Abstract
The transition from high throughput screening of collections of drug-like compounds to screening of fragment libraries via lower throughput methods with high sensitivity has revolutionized early drug discovery. It is highlighting the need for sensitive biophysical techniques for interaction analysis rather than high throughput methods. Biosensors with SPR detection are well suited for this novel scenario. In less than 20 years the technique has been launched, established and become a highly informative method for a variety of applications in drug discovery. It is no longer limited to the detection of proteins or other high molecular weight analytes, but the detection of weakly interacting fragments is now feasible. This paper discusses the theoretical and experimental limitations for such applications and reviews a number of successful studies in the area of fragment-based lead discovery that have recently been published. It can be anticipated that the evolution of this young technique will be significantly influenced by the requirements for efficient fragment-based lead discovery.
Keywords: SPR, biosensor, fragment-based lead discovery, interactions, kinetics, affinity, screening
Current Topics in Medicinal Chemistry
Title: Fragment Library Screening and Lead Characterization Using SPR Biosensors
Volume: 9 Issue: 18
Author(s): U. Helena Danielson
Affiliation:
Keywords: SPR, biosensor, fragment-based lead discovery, interactions, kinetics, affinity, screening
Abstract: The transition from high throughput screening of collections of drug-like compounds to screening of fragment libraries via lower throughput methods with high sensitivity has revolutionized early drug discovery. It is highlighting the need for sensitive biophysical techniques for interaction analysis rather than high throughput methods. Biosensors with SPR detection are well suited for this novel scenario. In less than 20 years the technique has been launched, established and become a highly informative method for a variety of applications in drug discovery. It is no longer limited to the detection of proteins or other high molecular weight analytes, but the detection of weakly interacting fragments is now feasible. This paper discusses the theoretical and experimental limitations for such applications and reviews a number of successful studies in the area of fragment-based lead discovery that have recently been published. It can be anticipated that the evolution of this young technique will be significantly influenced by the requirements for efficient fragment-based lead discovery.
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Cite this article as:
Danielson Helena U., Fragment Library Screening and Lead Characterization Using SPR Biosensors, Current Topics in Medicinal Chemistry 2009; 9 (18) . https://dx.doi.org/10.2174/156802609790102392
DOI https://dx.doi.org/10.2174/156802609790102392 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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