Kelety Bela, Diekert Kerstin, Tobien Joanna, Watzke Natalie, Dörner Wolfgang, Obrdlik Petr, Fendler Klaus
IonGate Biosciences, Frankfurt, Germany.
Assay Drug Dev Technol. 2006 Oct;4(5):575-82. doi: 10.1089/adt.2006.4.575.
Transporters are important targets in drug discovery. However, high throughput-capable assays for this class of membrane proteins are still missing. Here we present a novel drug discovery platform technology based on solid supported membranes. The functional principles of the technology are described, and a sample selection of transporter assays is discussed: the H(+)-dependent peptide transporter PepT1, the gastric proton pump, and the Na(+)/Ca(2+) exchanger. This technology promises to have an important impact on the drug discovery process.
转运蛋白是药物研发中的重要靶点。然而,针对这类膜蛋白的高通量检测方法仍然缺失。在此,我们提出一种基于固体支持膜的新型药物研发平台技术。描述了该技术的功能原理,并讨论了转运蛋白检测的样本选择:H⁺依赖性肽转运体PepT1、胃质子泵和Na⁺/Ca²⁺交换器。这项技术有望对药物研发过程产生重要影响。