التفاصيل البيبلوغرافية
| العنوان: |
Solid-Supported Membrane (SSM)-Based Electrophysiology Assays Using Surface Electrogenic Event Reader Technology (SURFE2R) in Early Drug Discovery |
| المؤلفون: |
Pommereau, Antje, Licher, Thomas, Bärenz, Felix |
| المصدر: |
Current Protocols, Volume 3, e650, (2023-03-13) |
| بيانات النشر: |
Wiley Periodicals LLC |
| سنة النشر: |
2023 |
| المجموعة: |
Zenodo |
| الوصف: |
This article presents detailed descriptions of procedures and troubleshootingtips for solid-supported membrane (SSM)-based electrophysiology assays (SURFE2R) to measure electrogenic solute carrier transporter proteins (SLCs)and assess the effects of compounds that modulate their activity. SURFE2R allows the use of the standard 96-well format, making it an ideal platform for tertiaryassays in a drug-discovery campaign. The assays are performed with cellline- derived membrane fractions or proteoliposomes containing the transporterof interest. Three main protocols are described for the isolation of membrane fractions from cell culture and the generation of proteoliposomes containingthe transporter of interest. Additionally, detailed protocols for SURFE2R single concentration and dose-response experiments are included to measure thepotencies of test compounds in stimulating or inhibiting transporter function (EC50 or IC50 values, respectively) and kinetic functional assays to calculateapparent affinity (kM) and maximal velocity (Vmax) of substrate uptake. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| Relation: |
https://doi.org/10.1002/cpz1.650; https://zenodo.org/communities/resolute; oai:zenodo.org:11085498 |
| DOI: |
10.1002/cpz1.650 |
| الاتاحة: |
https://doi.org/10.1002/cpz1.650 |
| Rights: |
info:eu-repo/semantics/openAccess ; Creative Commons Attribution Non Commercial No Derivatives 4.0 International ; https://creativecommons.org/licenses/by-nc-nd/4.0/legalcode |
| رقم الانضمام: |
edsbas.2C15A4B4 |
| قاعدة البيانات: |
BASE |