Hiroki Kakuta

Profile Information

Affiliation: Associate Professor, Okayama University
: 合成医薬品開発学

Degree: Ph.D.
博士（薬学）(東京大学)

ORCID ID: https://orcid.org/0000-0002-3633-8121
J-GLOBAL ID: 200901017150818697
researchmap Member ID: 5000092951

External link: http://www.cc.okayama-u.ac.jp/~kakuta-h/kakuta_lab_english/index.html

Research Interests

Research Areas

Life sciences / Pharmaceuticals - chemistry and drug development /

Research History

Apr, 2021

Associate Professor, Medicine, Dentistry and Pharmaceutical Sciences, Institute of Academic and Research, Okayama University
Apr, 2021

The Open University of Japan
Oct, 2008 - Mar, 2021

Graduate school of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
2007 - 2008

岡山大学医歯薬学総合研究科助教
2007 - 2008

Assistant Professor,Graduate School of Medicine, Dentistry and Pharmaceutical Sciences,Okayama University
2008

- Associate Professor,Graduate School of Medicine, Dentistry and Pharmaceutical Sciences,Okayama University
2004 - 2007

岡山大学医歯薬学総合研究科助手
2004 - 2007

Research Associate,Graduate School of Medicine, Dentistry and Pharmaceutical Sciences,Okayama University
2003 - 2004

Faculty of Pharmaceutical Sciences, Okayama University
2003 - 2004

Research Associate,Faculty of Pharmaceutical Sciences,Okayama University

Education

- 2003

The University of Tokyo
- 2003

The University of Tokyo
- 2003

Graduate School, Division of Pharmaceutical Sciences, The University of Tokyo
- 1997

Faculty of Pharmaceutical Sciences, Okayama University
- 1997

Faculty of Pharmaceutical Science, Okayama University

Committee Memberships

Awards

Jul, 2020

The Uchiyama Yuzo Science and Technology Award, Okayama Foundation for Science and Technology

Hiroki Kakuta
Jul, 2015

Science and Technology Award in Okayama Foundation of Science and Technology, Okayama Foundation for Science and Technology

KAKUTA Hiroki
Jun, 2015

日本ビタミン学会賞（奨励賞）, レチノイドＸ受容体を標的とした創薬に関する研究, 日本ビタミン学会

加来田博貴
Feb, 2012

2011 Young Top Researcher Award, Okayama University

KAKUTA Hiroki
Nov, 2010

Award for Excellent General Presentation in the Medicinal Chemistry Symposium

KAKUTA Hiroki
Nov, 2008

日本薬学会中国四国支部奨励賞

Papers

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

Kizuku Miura, Michiko Fujihara, Masaki Watanabe, Yuta Takamura, Mayu Kawasaki, Shogo Nakano, Hiroki Kakuta

Bioorganic & medicinal chemistry letters, 96 129536-129536, Oct 30, 2023
Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN

Mayu Kawasaki, Tomoharu Motoyama, Shoya Yamada, Masaki Watanabe, Michiko Fujihara, Akira Kambe, Shogo Nakano, Hiroki Kakuta, Sohei Ito

ACS Medicinal Chemistry Letters, 14(3) 291-296, Feb 20, 2023 Peer-reviewed
Structural characterization of 1,3-bis-tert-butyl monocyclic benzene derivatives with agonistic activity towards retinoid X receptor alpha.

Susumu Kodama, Shuzo Matsumoto, Yuta Takamura, Michiko Fujihara, Masaki Watanabe, Atsushi Ono, Hiroki Kakuta

Toxicology letters, 373 76-83, Nov 9, 2022 Peer-reviewed
Analysis of absorption-enhancing mechanisms for combinatorial use of spermine with sodium taurocholate in Caco-2 cells.

Masato Maruyama, Yohei Nishida, Hironori Tanaka, Takako Minami, Ken-Ichi Ogawara, Masateru Miyake, Yuta Takamura, Hiroki Kakuta, Kazutaka Higaki

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 180 332-343, Nov, 2022 Peer-reviewed
Teratogenicity and Fetal-Transfer Assessment of the Retinoid X Receptor Agonist Bexarotene.

