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Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10
AKR1B10 is a human aldo-keto reductase (AKR) found to be elevated in several cancer types and in precancerous lesions. In vitro, AKR1B10 exhibits a much higher retinaldehyde reductase activity thanExpand
Activation of Retinoic Acid Receptors by Dihydroretinoids
Vitamin A-derived metabolites act as ligands for nuclear receptors controlling the expression of a number of genes. Stereospecific saturation of the C13-C14 double bond of all-trans-retinol by theExpand
New analogues of amonafide and elinafide, containing aromatic heterocycles: synthesis, antitumor activity, molecular modeling, and DNA binding properties.
Amonafide- and elinafide-related mono and bisintercalators, modified by the introduction of a pi-excedent furan or thiophene ring fused to the naphthalimide moiety, have been synthesized. TheseExpand
Aldo-keto reductases from the AKR1B subfamily: retinoid specificity and control of cellular retinoic acid levels.
NADP(H)-dependent cytosolic aldo-keto reductases (AKRs) have been added to the group of enzymes which contribute to oxidoreductive conversions of retinoids. Recently, we found that two members fromExpand
Increased adiposity in the retinol saturase‐knockout mouse
The enzyme retinol saturase (RetSat) catalyzes the saturation of all‐irans‐retinol to produce (R)‐all‐trans‐13,14‐dihydroretinol. As a peroxisome pro‐liferator‐activated receptor (PPAR) γ target,Expand
Aldo-keto reductases in retinoid metabolism: search for substrate specificity and inhibitor selectivity.
Biological activity of natural retinoids requires the oxidation of retinol to retinoic acid (RA) and its binding to specific nuclear receptors in target tissues. The first step of this pathway, theExpand
Specificity of zebrafish retinol saturase: formation of all-trans-13,14-dihydroretinol and all-trans-7,8- dihydroretinol.
Metabolism of vitamin A, all-trans-retinol, leads to the formation of 11-cis-retinaldehyde, the visual chromophore, and all-trans-retinoic acid, which is involved in the regulation of gene expressionExpand
Synthesis and biological evaluation of analogues of butyrolactone I and molecular model of its interaction with CDK2.
A series of analogues of butyrolactone I, a natural product isolated from Aspergillus terreus that selectively inhibits the CDK2 and CDK1 kinases and that has been found to exhibit an interestingExpand
Kinetics of human alcohol dehydrogenase with ring-oxidized retinoids: effect of Tween 80.
Human alcohol dehydrogenases (ADH1 and ADH4) actively use retinoids oxidized at the cyclohexenyl ring (4-oxo-, 4-hydroxy-, and 3,4-didehydro-retinoids), which are functional compounds in severalExpand
Structural Determinants of the Selectivity of 3‐Benzyluracil‐1‐acetic Acids toward Human Enzymes Aldose Reductase and AKR1B10
The human enzymes aldose reductase (AR) and AKR1B10 have been thoroughly explored in terms of their roles in diabetes, inflammatory disorders, and cancer. In this study we identified two new leadExpand