首页>
外国专利>
Palladium complexes inhibit N-myristoyltransferase activity in vitro and cancer growth in vivo
Palladium complexes inhibit N-myristoyltransferase activity in vitro and cancer growth in vivo
展开▼
机译:钯配合物在体外抑制N-肉豆蔻酰转移酶活性并在体内抑制癌症生长
展开▼
页面导航
摘要
著录项
相似文献
摘要
Melanoma is a solid tumor that is notoriously resistant to chemotherapy, and its incidence is rapidly increasing. Recently, several signaling pathways have been demonstrated to contribute to melanoma tumorigenesis, including constitutive activation of MAP kinase, Akt and stat-3. The activation of multiple pathways may account in part for the difficulty in treatment of melanoma. In a recent screen of compounds, we found that an organopalladium complex showed significant antiproliferative activity against melanoma cells. This complex, tris(dibenzylideneacetone)dipalladium (Tris DBA), has activity against B16 murine and A375 human melanoma in vivo. Tris DBA inhibits several signaling pathways including activation of MAP kinase, Akt, stat-3 and S6 kinase activation. Tris(dibenzylideneacetone)dipalladium is thus a novel compound that is a member of a class of noble metal complexes with potential antitumor activity. Further preclinical evaluation of TrisDBA and related complexes is warranted.
展开▼
机译:黑色素瘤是众所周知对化学疗法有抗性的实体瘤,并且其发病率正在迅速增加。最近,已证明了几种信号通路可促进黑色素瘤的发生,包括MAP激酶,Akt和stat-3的组成性激活。多种途径的激活可能部分解释了黑素瘤治疗的困难。在最近的化合物筛选中,我们发现有机钯配合物对黑色素瘤细胞显示出显着的抗增殖活性。这种复合物,三(二亚苄基丙酮)二钯(Tris DBA),在体内对B16鼠和A375人黑素瘤具有活性。 Tris DBA抑制了几种信号传导途径,包括MAP激酶激活,Akt,stat-3和S6激酶激活。因此,三(二亚苄基丙酮)二钯是一种新型化合物,是具有潜在抗肿瘤活性的一类贵金属配合物的成员。有必要对TrisDBA及其相关复合物进行进一步的临床前评估。
展开▼