Yuta Takamura, Izumi Kato, Manami Fujita-Takahashi, Midori Azuma-Nishii, Masaki Watanabe, Rui Nozaki, Masaru Akehi, Takanori Sasaki, Hiroyuki Hirano, Hiroki Kakuta

ACS pharmacology & translational science, 5(9) 811-818, Sep 9, 2022 Peer-reviewedLast authorCorresponding author
Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo.

Negar Khazan, Kyu Kwang Kim, Jeanne N Hansen, Niloy A Singh, Taylor Moore, Cameron W A Snyder, Ravina Pandita, Myla Strawderman, Michiko Fujihara, Yuta Takamura …

Journal of Medicinal Chemistry, 65(8) 6039-6055, Apr 28, 2022 Peer-reviewedCorresponding author
Development of Scaled-Up Synthetic Method for Retinoid X Receptor Agonist NEt-3IB Contributing to Sustainable Development Goals

Yuta Takamura, Ken-ichi Morishita, Shota Kikuzawa, Masaki Watanabe, and Hiroki Kakuta

Chemical and Pharmaceutical Bulletin, 70(2) 146-154, Feb, 2022 Peer-reviewedLast authorCorresponding author
Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators

Masaki Watanabe, Mariko Nakamura-Nakayama, Michiko Fujihara, Mayu Kawasaki, Shogo Nakano, Hiroki Kakuta

ACS Medicinal Chemistry Letters, 13(2) 211-217, Jan 21, 2022 Peer-reviewedLast authorCorresponding author
Creation of Fluorescent RXR Antagonists Based on CBTF-EE and Application to a Fluorescence Polarization Binding Assay

Maho Takioku, Yuta Takamura, Michiko Fujihara, Masaki Watanabe, Shoya Yamada, Mayu Kawasaki, Sohei Ito, Shogo Nakano, Hiroki Kakuta

ACS Medicinal Chemistry Letters, Jun 10, 2021 Peer-reviewedLast authorCorresponding author
In Vivo Receptor Visualization and Evaluation of Receptor Occupancy with Positron Emission Tomography

Yuta Takamura, Hiroki Kakuta

Journal of Medicinal Chemistry, May 13, 2021 Peer-reviewedInvitedCorresponding author
Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers

Masaki Watanabe, Michiko Fujihara, Tomoharu Motoyama, Mayu Kawasaki, Shoya Yamada, Yuta Takamura, Sohei Ito, Makoto Makishima, Shogo Nakano, Hiroki Kakuta

Journal of Medicinal Chemistry, 64(1) 430-439, Jan 14, 2021 Peer-reviewedLast authorCorresponding author
A Retinoid X Receptor Agonist Directed to the Large Intestine Ameliorates T-Cell-Mediated Colitis in Mice.

Ryohtaroh Matsumoto, Daisuke Takahashi, Masaki Watanabe, Shunsuke Nakatani, Yuta Takamura, Yuji Kurosaki, Hiroki Kakuta, Koji Hase

Frontiers in pharmacology, 12 715752-715752, 2021 Peer-reviewedCorresponding author
Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343.

Hiroki Kakuta

Journal of Medicinal Chemistry, 64(1) 861-870, Dec 30, 2020 Peer-reviewedLast authorCorresponding author
Fluorescence properties of retinoid X receptor antagonist NEt-SB

Bioorg. Med. Chem. Lett., Nov, 2020 Peer-reviewedLast authorCorresponding author
Paclitaxel and Sorafenib: The Effective Combination of Suppressing the Self-Renewal of Cancer Stem Cells

Hend M Nawara, SAID M AFIFY, Ghmkin Hassan, Maram H. Zahra, Marwa Atallah, Hager Mansour, Hagar A. Abu Quora, Md Jahangir Alam, Amira Osman, Hiroki Kakuta …

