Abstract：
:One feature that contraindicates the wide therapeutic use of retinoids is their teratogenicity. Synthetic retinoids are distinguishable from each other on the basis of their partial or exclusive preference in binding and activation of all-trans retinoic acid receptors (RARs) or retinoid X receptors (RXRs). Using mouse embryo limb bud cells in micromass cultures as a bioassay, we examined the inhibitory activities of a number of standard and novel retinoids on chondrogenic cell differentiation. Transient cotransfection of HeLa cells was used to measure the ability of each retinoid to induce transcription of a reporter gene by activating RAR alpha, RAR beta, RAR gamma, or RXR alpha chimeric constructs. All retinoids in this study that activated RARs to any degree in the cotransfection assay also inhibited chondrogenesis in vitro, whereas retinoids that were either specific for RXR or inactive in the cotransfection assay did not. The activity of RAR-selective agonists and the inactivity of RXR-specific agonists in the cotransfection assay correlated well with the relative teratogenicity of six of the representative retinoids studied when orally administered at day 11 to pregnant ICR mice.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Jiang H,Penner JD,Beard RL,Chandraratna RA,Kochhar DMdoi
10.1016/0006-2952(95)00183-zsubject
Has Abstractpub_date
1995-08-25 00:00:00pages
669-76issue
5eissn
0006-2952issn
1873-2968pii
0006-2952(95)00183-Zjournal_volume
50pub_type
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1986-02-01 00:00:00
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pub_type： 杂志文章
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更新日期：1984-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(89)90645-x
更新日期：1989-12-15 00:00:00
