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Studies in Drug Albumin binding using HSA and RSA affinity methods

Reilly, John and Etheridge, Donnya and Porter, David and Springer, Clayton and Fairhurst, Robin and Everatt, Brian and Jiang, Zhengjin and Aldcroft, Clive and Wright, Penny and Clemens, Ian and Cox, Brian and Press, Neil and Watson, Simon (2010) Studies in Drug Albumin binding using HSA and RSA affinity methods. Journal of Liquid Chromatography and Related Technologies, 34 (4). pp. 317-327. ISSN 1082-6076

Abstract

A HPLC gradient methodology using an immobilised human serum albumin (HSA) and rat serum albumin (RSA) has been used as a tool to investigate the protein binding trends of novel discovery compounds. These methods have been set up to support a high throughput approach and have been shown to be complimentary to one another. Significant binding differences have been observed with some compounds when both methods have been employed. Discovery chemists are now also able to rank order molecules using these quick “trend analysis” albumin binding screens by submitting a 20l sub sample from the 10mM stock solution from the in-house compound archive. Additionally, chemists have the opportunity to predict trends in albumin binding by use of an internal QSAR model based upon a diverse 1200 compound result set, which had been previously analysed with the HSA methodology.

Keywords: Rat serum albumin; Human serum albumin; High performance liquid chromatography; Gradient; Plasma protein binding

Item Type: Article
Keywords: Rat serum albumin; Human serum albumin; High performance liquid chromatography; Gradient; Plasma protein binding
Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/3793

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