Vesely D L, Levey G S
Horm Metab Res. 1978 Sep;10(5):392-5. doi: 10.1055/s-0028-1093399.
Streptozotocin, a nitrosamide carcinogen, enhances the activity of guanylate cyclase. Six analogues of streptozotocin were studied in order to elucidate critical structure-activity relationships pertaining to the activation of guanylate cyclase. Analogue 1, known as chlorozotocin, has a nitroso group and increased guanylate cyclase activity 17 to 28-fold. Analogue III, which also has a nitroso group, but greater structural modifications with 4 acetate groups extending off of the glucose moiety, activated guanylate cyclase in colon but not in kidney. The other analogues (II,IV,VI, and VIII) lacking nitroso groups, either had no effect or produced mild decreases in guanylate cyclase activity.
链脲佐菌素是一种亚硝基酰胺类致癌物，可增强鸟苷酸环化酶的活性。为了阐明与鸟苷酸环化酶激活相关的关键构效关系，对链脲佐菌素的六种类似物进行了研究。类似物1，即氯脲霉素，含有一个亚硝基，可使鸟苷酸环化酶活性提高17至28倍。类似物III也含有一个亚硝基，但结构修饰更大，有4个乙酸基团从葡萄糖部分伸出，可激活结肠中的鸟苷酸环化酶，但对肾脏无此作用。其他缺乏亚硝基的类似物（II、IV、VI和VIII）要么没有影响，要么使鸟苷酸环化酶活性略有降低。
