Publications
分子構造の非平面化・非対称化による溶解度向上策と創薬化学への応用
石川稔、橋本祐一
有機合成化学協会誌 2013, 71, 625-636.
Structure–activity relationships of bisphenol A analogs at estrogen receptors (ERs): Discovery of an ERα-selective antagonist.
Keisuke Maruyama, Masaharu Nakamura, Shusuke Tomoshige, Kazuyuki Sugita, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2013, 23, 4031-4036.
Structure–activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators.
Yusuke Mita, Kosuke Dodo, Tomomi Noguchi-Yachide, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry 2013, 21, 993-1005.
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
Yusuke Mita, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto
Bioorganic & Medicinal Chemistry 2013, 21, 608-617.
2013
2012
生体有機化学
橋本祐一、村田道雄 編著 （分担執筆）
東京化学同人、東京、（2012）
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6Hdibenz[b,e]azepin-6-one skeleton.
Atsushi Aoyama, Kaori Endo-Umeda, Kenji Kishida, Kenji Ohgane, Tomomi Noguchi-Yachide, Hiroshi Aoyama, Minoru Ishikawa, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto
Journal of Medicinal Chemistry 2012, 55, 7360-7377.
Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist.
Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Keiichiro Okuhira, Mikihiko Naito, Yuichi Hashimoto
Bioorganic & Medicinal Chemistry Letters 2012, 22, 4453-4457.
2011
Confirmation of Molecular Planarity Disruption Effect on Aqueous Solubility Improvement of β-Naphthoflavone Analogs.
Yuji Fujita, Mitsuhiro Yonehara, Katsushi Kitahara, Jun Shimokawa, Yuichi Hashimoto, Minoru Ishikawa
Heterocycles 2011, 83, 2563-2575.
Design, Synthesis and Biological Evaluation of Nuclear Receptor-degradation Inducers.
Yukihiro Itoh, Risa Kitaguchi, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto
Bioorganic & Medicinal Chemistry 2011, 19, 6768-6778.
Inhibition of restriction enzymes EcoRI, BamHI and HindIII by phenethylphenylphthalimides derived from thalidomide.
Kazunori Motoshima, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita
Chemical & Pharmaceutical Bulletin 2011, 59, 880-884.
Development of Target Protein-Selective Degradation Inducer for Protein Knockdown.
Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto
Bioorganic & Medicinal Chemistry 2011, 19, 3229-3241.
Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists:Relationship between absolute configuration and subtype selectivity.
Kazunori Motoshima, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita
Bioorganic & Medicinal Chemistry 2011, 19, 3156-3172.
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists.
Kazunori Motoshima, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2011, 21, 3041-3045.
Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein.
Keiichiro Okuhira, Nobumichi Ohoka, Kimie Sai, Tomoko Nishimaki-Mogami, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Mikihiko Naito
FEBS Letters 2011, 585, 1147–1152.
Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry.
Minoru Ishikawa, Yuichi Hashimoto
Journal of Medicinal Chemistry (as a perspective) 2011, 54, 1539-1554.
Further Application of the Multi-Template Approach for Creation of Biological Response Modifiers: Discovery of a New Class of Multifunctional Anti-Diabetic Agents.
Kazunori Motoshima, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto, Kazuyuki Sugita
Heterocycles (as a review) 2011, 82, 1083-1101.
ビタミンD受容体−コアクチベーター相互作用阻害物質の創製
三田裕介、橋本祐一、石川稔
ビタミン, 2011, 85, 25-26.
Novel Selective Anti-androgens with a Diphenylpentane Skeleton.
Keisuke Maruyama, Tomomi Noguchi-Yachide, Kazuyuki Sugita, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2010, 20, 6661-6666.
Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ-selective partial agonists by disruption of molecular planarity/symmetry.
Jun-ichi Kasuga, Minoru Ishikawa, Mitsuhiro Yonehara, Makoto Makishima, Yuichi Hashimoto, Hiroyuki Miyachi
Bioorganic & Medicinal Chemistry 2010, 18, 7164-7173.
インテグリンαvβ3/αIIbβ3デュアル拮抗作用を有するRGDペプチド等価体の創製
石川稔
ペプチドニュースレター, 2010, 77, 4-6.
Anti-influenza Activity of Phenethylphenylphthalimide Analogs Derived from Thalidomide.
Yuma Iwai, Hitoshi Takahashi, Dai Hatakeyama, Kazunori Motoshima, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Yuichi Harada, Shigeyuki Itamura, Takato Odagiri, Masato Tashiro, Yoshihisa Sei, Kentaro Yamaguchi, Takashi Kuzuhara
Bioorganic & Medicinal Chemistry 2010, 18, 5379-5390.
