Literature DB >> 24900488

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

Hiroki Kakuta1, Nobumasa Yakushiji1, Ryosuke Shinozaki1, Fuminori Ohsawa1, Shoya Yamada1, Yui Ohta1, Kohei Kawata1, Mariko Nakayama1, Manabu Hagaya1, Chisa Fujiwara1, Makoto Makishima2, Shigeyuki Uno2, Akihiro Tai3, Ami Maehara4, Masaru Nakayama4, Toshitaka Oohashi4, Hiroyuki Yasui5, Yutaka Yoshikawa5.   

Abstract

Treating insulin resistance and type 2 diabetes in rodents, currently known retinoid X receptor (RXR) agonists induce significant adverse effects. Here we introduce a novel RXR partial agonist CBt-PMN (11b), which shows a potent glucose-lowering effect and improvements of insulin secretion and glucose tolerance without the serious adverse effects caused by RXR full agonists. We suggest that RXR partial agonists may be a new class of antitype 2 diabetes drug candidates.

Entities:  

Keywords:  Nuclear receptors; RXR; partial agonists; type 2 diabetes

Year:  2012        PMID： 24900488      PMCID： PMC4025743          DOI： 10.1021/ml300055n

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  26 in total

1.  Structural determinants of allosteric ligand activation in RXR heterodimers.

Authors:  Andrew I Shulman; Christopher Larson; David J Mangelsdorf; Rama Ranganathan
Journal:  Cell       Date:  2004-02-06       Impact factor: 41.582

Review 2.  Design of selective nuclear receptor modulators: RAR and RXR as a case study.

Authors:  Angel R de Lera; William Bourguet; Lucia Altucci; Hinrich Gronemeyer
Journal:  Nat Rev Drug Discov       Date:  2007-10       Impact factor: 84.694

Review 3.  The RXR heterodimers and orphan receptors.

Authors:  D J Mangelsdorf; R M Evans
Journal:  Cell       Date:  1995-12-15       Impact factor: 41.582

4.  The nuclear receptor LXR is a glucose sensor.

Authors:  Nico Mitro; Puiying A Mak; Leo Vargas; Cristina Godio; Eric Hampton; Valentina Molteni; Andreas Kreusch; Enrique Saez
Journal:  Nature       Date:  2006-12-24       Impact factor: 49.962

5.  Danthron functions as a retinoic X receptor antagonist by stabilizing tetramers of the receptor.

Authors:  Haitao Zhang; Rong Zhou; Li Li; Jing Chen; Lili Chen; Chenjing Li; Hong Ding; Liang Yu; Lihong Hu; Hualiang Jiang; Xu Shen
Journal:  J Biol Chem       Date:  2010-11-17       Impact factor: 5.157

6.  Phytanic acid, a natural peroxisome proliferator-activated receptor (PPAR) agonist, regulates glucose metabolism in rat primary hepatocytes.

Authors:  Manuel Heim; James Johnson; Franziska Boess; Igor Bendik; Peter Weber; Willi Hunziker; Beat Fluhmann
Journal:  FASEB J       Date:  2002-03-26       Impact factor: 5.191

7.  Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists.

Authors:  R Mukherjee; P J Davies; D L Crombie; E D Bischoff; R M Cesario; L Jow; L G Hamann; M F Boehm; C E Mondon; A M Nadzan; J R Paterniti; R A Heyman
Journal:  Nature       Date:  1997-03-27       Impact factor: 49.962

8.  Mechanism of selective retinoid X receptor agonist-induced hypothyroidism in the rat.

Authors:  Sha Liu; Kathleen M Ogilvie; Kay Klausing; Mark A Lawson; Diane Jolley; Danmei Li; James Bilakovics; Bernadette Pascual; Nancy Hein; Mary Urcan; Mark D Leibowitz
Journal:  Endocrinology       Date:  2002-08       Impact factor: 4.736

9.  SREBP-1c mediates the insulin-dependent hepatic glucokinase expression.

Authors:  So-Youn Kim; Ha-il Kim; Tae-Hyun Kim; Seung-Soon Im; Sang-Kyu Park; In-Kyu Lee; Kyung-Sup Kim; Yong-Ho Ahn
Journal:  J Biol Chem       Date:  2004-04-30       Impact factor: 5.157

10.  Stearoyl-CoA desaturase 1 gene expression is necessary for fructose-mediated induction of lipogenic gene expression by sterol regulatory element-binding protein-1c-dependent and -independent mechanisms.

Authors:  Makoto Miyazaki; Agnieszka Dobrzyn; Weng Chi Man; Kiki Chu; Harini Sampath; Hyoun-Ju Kim; James M Ntambi
Journal:  J Biol Chem       Date:  2004-04-05       Impact factor: 5.157
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  6 in total

Review 1.  Retinoid roles in blocking hepatocellular carcinoma.

Authors:  Yohei Shirakami; Hiroyasu Sakai; Masahito Shimizu
Journal:  Hepatobiliary Surg Nutr       Date:  2015-08       Impact factor: 7.293

Review 2.  A review of the molecular design and biological activities of RXR agonists.

Authors:  Nathalia Rodrigues de Almeida; Martin Conda-Sheridan
Journal:  Med Res Rev       Date:  2019-04-03       Impact factor: 12.944

3.  The Disappearing Director: The Case of Directed N-Arylation via a Removable Hydroxyl Group.

Authors:  Magdalena R Andrzejewska; Prasanna K Vuram; Narender Pottabathini; Venkateshwarlu Gurram; Siva Subrahmanyam Relangi; Kirill A Korvinson; Raju Doddipalla; Lothar Stahl; Michelle C Neary; Padmanava Pradhan; Somesh Sharma; Mahesh K Lakshman
Journal:  Adv Synth Catal       Date:  2018-04-16       Impact factor: 5.837

Review 4.  Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

Authors:  Paula Ruiz-Castillo; Stephen L Buchwald
Journal:  Chem Rev       Date:  2016-09-30       Impact factor: 60.622

5.  The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer.

Authors:  Jessica A Moerland; Di Zhang; Lyndsey A Reich; Sarah Carapellucci; Beth Lockwood; Ana S Leal; Teresa Krieger-Burke; Bilal Aleiwi; Edmund Ellsworth; Karen T Liby
Journal:  Sci Rep       Date:  2020-12-17       Impact factor: 4.379

6.  Modeling, Synthesis, and Biological Evaluation of Potential Retinoid-X-Receptor (RXR) Selective Agonists: Analogs of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahyro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(4-isobutoxy-3-isopropylphenyl)amino)nicotinic Acid (NEt-4IB).

Authors:  Peter W Jurutka; Orsola di Martino; Sabeeha Reshi; Sanchita Mallick; Zhela L Sabir; Lech J P Staniszewski; Ankedo Warda; Emma L Maiorella; Ani Minasian; Jesse Davidson; Samir J Ibrahim; San Raban; Dena Haddad; Madleen Khamisi; Stephanie L Suban; Bradley J Dawson; Riley Candia; Joseph W Ziller; Ming-Yue Lee; Chang Liu; Wei Liu; Pamela A Marshall; John S Welch; Carl E Wagner
Journal:  Int J Mol Sci       Date:  2021-11-16       Impact factor: 5.923
  6 in total

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