Klein C
J Biol Chem. 1979 Dec 25;254(24):12573-8.
Experiments using a phosphodiesterase-minus mutant of Dictyostelium discoideum indicate that ligand-induced loss of cell surface cyclic adenosine 3':5'-monophosphate binding sites (down regulation) can be evoked with concentrations of cyclic adenosine 3':5'-monophosphate as low as 10(-8) M. The loss of receptor sites is observed after 5 min of cell preincubation with cyclic adenosine 3':5'-monophosphate and can be as extensive as 75 to 80%. This decrease in binding sites is correlated with the appearance of a slowly dissociating cyclic adenosine 3':5'-monophosphate binding component. Radioactive cyclic adenosine 3':5'-monophosphate bound to this form of receptor cannot be competed for by nonradioactive cyclic adenosine 3':5'-monophosphate or adenosine 5'-monophosphate and is not accessible to hydrolysis by cyclic adenosine 3':5'-monophosphate phosphodiesterase. The extent of appearance of this binding component is dependent upon the concentration of cyclic adenosine 3':5'-monophosphate used to elicit the down regulation response and the temperature of the incubation medium.
使用盘基网柄菌磷酸二酯酶缺失突变体进行的实验表明,浓度低至10(-8)M的环腺苷3':5'-单磷酸就能引发配体诱导的细胞表面环腺苷3':5'-单磷酸结合位点丧失(下调)。在用环腺苷3':5'-单磷酸对细胞进行5分钟预孵育后,可观察到受体位点丧失,丧失程度可达75%至80%。结合位点的这种减少与一种缓慢解离的环腺苷3':5'-单磷酸结合成分的出现相关。与这种受体形式结合的放射性环腺苷3':5'-单磷酸不能被非放射性环腺苷3':5'-单磷酸或腺苷5'-单磷酸竞争,且不能被环腺苷3':5'-单磷酸磷酸二酯酶水解。这种结合成分出现的程度取决于用于引发下调反应的环腺苷3':5'-单磷酸的浓度以及孵育培养基的温度。