2,2'-联吡啶-6-碳硫酰胺的抗肿瘤活性：一种核糖核苷酸还原酶抑制剂
Antitumor activity of 2,2'-bipyridyl-6-carbothioamide: a ribonucleotide reductase inhibitor.
作者信息
Nocentini G, Barzi A
机构信息
Department of Clinical Medicine, Pathology and Pharmacology, University of Perugia, Italy.
出版信息
Gen Pharmacol. 1997 Nov;29(5):701-6. doi: 10.1016/s0306-3623(97)00011-6.
PMID:9347313
Abstract
- 2,2'-Bipyridyl-6-carbothioamide (BPYTA) is a synthesized compound with chelating properties demonstrating in vitro and in vivo antitumor activity. 2. The BPYTA cytotoxic effect is mainly due to the inhibition of ribonucleotide reductase (RR), a key enzyme in proliferating cells. The active form of BPYTA is its iron chelate [BPYTA-Fe(II), molar ratio 2:1], which destroys the tyrosyl radical of RR small subunit (R2). 3. The copper chelate of BPYTA [BPYTA-Cu(II), molar ratio 2:1] also has antiproliferative activity, but RR is not the only intracellular target. 4. BPYTA potently synergizes in vitro with hydroxyurea, the most widely used R2 inhibitor.
摘要
- 2,2'-联吡啶-6-碳硫酰胺（BPYTA）是一种合成化合物，具有螯合特性，在体外和体内均表现出抗肿瘤活性。2. BPYTA的细胞毒性作用主要归因于对核糖核苷酸还原酶（RR）的抑制，RR是增殖细胞中的关键酶。BPYTA的活性形式是其铁螯合物[BPYTA-Fe(II)，摩尔比2:1]，它会破坏RR小亚基（R2）的酪氨酰自由基。3. BPYTA的铜螯合物[BPYTA-Cu(II)，摩尔比2:1]也具有抗增殖活性，但RR不是唯一的细胞内靶点。4. BPYTA在体外与最广泛使用的R2抑制剂羟基脲具有强大的协同作用。
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