A multisample assay for inhibitors of phosphatidylinositol phospholipase C: identification of naturally occurring peptide inhibitors with antiproliferative activity.
A multisample assay for inhibitors of phosphatidylinositol phospholipase C: identification of naturally occurring peptide inhibitors with antiproliferative activity.
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发表时间：
1994-08
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通讯作者：
Hill;R. Bonjouklian;Garth Powis;Abraham Rt;Ashendel Cl;Zalkow Lh
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作者：
Hill;R. Bonjouklian;Garth Powis;Abraham Rt;Ashendel Cl;Zalkow Lh
本文报道了一种简便、可靠的筛选生长因子信号酶磷脂酰肌醇特异性磷脂酶C（PtdInsPLC）抑制剂的多样品分析方法。已鉴定出三种天然存在的PtdInsPLC肽抑制剂，myroridin K、链丝菌素B和依地因，IC 50值分别为8.3、6.7和16.1 μ M。所有三种肽均抑制HT-29人结肠腺癌细胞的集落形成，IC 50值分别为7.2、3.9和13.0 μ M。这些化合物还抑制了培养物中其他人类癌细胞的生长。其中一种肽，myroridin K，先前已报道具有体内抗肿瘤活性。PtdInsPLC的抑制可能是肽化合物的细胞生长抑制和抗肿瘤性质的原因。
A convenient and reliable multisample assay for the screening of inhibitors of the growth factor signalling enzyme phosphatidylinositol specific phospholipase C (PtdInsPLC) has been developed. Three naturally occurring peptide inhibitors of PtdInsPLC have been identified, myroridin K, streptothricin B and edeine, with IC50 values of 8.3, 6.7 and 16.1 microM, respectively. All three peptides inhibited colony formation of HT-29 human colon adenocarcinoma cells, with IC50 values of 7.2, 3.9 and 13.0 microM, respectively. The compounds also inhibited the growth of other human cancer cells in culture. One of the peptides, myroridin K, has previously been reported to have in vivo antitumour activity. It is possible that inhibition of PtdInsPLC is responsible for the cell growth inhibition and antitumour properties of the peptide compounds.