Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases
In the past decade, surface plasmon resonance (SPR) biosensor-based technology has been exploited more and more to characterize the interaction between drug targets and small-molecule modulators. Here, we report the successful application of SPR methodology for the analysis of small-molecule binding to two therapeutically relevant cAMP phosphodiesterases (PDEs), Trypanosoma brucei PDEB1 which is implicated in African sleeping sickness and human PDE4D which is implicated in a plethora of disease conditions including inflammatory pulmonary disorders such as asthma, chronic obstructive pulmonary disease and central nervous system (CNS) disorders. A protocol combining the use of directed capture using His-tagged PDE_CDs with covalent attachment to the SPR surface was developed. This methodology allows the determination of the binding kinetics of small-molecule PDE inhibitors and also allows testing their specificity for the two PDEs. The SPR-based assay could serve as a technology platform for the development of highly specific and high-affinity PDE inhibitors, accelerating drug discovery processes..
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2016 |
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| Erschienen: |
2016 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:503 |
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| Enthalten in: |
Analytical biochemistry - 503(2016), Seite 41-49 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Siderius, Marco [VerfasserIn] |
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| Links: |
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| doi: |
10.1016/j.ab.2016.03.013 |
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| 520 | |a In the past decade, surface plasmon resonance (SPR) biosensor-based technology has been exploited more and more to characterize the interaction between drug targets and small-molecule modulators. Here, we report the successful application of SPR methodology for the analysis of small-molecule binding to two therapeutically relevant cAMP phosphodiesterases (PDEs), Trypanosoma brucei PDEB1 which is implicated in African sleeping sickness and human PDE4D which is implicated in a plethora of disease conditions including inflammatory pulmonary disorders such as asthma, chronic obstructive pulmonary disease and central nervous system (CNS) disorders. A protocol combining the use of directed capture using His-tagged PDE_CDs with covalent attachment to the SPR surface was developed. This methodology allows the determination of the binding kinetics of small-molecule PDE inhibitors and also allows testing their specificity for the two PDEs. The SPR-based assay could serve as a technology platform for the development of highly specific and high-affinity PDE inhibitors, accelerating drug discovery processes. | ||
| 540 | |a Nutzungsrecht: © Elsevier Inc. | ||
| 540 | |a Copyright © 2016 Elsevier Inc. All rights reserved. | ||
| 700 | 1 | |a Shanmugham, Anitha |4 oth | |
| 700 | 1 | |a England, Paul |4 oth | |
| 700 | 1 | |a van der Meer, Tiffany |4 oth | |
| 700 | 1 | |a Bebelman, Jan Paul |4 oth | |
| 700 | 1 | |a Blaazer, Antoni R |4 oth | |
| 700 | 1 | |a de Esch, Iwan J.P |4 oth | |
| 700 | 1 | |a Leurs, Rob |4 oth | |
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| 856 | 4 | 2 | |u http://www.sciencedirect.com/science/article/pii/S0003269716001135 |
| 856 | 4 | 2 | |u http://www.ncbi.nlm.nih.gov/pubmed/27033007 |
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