Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists

Author:

Bobrovs Raitis1ORCID,Terentjeva Svetlana1,Olafsen Ninni Elise2ORCID,Dambrauskas Zilvinas3,Gulbinas Antanas3,Maimets Toivo4ORCID,Teino Indrek4,Jirgensons Aigars1ORCID,Matthews Jason25,Jaudzems Kristaps1ORCID

Affiliation:

1. Latvian Institute of Organic Synthesis, Aizkraukles 21, Riga, LV1006, Latvia

2. Department of Nutrition, Institute of Basic Medical Sciences, University of Oslo, 0317 Oslo, Norway

3. Surgical Gastroenterology Laboratory, Institute for Digestive Research, Lithuanian University of Health Sciences, Eiveniu 4, 50103 Kaunas, Lithuania

4. Institute of Molecular and Cell Biology, University of Tartu, Riia 23, 51010 Tartu, Estonia

5. Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON M5S 1A8, Canada

Abstract

The aryl hydrocarbon receptor (AHR) is a versatile ligand-dependent transcription factor involved in diverse biological processes, from metabolic adaptations to immune system regulation.

Funder

EEA Grants/Norway Grants

Publisher

Royal Society of Chemistry (RSC)

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