69776-17-6Relevant academic research and scientific papers
Determination of 3β-hydroxy-5-cholen-24-oic acid and its sulfate in human serum by gas chromatography-mass spectrometry
Tohma, Masahiko,Wajima, Hiromi,Mahara, Reijiro,Korosawa, Takao,Makino, Isao
, p. 47 - 56 (1984)
The glycine conjugate of 3β-hydroxy-5-cholen-24-oic acid and its sulfate labeled with deuterium at the C-2, -4 and -23 positions were synthesized.A highly sensitive and specific quantitative assay of the bile acid has been developed by selected ion monitoring in gas chromatography-mass spectrometry of the methyl ester trimethylsilyl ether derivatives using the deuterium labeled conjugates as internal standards.Calibration curves for the bile acid and its sulfate exhibited a linear relationship over the range of 0.01-100 μg/ml in human serum.
Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Epheephrin system
Castelli, Riccardo,Tognolini, Massimiliano,Vacondio, Federica,Incerti, Matteo,Pala, Daniele,Callegari, Donatella,Bertoni, Simona,Giorgio, Carmine,Hassan-Mohamed, Iftiin,Zanotti, Ilaria,Bugatti, Antonella,Rusnati, Marco,Festuccia, Claudio,Rivara, Silvia,Barocelli, Elisabetta,Mor, Marco,Lodola, Alessio
supporting information, p. 312 - 324 (2015/09/22)
The Eph receptoreephrin system is an emerging target for the development of novel anti-angiogenic therapies. Research programs aimed at developing small-molecule antagonists of the Eph receptors are still in their initial stage as available compounds suffer from pharmacological drawbacks, limiting their application in vitro and in vivo. In the present work, we report the design, synthesis and evaluation of structureeactivity relationships of a class of Δ5-cholenoyl-amino acid conjugates as Epheephrin antagonists. As a major achievement of our exploration, we identified N-(3ηb-hydroxy-Δ5-cholen-24-oyl)-Ltryptophan (UniPR1331) as the first small molecule antagonist of the Epheephrin system effective as an anti-angiogenic agent in endothelial cells, bioavailable in mice by the oral route and devoid of biological activity on G protein-coupled and nuclear receptors targeted by bile acid derivatives.
Preparation and antigenic properties of methyl 3β-hydroxy-19-oxo-5-cholen-24-oyl-glycinate 19-(O-carboxymethyl)oxime-bovine serum albumin conjugate
Yamauchi,Kojima,Nakayama
, p. 3088 - 3092 (2007/10/02)
The preparation and antigenic properties of 3β-hydroxy-5-cholen-24-oyl-glycine-bovine serum albumin (BSA) conjugate in which the hapten is linked to the carrier protein through an (O-carboxymethyl)oxime bridge at the C-19 position on the steroid portion are described. Antibody raised against the antigen in rabbits possessed high titer and specificity to 3β-hydroxy-5-cholen-24-oyl-glycine, exhibiting no significant cross-reactions with various bile acids.
