selectivity of the Marine Toxin Neodysiherbaine A and Its Synthetic Analogues to GluK1 and GluK2 Kainate Receptors. J. Mol. Biol. 413, 667-683. 2011.
Akaji K, Konno H, Mitsui H, Teruya K, Shimamoto Y, Hattori Y, Ozaki T, Kusunoki M, Sanjoh A. Structure-Based Design, Synthesis, and Evaluation of Peptide-mimetic SARS 3CL Protease Inhibitors. J. Med. Chem. 54, 7962-7973, 2011.
Kakizawa, T.; Sanjoh, A.; Kobayashi, A.; Hattori, Y.; Teruya, K.; Akaji, K. Evaluation of Superior BACE1 Cleavage Sequences Containing Unnatural Amino Acids. Bioorg. Med. Chem. 19, 2785-2789, 2011.
