"目录号: HY-14649
Metabolic Enzyme/ProteaseCell Cycle/DNA DamageNF-κB-
Retinoic acid 是一种天然的RAR/RXR核受体激动剂。Retinoic acid 也结合到PPARβ/δ，Kd为 17 nM。
RAR/RXRPPAR
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生物活性
Description
Retinoic acid is a natural agonist ofRAR/RXRnuclear receptors. Retinoic acid also bind toPPARβ/δ, withKdof 17 nM.
IC50& Target
RAR/RXR[1]
Kd: 17 nM (PPARβ/δ), 103 nM (PPARα), 178 (PPARγ)[2]
In Vitro
Retinoic acid (All-trans-retinoic acid, ATRA) is a highly potent derivative of vitamin A that is required for virtually all essential physiological processes and functions because of its involvement in transcriptional regulation of over 530 different genes. Retinoic acid exerts its actions by serving as an activating ligand of nuclear retinoic acid receptors (RARα-γ), which form heterodimers with retinoid X receptors (RXRα-γ)[1]. Retinoic acid (RA) bound to PPARα and PPARγ with a low affinity demonstrated by Kdvalues of 100-200 nM. In contrast, Retinoic acid associates with PPARβ/δ with a Kdof 17 nM, revealing both high affinity and isotype selectivity[2]. Undifferentiated P19 cells express the Retinoic acid (RA) receptors RARα, RARβ, RARγ, and PPARβ/δ, as well as the Retinoic acid -binding proteins CRABP-II and FABP5. Induction of differentiation by treatment of cells with Retinoic acid results in transient up-regulation of CRABP-II and down-regulation of FABP5 that are observed at the level of both the respective proteins and mRNAs. Following the initial decrease, the level of both FABP5 protein and mRNA increases to attain a 2-2.5-fold higher level in mature neurons as compared with undifferentiated P19 cells. Induction of differentiation does not markedly affect the levels of either RARα or PPARβ/δ. The level of RARγ mRNA decreases by about 5-fold by day 4 and remained low in mature neurons[3]. Retinoic acid (RA) is a morphogen derived from retinol (vitamin A) that plays important roles in cell growth, differentiation, and organogenesis. The Retinoic acid interacts with retinoic acid receptor (RAR) and retinoic acid X receptor (RXR) which then regulate the target gene expression[4].
Clinical Trial
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University of Colorado, Denver
Melanoma
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Phase 3
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Phase 3
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University of Ulm
Acute Myeloid Leukemia
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Phase 2-Phase 3
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Ulrike Kohlweyer-University Hospital Freiburg
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University of Bergen
Acute Myelogenous Leukemia
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