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undergraduate thesis
Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom
Zagreb: University of Zagreb, Faculty of Food Technology and Biotechnology, 2021. urn:nbn:hr:159:380806
Kovač, Gloria
University of Zagreb
Faculty of Food Technology and Biotechnology
Department of Chemistry and Biochemistry
Laboratory for Organic Chemistry

Institutional repository: Repository of the Faculty of Food Technology and Biotechnology

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Kovač, G. (2021). Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom (Undergraduate thesis). Zagreb: University of Zagreb, Faculty of Food Technology and Biotechnology. Retrieved from https://urn.nsk.hr/urn:nbn:hr:159:380806

Kovač, Gloria. "Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom." Undergraduate thesis, University of Zagreb, Faculty of Food Technology and Biotechnology, 2021. https://urn.nsk.hr/urn:nbn:hr:159:380806

Kovač, Gloria. "Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom." Undergraduate thesis, University of Zagreb, Faculty of Food Technology and Biotechnology, 2021. https://urn.nsk.hr/urn:nbn:hr:159:380806

Kovač, G. (2021). 'Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom', Undergraduate thesis, University of Zagreb, Faculty of Food Technology and Biotechnology, accessed 08 September 2024, https://urn.nsk.hr/urn:nbn:hr:159:380806

Kovač G. Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom [Undergraduate thesis]. Zagreb: University of Zagreb, Faculty of Food Technology and Biotechnology; 2021 [cited 2024 September 08] Available at: https://urn.nsk.hr/urn:nbn:hr:159:380806

G. Kovač, "Peptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom", Undergraduate thesis, University of Zagreb, Faculty of Food Technology and Biotechnology, Zagreb, 2021. Available at: https://urn.nsk.hr/urn:nbn:hr:159:380806

Metadata
TitlePeptidomimetički inhibitori SARS-CoV-2 3CLpro, proteaze odgovorne za replikaciju i infekciju koronavirusom
Title (english)Peptidomimetic inhibitors OF SARS-CoV-2 3CLpro, protease responsible for replication and coronavirus infection
AuthorGloria Kovač
MentorLidija Barišić (mentor)
GranterUniversity of Zagreb
Faculty of Food Technology and Biotechnology
(Department of Chemistry and Biochemistry)
(Laboratory for Organic Chemistry)
Zagreb
Defense date and country2021-09-16, Croatia
Scientific / art field,
discipline and subdiscipline		BIOTECHNICAL SCIENCES
Food Technology
Abstract
Peptidomimetici su molekule koje svojom 3D-strukturom oponašaju bioaktivnu konformaciju prirodnih peptida, a odlikuju se povećanom proteolitičkom stabilnošću i selektivnošću prema receptorima te većom bioraspoloživošću u odnosu na prirodne peptide. Nakon ulaska SARS-CoV-2 u stanicu, virusna RNA translatira se na ribosomima, a virusna proteaza SARS-CoV-2 3CLpro sudjeluje u hidrolizi nastalih poliproteina nakon čega slijedi tvorba novih viriona. Stoga se inhibicijom virusne proteaze onemogućava njegova replikacija. Opisani su peptidomimetički inhibitori virusne proteaze u kojima je aminokiselinska sekvencija iz prirodnog supstrata modificirana funkcijskom skupinom (aldehid, α-ketoamid ili Michaelov akceptor) pomoću koje s aktivnim mjestom enzima uspostavlja kovalentnu vezu. Time se kompleks inhibitora i proteaze dodatno stabilizira što dovodi do inhibicije enzima odnosno replikacije virusa. Usporedbom kristalnih struktura kompleksâ peptidomimetičkih inhibitora i SARS-CoV-2 3CLpro te evaluacijom njihovog inhibitornog djelovanja, najučinkovitijim inhibitorima pokazali su se peptidomimetici s umetnutom α-ketoamidnom skupinom.
Abstract (english)
Peptidomimetics are molecules whose 3D structure mimics the bioactive conformation of natural peptides. They are characterized by higher proteolytic stability, selectivity for receptors and higher bioavailability compared to natural peptides. After SARS- CoV-2 enters the cell, viral RNA is translated on the ribosomes, and the viral protease SARS- CoV-2 3CLpro is involved in the hydrolysis of the resulting polyproteins followed by the formation of new virions. Therefore, inhibition of the viral protease prevents viral replication. Peptidomimetic inhibitors of viral protease are described in which the amino acid sequence of a natural substrate is modified by a functional group (aldehyde, α-ketoamide or Michael acceptors) to allow covalent binding with the enzyme active site. This further stabilizes the complex of inhibitor and protease, resulting in inhibition of the enzyme or replication of the virus. Comparison of the crystal structures of the complex of peptidomimetic inhibitors and SARS-CoV-2 3CLpro and evaluation of their inhibitory activity revealed that peptidomimetics with inserted α-ketoamide group are the most efficient.
Keywords
Keywords (english)
Languagecroatian
URN:NBNurn:nbn:hr:159:380806
Study programmeTitle: Food Technology
Study programme type: university
Study level: undergraduate
Academic / professional title: sveučilišni/a prvostupnik/prvostupnica (baccalaureus/baccalaurea) inženjer/inženjerka prehrambene tehnologije (sveučilišni/a prvostupnik/prvostupnica (baccalaureus/baccalaurea) inženjer/inženjerka prehrambene tehnologije)
Type of resourceText
File originBorn digital
Access conditionsOpen access
Terms of useLicence Attribution-NoDerivatives 4.0 International (CC BY-ND 4.0) icon
Created on2021-09-29 09:42:09