Nivorozhkin Alexander L, Kolodziej Andrew F, Caravan Peter, Greenfield Matthew T, Lauffer Randall B, McMurry Thomas J
EPIX Medical, Inc. 71 Rogers Street Cambridge, MA 02142 (USA) Fax: (+1) 617-250-6128.
Angew Chem Int Ed Engl. 2001 Aug 3;40(15):2903-2906. doi: 10.1002/1521-3773(20010803)40:15<2903::AID-ANIE2903>3.0.CO;2-N.
Clinically relevant relaxivity enhancement of a magnetic resonance imaging (MRI) contrast agent has been achieved by using prodrug Gd complexes (see picture, DTPA=diethylenetriaminepentaaceto). Enzymatic cleavage of lysine residues from the prodrug exposes a group that has a high affinity to human serum albumin and promotes enhanced relaxivity, thus enabling the detection of targets at submicromolar concentrations.
通过使用前药钆配合物，实现了磁共振成像（MRI）造影剂与临床相关的弛豫率增强（见图，DTPA = 二乙三胺五乙酸）。前药中赖氨酸残基的酶促裂解暴露出一个对人血清白蛋白具有高亲和力的基团，并促进弛豫率增强，从而能够在亚微摩尔浓度下检测目标。
