RAR-RXR selectivity and biological activity of new retinoic acid analogues with heterocyclic or polycyclic aromatic systems.
The cell biological activity of novel retinoids and rexinoids is described. The stereochemistry of the new compounds was analyzed and ligand docking experiments revealed the structural basis of their RAR binding characteristics. The new ligands activate nuclear retinoic acid receptors (RAR, RXR) with distinct selectivity patterns, as determined in genetically engineered 'reporter' cells. The biological activity of the novel retinoids was assessed by differentiation of NB4 acute promyelocytic leukemia cells.
Ivanova
D
D
Institute of Organic Chemistry, Bulgarian Academy of Sciences, Sofia 1113, Bulgaria.
Gaudon
C
C
Rossin
A
A
Bourguet
W
W
Gronemeyer
H
H
D018168:Receptors, Retinoic Acid / Q000187:drug effects*; D047488:Retinoid X Receptors; D013237:Stereoisomerism; D014157:Transcription Factors / Q000187:drug effects*; D014212:Tretinoin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D014157:Transcription Factors; D014212:Tretinoin