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Yoshiaki Kiso

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TOP 3
Youhei Sohma; Atsuhiko Taniguchi; Moe Yamasaki; Masayuki Yamashita; Kenichi Akaji; Hiroyuki Kawashima; Hidehito Mukai; Yoshiaki Kiso
Comparative properties of Aβ1-42, Aβ11-42, and [Pyr¹¹]Aβ11-42 generated from O-acyl isopeptides.
Sho Konno; Kiyohiko Nakada; Kentaro Takayama; Pillaiyar Thanigaimalai; Fumika Yakushiji; Takehito Yamamoto; Yuri Yamazaki; Kenichi Akaji; Shen-En Chen; Ernesto Freire; Rie Kakiuchi; Yuko Kawasaki; Yoshiaki Kiso; Yoshio Hayashi
Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety.
Takaaki Mizuguchi; Ryunosuke Ninomiya; Naho Ohara; Kazuki Saito; Shinji Wada; Mika Iida; Yoshiaki Kiso; Kenichi Akaji
Evaluation of dimerization-inhibitory activities of cyclic peptides containing a β-hairpin loop sequence of the EGF receptor.

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2013: Youhei Sohma; Atsuhiko Taniguchi; Moe Yamasaki; Masayuki Yamashita; Kenichi Akaji; Hiroyuki Kawashima; Hidehito Mukai; Yoshiaki Kiso
Comparative properties of Aβ1-42, Aβ11-42, and [Pyr¹¹]Aβ11-42 generated from O-acyl isopeptides.
Bioorganic & medicinal chemistry letters 2013;23(5):1326-9.
2013: Sho Konno; Kiyohiko Nakada; Kentaro Takayama; Pillaiyar Thanigaimalai; Fumika Yakushiji; Takehito Yamamoto; Yuri Yamazaki; Kenichi Akaji; Shen-En Chen; Ernesto Freire; Rie Kakiuchi; Yuko Kawasaki; Yoshiaki Kiso; Yoshio Hayashi
Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety.
Bioorganic & medicinal chemistry 2013;21(2):412-24.
2012: Takaaki Mizuguchi; Ryunosuke Ninomiya; Naho Ohara; Kazuki Saito; Shinji Wada; Mika Iida; Yoshiaki Kiso; Kenichi Akaji
Evaluation of dimerization-inhibitory activities of cyclic peptides containing a β-hairpin loop sequence of the EGF receptor.
Bioorganic & medicinal chemistry 2012;20(19):5730-7.
2012: Yuri Yamazaki; Hiroyuki Yasui; Takumi Chinen; Yoshiki Hayashi; Yoshiaki Kiso; George Kenneth Lloyd; Yurika Masuda; Saskia T C Neuteboom; Michael Palladino; Barbara C M Potts; Makiko Sumikura; Takeo Usui; Fumika Yakushiji; Yoshio Hayashi
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
Bioorganic & medicinal chemistry 2012;20(14):4279-89.
2012: Yoshio Hamada; Koushi Hidaka; Shoichi Ishiura; Tomoya Nakanishi; Kenji Suzuki; Ryoji Yamaguchi; Takashi Hamada; Yoshiaki Kiso
Novel BACE1 inhibitors possessing a 5-nitroisophthalic scaffold at the P2 position.
Bioorganic & medicinal chemistry letters 2012;22(14):4640-4.
2012: Yuri Yamazaki; Hiroyuki Yasui; Tomoko Yoshida; Miki Akamatsu; Takumi Chinen; Gordafaried Deyanat-Yazdi; Kaneo Kanoh; Yoshiaki Kiso; Takayoshi Kitagawa; George Kenneth Lloyd; Brian R Miller; Saskia T C Neuteboom; Benjamin Nicholson; Akiko Oda; Sumie Orikasa; Michael Palladino; Barbara C M Potts; Yuki Shinozaki; Koji Tanaka; Takeo Usui; Fumika Yakushiji; Yoshio Hayashi
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
Journal of medicinal chemistry 2012;55(3):1056-71.
2012: Takaaki Mizuguchi; Kenichi Akaji; Hiroshi Kataoka; Yoshiaki Kiso; Hiromasa Uchimura; Kazuki Saito
Intact-cell-based surface plasmon resonance measurements for ligand affinity evaluation of a membrane receptor.
Analytical biochemistry 2012;420(2):185-7.
2011: Harichandra D Tagad; Jeffrey-Tri Nguyen; Youhei Sohma; Takashi Hamada; Yoshio Hamada; Koushi Hidaka; Tooru Kimura; Yoshiaki Kiso
Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.
Bioorganic & medicinal chemistry 2011;19(17):5238-46.
