List of works - Yosuke Demizu

A Helix-Stabilized Cell-Penetrating Peptide as an Intracellular Delivery Tool

scientific article published on 03 December 2015

A preorganized β-amino acid bearing a guanidinium side chain and its use in cell-penetrating peptides

scientific article published on 21 April 2015

A synthetic cannabinoid FDU-NNEI, two 2H-indazole isomers of synthetic cannabinoids AB-CHMINACA and NNEI indazole analog (MN-18), a phenethylamine derivative N–OH-EDMA, and a cathinone derivative dimethoxy-α-PHP, newly identified in illegal products

scientific article (publication date: 11 February 2015)

Amphipathic short helix-stabilized peptides with cell-membrane penetrating ability.

scientific article published on 13 March 2014

An extended planar C5 conformation and a 310-helical structure of peptide foldamer composed of diverse alpha-ethylated alpha,alpha-disubstituted alpha-amino acids

scientific article published on 01 July 2003

Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.

scientific article published in January 2007

Chiral centers in the side chains of alpha-amino acids control the helical screw sense of peptides

scientific article published on 01 October 2004

Conformational studies on peptides containing α,α-disubstituted α-amino acids: chiral cyclic α,α-disubstituted α-amino acid as an α-helical inducer

scientific article published on 25 March 2011

Conformations of helical Aib peptides containing a pair of L-amino acid and D-amino acid

scientific article published on 22 May 2012

Conformations of peptides containing a chiral cyclic α, α‐disubstituted α‐amino acid within the sequence of Aib residues ⬇️

scientific article published on November 1, 2010

Controlling 3(10)-helix and alpha-helix of short peptides in the solid state

scientific article published on 01 May 2007

Controlling the helical screw sense of peptides with C-terminal L-valine.

scientific article published in March 2010

De Novo Design of Cell-penetrating Foldamers

scientific article published on 28 May 2020

Design and synthesis of cell-permeable fluorescent nitrilotriacetic acid derivatives

scientific article published on 24 September 2018

Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.

scientific article published on 28 November 2011

Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton

scientific article published on 09 February 2018

Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton

scientific article published on 08 December 2016

Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator.

scientific article published on 4 December 2013

Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands ⬇️

scientific article published on August 17, 2011

Design, synthesis, and anti-HIV-1 activity of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N-3,5-dimethylbenzyl-substituted urea derivatives.

scientific article published on February 2015

Design, synthesis, and anti-HIV-1 activity of 1-substituted 3-(3,5-dimethylbenzyl)triazine derivatives.

scientific article published on 28 October 2015

Development of 2-aminoisobutyric acid (Aib)-rich cell-penetrating foldamers for efficient siRNA delivery

scientific article published on 01 July 2019

Development of Amphipathic Antimicrobial Peptide Foldamers Based on Magainin 2 Sequence

scientific article published on 06 November 2019

Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand.

scientific article published on 15 September 2016

Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins

scientific article published on 16 October 2019

Development of a Cell-penetrating Peptide that Exhibits Responsive Changes in its Secondary Structure in the Cellular Environment.

scientific article published on 9 September 2016

Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins.

scientific article published in May 2017

Development of a peptide-based inducer of nuclear receptors degradation

scientific article published on 07 April 2016

Development of a peptide-based inducer of protein degradation targeting NOTCH1.

scientific article published on 7 October 2017

Development of an ON/OFF switchable fluorescent probe targeting His tag fused proteins in living cells.

scientific article

Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription.

scientific article

Development of helix-stabilized antimicrobial peptides composed of lysine and hydrophobic α,α-disubstituted α-amino acid residues

scientific article published on 29 July 2017

Development of helix-stabilized cell-penetrating peptides containing cationic α,α-disubstituted amino acids as helical promoters.

scientific article published in February 2017

Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells.

scientific article published on 11 October 2013

Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.

scientific article published on 10 June 2013

Diastereomeric Right- and Left-Handed Helical Structures with Fourteen (R)-Chiral Centers

scientific article

Direct electrochemical alpha-cyanation of N-protected cyclic amines.

scientific article

Effect of one D-Leu residue on right-handed helical -L-Leu-Aib- peptides in the crystal state

scientific article published on 21 February 2011

Effects of D-Leu residues on the helical secondary structures of L-Leu-based nonapeptides

scientific article published on 01 January 2015

Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton

scientific article

Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic.

