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Retinoid receptor ligands act on retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Both are nuclear receptors with α, β and γ subtypes that bind DNA as RAR-RXR heterodimers and regulate gene transcription. A receptor for the morphogen retinoic acid was identified in 1987 as a member of the nuclear receptor family. In 1990 a second receptor responding to retinoic acid, later named RXRα, revealed a distinct retinoid pathway. Tretinoin, the all-trans form of retinoic acid, activates RARs, while tamibarotene and AM 580 favor RARα and CD 437 favors RARγ. Adapalene, tazarotene, acitretin and fenretinide are synthetic retinoids, whereas bexarotene is a ligand selective for RXRs.
PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