2011: Henri-Obadja Kumada; Jeffrey-Tri Nguyen; Yoshio Hayashi; Koushi Hidaka; Taeko Kakizawa; Tooru Kimura; Yoshiaki Kiso
Development of [Ile⁴⁰]HTLV-I protease inhibition assay using novel fluorogenic and chromogenic substrate.
Journal of peptide science : an official publication of the European Peptide Society 2011;17(8):569-75.
2011: Youhei Sohma; Atsuhiko Taniguchi; Hui Wang; Moe Yamasaki; Yuta Hirayama; Taeko Kakizawa; Hidehito Mukai; Yoshiaki Kiso
Self-assembly pathways of E22Δ-type amyloid β peptide mutants generated from non-aggregative O-acyl isopeptide precursors.
Bioorganic & medicinal chemistry 2011;19(12):3787-92.
2011: Hiromasa Uchimura; Yusam Kim; Takaaki Mizuguchi; Yoshiaki Kiso; Kazuki Saito
Quantitative evaluation of refolding conditions for a disulfide-bond-containing protein using a concise ¹⁸O-labeling technique.
Protein science : a publication of the Protein Society 2011;20(6):1090-6.
2011: Taku Yoshiya; Ayano Higa; Naoko Abe; Fukue Fukao; Tomomi Kuruma; Yuki Toda; Youhei Sohma; Yoshiaki Kiso
Click Peptide concept: o-acyl isopeptide of islet amyloid polypeptide as a nonaggregative precursor molecule.
Chembiochem : a European journal of chemical biology 2011;12(8):1216-22.
2011: Jeffrey-Tri Nguyen; Keiko Kato; Koushi Hidaka; Henri-Obadja Kumada; Tooru Kimura; Yoshiaki Kiso
Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.
Bioorganic & medicinal chemistry letters 2011;21(8):2425-9.
2011: Jeffrey-Tri Nguyen; Keiko Kato; Henri-Obadja Kumada; Koushi Hidaka; Tooru Kimura; Yoshiaki Kiso
Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(6):1832-7.
2011: Youhei Sohma; Yuta Hirayama; Atsuhiko Taniguchi; Hidehito Mukai; Yoshiaki Kiso
'Click peptide' using production of monomer Aβ from the O-acyl isopeptide: application to assay system of aggregation inhibitors and cellular cytotoxicity.
Bioorganic & medicinal chemistry 2011;19(5):1729-33.
2011: Yuri Yamazaki; Yui Kido; Koushi Hidaka; Hiroyuki Yasui; Yoshiaki Kiso; Fumika Yakushiji; Yoshio Hayashi
Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole.
Bioorganic & medicinal chemistry 2011;19(1):595-602.
2011: Taku Yoshiya; Youhei Sohma; Yuka Hasegawa; Wakana Kawamura; Hiroyuki Kawashima; Tooru Kimura; Yoshiaki Kiso
S-acyl isopeptide method: use of allyl-type protective group for improved preparation of thioester-containing S-acyl isopeptides by Fmoc-based SPPS.
Biopolymers 2011;96(2):228-39.
2010: Takuya Miura; Koushi Hidaka; Tsuyoshi Uemura; Keisuke Kashimoto; Yuto Hori; Yuko Kawasaki; Adam J Ruben; Ernesto Freire; Tooru Kimura; Yoshiaki Kiso
Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.
Bioorganic & medicinal chemistry letters 2010;20(16):4836-9.
2010: Taku Yoshiya; Hiroyuki Kawashima; Yuka Hasegawa; Kazuhiro Okamoto; Tooru Kimura; Youhei Sohma; Yoshiaki Kiso
Epimerization-free synthesis of cyclic peptide by use of the O-acyl isopeptide method.
Journal of peptide science : an official publication of the European Peptide Society 2010;16(8):437-42.
2010: Hidehito Mukai; Yoshiaki Kiso; Kaori Wakamatsu
[Discovery of cryptides and their novel signaling pathways].
Seikagaku. The Journal of Japanese Biochemical Society 2010;82(6):524-32.
2010: Taeko Kakizawa; Koushi Hidaka; Daisuke Hamada; Ryoji Yamaguchi; Tsuyoshi Uemura; Hitomi Kitamura; Harichandra D Tagad; Takashi Hamada; Zyta Ziora; Yoshio Hamada; Tooru Kimura; Yoshiaki Kiso
Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1.
Journal of peptide science : an official publication of the European Peptide Society 2010;16(6):257-62.
2010: Yuri Yamazaki; Makiko Sumikura; Koushi Hidaka; Hiroyuki Yasui; Yoshiaki Kiso; Fumika Yakushiji; Yoshio Hayashi
Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin.
Bioorganic & medicinal chemistry 2010;18(9):3169-74.
