Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor-Reference-Cited by-同舟云学术

Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor

Published:2020 Issue:9 Volume:11 Page:1032-1040
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Cunha Micael Rodrigues¹²³⁴⁵^ORCID,Bhardwaj Rajesh⁶⁷⁸⁹⁴^ORCID,Carrel Aline Lucie¹²³⁴^ORCID,Lindinger Sonja¹⁰¹¹¹²¹³^ORCID,Romanin Christoph¹⁰¹¹¹²¹³^ORCID,Parise-Filho Roberto⁵¹⁴¹⁵¹⁶^ORCID,Hediger Matthias A.⁶⁷⁸⁹⁴^ORCID,Reymond Jean-Louis¹²³⁴^ORCID

Affiliation:

1. Department of Chemistry and Biochemistry

2. University of Bern

3. 3012 Bern

4. Switzerland

5. Department of Pharmacy

6. Department of Nephrology and Hypertension

7. University Hospital Bern

8. Inselspital

9. 3010 Bern

10. Institute of Biophysics

11. Johannes Kepler University Linz

12. 4020 Linz

13. Austria

14. University of São Paulo

15. 05508-000 São Paulo

16. Brazil

Abstract

Natural product derived analogues were surveyed, and an oxygenated analog was identified as a potent and selective TRPV6 inhibitor, with high microsomal stability and low off-target effects.

Funder

Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung

Fundação de Amparo à Pesquisa do Estado de São Paulo

Austrian Science Fund

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2020/MD/D0MD00145G

Reference49 articles.

1. Human Calcium Transport Protein CaT1