Cancers, 12(6) 1360-1360, May, 2020 Peer-reviewed
Maternal gut microbiota in pregnancy influences offspring metabolic phenotype in mice

Ikuo Kimura, Junki Miyamoto, Ryuji Ohue-Kitano, Keita Watanabe, Takahiro Yamada, Masayoshi Onuki, Ryo Aoki, Yosuke Isobe, Daiji Kashihara, Daisuke Inoue, Akihiko Inaba, Yuta Takamura, Satsuki Taira, Shunsuke Kumaki, Masaki Watanabe, Masato Ito, Fumiyuki Nakagawa, Junichiro Irie, Hiroki Kakuta, Masakazu Shinohara, Ken Iwatsuki, Gozoh Tsujimoto, Hiroaki Ohno, Makoto Arita, Hiroshi Itoh, Koji Hase

Science, 367(6481), Feb 28, 2020 Peer-reviewed
Reversal of established liver fibrosis by IC-2-engineered mesenchymal stem cell sheets

Noriko Itaba, Yohei Kono, Kaori Watanabe, Tsuyoshi Yokobata, Hiroyuki Oka, Mitsuhiko Osaki, Hiroki Kakuta, Minoru Morimoto, Goshi Shiota

Scientific Reports, 9(1) 6841-6841, Dec, 2019 Peer-reviewed
Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening.

Shoya Yamada, Mayu Kawasaki, Michiko Fujihara, Masaki Watanabe, Yuta Takamura, Maho Takioku, Hiromi Nishioka, Yasuo Takeuchi, Makoto Makishima, Tomoharu Motoyama …

Journal of Medicinal Chemistry, 62(19) 8809-8818, Oct 10, 2019 Peer-reviewedLast authorCorresponding author
3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity

Yuta Takamura, Manami Takahashi, Midori Nishii, Osamu Shibahara, Masaki Watanabe, Michiko Fujihara, Hiroki Kakuta

Bioorganic & Medicinal Chemistry Letters, 29(15) 1891-1894, Aug, 2019 Peer-reviewedLast authorCorresponding author
Correction to 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 Tri

Shibahara O, Watanabe M, Takamura Y, Yamada S, Akehi M, Sasaki T, Akahoshi A, Hanada T, Hirano H, Nakatani S …

Journal of Medicinal Chemistry, 62(9) 4780-4781, May, 2019 Peer-reviewedLast authorCorresponding author

Misc.

F-containing retinoid X receptor (RXR) partial agonist F-CBt-PMN whose tissue transferability is affected by coadministration of another RXR ligand

Yuta Takamura, Osamu Shibahara, Masaki Watanabe, Michiko Fujihara, Masaru Akehi, Takanori Sasaki, Hiroki Kakuta

ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 258, Aug, 2019
PETイメージングに期待するビタミン研究の新展開

加来田博貴

ビタミン, 92(4) 194-195, Apr, 2018
催奇形性軽減化を志向した新規レキシノイドの創出研究

高村祐太, 芝原理, 渡邉将貴, 高橋愛海, 西井緑, 藤原美智子, 加来田博貴

ビタミン, 92(4) 230-230, Apr, 2018
経口吸収性RXRアンタゴニストの創出とその2型糖尿病モデルでの薬効評価

渡邉将貴, 藤原美智子, 西井緑, 加来田博貴

ビタミン, 92(4) 230-230, Apr, 2018
研究公正化、医薬品開発のスピードアップのための「信頼性確保の知識・方法論」の産学官での共有を目指してアカデミアでの悩み、それを解決するには?

加来田博貴

日本薬学会年会要旨集, 138年会(1) 143-143, Mar, 2018
hRXRαリガンドCBt-PMNのパーシャルアゴニスト活性の起源は何か?

