Evaluation of differentiation-inducing activity of retinoids on human leukemia cell lines HL-60 and NB4.
Retinoids, including all-trans-retinoic acid (ATRA), its isomers, and fifty synthetic retinoids (retinobenzoic acids), were tested for differentiation-inducing activity on human leukemia cell lines HL-60 and NB4. Binding activity of typical retinoids to nuclear retinoic acid receptors (RARs) was also investigated. A good linear correlation between the ED50 values of differentiation-inducing activity towards HL-60 cells and those towards NB4 cells was found. Binding activities of retinoids to RAR alpha and RAR beta also correlated well to the differentiation-inducing activities.
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
Y
Y
Hashimoto
H
H
Kagechika
E
E
Kawachi
H
H
Fukasawa
G
G
Saito
K
K
Shudo
D001565:Benzoates / Q000494:pharmacology; D002454:Cell Differentiation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D018168:Receptors, Retinoic Acid / Q000378:metabolism; D000072482:Retinoic Acid Receptor alpha; D012176:Retinoids / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014297:Trimethylsilyl Compounds / Q000494:pharmacology
D001565:Benzoates; C000607071:RARA protein, human; D018168:Receptors, Retinoic Acid; D000072482:Retinoic Acid Receptor alpha; D012176:Retinoids; C112689:TAC 101; D014297:Trimethylsilyl Compounds; C082925:retinoic acid receptor beta