Tooru Kimura

发表

Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-->N intramolecular acyl migration: Design, synthesis and kinetic study.

Y. Kiso, Y. Hamada, H. Matsumoto, 2004, Bioorganic & medicinal chemistry.

Establishment of a biological assay system for human retroviral protease activity.

A. Sakurai, T. Uchiyama, Y. Kiso, 2005, Microbes and infection.

beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.

Kazuki Saito, Y. Kiso, Y. Hamada, 2006, Bioorganic & medicinal chemistry letters.

Synthesis of novel amino acids, l-bis-tetrahydrofuranylglycines

T. Ishida, Y. Kiso, Tooru Kimura, 2002 .

An expedient synthesis of N(alpha)-protected-L-tetrahydrofuranylglycine and its application in the synthesis of novel substrate based inhibitors of HIV-1 protease.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2002, Bioorganic & medicinal chemistry letters.

Development of novel water-soluble photocleavable protective group and its application for design of photoresponsive paclitaxel prodrugs.

S. Hirota, M. Skwarczynski, Y. Kiso, 2008, Bioorganic & medicinal chemistry.

Rigid backbone moiety of KNI-272, a highly selective HIV protease inhibitor: methanol, acetone and dimethylsulfoxide solvated forms of 3-[3-benzyl-2-hydroxy-9-(isoquinolin-5-yloxy)-6-methylsulfanylmethyl-5,8-dioxo-4,7-diazanonanoyl]-N-tert-butyl-1,3-thiazolidine-4-carboxamide.

T. Ishida, Y. Kiso, Tooru Kimura, 2004, Acta crystallographica. Section B, Structural science.

BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.

Kazuki Saito, Y. Kiso, Y. Hamada, 2008, Bioorganic & medicinal chemistry letters.

Design of Potent Aspartic Protease Inhibitors to Treat Various Diseases

Y. Kiso, Y. Hamada, Tooru Kimura, 2008, Archiv der Pharmazie.

‘O-Acyl isopeptide method’ for the efficient synthesis of difficult sequence-containing peptides: use of ‘O-acyl isodipeptide unit’

M. Skwarczynski, Taku Yoshiya, Y. Kiso, 2006 .

KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.

B. Szabó, Y. Kiso, Tooru Kimura, 2003, Bioorganic & medicinal chemistry letters.

Development of first photoresponsive prodrug of paclitaxel.

S. Hirota, M. Skwarczynski, Y. Kiso, 2006, Bioorganic & medicinal chemistry letters.

“Click Peptide“: pH‐Triggered in Situ Production and Aggregation of Monomer Aβ1–42

K. Matsuzaki, Y. Kiso, Tooru Kimura, 2009, Chembiochem : a European journal of chemical biology.

click peptide based on the O-acyl isopeptide method : Control of Aβ1 42 production from a photo-triggered Aβ1 42 analogue

S. Hirota, K. Matsuzaki, Y. Kiso, 2006 .

‘Click peptide’: a novel ‘O‐acyl isopeptide method’ for peptide synthesis and chemical biology‐oriented synthesis of amyloid β peptide analogues

S. Hirota, M. Skwarczynski, Taku Yoshiya, 2006, Journal of peptide science : an official publication of the European Peptide Society.

High-affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor.

Jun Liu, D. Goldberg, E. Freire, 2003, Biochemistry.

"O-acyl isopeptide method" for peptide synthesis: synthesis of forty kinds of "O-acyl isodipeptide unit" Boc-Ser/Thr(Fmoc-Xaa)-OH.

M. Skwarczynski, Taku Yoshiya, Naoko Abe, 2007, Organic & biomolecular chemistry.

O-acyl isopeptide method: efficient synthesis of isopeptide segment and application to racemization-free segment condensation.

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2009, Organic & biomolecular chemistry.

Isopeptide method: development of S‐acyl isopeptide method for the synthesis of difficult sequence‐containing peptides

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2008, Journal of peptide science : an official publication of the European Peptide Society.

Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.

Y. Kiso, Tooru Kimura, J. Nguyen, 2011, Bioorganic & medicinal chemistry letters.

'O-Acyl isopeptide method' : racemization-free segment condensation in solid phase peptide synthesis

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2006 .

Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2004, Bioorganic & medicinal chemistry letters.

'O-Acyl isopeptide method' for the efficient preparation of amyloid beta peptide 1-42 mutants.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2005, Bioorganic & medicinal chemistry.

Development of [Ile40]HTLV‐I protease inhibition assay using novel fluorogenic and chromogenic substrate

Y. Kiso, Tooru Kimura, Y. Hayashi, 2011, Journal of peptide science : an official publication of the European Peptide Society.

