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Title:Kovalentna vezava pri zdravilnih učinkovinah - naj jo iščemo ali se ji izogibamo?
Authors:ID Strašek Benedik, Nika (Author)
ID Kavaš, Vid (Author)
ID Meden, Anže (Author)
Files:.pdf PDF - Presentation file, download (1,67 MB)
MD5: 28A81EEEABEED6B5D164686351CB36CD
 
Language:Slovenian
Typology:1.02 - Review Article
Organization:Logo SFD - Slovenian Pharmaceutical Society
Abstract:Kovalentne zdravilne učinkovine imajo pomembno vlogo v humani medicini. S tvorbo stabilnih kovalentnih vezi s specifičnimi aminokislinskimi ostanki v svojih makromolekularnih tarčah dosežejo močnejše in dolgotrajnejše terapevtske učinke kot klasične učinkovine, ki izkoriščajo le reverzibilne interakcije. Njihovo dolgo zadrževanje na tarči omogoča redkejše odmerjanje, kar lahko zmanjša pojav neželenih učinkov. Vseeno pa razvoj kovalentnih zdravilnih učinkovin ni brez izzivov, saj pomisleki glede izventarčne vezave in potencialne imunogenosti zahtevajo skrbno načrtovanje in optimizacijo za zagotavljanje varnosti in učinkovitosti. V zadnjem desetletju je prišlo do bistvenega napredka na področju načrtovanja, selektivnosti in razumevanja mehanizmov delovanja kovalentnih zdravilnih učinkovin, kar je omogočilo razvoj novih zdravil, zlasti v onkologiji, infektologiji in nevrologiji. Sodobne kovalentne zdravilne učinkovine dokazujejo, da je s premišljenim pristopom mogoče oblikovati učinkovite, selektivne in varne kovalentne učinkovine z velikim terapevtskim potencialom.
Keywords:bojna glava, ireverzibilni zaviralci, kovalentne zdravilne učinkovine, načrtovanje zdravilnih učinkovin
Publication status:Published
Publication version:Version of Record
Publication date:01.03.2026
Year of publishing:2026
Number of pages:str. 39-45
Numbering:Letn. 77, št. 1
PID:20.500.12556/DiRROS-31038 New window
UDC:615.015
ISSN on article:2536-4316
COBISS.SI-ID:273471747 New window
Note:Opis vira z dne 30. 3. 2026; Nasl. z nasl. zaslona;
Publication date in DiRROS:10.07.2026
Views:130
Downloads:62
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Record is a part of a journal

Title:Farmacevtski vestnik : strokovno glasilo slovenske farmacije
Publisher:Slovensko farmacevtsko društvo
ISSN:2536-4316
COBISS.SI-ID:288686336 New window

Licences

License:CC BY-NC 4.0, Creative Commons Attribution-NonCommercial 4.0 International
Link:http://creativecommons.org/licenses/by-nc/4.0/
Description:A creative commons license that bans commercial use, but the users don’t have to license their derivative works on the same terms.
Licensing start date:01.01.2025

Secondary language

Language:English
Title:Covalent binding drugs - something to be sought or shunned?
Abstract:Covalent drugs play an important role in human medicine. By forming stable covalent bonds with specific amino acid residues of their macromolecular targets, they can achieve stronger and longer-lasting therapeutic effects than conventional drugs, which form reversible interactions. Their prolonged target residence allows for less frequent dosing, which can reduce the incidence of adverse effects. however, the development of covalent drugs is not without challenges, as concerns about off-target binding and potential immunogenicity require careful design and optimization to ensure safety and efficacy. Over the past decade, significant progress has been made in the design, selectivity, and mechanistic understanding of covalent drugs, enabling the development of new therapeutics, especially in oncology, infectious diseases, and neurology. Modern covalent drugs demonstrate that with careful consideration and design effective, selective, and safe covalent drugs with high therapeutic potential can be developed.
Keywords:covalent drugs, drug design, irreversible inhibitors, warhead


Collection

This document is a part of these collections:
  1. Farmacevtski vestnik

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