Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases
Copyright © 2016 Elsevier Inc. All rights reserved..
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: |
E-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) vom: 15. Juni, Seite 41-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Siderius, Marco [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 04.05.2017 Date Revised 06.02.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ab.2016.03.013 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright © 2016 Elsevier Inc. All rights reserved. | ||
| 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a African sleeping disease | |
| 650 | 4 | |a Phosphodiesterase | |
| 650 | 4 | |a Small molecules | |
| 650 | 4 | |a Surface plasmon resonance | |
| 650 | 4 | |a Trypanosoma brucei | |
| 650 | 7 | |a Phosphodiesterase Inhibitors |2 NLM | |
| 650 | 7 | |a Protozoan Proteins |2 NLM | |
| 650 | 7 | |a Small Molecule Libraries |2 NLM | |
| 650 | 7 | |a 3',5'-Cyclic-AMP Phosphodiesterases |2 NLM | |
| 650 | 7 | |a EC 3.1.4.17 |2 NLM | |
| 650 | 7 | |a Cyclic Nucleotide Phosphodiesterases, Type 4 |2 NLM | |
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| 650 | 7 | |a PDE4D protein, human |2 NLM | |
| 650 | 7 | |a EC 3.1.4.17 |2 NLM | |
| 650 | 7 | |a PDEB1 protein, Trypanosoma brucei |2 NLM | |
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| 700 | 1 | |a Shanmugham, Anitha |e verfasserin |4 aut | |
| 700 | 1 | |a England, Paul |e verfasserin |4 aut | |
| 700 | 1 | |a van der Meer, Tiffany |e verfasserin |4 aut | |
| 700 | 1 | |a Bebelman, Jan Paul |e verfasserin |4 aut | |
| 700 | 1 | |a Blaazer, Antoni R |e verfasserin |4 aut | |
| 700 | 1 | |a de Esch, Iwan J P |e verfasserin |4 aut | |
| 700 | 1 | |a Leurs, Rob |e verfasserin |4 aut | |
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