Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
5 years ago

Nonacidic Farnesoid X Receptor Modulators

Nonacidic Farnesoid X Receptor Modulators
Jurema Schmidt, Mara Lindner, Daniel Flesch, Ewgenij Proschak, Kerstin Lüddens-Dämgen, Christina Lamers, Jan Heering, Jan Kramer, Manfred Schubert-Zsilavecz, Pascal Heitel, Matthias Gabler, Markus Hartmann, Hartmut Lüddens, Daniel Merk, Mario Wurglics, Astrid Kaiser, Sun-Yee Cheung
As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. Clinical results have validated FXR as therapeutic target in hepatic and metabolic diseases. To date, potent FXR agonists share a negatively ionizable function that might compromise their pharmacokinetic distribution and behavior. Here we report the development and characterization of a high-affinity FXR modulator not comprising an acidic residue.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00903

DOI: 10.1021/acs.jmedchem.7b00903

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.