Gunter Weimann

Cyclophosphates VI cyclophosphates as substrates and effectors of phosphodiesterase

Summary The synthesis and the chemical and physical properties of a major number of 3′,5′-cyclophosphates is described. These compounds are derivatives of 3′,5′-AMP, 3′,5′-IMP or 3′,5′-GMP, substituted in the 6-, 8-, 2- or 2′-position. Furthermore, the partial purification of phosphodiesterase from beef pituitary is described. The cyclophosphate analogues were tested for their splitting behavior at mM substrate concentration with several different phosphodiesterases. Due to the heterogenicity of this enzyme, the selection of the proper reference compound for calculating the relative splitting rates is of importance. The patterns of splitting rate changes caused by different substituents are discussed. Based on additional measurements of the mutual inhibition behavior, some conclusions on the relationship of splitting rates and inhibition effects are drawn.