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Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches

Authorized Users Only
2019
Authors
Albert, Lea
Penalver, Alberto
Đoković, Nemanja
Werel, Laura
Hoffarth, Malte
Ružić, Dušan
Xu, Jing
Essen, Lars-Oliver
Nikolić, Katarina
Dou, Yali
Vazquez, Olalla
Article (Published version)
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Abstract
Life relies on a myriad of carefully orchestrated processes, in which proteins and their direct interplay ultimately determine cellular function and disease. Modulation of this complex crosstalk has recently attracted attention, even as a novel therapeutic strategy. Herein, we describe the synthesis and characterization of two visible-light-responsive peptide backbone photoswitches based on azobenzene derivatives, to exert optical control over protein-protein interactions (PPI). The novel peptidomimetics undergo fast and reversible isomerization with low photochemical fatigue under alternatively blue-/green-light irradiation cycles. Both bind in the nanomolar range to the protein of interest. Importantly, the best peptidomimetic displays a clear difference between isomers in its protein-binding capacity and, in turn, in its potential to inhibit enzymatic activity through PPI disruption. In addition, crystal structure determination, docking and molecular dynamics calculations allow a mo...lecular interpretation and open up new avenues in the design and synthesis of future photoswitchable PPI modulators.

Keywords:
azobenzenes / isomerization / peptidomimetics / photochemistry / protein-protein interactions
Source:
Chembiochem, 2019, 20, 11, 1417-1429
Publisher:
  • Wiley-VCH Verlag GMBH, Weinheim
Projects:
  • Modeling and Numerical Simulations of Complex Many-Body Systems (RS-171017)

DOI: 10.1002/cbic.201800737

ISSN: 1439-4227

PubMed: 30675988

WoS: 000474071700012

Scopus: 2-s2.0-85065047737
[ Google Scholar ]
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URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/3258
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  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy

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