“Identification of Epigenetic Complex Disruptors” Takayoshi Suzuki The 145th Annual Meeting of Pharmaceutical Society of Japan; Mar. 29, 2025 (Fukuoka).
“Targeting KDM1A in neuroblastoma with NCL-1 induces a less aggressive phenotype and suppresses angiogenesis” Annika Sprüssel, Takayoshi Suzuki, Naoki Miyata, Kathy Astrahantseff, Annabell Szymansky, Jörn Toedling, Theresa M. Thole, Annika Ballagee, Marco Lodrini, Annette Künkele, Matthias Truss, Lukas C. Heukamp, Susanne Mathia, Falk Hertwig, Christian Rosenberger, Angelika Eggert, Hedwig E. Deubzer, Johannes H. Schulte. J. Clin. Med. 2024, 13, 6081 (Published 12 Oct 2024).
“Down‐regulation of IL‐8 and IL‐10 by LRRC8A inhibition through the NOX2‐Nrf2‐CEBPB transcriptional axis in THP‐1‐derived M2 macrophages” Miki Matsui, Junko Kajikuri, Hiroaki Kito, Elghareeb E. Elboray, Takayoshi Suzuki, Susumu Ohya. Int. J. Mol. Sci. 2024, 25, 9612 (Published 5 Sep).
“General Synthesis of meso-1,4-Dialdehydes and their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions” Runze Zhao, Ismiyarto, Da-Yang Zhou, Kaori Asano, Takayoshi Suzuki, Hiroaki Sasai, and Takeyuki Suzuki. ACS Omega2024, 9, 17945–17955.
“Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells” Yosuke Ota, Yukihiro Itoh, Yuri Takada, Yasunobu Yamashita, Chenliang Hu, Mano Horinaka, Yoshihiro Sowa, Mitsuharu Masuda, Toshiyuki Sakai, Takayoshi Suzuki. Bioorg. Med. Chem. 2024, 100, 1117632 (Published 9 Feb 2024).
“The impact of selective HDAC inhibitors on the transcriptome of early mouse embryos” Ruiqi Shao, Takayoshi Suzuki, Mikita Suyama, Yuichi Tsukada. BMC Genomics 2024, 25, 143 (Published 5 Feb 2024).
“Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity” Mitsuhiro Terao, Yasunobu Yamashita, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki. Bioorg. Med. Chem.2024, 98, 117579 (Published 15 Jan 2024).
“Identification of a Histone Deacetylase 8 Inhibitor Through Drug Screenings Based on Machine Learning” Atika Nurani, Yasunobu Yamashita, Yuuki Taki, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki. Chem. Pharm. Bull.2024, 72, 173–178 (Published 1 Feb 2024).
“A Structure-Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1” Yuri Takada, Kyohei Adachi, Yuka Fujinaga, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki. Chem. Pharm. Bull.2024, 72, 155–160 (Published 1 Feb 2024).
“Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation” Yukihiro Itoh, Peng Zhan, Toshifumi Tojo, Pattaporn Jaikhan, Yosuke Ota, Miki Suzuki, Ying Li, Zi Hui, Yukiko Moriyama, Yuri Takada, Yasunobu Yamashita, Makoto Oba, Shusaku Uchida, Mitsuharu Masuda, Shinji Ito, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki.J. Med. Chem. 2023, 66, 15171–15188 (17 Oct 2023).
“Pharmacological inhibition of KDM1A/LSD1 enhances estrogen receptor beta-mediated tumor suppression in ovarian cancer” Prabhakar Pitta Venkata, Sridharan Jayamohan, Yi He, Salvador Alejo, Jessica D. Johnson, Bridgitte E. Palacios, Uday P. Pratap, Yihong Chen, Zexuan Liu, Yi Zou, Lai Zhao, Takayoshi Suzuki, Suryavathi Viswanadhapalli, Susan T. Weintraub, Srinath Palakurthi, Philip T. Valente, Rajeshwar R. Tekmal, Edward Kost, Ratna K. Vadlamudi, Gangadhara R. Sareddy. Cancer Lett. 2023, 575, 21683 (Published 14 Sep 2023).
“SIRT2 Inhibition Rescues Neurodegenerative Pathology but Increases Systemic Inflammation in a Transgenic Mouse Model of Alzheimer’s Disease” Noemi Sola-Sevilla, Alberto Mesa-Lombardo, Mikel Aleixo, Sara Exposito, Teresa Diaz-Perdigón, Amaya Azqueta, Farzad Zamani, Takayoshi Suzuki, Silvia Maioli, Francesca Eroli, Anna Matton, Maria J. Ramı́rez, Maite Solas, Rosa M. Tordera, Eduardo D. Martı́n, Elena Puerta. J. Neuroimmune Pharmacol. 2023, 18, 529–550 (Published 12 Sep 2023) .
