Targeting VEGF receptors with non-neutralizing cyclopeptides for imaging applications
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Published on: June 11, 2020
Luisa Calvanese1, Andrea Caporale1,2, Giuseppina Focà2
1Istituto di Biostrutture e Bioimmagini del CNR, CIRPeB, University of Naples Federico II, via Mezzocannone, 16, 80134, Naples, Italy.
Abstract:
Pharmacological strategies aimed at preventing cancer growth are in most cases paralleled by diagnostic investigations for monitoring and prognosticating therapeutic efficacy. A relevant approach in cancer is the suppression of pathological angiogenesis, which is principally driven by vascular endothelial growth factor (VEGF) or closely related factors and by activation of specific receptors, prevailingly VEGFR1 and VEGFR2, set on the surface of endothelial cells. Monitoring the presence of these receptors in vivo is henceforth a way to predict therapy outcome. We have designed small peptides able to bind and possibly antagonize VEGF ligands by targeting VEGF receptors. Peptide systems have been designed to be small, cyclic and to host triplets of residues known to be essential for VEGF receptors recognition and we named them 'mini-factors'. They have been structurally characterized by CD, NMR and molecular dynamics (MD) simulations. Mini-factors do bind with different specificity and affinity VEGF receptors but none blocks receptor activity. Following derivatization with suitable tracers they have been employed as molecular probes for sensing receptors on cell surface without affecting their activity as is usually observed with other binders having neutralizing activity.
Insights
Researchers developed
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Cancer treatment efficacy is monitored using diagnostic tools.
- Pathological angiogenesis, driven by vascular endothelial growth factor (VEGF) and its receptors (VEGFR1/VEGFR2), is a key target in cancer therapy.
- In vivo monitoring of VEGF receptors can predict therapeutic outcomes.
Purpose of the Study:
- To design and characterize novel small peptides, termed 'mini-factors', capable of binding to VEGF receptors.
- To investigate the potential of these mini-factors as molecular probes for sensing VEGF receptors on cell surfaces without inhibiting their activity.
Main Methods:
- Design of small, cyclic peptides incorporating essential residues for VEGF receptor recognition.
- Structural characterization using Circular Dichroism (CD), Nuclear Magnetic Resonance (NMR), and Molecular Dynamics (MD) simulations.
- Assessment of mini-factor binding affinity and specificity to VEGF receptors.
- Derivatization of mini-factors with tracers for use as molecular probes.
Main Results:
- Mini-factors were successfully designed and structurally characterized.
- These mini-factors exhibit varying degrees of specificity and affinity for VEGF receptors.
- Crucially, none of the designed mini-factors blocked VEGF receptor activity.
- Derivatized mini-factors function as effective molecular probes for sensing cell-surface receptors without altering their biological function.
Conclusions:
- Mini-factors represent a novel class of small peptides targeting VEGF receptors.
- They serve as valuable molecular probes for non-inhibitory sensing of VEGF receptors in cancer diagnostics.
- This approach offers a new avenue for monitoring therapeutic efficacy in angiogenesis-targeted cancer treatments.
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