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Communication

Nostocyclopeptides as New Inhibitors of 20S Proteasome

1
Division of Marine Biotechnology, Institute of Oceanography, University of Gdańsk, Marszałka Józefa Piłsudskiego 46, PL-81378 Gdynia, Poland
2
Department of Biomedical Chemistry, Faculty of Chemistry, University of Gdańsk, Wita Stwosza 63, PL-80308 Gdańsk, Poland
3
Institute of Oceanology, Polish Academy of Sciences, Powstańców Warszawy 55, PL-81712 Sopot, Poland
4
School of Pharmacy and Life Sciences, Robert Gordon University, Aberdeen AB10 7GJ, UK
*
Author to whom correspondence should be addressed.
Academic Editor: Olivier Coux
Biomolecules 2021, 11(10), 1483; https://doi.org/10.3390/biom11101483
Received: 1 September 2021 / Revised: 29 September 2021 / Accepted: 5 October 2021 / Published: 8 October 2021
Nostocyclopeptides (Ncps) are a small class of bioactive nonribosomal peptides produced solely by cyanobacteria of the genus Nostoc. In the current work, six Ncps were isolated from Nostoc edaphicum strain CCNP1411. The bioactivity of these compounds was tested in vitro against 20S proteasome, a proteolytic complex that plays an important role in maintaining cellular proteostasis. Dysfunction of the complex leads to many pathological disorders. The assays indicated selective activity of specific Ncp variants. For two linear peptide aldehydes, Ncp-A2-L and Ncp-E2-L, the inhibitory effects on chymotrypsin-like activity were revealed, while the cyclic variant, Ncp-A2, inactivated the trypsin-like site of this enzymatic complex. The aldehyde group was confirmed to be an important element of the chymotrypsin-like activity inhibitors. The nostocyclopeptides, as novel inhibitors of 20S proteasome, increased the number of natural products that can be considered potential regulators of cellular processes.
Keywords: 20S proteasome inhibitors; cyanobacteria; Nostoc; nostocyclopeptides 20S proteasome inhibitors; cyanobacteria; Nostoc; nostocyclopeptides
MDPI and ACS Style

Fidor, A.; Cekała, K.; Wieczerzak, E.; Cegłowska, M.; Kasprzykowski, F.; Edwards, C.; Mazur-Marzec, H. Nostocyclopeptides as New Inhibitors of 20S Proteasome. Biomolecules 2021, 11, 1483. https://doi.org/10.3390/biom11101483

AMA Style

Fidor A, Cekała K, Wieczerzak E, Cegłowska M, Kasprzykowski F, Edwards C, Mazur-Marzec H. Nostocyclopeptides as New Inhibitors of 20S Proteasome. Biomolecules. 2021; 11(10):1483. https://doi.org/10.3390/biom11101483

Chicago/Turabian Style

Fidor, Anna, Katarzyna Cekała, Ewa Wieczerzak, Marta Cegłowska, Franciszek Kasprzykowski, Christine Edwards, and Hanna Mazur-Marzec. 2021. "Nostocyclopeptides as New Inhibitors of 20S Proteasome" Biomolecules 11, no. 10: 1483. https://doi.org/10.3390/biom11101483

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