List of works - Yukihiro Itoh

"Drug" Discovery with the Help of Organic Chemistry.

scientific article

C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors.

scientific article published on 22 August 2016

Chemical Biology for Pharmaceutical Sciences (Novel Ideas for "Drug" Discovery).

scientific article published in January 2017

Chemical Protein Degradation Approach and its Application to Epigenetic Targets

scientific article published on 12 June 2018

Computational analysis for selectivity of histone deacetylase inhibitor by replica-exchange umbrella sampling molecular dynamics simulations

article

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.

scientific article published on 6 May 2018

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers.

scientific article

Design, synthesis and evaluation of γ-turn mimetics as LSD1-selective inhibitors

scientific article published on 2 January 2018

Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylase 8-selective inhibitors.

scientific article published on 8 January 2014

Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors

scientific article

Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors.

scientific article published on 17 May 2007

Design, synthesis, and biological evaluation of a conjugate of 5-fluorouracil and an LSD1 inhibitor

scientific article published on 24 October 2018

Design, synthesis, and biological evaluation of novel ubiquitin-activating enzyme inhibitors.

scientific article published on 3 March 2018

Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.

scientific article published on August 2010

Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors

scientific article

Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor

scientific article published on 04 November 2019

Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist.

scientific article

Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches

scientific article published on 01 January 2020

Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide

scientific article published on 16 January 2016

False HDAC Inhibition by Aurone Compound

scientific article published on 01 January 2016

Highly Potent and Selective Histone Deacetylase 6 Inhibitors Designed Based on a Small-Molecular Substrate

Hippocampal MicroRNA-124 Enhances Chronic Stress Resilience in Mice.

scientific article published on July 2016

Histone H3 peptide based LSD1-selective inhibitors.

scientific article published on 20 March 2015

Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors.

scientific article

Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site

scientific article published on 12 June 2019

Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.

scientific article

Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells

scientific article published on 23 April 2015

Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators

scientific article published on 23 December 2015

Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.

scientific article published on 13 January 2007

Identification of highly selective and potent histone deacetylase 3 inhibitors using click chemistry-based combinatorial fragment assembly.

scientific article

Identification of novel SIRT2-selective inhibitors using a click chemistry approach

scientific article published on 20 March 2014

Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy

scientific article published on 04 February 2019

Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors

scientific article published on 21 March 2019

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity

scientific article

Isoform-selective histone deacetylase inhibitors.

scientific article published on January 2008

Late-Stage C-H Coupling Enables Rapid Identification of HDAC Inhibitors: Synthesis and Evaluation of NCH-31 Analogues

scientific article published on 3 March 2014

Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.

scientific article

Metabolic-Pathway-Oriented Screening Targeting S-Adenosyl-l-methionine Reveals the Epigenetic Remodeling Activities of Naturally Occurring Catechols

scientific article published on 23 December 2019

N-C-H···O Hydrogen bonds in protein-ligand complexes

scientific article published in Scientific Reports

Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, "selectivity pocket" and NAD+-binding site.

scientific article published on 21 July 2017

Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins.

scientific article published on April 2010

Search for a novel SIRT1 activator: structural modification of SRT1720 and biological evaluation.

scientific article published on 3 July 2013

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein.

scientific article published on 21 March 2011

Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors.

scientific article published on 26 March 2009

Synthesis, LSD1 Inhibitory Activity, and LSD1 Binding Model of Optically Pure Lysine-PCPA Conjugates

scientific article

Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen.

scientific article published on 24 November 2016

[Challenges of Young Chemists to Be Global]

scientific article published on 01 January 2019

List of works by Yukihiro Itoh

"Drug" Discovery with the Help of Organic Chemistry.

C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors.

Chemical Biology for Pharmaceutical Sciences (Novel Ideas for "Drug" Discovery).

Chemical Protein Degradation Approach and its Application to Epigenetic Targets

Computational analysis for selectivity of histone deacetylase inhibitor by replica-exchange umbrella sampling molecular dynamics simulations

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.

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers.

Design, synthesis and evaluation of γ-turn mimetics as LSD1-selective inhibitors

Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylase 8-selective inhibitors.

Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors

Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors.

Design, synthesis, and biological evaluation of a conjugate of 5-fluorouracil and an LSD1 inhibitor

Design, synthesis, and biological evaluation of novel ubiquitin-activating enzyme inhibitors.

Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.

Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors

Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor

Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist.

Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches

Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide

False HDAC Inhibition by Aurone Compound

Highly Potent and Selective Histone Deacetylase 6 Inhibitors Designed Based on a Small-Molecular Substrate

Hippocampal MicroRNA-124 Enhances Chronic Stress Resilience in Mice.

Histone H3 peptide based LSD1-selective inhibitors.

Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors.

Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site

Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.

Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells

Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators

Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.

Identification of highly selective and potent histone deacetylase 3 inhibitors using click chemistry-based combinatorial fragment assembly.

Identification of novel SIRT2-selective inhibitors using a click chemistry approach

Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy

Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity

Isoform-selective histone deacetylase inhibitors.

Late-Stage C-H Coupling Enables Rapid Identification of HDAC Inhibitors: Synthesis and Evaluation of NCH-31 Analogues

Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.

Metabolic-Pathway-Oriented Screening Targeting S-Adenosyl-l-methionine Reveals the Epigenetic Remodeling Activities of Naturally Occurring Catechols

N-C-H···O Hydrogen bonds in protein-ligand complexes

Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, "selectivity pocket" and NAD+-binding site.

Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins.

Search for a novel SIRT1 activator: structural modification of SRT1720 and biological evaluation.

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein.

Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors.

Synthesis, LSD1 Inhibitory Activity, and LSD1 Binding Model of Optically Pure Lysine-PCPA Conjugates

Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen.

[Challenges of Young Chemists to Be Global]