“Origin of the kinetic HDAC2-selectivity of an HDAC inhibitor” Hirokazu Mishima, Yukihiro Itoh, Takashi Kurohara, Takayoshi Suzuki, Naoya Asada, Ken-ichi Kusakabe, Yuko Okamoto. J. Comput. Chem.2023, 44, 1604–1609 (Published 19 Apr 2023).
“Lysine-specific histone demethylase 1A (KDM1A/LSD1) inhibition attenuates DNA double strand break repair and augments efficacy of temozolomide in glioblastoma” Salvador Alejo, Bridgitte E. Palacios, Prabhakar Pitta Venkata, Yi He, Wenjing Li, Jessica D. Johnson, Yihong Chen, Uday P. Pratap, Sridharan Jayamohan, Kyra Clarke, Yi Zou, Yingli Lv, Korri Weldon, Suryavathi Viswanadhapalli, Zhao Lai, Zhenqing Ye, Yidong Chen, Andrea R. Gilbert, Takayoshi Suzuki, Rajeshwar R. Tekmal, Weixing Zhao, Siyuan Zheng, Ratna K. Vadlamudi, Andrew J. Brenner, Gangadhara R. Sareddy. Neuro Oncol.2023, 25, 1249–1261 (Published 16 Jan 2023).
“The discovery of 3,3-dimethyl-1,2,3,4-tetrahydroquinoxaline-1-carboxamide as AMPD2 inhibitors with a novel mechanism of action” Yuki Kitao, Tadataka Saito, Satoshi Watanabe, Yasuhiro Oe, Koichi Takahashi, Tatsuo Akaki, Tsuyoshi Adachi, Satoki Doi, Kenji Yamanaka, Yasutaka Murai, Makoto Oba, Takayoshi Suzuki. Bioorg. Med. Chem. Lett. 2023, 80, 129110 (Published 20 Dec 2022).
“Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)” Jiranan Chotitumnavee, Yasunobu Yamashita, Yukari Takahashi, Yuri Takada, Tetsuya Iida, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki. Chem.Commun.2022, 58, 4635-4638 (Published 14 Mar 2022).
“Utilization of α and β Epimerization for Synthesis of Both Enantiomers of Enterolactone” Rui Jiang, Ismiyarto, Tsukasa Abe, Da-Yang Zhou, Kaori Asano, Takayoshi Suzuki, Hiroaki Sasai, Takeyuki Suzuki. J. Org. Chem.2022, 87, 5051-5056 (Published 4 Mar 2022).
“Novel Histone Modifications in Microglia Derived from a Mouse Model of Chronic Pain” Ping Zhang, Jennifer Guergues, Amy R. Alleyne, Thomas J. Cirino, Owen Nadeau, Ariana M. Figueroa, Heather M. Stacy, Takayoshi Suzuki, Jay P. McLaughlin, Stanley M. Stevens, Jr., Bin Liu. Proteomics 2022, 22, e2100137 (Published 26 Jan 2022).
“KDM1A inhibition augments the efficacy of rapamycin for the treatment of endometrial cancer” Prabhakar Pitta Venkata, Yihong Chen, Salvador Alejo, Yi He, Bridgitte E. Palacios, Ilanna Loeffel, Junhao Liu, Uday P. Pratap, Gabrielle Gray, Sureshkumar Mulampurath Achuthan Pillai, Yi Zou, Zhao Lai, Takayoshi Suzuki, Suryavathi Viswanadhapalli, Srinath Palakurthi, Rajeshwar R. Tekmal, Ratna K. Vadlamudi, Edward Kost, Gangadhara R. Sareddy. Cancer Lett.2022, 524, 219-231 (Published Jan 2022).
“Chemical Control of Epigenetics~Discovery of Histone Lysine Demethylase Inhibitors~” Takayoshi Suzuki. Lecture in Global Frontiers in Life Science A, Kyoto University; Jul 6, 2022 (Kyoto)
“Discovery of epigenetic enzyme inhibitors by target-guided synthesis” Takayoshi Suzuki. The 142nd Annual Meeting of Pharmaceutical Society of Japan; Mar. 27, 2022 (web).
