Structure-relaxivity relationships of serum albumin targeted MRI probes based on a single amino acid Gd complex.

Structure-relaxivity relationships of serum albumin targeted MRI probes based on a single amino acid Gd complex.
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DOI:
10.1021/jm4000177
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发表时间:
2013-02-28
影响因子:
7.3
通讯作者:
Caravan, Peter
Caravan, Peter
中科院分区:
医学1区
文献类型:
--
作者:
Boros, Eszter;Caravan, Peter

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DO3A-N-α-氨基丙酸的 Gd(III) 复合物 Gd(DOTAla) 用于生成针对人血清白蛋白 (HSA) 的假定 MRI 探针小型文库。通过多步有机合成合成了十种化合物,并研究了相应的 Gd 配合物在 HSA 不存在和存在下对 HSA 的亲和力、亲脂性和弛豫性。负电荷和中等亲脂性与 HSA 亲和力和弛豫性增加相关。
The Gd(III) complex of DO3A-N-α-amino-propionate, Gd(DOTAla), was used to generate a small library of putative MRI probes targeted to human serum albumin (HSA). Ten compounds were synthesized via multistep organic synthesis and the corresponding Gd complexes were investigated for their affinity to HSA, lipophilicity, and relaxivity in the absence and presence of HSA. Negative charge and moderate lipophilicity correlate with increased HSA affinity and relaxivity.
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