2010: Harichandra D Tagad; Yoshio Hamada; Jeffrey-Tri Nguyen; Takashi Hamada; Hamdy M Abdel-Rahman; Abdellah Yamani; Ayaka Nagamine; Hayato Ikari; Naoto Igawa; Koushi Hidaka; Youhei Sohma; Tooru Kimura; Yoshiaki Kiso
Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.
Bioorganic & medicinal chemistry 2010;18(9):3175-86.
2010: Kazuki Saito; Itsuki Yasuo; Hiromasa Uchimura; Shizuyo Koide-Yoshida; Takaaki Mizuguchi; Yoshiaki Kiso
Verification of protein disulfide bond arrangement by in-gel tryptic digestion under entirely neutral pH conditions.
Proteomics 2010;10(7):1505-9.
2010: Yuko Kawasaki; Eduardo E Chufan; Virginie Lafont; Koushi Hidaka; Yoshiaki Kiso; L Mario Amzel; Ernesto Freire
How much binding affinity can be gained by filling a cavity?
Chemical biology & drug design 2010;75(2):143-51.
2009: Koushi Hidaka; Tooru Kimura; Hamdy M Abdel-Rahman; Jeffrey-Tri Nguyen; Keith F McDaniel; William E Kohlbrenner; Akhteruzzaman Molla; Motoyasu Adachi; Taro Tamada; Ryota Kuroki; Noriko Katsuki; Yoshiaki Tanaka; Hikaru Matsumoto; Jun Wang; Yoshio Hayashi; Dale J Kempf; Yoshiaki Kiso
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
Journal of medicinal chemistry 2009;52(23):7604-17.
2009: Taku Yoshiya; Hiroyuki Kawashima; Youhei Sohma; Tooru Kimura; Yoshiaki Kiso
O-acyl isopeptide method: efficient synthesis of isopeptide segment and application to racemization-free segment condensation.
Organic & biomolecular chemistry 2009;7(14):2894-904.
2009: Hui Wang; Taeko Kakizawa; Atsuhiko Taniguchi; Takaaki Mizuguchi; Tooru Kimura; Yoshiaki Kiso
Synthesis of amyloid beta peptide 1-42 (E22Delta) click peptide: pH-triggered in situ production of its native form.
Bioorganic & medicinal chemistry 2009;17(14):4881-7.
2009: Takaaki Mizuguchi; Hiromasa Uchimura; Taeko Kakizawa; Tooru Kimura; Shigeyuki Yokoyama; Yoshiaki Kiso; Kazuki Saito
Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation.
Bioorganic & medicinal chemistry letters 2009;19(12):3279-82.
2009: Thomas Regnier; Diganta Sarma; Koushi Hidaka; Usman Bacha; Ernesto Freire; Yoshio Hayashi; Yoshiaki Kiso
New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(10):2722-7.
2009: Yoshio Hamada; Hiroko Ohta; Naoko Miyamoto; Diganta Sarma; Takashi Hamada; Tomoya Nakanishi; Moe Yamasaki; Abdellah Yamani; Shoichi Ishiura; Yoshiaki Kiso
Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.
Bioorganic & medicinal chemistry letters 2009;19(9):2435-9.
2009: Yoshio Hamada; Yoshiaki Kiso
Recent progress in the drug discovery of non-peptidic BACE1 inhibitors.
Expert opinion on drug discovery 2009;4(4):391-416.
2009: Atsuhiko Taniguchi; Youhei Sohma; Yuta Hirayama; Hidehito Mukai; Tooru Kimura; Yoshio Hayashi; Katsumi Matsuzaki; Yoshiaki Kiso
"Click peptide": pH-triggered in situ production and aggregation of monomer Abeta1-42.
Chembiochem : a European journal of chemical biology 2009;10(4):710-5.
2009: Maiko Ebina; Eugene Futai; Chiaki Tanabe; Noboru Sasagawa; Yoshiaki Kiso; Shoichi Ishiura
Inhibition by KMI-574 leads to dislocalization of BACE1 from lipid rafts.
Journal of neuroscience research 2009;87(2):360-8.
2009: Yuri Yamazaki; Kyoko Kohno; Hiroyuki Yasui; Yoshiaki Kiso; Saskia Neuteboom; Ana M Barral; Barbara Potts; G Kenneth Lloyd; Yoshio Hayashi
Synthesis of biotin-tagged diketopiperazine-based anti-microtubule agents and tubulin photoaffinity labeling.
Advances in experimental medicine and biology 2009;611():527-8.
2009: Yoshio Hayashi; Yuri Yamazaki; Mariusz Skwarczynski; Youhei Sohma; Atsuhiko Taniguchi; Mayo Noguchi; Tooru Kimura; Saskia Neuteboom; Barbara Potts; G Kenneth Lloy; Yoshiaki Kiso
Application of intramolecular migration reaction in peptide chemistry to chemical biology, chemical pharmaceutics and medicinal chemistry.