清水奏, 宮下由里奈, 松尾直也, 中野祥吾, 伊藤創平, 沼本修孝, 伊倉貞吉, 伊藤暢聡, 加来田博貴, 常盤広明

日本薬学会年会要旨集, 138年会(2) 111-111, Mar, 2018
経口吸収性を担保した新規RXRアンタゴニストの創出

渡邉将貴, 藤原美智子, 加来田博貴

日本薬学会年会要旨集, 138年会(2) 114-114, Mar, 2018
核内受容体転写因子複合体におけるRXRαパーシャルアゴニストのPPI制御能に関する構造生物学,熱化学,および理論化学的解析

清水奏, 宮下由里奈, 中野祥吾, 伊藤創平, 沼本修孝, 伊倉貞吉, 伊藤暢聡, 加来田博貴, 常盤広明

創薬懇話会講演要旨集, 2018, 2018
X線結晶構造及び相互作用解析に基づく蛍光性RXRαアゴニスト作用機序の解明

川崎真由, 中野祥吾, 本山智晴, 山田翔也, 渡邉将貴, 藤原美智子, 常盤広明, 加来田博貴, 伊藤創平

メディシナルケミストリーシンポジウム講演要旨集, 36th, 2018
Synthesis of 11C labeled RXR partial agonist CBt-PMN by [11C] carbon dioxide fixation via organolithiation of trialkyltin precursor and PET imaging thereof

Osamu Shibahara, Masaki Watanabe, Masaru Akehi, Takanori Sasaki, Takahisa Hanada, Akiya Akahoshi, Hiroyuki Hirano, Hiroki Kakuta

ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 254, Aug, 2017
PETイメージングを用いたRXRパーシャルアゴニストCBt-PMNの脳移行性の評価

芝原理, 小林俊貴, 渡邊将貴, 西井緑, 明日卓, 佐々木崇了, 赤星彰也, 花田貴寿, 平野裕之, 加来田博貴

日本薬学会年会要旨集, 137年会(2) 118-118, Mar, 2017
レチノイド関連化合物による肝癌細胞特異的な増殖抑制効果と機能解析

坪田智明, 神吉けい太, 影近弘之, 高橋典子, 加来田博貴, 汐田剛史

肝臓, 57(Suppl.1) A253-A253, Apr, 2016
レチノイドX受容体パーシャルアゴニストCBt-PMNの認知症改善効果

加来田博貴, 小林俊貴, 山田翔也, 芝原理, 藤原美智子, 西井緑

ビタミン, 90(4) 176-176, Apr, 2016
レチノイドX受容体を標的とした創薬に関する研究

加来田博貴

ビタミン, 90(3) 101-108, Mar, 2016
アレルギー性気道炎症マウスモデルにおけるレチノイドX受容体(RXR)パーシャルアゴニストの治療効果に関する研究

藤井詩子, 金廣有彦, 谷口暁彦, 森近大介, 小田尚廣, 栗本悦子, 古賀光, 早稲田公一, 加来田博貴, 宮原信明 …

日本呼吸器学会誌, 5(増刊) 178-178, Mar, 2016
RXRパーシャルアゴニストに関する理論的研究

夏目継介, 松尾直也, 岡崎誠司, 中野祥吾, 伊藤創平, 加来田博貴, 常盤広明

日本薬学会年会要旨集, 136年会(2) 170-170, Mar, 2016
iPSC-derived cancer stem cells provide a model of tumor vasculature

Hiroki Kakuta

American journal of cancer research, 6(9) 1906-1921, 2016 Peer-reviewed
生細胞内のアスコルビン酸濃度分布のイメージング化に関する試み

田井章博, 石股直, 加来田博貴

ビタミン, 89(12) 595-596, Dec, 2015
関節軟骨造影剤を用いた関節軟骨プロテオグリカンの評価

大橋俊孝, 加来田博貴, 芳谷学, 山田翔也, 大月孝志, 廣畑聡, 二宮善文, 西田圭一郎

日本結合組織学会学術大会プログラム・抄録集, 47回 97-97, May, 2015
レチノイドX受容体を標的とした創薬に関する研究

加来田博貴

ビタミン, 89(4) 177-178, Apr, 2015

Books and Other Publications

MEDCHEM NEWS

HIROKI KAKUTA

Nov, 2022
現代化学

東京化学同人, 2007
ファルマシア6月号

社団法人日本薬学会, 2004

Presentations

A Green and Scale-up Synthesis of Retinoid X Receptor Agonist NEt-3IB

Takamura, Yuta, Morishita, Ken-ichi, Kikuzawa, Shota, Watanabe, Masaki, Kakuta, Hiroki

