Personal information

medicinal chemistry, nuclear receptors, lipid metabolism, sugar metabolism, retinoids, RXR, arachidonic acid cascade, inflammation, immunoregulation
Japan

Activities

Employment (1)

Okayama University: Okayama, Okayama, JP

2008-10-01 to present | Associate Professor (Graduate School of Medicine, Dentistyry, adn Pharmaceutical Sciences)
Employment
Source: Self-asserted source
Hiroki Kakuta

Education and qualifications (1)

University of Tokyo: Tokyo, Tokyo, JP

1998-04-01 to 2003-03-27 | Ph.D. (Graduate School of Pharmaceutical Sciences)
Education
Source: Self-asserted source
Hiroki Kakuta

Professional activities (5)

Vitamin Society of Japan: Kyoto, JP

Membership
Source: Self-asserted source
Hiroki Kakuta

Pharmaceutical Society of Japan: Tokyo, JP

Membership
Source: Self-asserted source
Hiroki Kakuta

American Chemical Society: Washington D.C., District of Columbia, US

Membership
Source: Self-asserted source
Hiroki Kakuta

American Association for Cancer Research: Philadelphia, PA, US

Membership
Source: Self-asserted source
Hiroki Kakuta

The Open University of Japan: Chiba, JP

2021-04 to present
Invited position
Source: Self-asserted source
Hiroki Kakuta

Funding (1)

腫瘍部位におけるホウ素濃度の計測を可能とするBNCT用薬剤の創出

2019-04 to 2022-03 | Grant
Japan Society for the Promotion of Science (Sumitomo-Ichibancho FS Bldg., 8 Ichibancho, Chiyoda-ku, Tokyo102-8472, Japan, JP)
GRANT_NUMBER:

19K05735

Source: Self-asserted source
Hiroki Kakuta

Works (50 of 73)

Items per page:
Page 1 of 2

Simple Fluorescence Labeling Method Enables Detection of Intracellular Distribution and Expression Level of Retinoid X Receptors

ACS Medicinal Chemistry Letters
2024-05-09 | Journal article
Contributors: Yukina Tanaka; Michiko Fujihara; Yuta Takamura; Mayu Kawasaki; Shogo Nakano; Makoto Makishima; Hiroki Kakuta
Source: check_circle
Crossref

Direct evaluation of polarity of the ligand binding pocket in retinoid X receptor using a fluorescent solvatochromic agonist

Bioorganic & Medicinal Chemistry Letters
2023-11 | Journal article
Contributors: Kizuku Miura; Michiko Fujihara; Masaki Watanabe; Yuta Takamura; Mayu Kawasaki; Shogo Nakano; Hiroki Kakuta
Source: check_circle
Crossref

Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN

ACS Medicinal Chemistry Letters
2023-03-09 | Journal article
Contributors: Mayu Kawasaki; Tomoharu Motoyama; Shoya Yamada; Masaki Watanabe; Michiko Fujihara; Akira Kambe; Shogo Nakano; Hiroki Kakuta; Sohei Ito
Source: check_circle
Crossref

Teratogenicity and Fetal-Transfer Assessment of the Retinoid X Receptor Agonist Bexarotene

ACS Pharmacology & Translational Science
2022-09-09 | Journal article
Contributors: Yuta Takamura; Izumi Kato; Manami Fujita-Takahashi; Midori Azuma-Nishii; Masaki Watanabe; Rui Nozaki; Masaru Akehi; Takanori Sasaki; Hiroyuki Hirano; Hiroki Kakuta
Source: check_circle
Crossref

Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators

ACS Medicinal Chemistry Letters
2022-02-10 | Journal article
Contributors: Masaki Watanabe; Mariko Nakamura-Nakayama; Michiko Fujihara; Mayu Kawasaki; Shogo Nakano; Hiroki Kakuta
Source: check_circle
Crossref

Creation of Fluorescent RXR Antagonists Based on CBTF-EE and Application to a Fluorescence Polarization Binding Assay

ACS Medicinal Chemistry Letters
2021-06-10 | Journal article
Contributors: Maho Takioku; Yuta Takamura; Michiko Fujihara; Masaki Watanabe; Shoya Yamada; Mayu Kawasaki; Sohei Ito; Shogo Nakano; Hiroki Kakuta
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

In Vivo Receptor Visualization and Evaluation of Receptor Occupancy with Positron Emission Tomography

Journal of Medicinal Chemistry
2021-05-13 | Journal article
Contributors: Yuta Takamura; Hiroki Kakuta
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Fluorescence properties of retinoid X receptor antagonist NEt-SB

Bioorganic & Medicinal Chemistry Letters
2021-01 | Journal article
Contributors: Shoya Yamada; Yuta Takamura; Michiko Fujihara; Mayu Kawasaki; Sohei Ito; Shogo Nakano; Hiroki Kakuta
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers

Journal of Medicinal Chemistry
2021-01-14 | Journal article
Contributors: Masaki Watanabe; Michiko Fujihara; Tomoharu Motoyama; Mayu Kawasaki; Shoya Yamada; Yuta Takamura; Sohei Ito; Makoto Makishima; Shogo Nakano; Hiroki Kakuta
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343.