Development of Tryptase Inhibitors Derived from Thalidomide.
Masashi Tetsuhashi, Minoru Ishikawa, Mariko Hashimoto, Yuichi Hashimoto, Hiroshi Aoyama
Bioorganic & Medicinal Chemistry 2010, 18, 5323-5338.
Protein Knockdown Using Methyl Bestatin-ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-mediated Degradation of Cellular Retinoic Acid-Binding Proteins.
Yukihiro Itoh, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto
Journal of the American Chemical Society 2010, 132, 5820-5826.
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
Yusuke Mita, Kosuke Dodo, Tomomi Noguchi-Yachide, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2010, 20, 1712-1717.
β-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: Improvement of solubility by disruption of molecular planarity.
Yuji Fujita, Mitsuhiro Yonehara, Masashi Tetsuhashi, Tomomi Noguchi-Yachide, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry 2010, 18, 1194-1203.
2010
2015
Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules.
Shusuke Tomoshige, Mikihiko Naito, Yuichi Hashimoto, Minoru Ishikawa
Organic & Biomolecular Chemistry 2015, 13, 9746-9750.
Styrylphenylphthalimides as novel transrepression-selective liver X receptor (LXR) modulators.
Sayaka Nomura, Kaori Endo-Umeda, Atsushi Aoyama, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
ACS Medicinal Chemistry Letters 2015, 6, 902-907.
Improving the Water-Solubility of Compounds by Molecular Modification to Disrupt Crystal Packing.
Minoru Ishikawa, Yuichi Hashimoto
Chapter 31 in “The Practice of Medicinal Chemistry (Forth Edition)”, ed. by Camille Georges Wermuth, David Aldous, Pierre Raboisson and Didier Rognan, p747-765, Academic Press, Massachusetts, ISBN: 978-0-12-417205-0 (2015).
Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists.
Daisuke Kajita, Masaharu Nakamura, Yotaro Matsumoto, Minoru Ishikawa, Yuichi Hashimoto, Shinya Fujii
Bioorganic & Medicinal Chemistry Letters 2015, 25, 3350-3354.
Structure-Activity Relationships of Benzhydrol Derivatives Based on 1'-Acetoxychavicol Acetate (ACA) and their Inhibitory Activities on Multiple Myeloma Cell Growth via Inactivation of the NF-kB Pathway.
Takashi Misawa, Kosuke Dodo, Minoru Ishikawa, Yuichi Hashimoto, Morihiko Sagawa, Masahiro Kizaki, Hiroshi Aoyama
Bioorganic & Medicinal Chemistry 2015, 23, 2241-2246.
Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.
Taki Sakai, Yotaro Matsumoto, Minoru Ishikawa, Kazuyuki Sugita, Yuichi Hashimoto, Nobuhiko Wakai, Akio Kitao, Era Morishita, Chikashi Toyoshima, Tomoatsu Hayashi, Tetsu Akiyama
Bioorganic & Medicinal Chemistry 2015, 23, 328-339.
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
Yuko Nishiyama, Masahiko Nakamura, Takashi Misawa, Madoka Nakagomi, Makoto Makishima, Minoru Ishikawa, Yuichi Hashimoto
Bioorganic & Medicinal Chemistry 2014, 22, 2799-2808.
7-Dehydrocholesterol metabolites produced by sterol 27-hydroxylase(CYP27A1) modulate liver X receptor activity.
Kaori Endo-Umeda, Kaori Yasuda, Kazuyuki Sugita, Akira Honda, Miho Ohta, Minoru Ishikawa, Yuichi Hashimoto, Toshiyuki Sakaki, Makoto Makishima
Journal of Steroid Biochemistry & Molecular Biology 2014, 140, 7–16.
2014
2016
Development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists.
Sayaka Nomura, Kaori Endo-Umeda, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
ChemMedChem 2016, 11, 2347-2360.
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptorα/δ (PPARα/δ) dual agonists.
Shogo Okazaki, Ryuta Shioi, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima,Yuichi Hashimoto, Takao Yamaguchi
Bioorganic & Medicinal Chemistry 2016, 24, 5455-5461.
Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity.
Shogo Okazaki, Tomomi Noguchi-Yachide, Taki Sakai, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi
Bioorganic & Medicinal Chemistry 2016, 24, 5258-5269.
Improvement in aqueous solubility of retinoic acid receptor (RAR) agonists by bending the molecular structure.