scientific article published on 24 March 2017

Extent of Helical Induction Caused by Introducing α-Aminoisobutyric Acid into an Oligovaline Sequence

scientific article published on 14 June 2018

Front Cover: Recent Advances in PROTAC Technology Toward New Therapeutic Modalities (Chem. Biodiversity 11/2022)

scientific article published in 2022

Helical foldamer containing a combination of cyclopentane-1,2-diamine and 2,2-dimethylmalonic acid

scientific article published on 17 September 2013

Helical peptide-foldamers having a chiral five-membered ring amino acid with two azido functional groups

scientific article published on 16 September 2014

Helical-screw directions of diastereoisomeric cyclic alpha-amino acid oligomers.

scientific article published in March 2009

Identification of embryonic precursor cells that differentiate into thymic epithelial cells expressing autoimmune regulator

scientific article published on 11 July 2016

Identification of mutaprodenafil in a dietary supplement and its subsequent synthesis

scientific article published on 01 January 2011

Inhibition of β-amyloid-induced neurotoxicity by planar analogues of procyanidin B3

scientific article published on 23 July 2019

Isoheleproline: a new amino acid-sesquiterpene adduct from Inula helenium

scientific article published on 07 November 2013

Left-Handed Helix of Three-Membered Ring Amino Acid Homopeptide Interrupted by an N-H···Ethereal O-Type Hydrogen Bond

scientific article published on 30 November 2018

Lipase-catalyzed kinetic resolution of cyclic trans-1,2-diols bearing a diester moiety: synthetic application to chiral seven-membered-ring alpha,alpha-disubstituted alpha-amino acid

scientific article published on 22 August 2007

Low pH-triggering changes in peptide secondary structures

scientific article published in August 2017

Molecular Design, Synthesis, and Evaluation of SNIPER(ER) That Induces Proteasomal Degradation of ERα.

scientific article published in January 2016

Monoallylation of 1,2-diols by Pd/Sn bimetallic catalysis

scientific article published on 27 January 2012

NAD-dependent isocitrate dehydrogenase as a novel target of tributyltin in human embryonic carcinoma cells

scientific article

Oligopeptides with equal amounts of L- and D-amino acids may prefer a helix screw sense.

scientific article

One-handed helical screw direction of homopeptide foldamer exclusively induced by cyclic α-amino acid side-chain chiral centers

scientific article published on 20 January 2012

PNA monomers fully compatible with standard Fmoc-based solid-phase synthesis of pseudocomplementary PNA.

scientific article published on 3 June 2017

Peptide Nucleic Acid with a Lysine Side Chain at the β-Position: Synthesis and Application for DNA Cleavage.

scientific article published in January 2016

Plasmid DNA delivery by arginine-rich cell-penetrating peptides containing unnatural amino acids

scientific article published on 19 April 2016

Plasmid DNA delivery using fluorescein-labeled arginine-rich peptides.

scientific article published on 21 May 2015

Preorganized Cyclic α,α-Disubstituted α-Amino Acids Bearing Functionalized Side Chains That Act as Peptide-Helix Inducers

scientific article published on 15 September 2017

Rational Design and Synthesis of Post-Functionalizable Peptide Foldamers as Helical Templates.

scientific article published on 14 November 2017

Rational Design of Helix-Stabilized Antimicrobial Peptide Foldamers Containing α,α-Disubstituted Amino Acids or Side-Chain Stapling

scientific article published on 01 December 2020

Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

scientific article published on 04 April 2019

Regioselective protection of sugars catalyzed by dimethyltin dichloride

scientific article published on 10 October 2008

Screw-sense control of helical oligopeptides containing equal amounts of L- and D-amino acids

scientific article published on 23 August 2011

Side-chain chiral centers of amino acid and helical-screw handedness of its peptides

scientific article published on 01 August 2005

Simple and efficient knockdown of His-tagged proteins by ternary molecules consisting of a His-tag ligand, a ubiquitin ligase ligand, and a cell-penetrating peptide.

scientific article published on 2 August 2017

Structural Development of Cell-Penetrating Peptides Containing Cationic Proline Derivatives.

