List of works - Minoru Ishikawa

1α-Hydroxy derivatives of 7-dehydrocholesterol are selective liver X receptor modulators.

scientific article

7-Dehydrocholesterol metabolites produced by sterol 27-hydroxylase (CYP27A1) modulate liver X receptor activity

scientific article published on 21 November 2013

Chemical modification of pseurotin A: one-pot synthesis of synerazol and pseurotin E and determination of absolute stereochemistry of pseurotin E.

scientific article published in November 2008

Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules.

scientific article

Degradation of huntingtin mediated by a hybrid molecule composed of IAP antagonist linked to phenyldiazenyl benzothiazole derivative

scientific article published on 12 January 2018

Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists

scientific article published on 27 May 2015

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

scientific article

Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton

scientific article published on 02 December 2014

Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton

scientific article published on 27 August 2012

Development of Tetrachlorophthalimides as Liver X Receptor β (LXRβ)-Selective Agonists.

scientific article published on 30 September 2016

Development of target protein-selective degradation inducer for protein knockdown ⬇️

scientific article published on March 29, 2011

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.

scientific article published on 26 August 2016

Discovery of Small Molecules that Induce the Degradation of Huntingtin

scientific article

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

scientific article

Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton

scientific article published on 18 July 2018

Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand.

scientific article published on 20 May 2016

Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry ⬇️

scientific article published on February 23, 2011

Improvement in Aqueous Solubility of Retinoic Acid Receptor (RAR) Agonists by Bending the Molecular Structure.

scientific article published on 5 July 2016

Inhibition of restriction enzymes EcoRI, BamHI and HindIII by phenethylphenylphthalimides derived from thalidomide.

scientific article

LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators

scientific article published on 21 January 2010

Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists

scientific article published on 16 March 2011

Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton

scientific article published on 23 June 2018

Novel selective anti-androgens with a diphenylpentane skeleton ⬇️

scientific article published on September 9, 2010

Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity ⬇️

scientific article published on April 3, 2011

Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.

scientific article published on 22 April 2017

Photo-enhanced Aqueous Solubilization of an Azo-compound

scientific article published on 31 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

Pseurotin A and its analogues as inhibitors of immunoglobulin E [correction of immunoglobuline E] production

scientific article published on 15 January 2009

Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.

scientific article

Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.

scientific article

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

Specific fluorescence labeling of target proteins by using a ligand-4-azidophthalimide conjugate.

scientific article published on 20 July 2017

Structural basis for specific cleavage of Lys6-linked polyubiquitin chains by USP30.

scientific article

Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.

scientific article published on 13 December 2017

Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators

scientific article published on 05 December 2012

Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists

scientific article published in September 2016

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.

scientific article

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-κB pathway.

scientific article

Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.

scientific article published on 30 May 2013

Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression

scientific article published on 20 April 2017

Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.

scientific article published on 13 July 2015

Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists

scientific article published on 13 May 2017

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

scientific article

Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta3 antagonists. Part 1: design and synthesis of a lead compound exhibiting alpha(v)beta3/alpha(IIb)beta3 dual antagonistic activity.

scientific article published on 23 November 2005

Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta3 antagonists. Part III: synthesis of potent antagonists with alpha(v)beta3/alpha(IIb)beta3 dual activity and improved water solubility.

scientific article published on 22 November 2005

beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.

scientific article

meta-Non-flat substituents: a novel molecular design to improve aqueous solubility in small molecule drug discovery

scientific article published on 17 December 2020

List of works by Minoru Ishikawa

1α-Hydroxy derivatives of 7-dehydrocholesterol are selective liver X receptor modulators.

7-Dehydrocholesterol metabolites produced by sterol 27-hydroxylase (CYP27A1) modulate liver X receptor activity

Chemical modification of pseurotin A: one-pot synthesis of synerazol and pseurotin E and determination of absolute stereochemistry of pseurotin E.

Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules.

Degradation of huntingtin mediated by a hybrid molecule composed of IAP antagonist linked to phenyldiazenyl benzothiazole derivative

Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists

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

Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton

Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton

Development of Tetrachlorophthalimides as Liver X Receptor β (LXRβ)-Selective Agonists.

Development of target protein-selective degradation inducer for protein knockdown ⬇️

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.

Discovery of Small Molecules that Induce the Degradation of Huntingtin

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

Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton

Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand.

Improvement in Aqueous Solubility in Small Molecule Drug Discovery Programs by Disruption of Molecular Planarity and Symmetry ⬇️

Improvement in Aqueous Solubility of Retinoic Acid Receptor (RAR) Agonists by Bending the Molecular Structure.

Inhibition of restriction enzymes EcoRI, BamHI and HindIII by phenethylphenylphthalimides derived from thalidomide.

LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators

Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists

Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton

Novel selective anti-androgens with a diphenylpentane skeleton ⬇️

Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: Relationship between absolute configuration and subtype selectivity ⬇️

Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.

Photo-enhanced Aqueous Solubilization of an Azo-compound

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

Pseurotin A and its analogues as inhibitors of immunoglobulin E [correction of immunoglobuline E] production

Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.

Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.

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

Specific fluorescence labeling of target proteins by using a ligand-4-azidophthalimide conjugate.

Structural basis for specific cleavage of Lys6-linked polyubiquitin chains by USP30.

Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.

Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators

Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists

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.

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-κB pathway.

Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.

Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression

Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.

Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists

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

Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta3 antagonists. Part 1: design and synthesis of a lead compound exhibiting alpha(v)beta3/alpha(IIb)beta3 dual antagonistic activity.

Tricyclic pharmacophore-based molecules as novel integrin alpha(v)beta3 antagonists. Part III: synthesis of potent antagonists with alpha(v)beta3/alpha(IIb)beta3 dual activity and improved water solubility.

beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.

meta-Non-flat substituents: a novel molecular design to improve aqueous solubility in small molecule drug discovery