alexa Fluorescent Human EP3 Receptor Antagonists.


Natural Products Chemistry & Research

Author(s): Tomasch M, Schwed JS, Kuczka K, Meyer Dos Santos S, Harder S,

Abstract Share this page

Abstract Exchange of the lipophilc part of ortho-substituted cinnamic acid lead structures with different small molecule fluorophoric moieties via a dimethylene spacer resulted in hEP3R ligands with affinities in the nanomolar concentration range. Synthesized compounds emit fluorescence in the blue, green, and red range of light and have been tested concerning their potential as a pharmacological tool. hEP3Rs were visualized by confocal laser scanning microscopy on HT-29 cells, on murine kidney tissues, and on human brain tissues and functionally were characterized as antagonists on human platelets. Inhibition of PGE2 and collagen-induced platelet aggregation was measured after preincubation with novel hEP3R ligands. The pyryllium-labeled ligand 8 has been shown as one of the most promising structures, displaying a useful fluorescence and highly affine hEP3R antagonists.
This article was published in ACS Med Chem Lett and referenced in Natural Products Chemistry & Research

Relevant Expert PPTs

Relevant Speaker PPTs

  • Ines Bouaziz
    Water treatment containing organic compounds by coupling adsorption and electrochemical degradation at BDD anode: Sawdust adsorption performance for the treatment of dilute phenol solutions
    PPT Version | PDF Version
  • Lavanya Rayapu
    PPT Version | PDF Version
  • Heidi Schalchli
    Natural products of Anthracophyllum discolor: Ligninolytic enzymes and antifungal volatile compounds
    PPT Version | PDF Version
  • Soliman Khatib
    Analysis of volatile organic compounds in rats with dopaminergic lesion: possible application for early detection of Parkinson’s disease
    PPT Version | PDF Version
  • Adel Nefzi
    “Adel Nefzi-Torrey-Pines-Institute-for-Molecular-Studies-USA-Diversity-Oriented-Synthesis-of-low-Molecular-Weight-Acyclic-and-Heterocyclic-Compounds-from-Resin-bound-Polyamides-Application-for-Drug-Discovery”
    PPT Version | PDF Version
  • Pietro Tedesco
    Exploiting the cold environments: psychrophilic bacteria as a promising source of novel bioactive compounds
    PPT Version | PDF Version

Recommended Conferences

Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version