Selective synthetic ligands for human nuclear retinoic acid receptors.
From a series of naphthalene and benzoic acid derivatives we have identified synthetic retinoic acid analogues exhibiting high selectivity for the nuclear retinoic acid receptors RAR alpha (Am 580), RAR beta (CD 2019) and RAR gamma (CD 437) as well as ligands sharing high affinities for all RAR subtypes (CD 367). The compounds were evaluated in two complementary screening systems: (1) binding to nuclear proteins extracted from COS-7 cells after transfection with the appropriate expression vectors, and (2) induction of plasminogen activator in the embryonic mouse teratocarcinoma cell line F9. All compounds behaved as retinoic acid agonists in the F9 test.
Martin
B
B
Centre International de Recherches Dermatologiques Galderma, CIRD, Valbonne, France.
Bernardon
J M
JM
Cavey
M T
MT
Bernard
B
B
Carlavan
I
I
Charpentier
B
B
Pilgrim
W R
WR
Shroot
B
B
Reichert
U
U
D001667:Binding, Competitive; D002352:Carrier Proteins / Q000187:drug effects*; D002467:Cell Nucleus / Q000378:metabolism*; D002478:Cells, Cultured; D006801:Humans; D008024:Ligands; D010960:Plasminogen Activators / Q000187:drug effects; D018168:Receptors, Retinoic Acid; D012176:Retinoids / Q000378:metabolism* / Q000494:pharmacology; D014162:Transfection; D014212:Tretinoin
D002352:Carrier Proteins; D008024:Ligands; D018168:Receptors, Retinoic Acid; D012176:Retinoids; D014212:Tretinoin; D010960:Plasminogen Activators