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http://hdl.handle.net/2445/184996
Title: | Proteomic tools for the quantitative analysis of artificial peptide libraries: detection and characterization of target-amplified PD-1 inhibitors |
Author: | Gay i Marín, Marina Díaz Lobo, Mireia Gusi Vives, Mar Arauz-Garofalo, Gianluca Vilanova, Mar Giralt Lledó, Ernest Vilaseca Casas, Marta Guardiola Bagán, Salvador |
Keywords: | Proteòmica Termodinàmica Proteomics Thermodynamics |
Issue Date: | 1-Apr-2022 |
Publisher: | Wiley-VCH |
Abstract: | We report a quantitative proteomics data analysis pipeline which, coupled to protein-directed dynamic combinatorial chemistry (DDC) experiments, enables the rapid discovery and direct characterization of protein-protein interaction (PPI) modulators. A low-affinity PD-1 binder was incubated with a library of >100 D-peptides under thiol-exchange favoring conditions, in the presence of the target protein PD-1, and we determined the S-linked dimeric species that resulted amplified in the protein samples versus the controls. We chemically synthesized the target dimer candidates and validated them by thermophoresis binding and protein-protein interaction assays. The results provide a proof-of-concept for using this strategy in the high-throughput search of improved drug-like peptide binders that block therapeutically relevant protein-protein interactions. |
Note: | Versió postprint del document publicat a: https://doi.org/10.1002/cbic.202200152 |
It is part of: | ChemBioChem, 2022 |
URI: | http://hdl.handle.net/2445/184996 |
Related resource: | https://doi.org/10.1002/cbic.202200152 |
ISSN: | 1439-7633 |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona)) |
Files in This Item:
File | Description | Size | Format | |
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ChemBioChem_Guardiola_2022.pdf | 1.27 MB | Adobe PDF | View/Open |
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