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Volume 15
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10.3390/ph15050540
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Article

Design of D-Amino Acids SARS-CoV-2 Main Protease Inhibitors Using the Cationic Peptide from Rattlesnake Venom as a Scaffold

by
Raphael J. Eberle
1,2,
Ian Gering
1,
Markus Tusche
1,
Philipp N. Ostermann
3,
Lisa Müller
3,
Ortwin Adams
3,
Heiner Schaal
3,
Danilo S. Olivier
4,
Marcos S. Amaral
5,
Raghuvir K. Arni
6,
Dieter Willbold
1,2,7 and
Mônika A. Coronado
1,*
1
Institute of Biological Information Processing (IBI-7: Structural Biochemistry), Forschungszentrum Jülich, 52428 Jülich, Germany
2
Institut für Physikalische Biologie, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße, 40225 Düsseldorf, Germany
3
Institute of Virology, Medical Faculty, University Hospital Düsseldorf, Heinrich-Heine-Universität Düsseldorf, 40225 Düsseldorf, Germany
4
Integrated Sciences Center, Campus Cimba, Federal University of Tocantins, Araguaína 77824-838, TO, Brazil
5
Institute of Physics, Federal University of Mato Grosso do Sul, Campo Grande 79070-900, MS, Brazil
6
Multiuser Center for Biomolecular Innovation, Department of Physics, IBILCE, Universidade Estadual Paulista (UNESP), São José do Rio Preto 15054-000, SP, Brazil
7
JuStruct: Jülich Centre for Structural Biology, Forschungszentrum Jülich, 52428 Jülich, Germany
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2022, 15(5), 540; https://doi.org/10.3390/ph15050540
Submission received: 28 February 2022 / Revised: 18 April 2022 / Accepted: 25 April 2022 / Published: 27 April 2022
(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
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Abstract

The C30 endopeptidase (3C-like protease; 3CLpro) is essential for the life cycle of SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) since it plays a pivotal role in viral replication and transcription and, hence, is a promising drug target. Molecules isolated from animals, insects, plants, or microorganisms can serve as a scaffold for the design of novel biopharmaceutical products. Crotamine, a small cationic peptide from the venom of the rattlesnake Crotalus durissus terrificus, has been the focus of many studies since it exhibits activities such as analgesic, in vitro antibacterial, and hemolytic activities. The crotamine derivative L-peptides (L-CDP) that inhibit the 3CL protease in the low µM range were examined since they are susceptible to proteolytic degradation; we explored the utility of their D-enantiomers form. Comparative uptake inhibition analysis showed D-CDP as a promising prototype for a D-peptide-based drug. We also found that the D-peptides can impair SARS-CoV-2 replication in vivo, probably targeting the viral protease 3CLpro.
Keywords: SARS-CoV-2; COVID-19; 3CLpro; main protease; inhibitor; crotamine derivative peptides; D-peptides SARS-CoV-2; COVID-19; 3CLpro; main protease; inhibitor; crotamine derivative peptides; D-peptides

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MDPI and ACS Style

Eberle, R.J.; Gering, I.; Tusche, M.; Ostermann, P.N.; Müller, L.; Adams, O.; Schaal, H.; Olivier, D.S.; Amaral, M.S.; Arni, R.K.; et al. Design of D-Amino Acids SARS-CoV-2 Main Protease Inhibitors Using the Cationic Peptide from Rattlesnake Venom as a Scaffold. Pharmaceuticals 2022, 15, 540. https://doi.org/10.3390/ph15050540

AMA Style

Eberle RJ, Gering I, Tusche M, Ostermann PN, Müller L, Adams O, Schaal H, Olivier DS, Amaral MS, Arni RK, et al. Design of D-Amino Acids SARS-CoV-2 Main Protease Inhibitors Using the Cationic Peptide from Rattlesnake Venom as a Scaffold. Pharmaceuticals. 2022; 15(5):540. https://doi.org/10.3390/ph15050540

Chicago/Turabian Style

Eberle, Raphael J., Ian Gering, Markus Tusche, Philipp N. Ostermann, Lisa Müller, Ortwin Adams, Heiner Schaal, Danilo S. Olivier, Marcos S. Amaral, Raghuvir K. Arni, and et al. 2022. "Design of D-Amino Acids SARS-CoV-2 Main Protease Inhibitors Using the Cationic Peptide from Rattlesnake Venom as a Scaffold" Pharmaceuticals 15, no. 5: 540. https://doi.org/10.3390/ph15050540

APA Style

Eberle, R. J., Gering, I., Tusche, M., Ostermann, P. N., Müller, L., Adams, O., Schaal, H., Olivier, D. S., Amaral, M. S., Arni, R. K., Willbold, D., & Coronado, M. A. (2022). Design of D-Amino Acids SARS-CoV-2 Main Protease Inhibitors Using the Cationic Peptide from Rattlesnake Venom as a Scaffold. Pharmaceuticals, 15(5), 540. https://doi.org/10.3390/ph15050540

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