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Studies in drug albumin binding using HSA and RSA affinity methods

journal contribution
posted on 2023-06-08, 19:29 authored by John Reilly, Donnya Etheridge, Brian Everatt, Zhengjin Jiang, Clive Aldcroft, Penny Wright, Ian Clemens, Brian Cox, Neil J Press, Simon Watson, David Porter, Clayton Springer, Robin A Fairhurst
A HPLC gradient methodology using immobilized 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 complementary 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 µl sample from the 10 mM stock solution from the inhouse 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 analyzed with the HSA methodology.

History

Publication status

  • Published

Journal

Journal of Liquid Chromatography and Related Technologies

ISSN

1082-6076

Publisher

Taylor & Francis

Issue

4

Volume

34

Page range

317-327

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-12

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