De Haen Replies

HAEN, PAUL de

doi:10.1177/106002807500901208

Cited by 1 publication

(2 citation statements)

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“…For example, the Gd-DTPA based agents B22956/1, which has been extensively evaluated as an angiographic contrast agent, utilizes 3-deoxycholic acid as an albumin targeting group. [23][24][25][26][479][480][481][482] A biological function of serum albumin is to transport lipopilic anions. The high concentration of serum albumin and its ability to promiscuously binding many classes of compounds makes it possible to generate a large number of albumin-targeted agents.…”

Section: Serum Albuminmentioning

confidence: 99%

“…OATP mediated internalization has been utilized to develop liver targeting agents such as the commercially available Gd-BOPTA and Gd-EOB-DTPA. [521][522][523] Although these clinical agents are not typically thought of as biochemically-targeted contrast agents, the strong liver contrast observed following injection is the result of receptor mediated pooling of the agent in hepatocytes. OATPs are highly abundant on the surface of normal hepatocytes but are under-expressed on the surface of malignant cells and thus OATPtargeted agents are used to render malignant hepatocellular lesions conspicuously hypointense relative to healthy liver parenchyma.…”

Section: Organic Anion Transporting Peptidesmentioning

confidence: 99%

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Chemistry of MRI Contrast Agents: Current Challenges and New Frontiers

et al. 2018

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Tens of millions of contrast enhanced magnetic resonance imaging (MRI) exams are performed annually around the world. The contrast agents, which improve diagnostic accuracy, are almost exclusively small, hydrophilic gadolinium(III) based chelates. In recent years concerns have arisen surrounding the long term safety of these compounds, and this has spurred research into alternatives. There has also been a push to develop new molecularly targeted contrast agents or agents that can sense pathological changes in the local environment. This comprehensive review describes the state of the art of clinically approved contrast agents, their mechanism of action, and factors influencing their safety. From there we describe different mechanisms of generating MR image contrast such as relaxation, chemical exchange saturation transfer, and direct detection and the types of molecules that are effective for these purposes. Next we describe efforts to make safer contrast agents either by increasing relaxivity, increasing resistance to metal ion release, or by moving to gadolinium(III)-free alternatives. Finally we survey approaches to make contrast agents more specific for pathology either by direct biochemical targeting or by the design of responsive or activatable contrast agents.

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