Journal of medicinal chemistry
2020-12-30 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Paclitaxel and Sorafenib: The Effective Combination of Suppressing the Self-Renewal of Cancer Stem Cells

Cancers
2020-05-26 | Journal article
Contributors: Hend Nawara; Said Afify; Ghmkin Hassan; Maram Zahra; Marwa Atallah; Hager Mansour; Hagar Abu Quora; Md Alam; Amira Osman; Hiroki Kakuta et al.
Source: check_circle
Crossref
grade
Preferred source (of 3)‎

Maternal gut microbiota in pregnancy influences offspring metabolic phenotype in mice

Science
2020-02-28 | Journal article
Part of ISSN: 0036-8075
Part of ISSN: 1095-9203
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

A partial agonist for retinoid X receptor mitigates experimental colitis

International Immunology
2019 | Journal article
EID:

2-s2.0-85064134177

Part of ISSN: 14602377 09538178
Contributors: Masayoshi, O.; Masaki, W.; Narumi, I.; Koichiro, S.; Kei, T.; Masato, H.; Takahiro, Y.; Aiko, E.; Osamu, S.; Midori, N. et al.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

A retinoid X receptor partial agonist attenuates pulmonary emphysema and airway inflammation

Respiratory Research
2019 | Journal article
EID:

2-s2.0-85059502773

Part of ISSN: 1465993X 14659921
Contributors: Morichika, D.; Miyahara, N.; Fujii, U.; Taniguchi, A.; Oda, N.; Senoo, S.; Kataoka, M.; Tanimoto, M.; Kakuta, H.; Kiura, K. et al.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Correction to: Synthesis of <sup>11</sup>C-Labeled RXR Partial Agonist 1-[(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic Acid (CBt-PMN) by Direct [<sup>11</sup>C]Carbon Dioxide Fixation via Organolithiation of Trialkyltin Precursor and PET Imaging Thereof (Journal of Medicinal Chemistry (2017) 60:16 (7139-7145) DOI: 10.1021/acs.jmedchem.7b00817)

Journal of Medicinal Chemistry
2019 | Journal article
EID:

2-s2.0-85065541322

Part of ISSN: 15204804 00222623
Contributors: Shibahara, O.; Watanabe, M.; Takamura, Y.; Yamada, S.; Akehi, M.; Sasaki, T.; Akahoshi, A.; Hanada, T.; Hirano, H.; Nakatani, S. et al.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Problems with laboratory notebooks in academia and how to resolve them

Yakugaku Zasshi
2019 | Journal article
EID:

2-s2.0-85067112311

Part of ISSN: 13475231 00316903
Contributors: Kakuta, H.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Towards further sharing of knowledge and activities on standards of quality assurance (Qa) across industry, academia and government to promote research integrity and accelerate drug discovery

Yakugaku Zasshi
2019 | Journal article
EID:

2-s2.0-85067103233

Part of ISSN: 13475231 00316903
Contributors: Kakuta, H.; Sudo, H.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening

Journal of Medicinal Chemistry
2019-09-18 | Journal article
Part of ISSN: 0022-2623
Part of ISSN: 1520-4804
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity

Bioorganic & Medicinal Chemistry Letters
2019-08 | Journal article
Contributors: Yuta Takamura; Manami Takahashi; Midori Nishii; Osamu Shibahara; Masaki Watanabe; Michiko Fujihara; Hiroki Kakuta
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Fluorine-18 (18F)-labeled retinoid x receptor (RXR) partial agonist whose tissue transferability is affected by other RXR ligands

Bioorganic & Medicinal Chemistry
2019-05 | Journal article
Part of ISSN: 0968-0896
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Reversal of established liver fibrosis by IC-2-engineered mesenchymal stem cell sheets

Scientific Reports
2019-05-02 | Journal article
Contributors: Noriko Itaba; Yohei Kono; Kaori Watanabe; Tsuyoshi Yokobata; Hiroyuki Oka; Mitsuhiko Osaki; Hiroki Kakuta; Minoru Morimoto; Goshi Shiota
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Dual conformation of the ligand induces the partial agonistic activity of retinoid X receptor α (RXRα)

FEBS Letters
2019-01 | Journal article
Contributors: Yurina Miyashita; Nobutaka Numoto; Sundaram Arulmozhiraja; Shogo Nakano; Naoya Matsuo; Kanade Shimizu; Osamu Shibahara; Michiko Fujihara; Hiroki Kakuta; Sohei Ito et al.
Source: check_circle
Crossref
grade
Preferred source (of 2)‎

Retinoid X Receptor Antagonists

International journal of molecular sciences
2018 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 5)‎

Strategy for Tumor-Selective Disruption of Androgen Receptor Function in the Spectrum of Prostate Cancer

Clinical cancer research : an official journal of the American Association for Cancer Research
2018 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Effect of a retinoid X receptor partial agonist on airway inflammation and hyperresponsiveness in a murine model of asthma

Respiratory research
2017 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Retinoid X Receptor Ligands with Anti-Type 2 Diabetic Activity