Michiaki Hiramatsu, Yuki Ichikawa, Shusuke Tomoshige, Makoto Makishima, Atsuya Muranaka, Masanobu Uchiyama, Takao Yamaguchi, Yuichi Hashimoto, Minoru Ishikawa
Chemistry an Asian Journal 2016, 11, 2210-2217.
Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand.
Shusuke Tomoshige, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry 2016, 24, 3144-3148.
2017
Structural basis for specific cleavage of Lys6-linked polyubiquitin chains by USP30.
Yusuke Sato, Kei Okatsu, Yasushi Saeki, Koji Yamano, Noriyuki Matsuda, Ai Kaiho, Atsushi Yamagata, Sakurako Goto-Ito, Minoru Ishikawa, Yuichi Hashimoto, Keiji Tanaka, Shuya Fukai
Nature Structural & Molecular Biology 2017, 24, 911-919.
Discovery of small molecules that induce degradation of huntingtin.
Shusuke Tomoshige, Sayaka Nomura, Kenji Ohgane, Yuichi Hashimoto, Minoru Ishikawa
Angewandte Chemie International Edition 2017, 56, 11530-11533.
Photo-enhanced aqueous solubilization of an azo-compound.
Minoru Ishikawa, Takuya Ohzono, Takao Yamaguchi, Yasuo Norikane
Scientific Reports 2017, 7, 6909.
1α-Hydroxy derivatives of 7-dehydrocholesterol are selective liver X receptor modulators.
Kaori Endo-Umeda, Atsushi Aoyama, Masato Shimizu, Minoru Ishikawa, Yuichi Hashimoto, Sachiko Yamada, Makoto Makishima
Journal of Steroid Biochemistry & Molecular Biology 2017, 172, 136-148.
Specific fluorescence labeling of target protein by using ligand–4-azidophthalimide conjugate.
Kosuke Chiba, Miwako Asanuma, Minoru Ishikawa, Yuichi Hashimoto, Kosuke Dodo, Mikiko Sodeoka, and Takao Yamaguchi
Chemical Communications 2017, 53, 8751-8754.
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
Ryuta Shioi, Shogo Okazaki, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi
Bioorganic & Medicinal Chemistry Letters 2017, 27, 3131-3134.
Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.
Hiromitsu Fukuda, Fumika Karaki, Kosuke Dodo, Tomomi Noguchi-Yachide, Minoru Ishikawa, Yuichi Hashimoto, Kenji Ohgane
Bioorganic & Medicinal Chemistry Letters 2017, 27, 2781-2787.
Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
Yosuke Toyota, Sayaka Nomura, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2017, 27, 2776-2780.
Structural development studies of pyrazoloketone-derived acetyl-CoA carboxylase inhibitors.
Shogo Okazaki, Taki Sakai, Minoru Ishikawa, Yuichi Hashimoto, Takao Yamaguchi
Heterocycles 2017, 95, 595-607.
Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules.
Keiichiro Okuhira, Takuji Shoda, Risa Omura, Nobumichi Ohoka, Takayuki Hattori, Norihito Shibata, Yosuke Demizu, Ryo Sugihara, Asato Ichino, Haruka Kawahara, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Masaaki Kurihara, Susumu Itoh, Hiroyuki Saito and Mikihiko Naito
Molecular Pharmacology 2017, 91, 159-166.
2018
Efficient lead finding, activity enhancement and preliminary selectivity control of nuclear receptor ligands bearing a phenanthridinone skeleton
Yuko Nishiyama, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
International Journal of Molecular Sciences 2018, 19, 2090.
Novel non-steroidal progesterone receptor (PR) antagonists with a phenanthridinone skeleton
Yuko Nishiyama, Shuichi Mori, Makoto Makishima, Shinya Fujii, Hiroyuki Kagechika, Yuichi Hashimoto, Minoru Ishikawa
ACS Medicinal Chemistry Letters 2018, 9, 641-645.
神経変性疾患原因タンパク質のケミカルノックダウン
石川稔、友重秀介、野村さやか、山下博子、大金賢司
MEDCHEM NEWS 2018, 28, 88-92.
Structural Development of Tetrachlorophthalimides as Liver X Receptor β (LXRβ)
Selective Agonists with Improved Aqueous Solubility
Sayaka Nomura, Kaori Endo-Umeda, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto,
Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2018, 28, 796-801
Degradation of huntingtin mediated by a hybrid molecule composed of IAP antagonist
linked to phenyldiazenyl benzothiazole derivative
Shusuke Tomoshige, Sayaka Nomura, Kenji Ohgane, Yuichi Hashimoto, Minoru Ishikawa
Bioorganic & Medicinal Chemistry Letters 2018, 28, 707-710.