PacifiChem2021 Invited
GatekeeperレチノイドX受容体アンタゴニストCBTF-EEを骨格とする新規蛍光性RXRアンタゴニストの創出とリガンド結合試験法への展開

高村祐太, 瀧奥真歩, 藤原美智子, 川﨑真由, 中野祥吾, 加来田博貴

日本ビタミン学会第73回大会, Jun 12, 2021
RXRアゴニスト NEt-3IPの抗アレルギー作用について

日本薬学会第１２９年会, 2010
チアゾリジンジオン骨格を有する新規選択的血管新生阻害剤GPU-4の開発発表形式：ポスター

日本薬学会第１２９年会, 2010
新規レチノイドX受容体アゴニスト NEt-3IP のラットにおける体内動態評価

日本薬学会第１２９年会, 2010
ヒドロキサム酸を有さない新規 MMP 阻害剤の開発研究発表形式：ポスター

日本薬学会第１２９年会, 2010
パーミッシブ機構に着目したRXRパーシャルアゴニストの挙動検証

創薬懇話会2009, 2009
白血病治療薬を志向した新規低脂溶性RARβ選択的アゴニストの創製研究

メディシナルケミストリーシンポジウム, 2009
RXRアゴニストNEt-3IPの樹状細胞分化抑制・制御性T細胞誘導能と抗アレルギー作用

メディシナルケミストリーシンポジウム, 2009
COX-1-selective inhibitors are new attractive agents for cancer treatment without the gastric damage: Design, in vitro and in vivo evaluation of a structurally-simple benzamide-type COX-1 selective inhibitor, TFAP

American Association for Cancer Research Annual Meeting 2008, 2008
COX-1-selective inhibitors are new attractive targets for analgesics without the gastric damage. Design, in vitro and in vivo evaluation of structurally-simple COX-1 inhibitors

Takeda Symposium, 2007
RXRα/βデュアルアゴニストNEt-3IPの抗炎症及び抗がん作用の検証

メディシナルケミストリーシンポジウム, 2007
高活性RXRα/β選択的アゴニストNEt-3IPの開発－脂溶性部位にアルコキシ基を有する－

メディシナルケミストリーシンポジウム, 2007
RXRアゴニスト脂溶性部位の脂溶性低減によるRXRサブタイプ指向性の創出 ―リンカー部位にスルホンアミド基を有する―

メディシナルケミストリーシンポジウム, 2007
一工程で合成可能な非サルファ剤型抗MRSA・VREベンゼンスルホンアニリド誘導体

メディシナルケミストリーシンポジウム, 2007
安価なイソニコチン酸から2ステップで合成可能なビスカチオン型抗マラリア化合物の開発

メディシナルケミストリーシンポジウム（相模原）, 2007
RXRα/βデュアルアゴニストNEt-3IPの抗炎症及び抗がん作用の検証

メディシナルケミストリーシンポジウム, 2007
高活性RXRα/β選択的アゴニストNEt-3IPの開発－脂溶性部位にアルコキシ基を有する－

メディシナルケミストリーシンポジウム, 2007
RXRアゴニスト脂溶性部位の脂溶性低減によるRXRサブタイプ指向性の創出 ―リンカー部位にスルホンアミド基を有する―

メディシナルケミストリーシンポジウム, 2007
一工程で合成可能な非サルファ剤型抗MRSA・VREベンゼンスルホンアニリド誘導体

メディシナルケミストリーシンポジウム, 2007

Major Teaching Experience

Professional Memberships

Research Projects

Creation of new agents for BNCT that enable to measure boron concentration at tumor site

Grants-in-Aid for Scientific Research Grant-in-Aid for Scientific Research (C), Grant-in-Aid for Scientific Research (C), Japan Society for the Promotion of Science, Apr, 2019 - Mar, 2022

Kakuta Hiroki
Establishment of in vivo imaging and quantification of articular cartilage by using a cartilage-specific probe.

