鸟嘌呤
嘌呤核苷磷酸化酶
鸟苷
生物化学
化学
鸟苷酸激酶
肉瘤
基质(水族馆)
嘌呤
激酶
次黄嘌呤
脱氧鸟苷
核苷
酶
生物
DNA
核苷酸
医学
病理
生态学
膜蛋白
膜
基因
作者
Albert Ross,Khushboo Agarwal,Shih‐Hsi Chu,Robert E. Parks
标识
DOI:10.1016/0006-2952(73)90268-2
摘要
Survival studies were performed in mice bearing Sarcoma 180 ascites tumor treated with 6-thio and 6-seleno analogs of guanine and guanosine. The selenium-containing analogs were somewhat superior to the sulfur-containing compounds in antitumor activity and therapeutic index. The formation of 6-SeGMP from 6-seleno-guanine (6-SeG) was demonstrated in Sarcoma 180 ascites cells. Guanine, 6-thioguanine (6-TG) and 6-SeG show comparable substrate activity whereas 8-azaguanine is a much poorer substrate for hypoxanthine-guanine phosphoribosyl transferase from Sarcoma 180 cells. Both 6-TG and 6-SeG are good substrates for purine nucleoside phosphorylase from Sarcoma 180 cells. Chemically and enzymatically synthesized 6-SeGMP behaved as a competitive inhibitor (Ki 1 × 10−4 M) of erythrocytic and Sarcoma 180 guanylate kinases. Weak substrate activity was demonstrated in the presence of large amounts of erythrocytic guanylate kinase.
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