3dy6 › Citations

Discovery of a novel class of PPARdelta partial agonists.

Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, Willson TM
Bioorg Med Chem Lett 18 5018-22 (2008)
Cited: 10 times
EuropePMC logo PMID: 18722772

Abstract

Anthranilic acid GW9371 was identified as a novel class of PPARdelta partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.

Reviews - 3dy6 mentioned but not cited (2)

  1. Activation of PPARδ: from computer modelling to biological effects. Kahremany S, Livne A, Gruzman A, Senderowitz H, Sasson S. Br J Pharmacol 172 754-770 (2015)
  2. The PPAR Ω Pocket: Renewed Opportunities for Drug Development. Kaupang Å, Hansen TV. PPAR Res 2020 9657380 (2020)

Articles - 3dy6 mentioned but not cited (1)

  1. Knowledge-Based Methods To Train and Optimize Virtual Screening Ensembles. Swift RV, Jusoh SA, Offutt TL, Li ES, Amaro RE. J Chem Inf Model 56 830-842 (2016)


Reviews citing this publication (3)

  1. Discovery and development of selective PPAR gamma modulators as safe and effective antidiabetic agents. Doshi LS, Brahma MK, Bahirat UA, Dixit AV, Nemmani KV. Expert Opin Investig Drugs 19 489-512 (2010)
  2. Current and Future Treatments in the Fight Against Non-Alcoholic Fatty Liver Disease. Smeuninx B, Boslem E, Febbraio MA. Cancers (Basel) 12 E1714 (2020)
  3. Migraine signaling pathways: amino acid metabolites that regulate migraine and predispose migraineurs to headache. Biringer RG. Mol Cell Biochem 477 2269-2296 (2022)

Articles citing this publication (4)

  1. Regulation of tissue-specific carboxylesterase expression by pregnane x receptor and constitutive androstane receptor. Xu C, Wang X, Staudinger JL. Drug Metab Dispos 37 1539-1547 (2009)
  2. Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists. Maltarollo VG, Togashi M, Nascimento AS, Honorio KM. PLoS One 10 e0118790 (2015)
  3. Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy. Evans KA, Shearer BG, Wisnoski DD, Shi D, Sparks SM, Sternbach DD, Winegar DA, Billin AN, Britt C, Way JM, Epperly AH, Leesnitzer LM, Merrihew RV, Xu RX, Lambert MH, Jin J. Bioorg Med Chem Lett 21 2345-2350 (2011)
  4. Synthesis and anti-inflammatory evaluation of N-sulfonyl anthranilic acids via Ir(III)-catalyzed C-H amidation of benzoic acids. Han SH, Suh HS, Jo H, Oh Y, Mishra NK, Han S, Kim HS, Jung YH, Lee BM, Kim IS. Bioorg Med Chem Lett 27 2129-2134 (2017)


Quick links