The ‘O‐acyl isopeptide method’ for the synthesis of difficult sequence‐containing peptides: application to the synthesis of Alzheimer's disease‐related amyloid β peptide (Aβ) 1–42

Y. Kiso, Tooru Kimura, Y. Hayashi, 2005, Journal of peptide science : an official publication of the European Peptide Society.

Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.

Y. Kiso, Y. Hamada, Tooru Kimura, 2011, Bioorganic & medicinal chemistry.

ON intramolecular acyl migration reaction in the development of prodrugs and the synthesis of difficult sequence‐containing bioactive peptides

M. Skwarczynski, Y. Kiso, Y. Hamada, 2004, Biopolymers.

Novel non-peptidic and small-sized BACE1 inhibitors.

Kazuki Saito, Y. Kiso, Y. Hamada, 2008, Bioorganic & medicinal chemistry letters.

Efficient solid phase peptide synthesis

Y. Kiso, Tooru Kimura, K. Akaji, 2009 .

Fluoren-9-ylmethyloxycarbonyl (Fmoc) amino acid chloride as an efficient reagent for anchoring Fmoc amino acid to 4-alkoxybenzyl alcohol resin.

Y. Kiso, Tooru Kimura, K. Akaji, 1990 .

Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in mutant HIV.

Y. Kiso, Y. Hamada, Tooru Kimura, 2008, Journal of medicinal chemistry.

Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.

Y. Kiso, Y. Hamada, Tooru Kimura, 2010, Bioorganic & medicinal chemistry.

Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.

Kazuki Saito, Y. Kiso, Y. Hamada, 2006, Bioorganic & medicinal chemistry letters.

Development of O-acyl isopeptide method.

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2007, Biopolymers.

EFFICIENT SOLID PHASE PEPTIDE SYNTHESIS ON A PHENACYL-RESIN BY A METHANESULFONIC ACID α-AMINO DEPROTECTING PROCEDURE

Y. Kiso, Tooru Kimura, K. Akaji, 1990 .

O-N intramolecular alkoxycarbonyl migration of typical protective groups in hydroxyamino acids.

M. Skwarczynski, Y. Kiso, Tooru Kimura, 2006, The Journal of organic chemistry.

Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.

Y. Kiso, Y. Hamada, Tooru Kimura, 2005, Bioorganic & medicinal chemistry letters.

KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.

S. Kitazume, T. Saido, Y. Kiso, 2004, Bioorganic & medicinal chemistry letters.

Application of intramolecular migration reaction in peptide chemistry to chemical biology, chemical pharmaceutics and medicinal chemistry.

S. Neuteboom, M. Skwarczynski, Y. Kiso, 2009, Advances in experimental medicine and biology.

O—N Intramolecular Alkoxycarbonyl Migration of Typical Protective Groups in Hydroxyamino Acids.

M. Skwarczynski, Y. Kiso, Tooru Kimura, 2006 .

Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2007, Bioorganic & medicinal chemistry letters.

Search for substrate‐based inhibitors fitting the S2′ space of malarial aspartic protease plasmepsin II

E. Freire, Y. Kiso, Tooru Kimura, 2004, Journal of peptide science : an official publication of the European Peptide Society.

Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases

E. Freire, Y. Kiso, Tooru Kimura, 2004, Biological chemistry.

Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors.

K. Nishiyama, Y. Kiso, Tooru Kimura, 2007, Bioorganic & medicinal chemistry letters.

Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors.

Y. Kiso, Tooru Kimura, J. Nguyen, 2011, Bioorganic & medicinal chemistry letters.

Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2008, Bioorganic & medicinal chemistry.

Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2008, Bioorganic & medicinal chemistry.

Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.

K. Nishiyama, Y. Kiso, Tooru Kimura, 2008, Bioorganic & medicinal chemistry letters.

Analysis of Amide Bond Formation with an α-Hydroxy-β-amino Acid Derivative, 3-Amino-2-hydroxy-4-phenylbutanoic Acid, as an Acyl Component: Byproduction of Homobislactone

Y. Kiso, Tooru Kimura, Y. Hayashi, 2001 .

Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.

E. Freire, Y. Kiso, Tooru Kimura, 2007, Bioorganic & medicinal chemistry letters.

Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target.

E. Freire, I. Luque, Y. Kiso, 2002, Biochemistry.

Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2003, Bioorganic & medicinal chemistry letters.

New water-soluble prodrugs of HIV protease inhibitors based on O-->N intramolecular acyl migration.

Y. Kiso, Y. Hamada, Tooru Kimura, 2002, Bioorganic & medicinal chemistry.

Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.

A. Molla, D. Kempf, R. Kuroki, 2009, Journal of medicinal chemistry.

Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.