scientific article published in January 2018

Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon

scientific article published on 09 November 2018

Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription.

scientific article

Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors

scientific article published on 12 January 2015

Synthesis and Evaluation of Novel Carbocyclic Oxetanocin A (COA-Cl) Derivatives as Potential Tube Formation Agents

scientific article published on January 2015

Synthesis and Resolution of Substituted [5]Carbohelicenes

scientific article published on 09 June 2015

Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives

scientific article published in March 2006

Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator

scientific article published on 07 May 2016

Synthesis and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.

scientific article published on 11 May 2015

Synthesis of 6-arylthio analogs of 2',3'-dideoxy-3'-fluoroguanosine and their effect against hepatitis B virus replication

scientific article published on January 2006

Synthesis of chiral five-membered carbocyclic ring amino acids with an acetal moiety and helical conformations of its homo-chiral homopeptides

scientific article published on 01 November 2016

Tamoxifen and Fulvestrant Hybrids Showed Potency as Selective Estrogen Receptor Down-Regulators.

scientific article published on 5 August 2016

Targeted Degradation of Proteins Localized in Subcellular Compartments by Hybrid Small Molecules.

scientific article

The side-chain hydroxy groups of a cyclic α,α-disubstituted α-amino acid promote oligopeptide 310 -helix packing in the crystalline state.

scientific article

Three-dimensional structural control of diastereomeric Leu-Leu-Aib-Leu-Leu-Aib sequences in the solid state

scientific article published on 01 August 2010

Topological Study of the Structures of Heterochiral Peptides Containing Equal Amounts of l-Leu and d-Leu

scientific article published on 22 August 2015

Twisted structure of a cyclic hexapeptide containing a combination of alternating L-Leu-D-Leu-Aib segments

scientific article published on 03 October 2012

β-PNA: peptide nucleic acid (PNA) with a chiral center at the β-position of the PNA backbone

scientific article published on 13 October 2011

List of works by Yosuke Demizu

A Helix-Stabilized Cell-Penetrating Peptide as an Intracellular Delivery Tool

A preorganized β-amino acid bearing a guanidinium side chain and its use in cell-penetrating peptides

A synthetic cannabinoid FDU-NNEI, two 2H-indazole isomers of synthetic cannabinoids AB-CHMINACA and NNEI indazole analog (MN-18), a phenethylamine derivative N–OH-EDMA, and a cathinone derivative dimethoxy-α-PHP, newly identified in illegal products

Amphipathic short helix-stabilized peptides with cell-membrane penetrating ability.

An extended planar C5 conformation and a 310-helical structure of peptide foldamer composed of diverse alpha-ethylated alpha,alpha-disubstituted alpha-amino acids

Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.

Chiral centers in the side chains of alpha-amino acids control the helical screw sense of peptides

Conformational studies on peptides containing α,α-disubstituted α-amino acids: chiral cyclic α,α-disubstituted α-amino acid as an α-helical inducer

Conformations of helical Aib peptides containing a pair of L-amino acid and D-amino acid

Conformations of peptides containing a chiral cyclic α, α‐disubstituted α‐amino acid within the sequence of Aib residues ⬇️

Controlling 3(10)-helix and alpha-helix of short peptides in the solid state

Controlling the helical screw sense of peptides with C-terminal L-valine.

De Novo Design of Cell-penetrating Foldamers

Design and synthesis of cell-permeable fluorescent nitrilotriacetic acid derivatives

Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.

Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton

Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton

Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator.

Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands ⬇️

Design, synthesis, and anti-HIV-1 activity of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N-3,5-dimethylbenzyl-substituted urea derivatives.

Design, synthesis, and anti-HIV-1 activity of 1-substituted 3-(3,5-dimethylbenzyl)triazine derivatives.

Development of 2-aminoisobutyric acid (Aib)-rich cell-penetrating foldamers for efficient siRNA delivery

Development of Amphipathic Antimicrobial Peptide Foldamers Based on Magainin 2 Sequence

Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand.

Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins

Development of a Cell-penetrating Peptide that Exhibits Responsive Changes in its Secondary Structure in the Cellular Environment.

Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins.

Development of a peptide-based inducer of nuclear receptors degradation

Development of a peptide-based inducer of protein degradation targeting NOTCH1.