Advances in experimental medicine and biology 2009;611():513-4.
2009: Hiromi Koder; Naoki Nishishita; Yoshiaki Hirano; Yoshiaki Kiso; Yoshio Hayashi
Synthesis of polylactides with side chain functionality: ring-opening polymerimerization of a homobislactone prepared from lysine.
Advances in experimental medicine and biology 2009;611():243-4.
2009: Taku Yoshiya; Youhei Sohma; Yoshio Hamada; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Racemization-free segment condensation based on the O-acyl isopeptide method: toward a chemical protein synthesis on solid support.
Advances in experimental medicine and biology 2009;611():161-2.
2009: Yoshio Hayashi; Shigenobu Nishiguchi; Magne O Sydnes; Thomas Regnier; Jun-Ya Hasegawa; Takahiro Katoh; Tetsuya Kajimoto; Manabu Node; Yoshiaki Kiso
A new synthesis of (+)-negamycin and its derivatives as a potential therapeutic agent for Duchenne muscular dystrophy treatment.
Advances in experimental medicine and biology 2009;611():137-8.
2008: Koushi Hidaka; Tooru Kimura; Adam J Ruben; Tsuyoshi Uemura; Mami Kamiya; Aiko Kiso; Tetsuya Okamoto; Yumi Tsuchiya; Yoshio Hayashi; Ernesto Freire; Yoshiaki Kiso
Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.
Bioorganic & medicinal chemistry 2008;16(23):10049-60.
2008: Kentaro Takayama; Yuka Suehisa; Takuya Fujita; Jeffrey-Tri Nguyen; Shiroh Futaki; Akira Yamamoto; Yoshiaki Kiso; Yoshio Hayashi
Oligoarginine-based prodrugs with self-cleavable spacers for caco-2 cell permeation.
Chemical & pharmaceutical bulletin 2008;56(11):1515-20.
2008: Taku Yoshiya; Nui Ito; Tooru Kimura; Yoshiaki Kiso
Isopeptide method: development of S-acyl isopeptide method for the synthesis of difficult sequence-containing peptides.
Journal of peptide science : an official publication of the European Peptide Society 2008;14(11):1203-8.
2008: Jeffrey-Tri Nguyen; Yoshio Hamada; Tooru Kimura; Yoshiaki Kiso
Design of potent aspartic protease inhibitors to treat various diseases.
Archiv der Pharmazie 2008;341(9):523-35.
2008: Meihui Zhang; Jeffrey-Tri Nguyen; Henri-Obadja Kumada; Tooru Kimura; Maosheng Cheng; Yoshio Hayashi; Yoshiaki Kiso
Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.
Bioorganic & medicinal chemistry 2008;16(14):6880-90.
2008: Katsumi Matsuzaki; Takuma Okada; Miho Tsukuda; Keisuke Ikeda; Youhei Sohma; Yousuke Chiyomori; Atsuhiko Taniguchi; Setsuko Nakamura; Nui Ito; Yoshio Hayashi; Yoshiaki Kiso
Design, synthesis, and biophysical properties of a helical Abeta1-42 analog: Inhibition of fibrillogenesis and cytotoxicity.
Biochemical and biophysical research communications 2008;371(4):777-80.
2008: Usman Bacha; Jennifer Barrila; Sandra B. Gabelli; Yoshiaki Kiso; L Mario Amzel; Ernesto Freire
Development of broad-spectrum halomethyl ketone inhibitors against coronavirus main protease 3CL(pro).
Chemical biology & drug design 2008;72(1):34-49.
2008: Yoshio Hayashi; Thomas Regnier; Shigenobu Nishiguchi; Magne O Sydnes; Daisuke Hashimoto; Junya Hasegawa; Takahiro Katoh; Tetsuya Kajimoto; Masataka Shiozuka; Ryoichi Matsuda; Manabu Node; Yoshiaki Kiso
Efficient total synthesis of (+)-negamycin, a potential chemotherapeutic agent for genetic diseases.
Chemical communications (Cambridge, England) 2008;(20):2379-81.
2008: Shingo Nakatani; Koushi Hidaka; Ei'ichi Ami; Koichiro Nakahara; Akihiko Sato; Jeffrey-Tri Nguyen; Yoshio Hamada; Yasuko Hori; Nobuyuki Ohnishi; Akinori Nagai; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in mutant HIV.
Journal of medicinal chemistry 2008;51(10):2992-3004.
2008: Mayo Noguchi; Mariusz Skwarczynski; Halan Prakash; Shun Hirota; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Development of novel water-soluble photocleavable protective group and its application for design of photoresponsive paclitaxel prodrugs.
