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首页> 外文期刊>Chemistry: A European journal >A Pyrazolato-Bridged Dinuclear Platinum(II)Complex Induces Only Minor Distortions upon DNA-Binding
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A Pyrazolato-Bridged Dinuclear Platinum(II)Complex Induces Only Minor Distortions upon DNA-Binding

机译：Pyrazolato桥连双核铂（II）复合物仅在DNA结合时引起较小的扭曲。

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摘要

The cytotoxic,pyrazolato-bridged dinuclear platinum(II)complex [(cis-(Pt(NH_3)_2})_2(mu-OH)(mu-pz)]~(2+)(pz=pyrazolate)has been found to cross-link two adjacent guanines of a double-stranded DNA decamer without destabilizing the duplex and without changing the directionality of the helix axis.A ~1H NMR study of the oligonucleotide d(CTCTG*G*TCTC)-d(GAGACCAGAG),cross-linked at the two G* guanines by [(cis-{Pt-(NH_3)_2})_2(mu-pz)]~(3+),and molecular dynamics simulations of the explicitly solvated duplex were performed to characterize the structural details of the adduct.The dinuclear platinum crosslink unwinds the helix by approximately 15 deg,that is,to a similar extent as the widely used antitumor drug cisplatin,but,in contrast to the latter,induces no significant bend in the helix axis.The Watson-Crick base-pairing remains intact,and the melting temperature of the duplex is unaffected by the crosslink.The helical twist is considerably reduced between the two platinated bases,as becomes manifest in an unusually short sequential H1'-H1'distance.This unwinding also affects the sugar ring of the guanosine in the 3'-position to the cross-link,which presents an N-><-S equilibrium.This is the first cytotoxic platinum complex that has been successfully designed by envisioning the structural consequences of its binding to DNA.
机译：发现具有细胞毒性的吡唑并桥联的双核铂（II）络合物[（顺式-（Pt（NH_3）_2}）_ 2（mu-OH）（mu-pz）]〜（2 +）（pz =吡唑酸盐）交联双链DNA decamer的两个相邻鸟嘌呤而不破坏双链体的稳定性并且不改变螺旋轴的方向性。寡核苷酸d（CTCTG * G * TCTC）-d（GAGACCAGAG）的〜1H NMR研究[[cis- {Pt-（NH_3）_2}）_ 2（mu-pz）]〜（3+）连接在两个G *鸟嘌呤上，并对明确溶剂化的双链体进行了分子动力学模拟，以表征结构双核铂交联键使螺旋线解开约15度，即与广泛使用的抗肿瘤药物顺铂相似的程度，但与后者相反，在螺旋线轴上未引起明显弯曲。 Watson-Crick碱基配对保持完整，并且双链体的熔融温度不受交联的影响。随着温度的升高，两个镀铂碱基之间的螺旋扭曲大大降低。 s表现为异常短的连续H1'-H1'距离。这种解开也影响鸟苷在交联键3'位置的糖环，呈现N-> <-S平衡。第一个具有细胞毒性的铂复合物，已通过设想其与DNA结合的结构后果而成功设计。

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