Original Articles
“Identification of novel histone deacetylase 6-selective inhibitors bearing 3,3,3-trifluorolactic amide (TFLAM) motif as a zinc binding group” Takashi Kurohara, Keita Tanaka, Daisuke Takahashi, Satoshi Ueda, Yasunobu Yamashita, Yuri Takada, Hirokazu Takeshima, Shengwang Yu, Yukihiro Itoh, Koji Hase, Takayoshi Suzuki. ChemBioChem2021, 22, 3158-3163. (Published 05 July 2021)
“Identification of Potent and Selective Inhibitors of Fat Mass Obesity Associated Protein Using a Fragment-Merging Approach” Muthuraj Prakash, Yukihiro Itoh, Yoshie Fujiwara,Yukari Takahashi, Yuri Takada, Paolo Mellini, Elghareeb E. Elboray, Mitsuhiro Terao, Yasunobu Yamashita, Chika Yamamoto, Takao Yamaguchi, Masayuki Kotoku, Yuki Kitao, Ritesh Singh, Rohini Roy, Satoshi Obika, Makoto Oba, Dan Ohtan Wang, and Takayoshi Suzuki. J. Med. Chem. 2021, 64, 15810–15824. (Published: 3 November 2021)
“Ca2+-activated K+ channel KCa1.1 as a therapeutic target to overcome chemoresistance in three-dimensional sarcoma spheroid models” Susumu Ohya, Junko Kajikuri, Kyoko Endo, Hiroaki Kito, Elghareeb Elboray, Takayoshi Suzuki. Cancer Sci.2021, 112, 3769-3783. (Published: 28 June 2021)
“Catalytic Enantioselective Tishchenko Reaction of meso-Dialdehyde: Catalytic Asymmetric Synthesis of Cedarmycins” Ismiyarto, Nobuki Kishi, Yuki Adachi, Rui Jiang, Takahiro Doi, Da-Yang Zhou, Kaori Asano, Yasushi Obora, Takayoshi Suzuki, Hiroaki Sasai, and Takeyuki Suzuki. RSC Adv.2021, 11, 11606–11609. (Published: 22 March 2021)
“Discovery of novel tetrahydrobenzo[b]thiophene-3-carbonitriles as histone deacetylase inhibitors” Piyush Gediya, Vivek K. Vyas, Vincenzo Carafa, Nikum Sitwala, Laura Della Torre, Angelita Poziello, Takashi Kurohara, Takayoshi Suzuki, Varalakshmi Raghuraman, K. Suthindhiran, Debarpan Ghosh, Dhiraj Bhatia, Lucia Altucci, Manjunath D. Ghate. Bioorg. Chem. 2021, 110, 104801. (Published: 5 March)
“Simplifying Submission Requirements for the Journal of Medicinal Chemistry” Craig W. Lindsley, James Barrow, Kelly Chibale, Maria Laura Bolognesi, Stuart Conway, William Denny, Ke Ding, Stefan Laufer, Luhua Lai, Hong Liu, Nouri Neamati, Takayoshi Suzuki, Nicholas Meanwell, Wendy Young. J. Med. Chem.2021, 64, 7877–7878. (Published: 15 June 2021)
“Chemical Control of Epigenetics~Discovery of Histone Lysine Demethylase Inhibitors~” Takayoshi Suzuki. Lecture in Global Frontiers in Life Science A, Kyoto University; May 19, 2021 (Web)
“KDM1A inhibition is effective in reducing stemness and treating triple negative breast cancer” Mei Zhou, Prabhakar Pitta Venkat, Suryavathi Viswanadhapalli, Bridgitte Palacios, Salvador Alejo, Yihong Chen, Yi He, Uday Pratap, Yi Zou, Zhao Lai, Takayoshi Suzuki, Andrew Brenner, Rajeshwar R. Tekmal, Ratna K. Vadlamudi, Gangadhara R. Sareddy. Breast Cancer Res. Treat.2020, 185, 343–357.(Published: 14 October 2020)
“Downregulation of the Ca2+-activated K+ channel KCa3.1 in mouse preosteoblast cells treated with vitamin D receptor agonist” Hiroaki Kito, Haruka Morihiro, Yuka Sakakibara, Kyoko Endo, Junko Kajikuri, Takayoshi Suzuki, Susumu Ohya. Am. J. Physiol. Cell Physiol.2020, 319, C345–C358.(Published: 28 July 2020)
“Cross-Species Chromatin Interactomes Drive Heterochromatin, Enhancer, and Transcriptional Rewiring in Epstein-Barr Virus Positive Gastric Adenocarcinoma” Atsushi Okabe, Kie Kyon Huang, Keisuke Matsusaka, Masaki Fukuyo, Manjie Xing, Xuewen Ong, Takayuki Hoshii, Genki Usui, Motoaki Seki, Yasunobu Mano, Bahityar Rahmutulla, Teru Kanda, Takayoshi Suzuki, Sun Young Rha, Tetsuo Ushiku, Masashi Fukayama, Patrick Tan, Atsushi Kaneda. Nat. Genet.2020, 52, 919–930.(Published: 27 July 2020)