Current topics in medicinal chemistry
2017 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Synthesis of 11C-Labeled RXR Partial Agonist 1-[(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic Acid (CBt-PMN) by Direct [11C]Carbon Dioxide Fixation via Organolithiation of Trialkyltin Precursor and PET Imaging Thereof

Journal of medicinal chemistry
2017 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 3)‎

iPSC-derived cancer stem cells provide a model of tumor vasculature

American journal of cancer research
2016 | Journal article
Source: Self-asserted source
Hiroki Kakuta

iPSC-derived cancer stem cells provide a model of tumor vasculature

American Journal of Cancer Research
2016 | Journal article
EID:

2-s2.0-84992186980

Part of ISSN: 21566976
Contributors: Prieto-Vila, M.; Yan, T.; Calle, A.S.; Nair, N.; Hurley, L.; Kasai, T.; Kakuta, H.; Masuda, J.; Murakami, H.; Mizutani, A. et al.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Positron emission tomography to elucidate pharmacokinetic differences of regioisomeric retinoid x receptor agonists

ACS medicinal chemistry letters
2015 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

RXR partial agonist produced by side chain repositioning of alkoxy RXR full agonist retains antitype 2 diabetes activity without the adverse effects

Journal of medicinal chemistry
2015 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

In vitro anti-proliferative and anti-angiogenic activities of thalidomide dithiocarbamate analogs

International immunopharmacology
2014 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Interspecies comparison of hepatic metabolism of six newly synthesized retinoid X receptor agonistic compounds possessing a 6-[N-ethyl-N-(alkoxyisopropylphenyl)amino]nicotinic acid skeleton in rat and human liver microsomes

Drug development and industrial pharmacy
2014 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Involvement of glucocorticoid receptor activation on anti-inflammatory effect induced by peroxisome proliferator-activated receptor γ agonist in mice

International immunopharmacology
2014 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Retinoid X receptor ligands: a patent review (2007 - 2013)

Expert opinion on therapeutic patents
2014 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency

Journal of medicinal chemistry
2013 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Feasibility of structural modification of retinoid X receptor agonists to separate blood glucose-lowering action from adverse effects: studies in KKA(y) type 2 diabetes model mice

Biological & pharmaceutical bulletin
2012 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Relevance of nuclear receptor expression in a Tchreg cell line, HOZOT: RXRα and PPARγ negatively regulate IFN-γ production

Results in immunology
2012 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists

ACS medicinal chemistry letters
2012 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

[Challenge of creating single-agents for the treatment of type 1 and 2 diabetes by targeting retinoid X receptor]

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

[Significance and creation of novel cyclooxygenase-1 (COX-1) selective inhibitors]

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

An arylidene-thiazolidinedione derivative, GPU-4, without PPARγ activation, reduces retinal neovascularization

Current neurovascular research
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Design and synthesis of novel cyclooxygenase-1 inhibitors as analgesics: 5-amino-2-ethoxy-N-(substituted-phenyl)benzamides

ChemMedChem
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB

ACS medicinal chemistry letters
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Involvement of the Retinoid X Receptor Ligand in the Anti-Inflammatory Effect Induced by Peroxisome Proliferator-Activated Receptor γ Agonist In Vivo

PPAR research
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Pharmacokinetic properties of newly synthesized retinoid X receptor agonists possessing a 6-[N-ethyl-N-(3-alkoxy-4-isopropylphenyl)amino]nicotinic acid skeleton in rats

Drug development and industrial pharmacy
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Replacement of the hydrophobic part of 9-cis-retinoic acid with cyclic terpenoid moiety results in RXR-selective agonistic activity

Bioorganic & medicinal chemistry
2011 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Cyclic-tri(N-methyl-meta-benzamide)s: Substituent effects on the bowl-shaped conformation in the crystal and solution states

Tetrahedron
2010 | Journal article
EID:

2-s2.0-77957192377

Part of ISSN: 00404020
Contributors: Kakuta, H.; Azumaya, I.; Masu, H.; Matsumura, M.; Yamaguchi, K.; Kagechika, H.; Tanatani, A.
Source: Self-asserted source
Hiroki Kakuta via Scopus - Elsevier

Effect of 5-aminosalicylate on allergic rhinitis model in mice

International immunopharmacology
2010 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎

Fluorescent retinoid X receptor ligands for fluorescence polarization assay

Bioorganic & medicinal chemistry letters
2010 | Journal article
Source: Self-asserted source
Hiroki Kakuta
grade
Preferred source (of 2)‎
Items per page:
Page 1 of 2

Peer review (37 reviews for 11 publications/grants)

Review activity for ACS chemical biology. (1)
Review activity for ACS medicinal chemistry letters. (2)
Review activity for ACS omega. (1)
Review activity for Aspects of molecular medicine. (1)
Review activity for Bioorganic & medicinal chemistry letters. (3)
Review activity for Bioorganic & medicinal chemistry. (2)
Review activity for Chemistry. (1)
Review activity for ChemMedChem. (3)
Review activity for Journal of medicinal chemistry. (20)
Review activity for Journal of the American Chemical Society. (2)
Review activity for Natural medicines. (1)