The Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, 149 Thirteenth Street, Suite 2301, Charlestown, Massachusetts 02129, United States.
J Med Chem. 2013 Feb 28;56(4):1782-6. doi: 10.1021/jm4000177. Epub 2013 Feb 19.
The Gd(III) complex of DO3A-N-α-aminopropionate, 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.
以 DO3A-N-α-氨基丙酸盐(DOTAla)为配体的 Gd(III) 配合物(Gd(DOTAla))被用来生成针对人血清白蛋白(HSA)的假定 MRI 探针的小分子文库。通过多步有机合成合成了 10 种化合物,并研究了它们与 HSA 的亲和力、亲脂性以及在不存在和存在 HSA 时的弛豫率。带负电荷和适度的亲脂性与 HSA 亲和力和弛豫率的提高相关。