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From RORγt Agonist to Two Types of RORγt Inverse Agonists
- Source :
- ACS Medicinal Chemistry Letters. 9:120-124
- Publication Year :
- 2018
- Publisher :
- American Chemical Society (ACS), 2018.
-
Abstract
- Biaryl amides as new RORγt modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with RORγt ligand binding domain (LBD) was resolved, and both “short” and “long” inverse agonists were obtained by removing from 6 or adding to 6 a proper structural moiety. While “short” inverse agonist (8) recruits a corepressor peptide and dispels a coactivator peptide, “long” inverse agonist (9) dispels both. The two types of inverse agonists can be utilized as potential tools to study mechanisms of Th17 transcriptional network inhibition and related disease biology.
- Subjects :
- 0301 basic medicine
chemistry.chemical_classification
Agonist
Stereochemistry
medicine.drug_class
Organic Chemistry
Peptide
Biochemistry
03 medical and health sciences
chemistry.chemical_compound
030104 developmental biology
chemistry
RAR-related orphan receptor gamma
Amide
Drug Discovery
Coactivator
medicine
Moiety
Inverse agonist
Corepressor
Subjects
Details
- ISSN :
- 19485875
- Volume :
- 9
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....55a87da15f60b2a1ed850fe7080392df