The structural basis of aldo-keto reductase 1C3 inhibition by 17α-picolyl and 17(E)-picolinylidene androstane derivatives [PDF]
Journal of Enzyme Inhibition and Medicinal ChemistryHuman aldo-keto reductase 1C3 (AKR1C3) is a steroid modifying enzyme involved in cancer progression. Here, A-ring modified 17α-picolyl and 17(E)-picolinylidene androstane derivatives are shown to inhibit AKR1C3 activity in vitro.
Jovana J. Plavša-Puž +7 more
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Neurosteroids as Selective Inhibitors of Glycine Receptor Activity: Structure-Activity Relationship Study on Endogenous Androstanes and Androstenes [PDF]
Frontiers in Molecular Neuroscience, 2020 The ability of androstane and androstene neurosteroids with modifications at C-17, C-5, and C-3 (compounds 1-9) to influence the functional activity of inhibitory glycine and γ-aminobutyric acid (GABA) receptors was estimated.
Julia V. Bukanova +2 more
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Studies of Coumarin Derivatives for Constitutive Androstane Receptor (CAR) Activation [PDF]
Molecules, 2020 Constitutive androstane receptor (CAR) activation has found to ameliorate diabetes in animal models. However, no CAR agonists are available clinically. Therefore, a safe and effective CAR activator would be an alternative option.
Shin-Hun Juang +11 more
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Pseudomonas μtant strains that accumulate androstane and seco-androstane intermediates from bile acids [PDF]
Biochemical Journal, 1987 Transposon mutant strains which were affected in bile acid catabolism were isolated from four Pseudomonas spp. Two of the mutant groups isolated were found to accumulate 12 alpha-hydroxyandrosta-1,4-diene-3,17-dione as the major product from deoxycholic acid. Strains in one of these two groups were able to grow on steroids such as chenodeoxycholic acid,
R A Leppik, D J Sinden
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Redetermination of 5α-androstane-3,17-dione [PDF]
Acta Crystallographica Section E, 2010 The structure of the title compound, C19H28O2, has been redermined at 295 (2) K, with much improved precision. The structure and molecular packing of the title compound was first reported by Coiro et al. [Acta Cryst. (1973). B29, 1404&
Jerry P. Jasinski +4 more
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Synthesis of New Brassinosteroid Analogs with Androstane Skeleton and Heterocyclic Acyl Side Chains: Preliminary Molecular Docking Studies [PDF]
MoleculesBrassinosteroid analogs with heterocyclic rings in the side chain are interesting because important biological activity has been shown by these compounds.
Omara Araya +4 more
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The Use of the LanthaScreen TR-FRET CAR Coactivator Assay in the Characterization of Constitutive Androstane Receptor (CAR) Inverse Agonists [PDF]
Sensors, 2015 The constitutive androstane receptor (CAR) is a critical nuclear receptor in the gene regulation of xenobiotic and endobiotic metabolism. The LanthaScreenTM TR-FRET CAR coactivator assay provides a simple and reliable method to analyze the affinity of a ...
Alejandro Carazo, Petr Pávek
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Comprehensive Chemometric and Chromatographic Investigation of Lipophilicity of Biologically Active Androstane-3-Oxime Derivatives Across Diverse UHPLC Systems [PDF]
PharmaceuticalsBackground/Objectives: Previously reported analyses show that some androstane-3-oxime derivatives with picolyl and picolinylidene functional groups possess a significant anticancer activity towards various cancer cell lines.
Strahinja Z. Kovačević +4 more
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Nucleophosmin 1 induction is an early event in a Phenobarbital induced proliferation response in rat but not human liver 3D microtissues [PDF]
Toxicology ReportsA key event in the process of rat but not human liver carcinogenesis caused by constitutive androstane receptor activators such as phenobarbital (PB) is hepatocyte proliferation, but the mechanism(s) underpinning this response is not fully understood ...
Matthew Elcombe +2 more
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Constitutive Androstane Receptor: A Peripheral and a Neurovascular Stress or Environmental Sensor [PDF]
Cells, 2020 Xenobiotic nuclear receptors (NR) are intracellular players involved in an increasing number of physiological processes. Examined and characterized in peripheral organs where they govern metabolic, transport and detoxification mechanisms, accumulating ...
Fabiana Oliviero +6 more
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