Research Article Details
| Article ID: | A09435 |
| PMID: | 31751137 |
| Source: | J Med Chem |
| Title: | Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist. |
| Abstract: | The liver receptor homolog-1 (LRH-1, NR5A2), a member of the nuclear receptor superfamily, has emerged as a promising drug target for the treatment of diabetes, nonalcoholic fatty liver disease, inflammatory bowel disease, and cancers. However, the discovery of LRH-1 modulators remains a challenge since the large and hydrophobic ligand binding pocket of LRH-1 has been difficult to target. This Viewpoint discusses the recent discovery, published in this journal, that the first low nanomolar LRH-1 agonist was identified through structure-guided design. The agonist binds deep inside the LRH-1 ligand binding pocket by a novel mechanism of action. |
| DOI: | 10.1021/acs.jmedchem.9b01753 |
| Strategy ID | Therapy Strategy | Synonyms | Therapy Targets | Therapy Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
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| Drug ID | Drug Name | Type | DrugBank ID | Targets | Category | Latest Progress |
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