Comparison of the effects of chemical and isotopic dilution on the dissociation of bound labeled ligands

The dissociation of a labeled ligand from a binding structure to which it is reversibly attached can be promoted either by dilution or by chase. The kinetics of the dissociation brought up by dilution can be modified or not by the presence of various concentrations of cold ligand, according to the molecular mechanism of interaction. Analog computer simulation leads to the following results: (i) no cooperativity, monomolecular dissociation: no modification; (ii) positive or negative cooperativity (sequential models): acceleration, no modification, or slowing down (according to the kinetic constants); (iii) positive cooperativity (concerted model): no modification; (iv) two-step interaction: no modification if both interaction steps take place in the same phase, otherwise acceleration; and, (v) bimolecular association and dissociation: acceleration. This methodology could be used in order to characterize the molecular properties of various binding structures in the field of drug and hormone receptors as well as in enzymology.     

A new method to characterize saturation functions by their first four moments

The calculation of the first four moments of saturation functions is proposed as a method to describe the properties of enzymes or receptors models. The values of these moments in the case of the Langmuir or Michaelis-Menten equation and the Hill equation are reviewed. They have been calculated for the second degree Adair equation and in the case of binding site heterogeneity. A method for generalization to cases of greater complexity is also proposed. The advantage of this method over the classical ones—graphical representations and derivation of coefficients like n_H, $\text{[L]0.9}\text{[L]0.1}$…—is essentially that the moments are defined by one single value independently of any particular model for the whole of the saturation curve.     

Prostacyclin production by the bovine aortic smooth muscle

It is well known that cultured aortic smooth muscle cells, the phenotype of which has modulated from contractile to synthetic, are able to release prostacyclin (PGI2). We have studied the release of PGI2 from cultured explants of bovine aortic media, which represent an homogeneous population of smooth muscle cells with a contractile phenotype. These explants released spontaneously huge amounts of PGI2, which was the major eicosanoid produced. PGI2 release was stimulated by serum and by serotonin. This experimental model seems useful to evaluate the contribution of smooth muscle to the biosynthesis of PGI2 by the arterial wall.