Bioorganic & medicinal chemistry 2008;16(10):5389-97.
2008: Meihui Zhang; Jeffrey-Tri Nguyen; Henri-Obadja Kumada; Tooru Kimura; Maosheng Cheng; Yoshio Hayashi; Yoshiaki Kiso
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.
Bioorganic & medicinal chemistry 2008;16(10):5795-802.
2008: Yoshio Hamada; Hiroko Ohta; Naoko Miyamoto; Ryoji Yamaguchi; Abdellah Yamani; Koushi Hidaka; Tooru Kimura; Kazuki Saito; Yoshio Hayashi; Shoichi Ishiura; Yoshiaki Kiso
Novel non-peptidic and small-sized BACE1 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(5):1643-7.
2008: Yoshio Hamada; Hamdy Abdel-Rahman; Abdellah Yamani; Jeffrey-Tri Nguyen; Monika Stochaj; Koushi Hidaka; Tooru Kimura; Yoshio Hayashi; Kazuki Saito; Shoichi Ishiura; Yoshiaki Kiso
BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.
Bioorganic & medicinal chemistry letters 2008;18(5):1649-53.
2008: Taeko Kakizawa; Shizuyo Koide-Yoshida; Tooru Kimura; Hiromasa Uchimura; Yoshio Hayashi; Kazuki Saito; Yoshiaki Kiso
Fmoc-based solid phase chemical synthesis of 71-meric neuregulin 1-beta1, an epidermal growth factor-like domain.
Journal of peptide science : an official publication of the European Peptide Society 2008;14(3):261-6.
2008: Jeffrey-Tri Nguyen; Meihui Zhang; Henri-Obadja Kumada; Ayako Itami; Keiji Nishiyama; Tooru Kimura; Maosheng Cheng; Yoshio Hayashi; Yoshiaki Kiso
Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(1):366-70.
2007: Atsuhiko Taniguchi; Taku Yoshiya; Naoko Abe; Fukue Fukao; Youhei Sohma; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
'O-Acyl isopeptide method' for peptide synthesis: Solvent effects in the synthesis of Abeta1-42 isopeptide using 'O-acyl isodipeptide unit'.
Journal of peptide science : an official publication of the European Peptide Society 2007;13(12):868-74.
2007: Yoshio Hayashi; Kentaro Takayama; Yuka Suehisa; Takuya Fujita; Jeffrey-Tri Nguyen; Shiroh Futaki; Akira Yamamoto; Yoshiaki Kiso
Development of oligoarginine-drug conjugates linked to new peptidic self-cleavable spacers toward effective intestinal absorption.
Bioorganic & medicinal chemistry letters 2007;17(18):5129-32.
2007: Ei'ichi Ami; Koichiro Nakahara; Akihiko Sato; Jeffrey-Tri Nguyen; Koushi Hidaka; Yoshio Hamada; Shingo Nakatani; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties.
Bioorganic & medicinal chemistry letters 2007;17(15):4213-7.
2007: Tooru Kimura; Jeffrey-Tri Nguyen; Hikoichiro Maegawa; Keiji Nishiyama; Yasuhiro Arii; Yasuko Matsui; Yoshio Hayashi; Yoshiaki Kiso
Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(12):3276-80.
2007: Taku Yoshiya; Atsuhiko Taniguchi; Youhei Sohma; Fukue Fukao; Setsuko Nakamura; Naoko Abe; Nui Ito; Mariusz Skwarczynski; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
"O-acyl isopeptide method" for peptide synthesis: synthesis of forty kinds of "O-acyl isodipeptide unit" Boc-Ser/Thr(Fmoc-Xaa)-OH.
Organic & biomolecular chemistry 2007;5(11):1720-30.
2007: Virginie Lafont; Anthony A Armstrong; Hiroyasu Ohtaka; Yoshiaki Kiso; L Mario Amzel; Ernesto Freire
Compensating enthalpic and entropic changes hinder binding affinity optimization.
Chemical biology & drug design 2007;69(6):413-22.
2007: Koushi Hidaka; Tooru Kimura; Yumi Tsuchiya; Mami Kamiya; Adam J Ruben; Ernesto Freire; Yoshio Hayashi; Yoshiaki Kiso
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.
Bioorganic & medicinal chemistry letters 2007;17(11):3048-52.
2007: Zyta Ziora; Soko Kasai; Koushi Hidaka; Ayaka Nagamine; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid.
Bioorganic & medicinal chemistry letters 2007;17(6):1629-33.
2007: Mariusz Skwarczynski; Yoshiaki Kiso
Application of the O-N intramolecular acyl migration reaction in medicinal chemistry.
Current medicinal chemistry 2007;14(26):2813-23.
2007: Youhei Sohma; Taku Yoshiya; Atsuhiko Taniguchi; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Development of O-acyl isopeptide method.
