Peptidomimetici kao inhibitori HIV-proteaze

undergraduate thesis

• Title (english): Peptidomimetics as inhibitors of HIV-protease
• Author: Bosiljka Studen
• Mentor: Lidija Barišić (mentor)
• Granter: University of Zagreb; Faculty of Food Technology and Biotechnology; (Department of Chemistry and Biochemistry); (Laboratory for Organic Chemistry); Zagreb
• Defense date and country: 2015-09-09, Croatia
• Scientific / art field, discipline and subdiscipline: BIOTECHNICAL SCIENCES; Nutrition; Food Chemistry and Biochemistry

Abstract

Peptidomimetici oponašaju biološku aktivnost prirodnih peptida te unapređuju njhovu selektivnost, biodostupnost i funkcionalnost, zbog čega dizajn i sinteza peptidomimetika predstavljaju važno oruđe u pronalasku lijekova. Virus humane imunodeficijencije (HIV) uzročnik je Sindroma stečene imunodeficijencije (AIDS). Definiranjem strukture i mehanizma djelovanja enzima HIV-proteaze, koji je odgovoran za razvoj virusa HIV-a, dizajniran je niz peptidomimetičkih lijekova kao inhibitora HIV-proteaze. Učinkovitost lijekova prve generacije ovisi o konformaciji aktivnog mjesta enzima, te opada ukoliko dođe do mutacije virusa, što je dovelo do razvoja druge generacije lijekova koji su manje osjetljivi na mutacije virusa. Danas se aktivno radi na dizajnu cikličkih inhibitora koji imaju povećanu potentnost lijeka, poboljšana farmakokinetička svojstva i djelovanje na mutirane sojeve virusa.

Abstract (english)

Peptidomimetics mimic the biological activity of natural peptides with improved selectivity, bioavailability and functionality which makes the design and synthesis of peptidomimetics a valuable tool in finding a cure for different disseasses. Human immunodeficiency virus (HIV) is the causative agent of Acquired Immune Deficiency Syndrome (AIDS). Designe of a series of peptidomimetic drugs, inhibitors of HIV-protease, was enabled by defining the structure and mechanism of action of the HIV-protease, enzyme that is responsible for the development of the HIV virus. The efficiency of the drugs of the first-generation is dependent on the conformation of the active site of the enzyme, and they lose on the inhibitory effect in case of mutation of the virus, leading to the development of second-generation drugs which are less sensitive to mutation of the virus. Today, great effort has been made in the design of cyclic inhibitors which have enhanced potency, improved pharmacokinetic properties and activity for the mutant strains.

• Keywords: peptidomimetici; HIV; HIV-proteaza; inhibitori HIV-proteaze; ciklički inhibitori
• Keywords (english): peptidomimetics; HIV; HIV-protease; inhibitors of HIV-protease; cyclic inhibitors
• Language: croatian
• URN:NBN: urn:nbn:hr:159:960607
• Study programme: Title: Nutrition; Study programme type: university; Study level: undergraduate; Academic / professional title: sveučilišni/a prvostupnik/prvostupnica (baccalaureus/baccalaurea) nutricionizma (sveučilišni/a prvostupnik/prvostupnica (baccalaureus/baccalaurea) nutricionizma)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2015-12-14 10:52:37