Literature DB >> 28749691

Nonacidic Farnesoid X Receptor Modulators.

Daniel Flesch1, Sun-Yee Cheung1, Jurema Schmidt1, Matthias Gabler1, Pascal Heitel1, Jan Kramer1, Astrid Kaiser1, Markus Hartmann1, Mara Lindner2, Kerstin Lüddens-Dämgen3, Jan Heering2, Christina Lamers1, Hartmut Lüddens3, Mario Wurglics1, Ewgenij Proschak1, Manfred Schubert-Zsilavecz1, Daniel Merk1.   

Abstract

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.

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Year:  2017        PMID： 28749691     DOI： 10.1021/acs.jmedchem.7b00903

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  17 in total

1.  Scaffold hopping from synthetic RXR modulators by virtual screening and de novo design.

Authors:  Daniel Merk; Francesca Grisoni; Lukas Friedrich; Elena Gelzinyte; Gisbert Schneider
Journal:  Medchemcomm       Date:  2018-06-06       Impact factor: 3.597

2.  A dual farnesoid X receptor/soluble epoxide hydrolase modulator treats non-alcoholic steatohepatitis in mice.

Authors:  Md Abdul Hye Khan; Jurema Schmidt; Anna Stavniichuk; John D Imig; Daniel Merk
Journal:  Biochem Pharmacol       Date:  2019-05-23       Impact factor: 5.858

3.  Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.

Authors:  Jan S Kramer; Stefano Woltersdorf; Thomas Duflot; Kerstin Hiesinger; Felix F Lillich; Felix Knöll; Sandra K Wittmann; Franca-M Klingler; Steffen Brunst; Apirat Chaikuad; Christophe Morisseau; Bruce D Hammock; Carola Buccellati; Angelo Sala; G Enrico Rovati; Matthieu Leuillier; Sylvain Fraineau; Julie Rondeaux; Victor Hernandez-Olmos; Jan Heering; Daniel Merk; Denys Pogoryelov; Dieter Steinhilber; Stefan Knapp; Jeremy Bellien; Ewgenij Proschak
Journal:  J Med Chem       Date:  2019-09-17       Impact factor: 7.446

4.  The Transcriptional Repressor Orphan Nuclear Receptor TLX Is Responsive to Xanthines.

Authors:  Giuseppe Faudone; Whitney Kilu; Xiaomin Ni; Apirat Chaikuad; Sridhar Sreeramulu; Pascal Heitel; Harald Schwalbe; Stefan Knapp; Manfred Schubert-Zsilavecz; Jan Heering; Daniel Merk
Journal:  ACS Pharmacol Transl Sci       Date:  2021-11-23

5.  Nonacidic Chemotype Possessing N-Acylated Piperidine Moiety as Potent Farnesoid X Receptor (FXR) Antagonists.

Authors:  Naoki Teno; Yukiko Yamashita; Yusuke Iguchi; Ko Fujimori; Mizuho Une; Tomoko Nishimaki-Mogami; Takie Hiramoto; Keigo Gohda
Journal:  ACS Med Chem Lett       Date:  2018-01-04       Impact factor: 4.345

6.  Differential Therapeutic Effects of FXR Activation, sEH Inhibition, and Dual FXR/sEH Modulation in NASH in Diet-Induced Obese Mice.

Authors:  Moritz Helmstädter; Jurema Schmidt; Astrid Kaiser; Lilia Weizel; Ewgenij Proschak; Daniel Merk
Journal:  ACS Pharmacol Transl Sci       Date:  2021-03-29

7.  Scaffold-Hopping from Synthetic Drugs by Holistic Molecular Representation.

Authors:  Francesca Grisoni; Daniel Merk; Ryan Byrne; Gisbert Schneider
Journal:  Sci Rep       Date:  2018-11-07       Impact factor: 4.379

8.  Molecular tuning of farnesoid X receptor partial agonism.

Authors:  Daniel Merk; Sridhar Sreeramulu; Denis Kudlinzki; Krishna Saxena; Verena Linhard; Santosh L Gande; Fabian Hiller; Christina Lamers; Ewa Nilsson; Anna Aagaard; Lisa Wissler; Niek Dekker; Krister Bamberg; Manfred Schubert-Zsilavecz; Harald Schwalbe
Journal:  Nat Commun       Date:  2019-07-02       Impact factor: 14.919

9.  Allosteric modulation of the farnesoid X receptor by a small molecule.

Authors:  Matthias Gabler; Jan Kramer; Jurema Schmidt; Julius Pollinger; Julia Weber; Astrid Kaiser; Frank Löhr; Ewgenij Proschak; Manfred Schubert-Zsilavecz; Daniel Merk
Journal:  Sci Rep       Date:  2018-05-01       Impact factor: 4.379

10.  Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro.

Authors:  Pascal Heitel; Leonie Gellrich; Jan Heering; Tamara Goebel; Astrid Kahnt; Ewgenij Proschak; Manfred Schubert-Zsilavecz; Daniel Merk
Journal:  Sci Rep       Date:  2018-09-10       Impact factor: 4.379
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