5 research outputs found
Inverse relationship between hSHBG affinity for testosterone and hSHBG concentration revealed by surface plasmon resonance
No full textcited By 4International audienceA wide range of human sex hormone-binding globulin (hSHBG) affinity constants for testosterone (KAₕSHBG) has been reported in literature. To bring new insight on the KAₕSHBG value, we implemented a study of the molecular interactions occurring between testosterone and its plasma transport proteins by using surface plasmon resonance. The immobilization on the sensorchip of a testosterone derivative was performed by an oligoethylene glycol linker. For different plasmas with hSHBG concentrations, an assessment of the KAₕSHBG was obtained from a set of sensorgrams and curve-fitting these data. We observed that KAₕSHBG decreased, from at least two decades, when the plasma hSHBG concentration increased from 4.4 to 680 nmol/L. Our study shows a wide biological variability of KAₕSHBG that is related to the hSHBG concentration. These unexpected results may have a physiological significance and question the validity of current methods that are recommended for calculating free testosterone concentrations to evaluate androgen disorders in humans. © 2014 Elsevier Ireland Ltd
Synthesis of specific inhibitors of Haspin for potential cancer treatment.
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