“Selective lysine specific demethylase 1 inhibitor, NCL1, could cause testicular toxicity via the regulation of apoptosis” Satoshi Nozaki, Taku Naiki, Aya Naiki-Ito, Shoichiro Iwatsuki, Tomoki Takeda, Toshiki Etani, Takashi Nagai, Keitaro Iida, Takayoshi Suzuki, Satoru Takahashi, Takahiro Yasui, Yukihiro Umemoto. Andrology2020, 8, 1895–1906.(Published: 29 June 2020)
“Metalloprotein-Catalyzed Click Reaction for In Situ Generation of a Potent Inhibitor” Yuka Miyake, Yukihiro Itoh, Yoshinori Suzuma, Hidehiko Kodama, Takashi Kurohara, Yasunobu Yamashita, Remy Narozny, Yutaro Hanatani, Shusaku Uchida, Takayoshi Suzuki. ACS Catal.2020, 10, 5383–5392.(Published: 13 April 2020)
“Possible contribution of inflammation-associated hypoxia to increased K2P1 K+ channel expression in CD4+ T cells of the mouse model for inflammatory bowel disease” Kyoko Endo, Hiroaki Kito, Ryo Tanaka, Junko Kajikuri, Satoshi Tanaka, Elghareeb E. Elboray, Takayoshi Suzuki, Susumu Ohya. Int. J. Mol. Sci.2020, 21, 38.(Published: 19 December 2019)
“Discovery of gamma-mangostin from Garcinia mangostana as potent and selective natural SIRT2 inhibitor” Keng Yoon Yeong, Kooi Yeong Khaw, Yukari Takahashi, Yukihiro Itoh, Vikneswaran Murugaiyah, Takayoshi Suzuki. Bioorg. Chem.2020, 94, 103403.(Published:4 November 2019)
“LSD1-mediated repression of GFI1 super-enhancer plays an essential role in erythroleukemia” Goichi Tatsumi, Masahiro Kawahara, Ryusuke Yamamoto, Masakatsu Hishizawa, Katsuyuki Kito, Takayoshi Suzuki, Akifumi Takaori-Kondo, Akira Andoh. Leukemia2020, 34, 746–758.(Published: 01 November 2019)
“Early sirtuin 2 inhibition prevents age-related cognitive decline in a senescence accelerated mouse model” Teresa Diaz-Perdigon, Borja Belloch, Ana Ricobaraza, Elghareeb Elboray, Takayoshi Suzuki, Rosa Tordera, Elena Puerta. Neuropsychopharmacolgy2020, 45, 347–357.(Published: 30 August 2019)
Books
“Epigenetic Control Using Small Molecules in Cancer” Tomohiro Kozako, Yukihiro Itoh, Shin-ichiro Honda, Takayoshi Suzuki Approaching Complex Diseases (Springer) 2020, pp 111–148.(Published: April 2020)
“Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors” Takayoshi Suzuki Chemical Epigenetics (Springer) 2020, pp 197–219. (Published: April 2020)
“Identification of Epigenetic Inhibitors by Target-Guided Synthesis” Academia Sinica-Osaka University Symposium 2020; Nov 17, 2020 (Web)
“Chemical Control of Epigenetics~Discovery of Histone Lysine Demethylase Inhibitors~” Takayoshi Suzuki; Lecture in Global Frontiers in Life Science A, Kyoto University; Jul 15, 2020 (Kyoto)
“Genome-wide ChIP-seq data with a transcriptome analysis reveals the groups of genes regulated by histone demethylase LSD1 inhibition in esophageal squamous cell carcinoma cells” Isamu Hoshino, Masahiko Takahashi, Yasunori Akutsu, Kentaro Murakami, Yasunori Matsumoto, Hiroshi Suito, Nobufumi Sekino, Aki Komatsu, Keiko Iida, Takayoshi Suzuki, Itsuro Inoue, Fumitaka Ishige, Yosuke Iwatate, Hisahiro Matsubara. Oncol. Lett.2019, 18, 872–881.(Published: May 13, 2019)
Invited lectures
“Identification of Epigenetic Inhibitors by Target-Guided Synthesis” Academia Sinica-Osaka University Symposium 2020; Nov 17, 2020 (Web)
“Discovery of Epigenetic Inhibitors Using Target-Guided Synthesis” Takayoshi Suzuki; The 4th Roundtable Meeting on Chemical Probe Research Hub; Nov 19, 2019 (Sendai)
“Discovery of histone demethylase inhibitors: drug design focusing on C-H···O hydrogen bonds” Takayoshi Suzuki; The 6th International Cancer Epigenomics Symposium 2019, Seminar in Hematologic Malignancies and Epigenetics; Sep 13, 2019 (Chiba)
“Chemical Control of Epigenetics~Discovery of Histone Lysine Demethylase Inhibitors and Histone Deacetylase Inhibitors~” Takayoshi Suzuki; Lecture in Global Frontiers in Life Science A, Kyoto University; Jun 26, 2019 (Kyoto)