Biopolymers 2007;88(2):253-62.
2006: Mariusz Skwarczynski; Yoshio Hayashi; Yoshiaki Kiso
Paclitaxel prodrugs: toward smarter delivery of anticancer agents.
Journal of medicinal chemistry 2006;49(25):7253-69.
2006: Youhei Sohma; Atsuhiko Taniguchi; Taku Yoshiya; Yousuke Chiyomori; Fukue Fukao; Setsuko Nakamura; Mariusz Skwarczynski; Takuma Okada; Keisuke Ikeda; Yoshio Hayashi; Tooru Kimura; Shun Hirota; Katsumi Matsuzaki; Yoshiaki Kiso
'Click peptide': a novel 'O-acyl isopeptide method' for peptide synthesis and chemical biology-oriented synthesis of amyloid beta peptide analogues.
Journal of peptide science : an official publication of the European Peptide Society 2006;12(12):823-8.
2006: Masatoshi Inden; Takahiro Taira; Yoshihisa Kitamura; Takashi Yanagida; Daiju Tsuchiya; Kazuyuki Takata; Daijiro Yanagisawa; Kaneyasu Nishimura; Takashi Taniguchi; Yoshiaki Kiso; Kanji Yoshimoto; Tomohiro Agatsuma; Shizuyo Koide-Yoshida; Sanae M M Iguchi-Ariga; Shun Shimohama; Hiroyoshi Ariga
PARK7 DJ-1 protects against degeneration of nigral dopaminergic neurons in Parkinson's disease rat model.
Neurobiology of disease 2006;24(1):144-58.
2006: Mariusz Skwarczynski; Mayo Noguchi; Shun Hirota; Youhei Sohma; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Development of first photoresponsive prodrug of paclitaxel.
Bioorganic & medicinal chemistry letters 2006;16(17):4492-6.
2006: Yoshio Hamada; Naoto Igawa; Hayato Ikari; Zyta Ziora; Jeffrey-Tri Nguyen; Abdellah Yamani; Koushi Hidaka; Tooru Kimura; Kazuki Saito; Yoshio Hayashi; Maiko Ebina; Shoichi Ishiura; Yoshiaki Kiso
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
Bioorganic & medicinal chemistry letters 2006;16(16):4354-9.
2006: Tooru Kimura; Yoshio Hamada; Monika Stochaj; Hayato Ikari; Ayaka Nagamine; Hamdy Abdel-Rahman; Naoto Igawa; Koushi Hidaka; Jeffrey-Tri Nguyen; Kazuki Saito; Yoshio Hayashi; Yoshiaki Kiso
Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.
Bioorganic & medicinal chemistry letters 2006;16(9):2380-6.
2006: Mariusz Skwarczynski; Youhei Sohma; Mayo Noguchi; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
O-N intramolecular alkoxycarbonyl migration of typical protective groups in hydroxyamino acids.
The Journal of organic chemistry 2006;71(6):2542-5.
2006: Atsuhiko Taniguchi; Youhei Sohma; Maiko Kimura; Takuma Okada; Keisuke Ikeda; Yoshio Hayashi; Tooru Kimura; Shun Hirota; Katsumi Matsuzaki; Yoshiaki Kiso
"Click peptide" based on the "o-acyl isopeptide method": control of A beta1-42 production from a photo-triggered A beta1-42 analogue.
Journal of the American Chemical Society 2006;128(3):696-7.
2006: Jeffrey-Tri Nguyen; Abdellah Yamani; Yoshiaki Kiso
Views on amyloid hypothesis and secretase inhibitors for treating Alzheimer's disease: progress and problems.
Current pharmaceutical design 2006;12(33):4295-312.
2006: Adam J Ruben; Yoshiaki Kiso; Ernesto Freire
Overcoming roadblocks in lead optimization: a thermodynamic perspective.
Chemical biology & drug design 2006;67(1):2-4.
2006: Masashi Asai; Chinatsu Hattori; Nobuhisa Iwata; Takaomi C Saido; Noboru Sasagawa; Beáta Szabó; Yasuhiro Hashimoto; Kei Maruyama; Sei-ichi Tanuma; Yoshiaki Kiso; Shoichi Ishiura
The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice.
Journal of neurochemistry 2006;96(2):533-40.
2005: Youhei Sohma; Yousuke Chiyomori; Maiko Kimura; Fukue Fukao; Atsuhiko Taniguchi; Yoshio Hayashi; Tooru Kimura; Yoshiaki Kiso
'O-Acyl isopeptide method' for the efficient preparation of amyloid beta peptide 1-42 mutants.
Bioorganic & medicinal chemistry 2005;13(22):6167-74.