Grants-in-Aid for Scientific Research Grant-in-Aid for Challenging Exploratory Research, Grant-in-Aid for Challenging Exploratory Research, Japan Society for the Promotion of Science, Apr, 2015 - Mar, 2017

Oohashi Toshitaka, HIROHATA Satoshi, OHTSUKI Takakashi, ASZDI Attila
Development of the strategy for fundamental therapy of cancer using iPS derived Cancer Stem cell models

Grants-in-Aid for Scientific Research Grant-in-Aid for Scientific Research (A), Grant-in-Aid for Scientific Research (A), Japan Society for the Promotion of Science, Oct, 2013 - Mar, 2017

Seno Masaharu
Exploratory research of high activity metal complexes by organic and inorganic nano-composite with anti-diabetic effect

Grants-in-Aid for Scientific Research Grant-in-Aid for Scientific Research (C), Grant-in-Aid for Scientific Research (C), Japan Society for the Promotion of Science, Apr, 2013 - Mar, 2016

YOSHIKAWA Yutaka, KAKUTA Hiroki, NAITO Yuki
Creation of articular cartilage-specific bio-molecular imaging probe with potentials of dual modalities.

Grants-in-Aid for Scientific Research Grant-in-Aid for Challenging Exploratory Research, Grant-in-Aid for Challenging Exploratory Research, Japan Society for the Promotion of Science, Apr, 2013 - Mar, 2015

OOHASHI Toshitaka, NISHIDA Keiichiro, KAKUTA Hiroki
Creation and evaluation of RXR partial agonists for the substitutes of steroidal anti-inflammatory agents

Grants-in-Aid for Scientific Research Grant-in-Aid for Young Scientists (B), Grant-in-Aid for Young Scientists (B), Japan Society for the Promotion of Science, 2010 - 2011

KAKUTA Hiroki
Creation of drug candidates for the treatment of inflammatory orphan disease

Grants-in-Aid for Scientific Research Grant-in-Aid for Young Scientists (B), Grant-in-Aid for Young Scientists (B), Japan Society for the Promotion of Science, 2008 - 2009

KAKUTA Hiroki
細胞分化を制御する複素環化合物の創製

科学研究費助成事業若手研究(B), 若手研究(B), 日本学術振興会, 2005 - 2006

加来田博貴

Major Industrial Property Rights

特許第6804768号炎症性腸疾患の予防又は治療用薬剤

加来田博貴
特許第4691619号アルコキシ基を有するレキシノイド化合物

加来田博貴, 佐々木健二, 高松佳代, 高野敦史, 薬師寺信匡, 師橋一徳, 森下健一

Media Coverage

悪性リンパ腫治療薬「bexarotene(ベキサロテン)」のラット胎児奇形や胎児移行性を明らかに〜催奇形性を軽減した新たな創薬に期待〜

岡山大学プレスリリース, https://www.okayama-u.ac.jp/tp/release/release_id1008.html, Sep, 2022 Internet
Hope for inflammatory bowel disease with novel “green” synthesis of drug candidate

EurekAlert!, https://www.eurekalert.org/news-releases/945672, Mar, 2022 Internet
Developing an environmentally friendly mass synthetic method for NEt-3IB candidates for inflammatory bowel diseases ～From the perspective of contributing to SDGs by reducing the volume of waste liquid in synthesizing drug substances～

http://www.okayama-u.ac.jp/eng/research_highlights/index_id154.html, Feb, 2022 Internet

Profile Information

Research Interests

Research Areas

Research History

Education

Committee Memberships

Awards

Papers

Misc.

Books and Other Publications

Presentations

Major Teaching Experience

Professional Memberships

Research Projects

Major Industrial Property Rights

Media Coverage

Menu

Coauthors