E. Freire, Y. Kiso, Tooru Kimura, 2010, Bioorganic & medicinal chemistry letters.

A novel approach of water-soluble paclitaxel prodrug with no auxiliary and no byproduct: design and synthesis of isotaxel.

M. Skwarczynski, Y. Kiso, Y. Hamada, 2003, Journal of medicinal chemistry.

O-N intramolecular acyl migration strategy in water-soluble prodrugs of taxoids.

M. Skwarczynski, Y. Kiso, Tooru Kimura, 2003, Bioorganic & medicinal chemistry letters.

Design and synthesis of a novel water-soluble Aβ1-42 isopeptide: an efficient strategy for the preparation of Alzheimer's disease-related peptide, Aβ1-42, via O–N intramolecular acyl migration reaction

Y. Kiso, Tooru Kimura, Y. Hayashi, 2004 .

O—N Intramolecular Acyl Migration Strategy in Water-Soluble Prodrugs of Taxoids.

M. Skwarczynski, Y. Kiso, Tooru Kimura, 2004 .

Effect of the acyl groups on O-->N acyl migration in the water-soluble prodrugs of HIV-1 protease inhibitor.

Y. Kiso, Y. Hamada, H. Matsumoto, 2003, Bioorganic & medicinal chemistry letters.

S‐acyl isopeptide method: Use of allyl‐type protective group for improved preparation of thioester‐containing S‐acyl isopeptides by Fmoc‐based SPPS

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2011, Biopolymers.

Synthesis of amyloid beta peptide 1-42 (E22Delta) click peptide: pH-triggered in situ production of its native form.

Y. Kiso, Tooru Kimura, Taeko Kakizawa, 2009, Bioorganic & medicinal chemistry.

Controlled Production of Amyloid β Peptide from a Photo‐Triggered, Water‐Soluble Precursor “Click Peptide“

S. Hirota, M. Skwarczynski, K. Matsuzaki, 2008, Chembiochem : a European journal of chemical biology.

‘O‐Acyl isopeptide method’ for peptide synthesis: Solvent effects in the synthesis of Aβ1–42 isopeptide using ‘O‐acyl isodipeptide unit’

Taku Yoshiya, Naoko Abe, Y. Kiso, 2007, Journal of peptide science : an official publication of the European Peptide Society.

The “ O -Acyl Isopeptide Method” for the Synthesis of Alzheimer’s Disease-Related Amyloid β Peptide (Aβ) 1–42

Y. Kiso, Tooru Kimura, Y. Hayashi, 2006 .

Novel and efficient synthesis of difficult sequence-containing peptides through O-N intramolecular acyl migration reaction of O-acyl isopeptides.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2004, Chemical communications.

Epimerization‐free synthesis of cyclic peptide by use of the O‐acyl isopeptide method

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2010, Journal of peptide science : an official publication of the European Peptide Society.

Fmoc‐based solid phase chemical synthesis of 71‐meric neuregulin 1‐β1, an epidermal growth factor‐like domain

Y. Kiso, Tooru Kimura, Y. Hayashi, 2008, Journal of peptide science : an official publication of the European Peptide Society.

No auxiliary, no byproduct strategy for water-soluble prodrugs of taxoids: scope and limitation of O-N intramolecular acyl and acyloxy migration reactions.

M. Skwarczynski, Y. Kiso, Y. Hamada, 2005, Journal of medicinal chemistry.

Syntheses of Natriuretic Peptides Using a New S -Protecting Group, S -Trimethylacetamidomethyl (Tacm) Group

Y. Kiso, Makoto Yoshida, Tooru Kimura, 1994 .

A new thiol protecting trimethylacetamidomethyl group. Synthesis of a new porcine brain natriuretic peptide using the S-trimethylacetamidomethyl-cysteine

Y. Kiso, Makoto Yoshida, Tooru Kimura, 1989 .

A new stepwise deprotection method using reductive acidolysis followed by fluoride ion in solid phase peptide synthesis

Y. Kiso, Tooru Kimura, K. Akaji, 1993 .

A New Stepwise Deprotection Method using Reductive Acidolysis Followed by Fluoride Ion in Solid Phase Peptide Synthesis.

Y. Kiso, Tooru Kimura, K. Akaji, 1994 .

A new reductive acidolysis final deprotection strategy in solid phase peptide synthesis. Use of a new safety-catch linker

Y. Kiso, Tooru Kimura, T. Fukui, 1994 .

Deprotecting Reagents : SiCl4-CF3COOH-Scavenger

Y. Kiso, Tooru Kimura, 1990 .

Anchoring of Fmoc amino acid to 4-alkoxybenzyl alcohol resin using a new esterification reagent

Y. Kiso, Tooru Kimura, K. Akaji, 1992 .

A new deprotecting procedure in peptide synthesis

Y. Kiso, Makoto Yoshida, Tooru Kimura, 1991 .

Tetrafluoroboric acid as a useful deprotecting reagent in Fmoc-based solid-phase peptide syntheses (Fmoc = fluoren-9-ylmethoxycarbonyl)

Y. Kiso, Makoto Yoshida, Tooru Kimura, 1990 .

A new class of amino protecting group removable by reductive acidolysis: the 4-methylsulphinylbenzyloxycarbonyl (Msz) group

Y. Kiso, Makoto Yoshida, Tooru Kimura, 1989 .

Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation.