2005: Youhei Sohma; Yoshio Hayashi; Maiko Kimura; Yousuke Chiyomori; Atsuhiko Taniguchi; Masato Sasaki; Tooru Kimura; Yoshiaki Kiso
The 'O-acyl isopeptide method' for the synthesis of difficult sequence-containing peptides: application to the synthesis of Alzheimer's disease-related amyloid beta peptide (Abeta) 1-42.
Journal of peptide science : an official publication of the European Peptide Society 2005;11(8):441-51.
2005: Mariusz Skwarczynski; Youhei Sohma; Mayo Noguchi; Maiko Kimura; Yoshio Hayashi; Yoshio Hamada; Tooru Kimura; Yoshiaki Kiso
No auxiliary, no byproduct strategy for water-soluble prodrugs of taxoids: scope and limitation of O-N intramolecular acyl and acyloxy migration reactions.
Journal of medicinal chemistry 2005;48(7):2655-66.
2005: Tooru Kimura; Daisuke Shuto; Yoshio Hamada; Naoto Igawa; Soko Kasai; Ping Liu; Koushi Hidaka; Takashi Hamada; Yoshio Hayashi; Yoshiaki Kiso
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Bioorganic & medicinal chemistry letters 2005;15(1):211-5.
2004: Hikoichiro Maegawa; Tooru Kimura; Yasuhiro Arii; Yasuko Matsui; Soko Kasai; Yoshio Hayashi; Yoshiaki Kiso
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.
Bioorganic & medicinal chemistry letters 2004;14(23):5925-9.
2004: Hamdy M Abdel-Rahman; Tooru Kimura; Koushi Hidaka; Aiko Kiso; Azin Nezami; Ernesto Freire; Yoshio Hayashi; Yoshiaki Kiso
Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases.
Biological chemistry 2004;385(11):1035-9.
2004: Aiko Kiso; Koushi Hidaka; Tooru Kimura; Yoshio Hayashi; Azin Nezami; Ernesto Freire; Yoshiaki Kiso
Search for substrate-based inhibitors fitting the S2' space of malarial aspartic protease plasmepsin II.
Journal of peptide science : an official publication of the European Peptide Society 2004;10(11):641-7.
2004: Sonia Vega; Lin-Woo Kang; Adrian Velazquez-Campoy; Yoshiaki Kiso; Mario Amzel; Ernesto Freire
A structural and thermodynamic escape mechanism from a drug resistant mutation of the HIV-1 protease.
Proteins 2004;55(3):594-602.
2004: Tooru Kimura; Daisuke Shuto; Soko Kasai; Ping Liu; Koushi Hidaka; Takashi Hamada; Yoshio Hayashi; Chinatsu Hattori; Masashi Asai; Shinobu Kitazume; Takaomi C Saido; Shoichi Ishiura; Yoshiaki Kiso
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Bioorganic & medicinal chemistry letters 2004;14(6):1527-31.
2004: Youhei Sohma; Masato Sasaki; Yoshio Hayashi; Tooru Kimura; Yoshiaki Kiso
Novel and efficient synthesis of difficult sequence-containing peptides through O-N intramolecular acyl migration reaction of O-acyl isopeptides.
Chemical communications (Cambridge, England) 2004;(1):124-5.
2004: Yoshio Hamada; Hikaru Matsumoto; Satoshi Yamaguchi; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-->N intramolecular acyl migration: Design, synthesis and kinetic study.
Bioorganic & medicinal chemistry 2004;12(1):159-70.
2004: Youhei Sohma; Yoshio Hayashi; Mariusz Skwarczynski; Yoshio Hamada; Masato Sasaki; Tooru Kimura; Yoshiaki Kiso
O-N intramolecular acyl migration reaction in the development of prodrugs and the synthesis of difficult sequence-containing bioactive peptides.
Biopolymers 2004;76(4):344-56.
2003: Mariusz Skwarczynski; Youhei Sohma; Maiko Kimura; Yoshio Hayashi; Tooru Kimura; Yoshiaki Kiso
O-N intramolecular acyl migration strategy in water-soluble prodrugs of taxoids.
Bioorganic & medicinal chemistry letters 2003;13(24):4441-4.
2003: Daisuke Shuto; Soko Kasai; Tooru Kimura; Ping Liu; Koushi Hidaka; Takashi Hamada; Saeko Shibakawa; Yoshio Hayashi; Chinatsu Hattori; Beata Szabo; Shoichi Ishiura; Yoshiaki Kiso
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.
Bioorganic & medicinal chemistry letters 2003;13(24):4273-6.
2003: Youhei Sohma; Yoshio Hayashi; Tomoko Ito; Hikaru Matsumoto; Tooru Kimura; Yoshiaki Kiso
Development of water-soluble prodrugs of the HIV-1 protease inhibitor KNI-727: importance of the conversion time for higher gastrointestinal absorption of prodrugs based on spontaneous chemical cleavage.
