Literature DB >> 16644217

Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4.

Christopher Blackburn1, Bing Guan, James Brown, Courtney Cullis, Stephen M Condon, Tracy J Jenkins, Stephane Peluso, Yingchun Ye, Ruth E Gimeno, Sandhya Punreddy, Ying Sun, Hui Wu, Brian Hubbard, Virendar Kaushik, Peter Tummino, Praveen Sanchetti, Dong Yu Sun, Tom Daniels, Effie Tozzo, Suresh K Balani, Prakash Raman.   

Abstract

Several potent, cell permeable 4-aryl-dihydropyrimidinones have been identified as inhibitors of FATP4. Lipophilic ester substituents at the 5-position and substitution at the para-position (optimal groups being -NO(2) and CF(3)) of the 4-aryl group led to active compounds. In two cases racemates were resolved and the S enantiomers shown to have higher potencies.

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Year:  2006        PMID: 16644217     DOI: 10.1016/j.bmcl.2006.03.102

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


  18 in total

1.  FATP2 is a hepatic fatty acid transporter and peroxisomal very long-chain acyl-CoA synthetase.

Authors:  Alaric Falcon; Holger Doege; Amy Fluitt; Bernice Tsang; Nicki Watson; Mark A Kay; Andreas Stahl
Journal:  Am J Physiol Endocrinol Metab       Date:  2010-06-08       Impact factor: 4.310

2.  Development and validation of a high-throughput screening assay for human long-chain fatty acid transport proteins 4 and 5.

Authors:  Wei Zhou; Peter Madrid; Amy Fluitt; Andreas Stahl; Xinmin Simon Xie
Journal:  J Biomol Screen       Date:  2010-05-06

3.  Gut triglyceride production.

Authors:  Xiaoyue Pan; M Mahmood Hussain
Journal:  Biochim Biophys Acta       Date:  2011-10-02

4.  The Concise Guide to PHARMACOLOGY 2013/14: transporters.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

5.  Long-chain acyl-CoA synthetases and fatty acid channeling.

Authors:  Douglas G Mashek; Lei O Li; Rosalind A Coleman
Journal:  Future Lipidol       Date:  2007-08

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

Authors:  Constance Ahowesso; Paul N Black; Nipun Saini; David Montefusco; Jessica Chekal; Chrysa Malosh; Craig W Lindsley; Shaun R Stauffer; Concetta C DiRusso
Journal:  Biochem Pharmacol       Date:  2015-09-21       Impact factor: 5.858

7.  Measurement of long-chain fatty acid uptake into adipocytes.

Authors:  Elena Dubikovskaya; Rostislav Chudnovskiy; Grigory Karateev; Hyo Min Park; Andreas Stahl
Journal:  Methods Enzymol       Date:  2014       Impact factor: 1.600

8.  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

Review 9.  SLC27 fatty acid transport proteins.

Authors:  Courtney M Anderson; Andreas Stahl
Journal:  Mol Aspects Med       Date:  2013 Apr-Jun

10.  Targeting the fatty acid transport proteins (FATP) to understand the mechanisms linking fatty acid transport to metabolism.

Authors:  Paul N Black; Angel Sandoval; Elsa Arias-Barrau; Concetta C DiRusso
Journal:  Immunol Endocr Metab Agents Med Chem       Date:  2009-09
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