S. Yokoyama, Y. Kiso, Tooru Kimura, 2009, Bioorganic & medicinal chemistry letters.

Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.

D. Kempf, R. Kuroki, Y. Kiso, 2018, Journal of medicinal chemistry.

Design and synthesis of a new polymer-supported Evans-type oxazolidinone: an efficient chiral auxiliary in the solid-phase asymmetric alkylation reactions

Y. Kiso, Tooru Kimura, Y. Hayashi, 2005 .

A new polymer-supported Evans-type chiral auxiliary derived from α-hydroxy-β-amino acid, phenylnorstatine: synthesis and application in solid-phase asymmetric alkylation reactions

Y. Kiso, Tooru Kimura, Y. Hayashi, 2004 .

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.

Tomoko Ito, Y. Kiso, H. Matsumoto, 2003, Journal of medicinal chemistry.

Structure of HIV-1 protease in complex with potent inhibitor KNI-272 determined by high-resolution X-ray and neutron crystallography

Yusuke Mori, Hiroaki Adachi, Kazuo Kurihara, 2009, Proceedings of the National Academy of Sciences.

Structure of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae bound to an allophenylnorstatine-based inhibitor.

Tooru Kimura, Yoshio Hayashi, Robert McKenna, 2006, Acta crystallographica. Section D, Biological crystallography.

Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.

E. Freire, Y. Kiso, Tooru Kimura, 2008, Bioorganic & medicinal chemistry.

Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties.

Y. Kiso, Y. Hamada, Tooru Kimura, 2007, Bioorganic & medicinal chemistry letters.

KNI‐577, a Potent Small‐Sized HIV Protease Inhibitor Based on the Dipeptide Containing the Hydroxymethylcarbonyl Isostere as an Ideal Transition‐State Mimic

R. Kato, Y. Kiso, H. Matsumoto, 1998, Archiv der Pharmazie.

Small-sized BACE1 inhibitors

Y. Kiso, Tooru Kimura, Z. Ziora, 2006 .

The ‘O‐acyl isopeptide method’ for the synthesis of difficult sequence‐containing peptides: application to the synthesis of Alzheimer's disease‐related amyloid β peptide (Aβ) 1–42

Y. Kiso, Tooru Kimura, Y. Hayashi, 2005, Journal of peptide science : an official publication of the European Peptide Society.

Synthesis of HIV-1 protease analog by ligation of bromoacetyl and mercaptoethylamide peptide prepared using disulfide linkage to solid-support

Y. Kiso, H. Matsumoto, Tooru Kimura, 2002 .

Potent dipeptide HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimetic

R. Kato, Y. Kiso, H. Matsumoto, 2002 .

Allophenylnorstatine containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 ligands

Y. Kiso, H. Matsumoto, Tooru Kimura, 2005 .

Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.

Y. Kiso, Tooru Kimura, Y. Hayashi, 2008, Bioorganic & medicinal chemistry.

Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.

E. Freire, Y. Kiso, Tooru Kimura, 2008, Bioorganic & medicinal chemistry.

O-acyl isopeptide method: efficient synthesis of isopeptide segment and application to racemization-free segment condensation.

Taku Yoshiya, Y. Kiso, Tooru Kimura, 2009, Organic & biomolecular chemistry.

Controlled drug release: new water-soluble prodrugs of an HIV protease inhibitor.

Y. Kiso, H. Matsumoto, Tooru Kimura, 2001, Bioorganic & medicinal chemistry letters.

Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation.

S. Yokoyama, Y. Kiso, Tooru Kimura, 2009, Bioorganic & medicinal chemistry letters.

Evaluation of Malarial Protease Plasmepsin Inhibitors Containing Hydroxymethylcarbonyl Isostere

E. Freire, Y. Kiso, Tooru Kimura, 2006 .

Tetrapeptides, as small‐sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1

Y. Kiso, Y. Hamada, Tooru Kimura, 2010, Journal of peptide science : an official publication of the European Peptide Society.

Design, synthesis, and biological evaluation of anti-HIV double-drugs. conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor through spontaneously cleavable linkers.

K. Sano, Y. Kiso, H. Matsumoto, 2001, Bioorganic & medicinal chemistry.