Development of an ON/OFF switchable fluorescent probe targeting His tag fused proteins in living cells.

Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription.

Development of helix-stabilized antimicrobial peptides composed of lysine and hydrophobic α,α-disubstituted α-amino acid residues

Development of helix-stabilized cell-penetrating peptides containing cationic α,α-disubstituted amino acids as helical promoters.

Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells.

Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.

Diastereomeric Right- and Left-Handed Helical Structures with Fourteen (R)-Chiral Centers

Direct electrochemical alpha-cyanation of N-protected cyclic amines.

Effect of one D-Leu residue on right-handed helical -L-Leu-Aib- peptides in the crystal state

Effects of D-Leu residues on the helical secondary structures of L-Leu-based nonapeptides

Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton

Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic.

Extent of Helical Induction Caused by Introducing α-Aminoisobutyric Acid into an Oligovaline Sequence

Front Cover: Recent Advances in PROTAC Technology Toward New Therapeutic Modalities (Chem. Biodiversity 11/2022)

Helical foldamer containing a combination of cyclopentane-1,2-diamine and 2,2-dimethylmalonic acid

Helical peptide-foldamers having a chiral five-membered ring amino acid with two azido functional groups

Helical-screw directions of diastereoisomeric cyclic alpha-amino acid oligomers.

Identification of embryonic precursor cells that differentiate into thymic epithelial cells expressing autoimmune regulator

Identification of mutaprodenafil in a dietary supplement and its subsequent synthesis

Inhibition of β-amyloid-induced neurotoxicity by planar analogues of procyanidin B3

Isoheleproline: a new amino acid-sesquiterpene adduct from Inula helenium

Left-Handed Helix of Three-Membered Ring Amino Acid Homopeptide Interrupted by an N-H···Ethereal O-Type Hydrogen Bond

Lipase-catalyzed kinetic resolution of cyclic trans-1,2-diols bearing a diester moiety: synthetic application to chiral seven-membered-ring alpha,alpha-disubstituted alpha-amino acid

Low pH-triggering changes in peptide secondary structures

Molecular Design, Synthesis, and Evaluation of SNIPER(ER) That Induces Proteasomal Degradation of ERα.

Monoallylation of 1,2-diols by Pd/Sn bimetallic catalysis

NAD-dependent isocitrate dehydrogenase as a novel target of tributyltin in human embryonic carcinoma cells

Oligopeptides with equal amounts of L- and D-amino acids may prefer a helix screw sense.

One-handed helical screw direction of homopeptide foldamer exclusively induced by cyclic α-amino acid side-chain chiral centers

PNA monomers fully compatible with standard Fmoc-based solid-phase synthesis of pseudocomplementary PNA.

Peptide Nucleic Acid with a Lysine Side Chain at the β-Position: Synthesis and Application for DNA Cleavage.

Plasmid DNA delivery by arginine-rich cell-penetrating peptides containing unnatural amino acids

Plasmid DNA delivery using fluorescein-labeled arginine-rich peptides.

Preorganized Cyclic α,α-Disubstituted α-Amino Acids Bearing Functionalized Side Chains That Act as Peptide-Helix Inducers

Rational Design and Synthesis of Post-Functionalizable Peptide Foldamers as Helical Templates.

Rational Design of Helix-Stabilized Antimicrobial Peptide Foldamers Containing α,α-Disubstituted Amino Acids or Side-Chain Stapling

Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

Regioselective protection of sugars catalyzed by dimethyltin dichloride

Screw-sense control of helical oligopeptides containing equal amounts of L- and D-amino acids

Side-chain chiral centers of amino acid and helical-screw handedness of its peptides

Simple and efficient knockdown of His-tagged proteins by ternary molecules consisting of a His-tag ligand, a ubiquitin ligase ligand, and a cell-penetrating peptide.

Structural Development of Cell-Penetrating Peptides Containing Cationic Proline Derivatives.

Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon

Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription.

Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors

Synthesis and Evaluation of Novel Carbocyclic Oxetanocin A (COA-Cl) Derivatives as Potential Tube Formation Agents

Synthesis and Resolution of Substituted [5]Carbohelicenes

Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives

Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator

Synthesis and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.