Literature DB >> 23528296

Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties.

Tetsuyoshi Matsufuji1, Mika Ikeda, Asuka Naito, Masakazu Hirouchi, Shoichi Kanda, Masanori Izumi, Jun Harada, Tsuyoshi Shinozuka.   

Abstract

The discovery and optimization of a novel series of FATP1 inhibitors are described. Through the derivatization process, arylpiperazine derivatives 5k and 12a were identified as possessing potent in vitro activity against human and mouse FATP1s as well as excellent pharmacokinetic properties. In vivo evaluation of triglyceride accumulation in the liver, white gastrocnemius muscle and soleus is also described.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23528296     DOI： 10.1016/j.bmcl.2013.02.116

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

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Journal:  Hepatology       Date:  2016-03-25       Impact factor: 17.425

2.  Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death.

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3.  Fatty Acid Transport Proteins: Targeting FATP2 as a Gatekeeper Involved in the Transport of Exogenous Fatty Acids.

Authors:  Paul N Black; Constance Ahowesso; David Montefusco; Nipun Saini; Concetta C DiRusso
Journal:  Medchemcomm       Date:  2016-02-19       Impact factor: 3.597

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Journal:  Tetrahedron       Date:  2018-07-17       Impact factor: 2.457

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Authors:  Cindy Mendes; Filipa Lopes-Coelho; Cristiano Ramos; Filipa Martins; Inês Santos; Armanda Rodrigues; Fernanda Silva; Saudade André; Jacinta Serpa
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Review 6.  Fatty acid metabolism and acyl-CoA synthetases in the liver-gut axis.

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Journal:  World J Hepatol       Date:  2021-11-27

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Authors:  Rens Peeters; Jorge Cuenca-Escalona; Esther A Zaal; Anna T Hoekstra; Anouk C G Balvert; Marcos Vidal-Manrique; Niek Blomberg; Sjoerd J van Deventer; Rinke Stienstra; Julia Jellusova; Martin Giera; Luciana Hannibal; Ute Spiekerkoetter; Martin Ter Beest; Celia R Berkers; Annemiek B van Spriel
Journal:  Nat Commun       Date:  2022-09-13       Impact factor: 17.694

Review 8.  Molecular and Metabolic Reprogramming: Pulling the Strings Toward Tumor Metastasis.

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Authors:  Nattavatchara Limsuwat; Chompunuch Boonarkart; Supinya Phakaratsakul; Ornpreya Suptawiwat; Prasert Auewarakul
Journal:  Arch Virol       Date:  2020-03-29       Impact factor: 2.574
  9 in total

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