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LGD-1550
- Development stage
- Unknown
- Lead developer
- Ligand Pharmaceuticals
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
LGD-1550 is an orally-active synthetic aromatic retinoic acid agent with potential antineoplastic and chemopreventive activities. Structurally related to all-trans-retinoic acid and classified as a synthetic retinoid (aromatic retinoid), it selectively binds to all three retinoic acid receptors—RAR-alpha, RAR-beta, and RAR-gamma—resulting in alterations in the expression of genes responsible for cell differentiation and proliferation. Additionally, LGD-1550 acts as an inhibitor of activator protein 1 (AP-1), a transcription factor involved in trophic responses and malignant transformation. Preclinical studies have shown that LGD-1550 potently inhibits proliferation of human breast cancer cell lines expressing retinoic acid receptor alpha but not those lacking this receptor. Human exposure has been limited to clinical trials[1][2][3][5][6].
- Other names
- (2E,4E,6E)-7-(3,5-Di-tert-butylphenyl)-3-methylocta-2,4,6-trienoic acid
02
Targets
RARB (Retinoic acid receptor beta)FOS (Activator Protein 1)RARA (Retinoic acid receptor alpha)RARG (Retinoic acid receptor gamma)
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