Journal of medicinal chemistry 2003;46(19):4124-35.
2003: Yoshio Hayashi; Mariusz Skwarczynski; Yoshio Hamada; Youhei Sohma; Tooru Kimura; Yoshiaki Kiso
A novel approach of water-soluble paclitaxel prodrug with no auxiliary and no byproduct: design and synthesis of isotaxel.
Journal of medicinal chemistry 2003;46(18):3782-4.
2003: Yoshio Hamada; Hikaru Matsumoto; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Effect of the acyl groups on O-->N acyl migration in the water-soluble prodrugs of HIV-1 protease inhibitor.
Bioorganic & medicinal chemistry letters 2003;13(16):2727-30.
2003: Azin Nezami; Tooru Kimura; Koushi Hidaka; Aiko Kiso; Jun Liu; Yoshiaki Kiso; Daniel E Goldberg; Ernesto Freire
High-affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor.
Biochemistry 2003;42(28):8459-64.
2002: S Rajesh; Ei'ichi Ami; Tomoya Kotake; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
An expedient synthesis of N(alpha)-protected-L-tetrahydrofuranylglycine and its application in the synthesis of novel substrate based inhibitors of HIV-1 protease.
Bioorganic & medicinal chemistry letters 2002;12(24):3615-7.
2002: Yoshio Hamada; Jun Ohtake; Youhei Sohma; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
New water-soluble prodrugs of HIV protease inhibitors based on O-->N intramolecular acyl migration.
Bioorganic & medicinal chemistry 2002;10(12):4155-67.
2002: Azin Nezami; Irene Luque; Tooru Kimura; Yoshiaki Kiso; Ernesto Freire
Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target.
Biochemistry 2002;41(7):2273-80.
2001: M Song; S Rajesh; Yoshio Hayashi; Yoshiaki Kiso
Design and synthesis of new inhibitors of HIV-1 protease dimerization with conformationally constrained templates.
Bioorganic & medicinal chemistry letters 2001;11(18):2465-8.
2001: Yoshio Hayashi; Y Kinoshita; Koushi Hidaka; Aiko Kiso; H Uchibori; Tooru Kimura; Yoshiaki Kiso
Analysis of amide bond formation with an alpha-hydroxy-beta-amino acid derivative, 3-amino-2-hydroxy-4-phenylbutanoic acid, as an acyl component: byproduction of homobislactone.
The Journal of organic chemistry 2001;66(16):5537-44.
2001: Adrian Velazquez-Campoy; Yoshiaki Kiso; Ernesto Freire
The binding energetics of first- and second-generation HIV-1 protease inhibitors: implications for drug design.
Archives of biochemistry and biophysics 2001;390(2):169-75.
2001: Hikaru Matsumoto; Tooru Kimura; T Hamawaki; A Kumagai; T Goto; K Sano; Yoshio Hayashi; Yoshiaki Kiso
Design, synthesis, and biological evaluation of anti-HIV double-drugs. conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor through spontaneously cleavable linkers.
Bioorganic & medicinal chemistry 2001;9(6):1589-600.
2001: Hikaru Matsumoto; Youhei Sohma; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Controlled drug release: new water-soluble prodrugs of an HIV protease inhibitor.
Bioorganic & medicinal chemistry letters 2001;11(4):605-9.
2001: Hikaru Matsumoto; T Matsuda; S Nakata; T Mitoguchi; Tooru Kimura; Yoshio Hayashi; Yoshiaki Kiso
Synthesis and biological evaluation of prodrug-type anti-HIV agents: ester conjugates of carboxylic acid-containing dipeptide HIV protease inhibitors and a reverse transcriptase inhibitor.
Bioorganic & medicinal chemistry 2001;9(2):417-30.
2000: Yoshio Hayashi; S Orikasa; K Tanaka; K Kanoh; Yoshiaki Kiso
Total synthesis of anti-microtubule diketopiperazine derivatives: phenylahistin and aurantiamine.
The Journal of organic chemistry 2000;65(24):8402-5.
2000: Adrian Velazquez-Campoy; Irene Luque; MJ Todd; M Milutinovich; Yoshiaki Kiso; Ernesto Freire
Thermodynamic dissection of the binding energetics of KNI-272, a potent HIV-1 protease inhibitor.
Protein science : a publication of the Protein Society 2000;9(9):1801-9.
2000: Hikaru Matsumoto; T Hamawaki; H Ota; Tooru Kimura; T Goto; K Sano; Yoshio Hayashi; Yoshiaki Kiso
'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.
Bioorganic & medicinal chemistry letters 2000;10(11):1227-31.