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Pharmaceuticals
Volume 17
Issue 2
10.3390/ph17020190
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Article

Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1

by
Bartłomiej Fedorczyk
1,
Patrycja Redkiewicz
2,
Joanna Matalińska
2,
Radosław Piast
1,
Piotr Kosson
2 and
Rafał Wieczorek
1,*
1
Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland
2
Mossakowski Medical Research Centre Polish Academy of Science, 5 Pawinskiego Street, 02-106 Warsaw, Poland
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2024, 17(2), 190; https://doi.org/10.3390/ph17020190
Submission received: 27 November 2023 / Revised: 19 January 2024 / Accepted: 19 January 2024 / Published: 31 January 2024
(This article belongs to the Special Issue Vascular Endothelial Growth Factor (VEGF) and VEGF Receptor Inhibitors in Health and Disease)
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Abstract

The interaction of Neuropilin-1 (NRP-1) with vascular endothelial growth factor (VEGF) has been shown to promote angiogenesis under physiological and pathological conditions. Angiogenesis around tumors is a major factor allowing for their growth and spread. Disrupting NRP-1/VEGF complex formation is thus a promising pathway for the development of new anticancer pharmaceuticals. A large body of work has been produced in the last two decades detailing the development of inhibitors of NRP-1/VEGF complex formation. Among those were peptide A7R and its smaller derivatives KXXR and K(Har)XXR. It has been previously reported that replacement of the XX backbone with triazole residues has a positive effect on the proteolytic stability of inhibitors. It has also been reported that a higher dihedral angle range restriction of the XX backbone has a positive effect on the activity of inhibitors. In this work, we have designed new triazole derivatives of K(Har)XXR inhibitors with substitution allowing for higher range restriction of the XX backbone. The obtained peptidomimetics have greater activity than their less restricted counterparts. One of the newly obtained structures has greater affinity than the reference peptide A7R.
Keywords: VEGF-165; neuropilin-1; peptidomimetics; triazole; structure–activity relationship VEGF-165; neuropilin-1; peptidomimetics; triazole; structure–activity relationship

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MDPI and ACS Style

Fedorczyk, B.; Redkiewicz, P.; Matalińska, J.; Piast, R.; Kosson, P.; Wieczorek, R. Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1. Pharmaceuticals 2024, 17, 190. https://doi.org/10.3390/ph17020190

AMA Style

Fedorczyk B, Redkiewicz P, Matalińska J, Piast R, Kosson P, Wieczorek R. Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1. Pharmaceuticals. 2024; 17(2):190. https://doi.org/10.3390/ph17020190

Chicago/Turabian Style

Fedorczyk, Bartłomiej, Patrycja Redkiewicz, Joanna Matalińska, Radosław Piast, Piotr Kosson, and Rafał Wieczorek. 2024. "Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1" Pharmaceuticals 17, no. 2: 190. https://doi.org/10.3390/ph17020190

APA Style

Fedorczyk, B., Redkiewicz, P., Matalińska, J., Piast, R., Kosson, P., & Wieczorek, R. (2024). Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1. Pharmaceuticals, 17(2), 190. https://doi.org/10.3390/ph17020190

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