alexa Fluorescent Human EP3 Receptor Antagonists.
Chemistry

Chemistry

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
    EVALUATION OF ANTI-DIABETIC PROPERTIES OF THE COMPOUNDS ISOLATED FROM MARINE MACROALGAE
    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

Relevant Topics

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

Agri, Food, Aqua and Veterinary Science Journals

Dr. Krish

[email protected]

1-702-714-7001 Extn: 9040

Clinical and Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemical Engineering and Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001 Extn: 9040

Earth & Environmental Sciences

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

General Science and Health care Journals

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics and Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001 Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Informatics Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Material Sciences Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Mathematics and Physics Journals

Jim Willison

[email protected]

1-702-714-7001 Extn: 9042

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001 Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

John Behannon

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001 Extn: 9042

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