Rothbard Jonathan B, Jones Lisa R
Division of Rheumatology, Department of Medicine, Stanford University School of Medicine, Stanford, CA, USA.
Methods Mol Biol. 2011;683:487-504. doi: 10.1007/978-1-60761-919-2_35.
A major challenge confronting the further advancement of using molecular transporters conjugated to small molecular weight therapeutics in the clinic is the development of linkers that would allow for the controllable release of a free drug/probe only after cell entry. Development of assays that would allow for the rapid real-time quantification of transporter conjugate uptake and cargo release in cells and animals would greatly help in their development. In this chapter, we describe a imaging method that quantitatively measures transporter conjugate uptake and cargo release in real-time in both cell culture and animal models.
在临床上进一步推进将分子转运体与小分子量治疗药物偶联使用面临的一个主要挑战是开发连接子，该连接子要能使游离药物/探针仅在进入细胞后才可控释放。开发能够快速实时定量细胞和动物中转运体偶联物摄取及货物释放的检测方法将极大地有助于其研发。在本章中，我们描述了一种成像方法，可在细胞培养和动物模型中实时定量测量转运体偶联物的摄取及货物释放。
