دورية أكاديمية
Covalent reversible inhibitors of cysteine proteases containing the nitrile warhead: recent advancement in the field of viral and parasitic diseases
| العنوان: | Covalent reversible inhibitors of cysteine proteases containing the nitrile warhead: recent advancement in the field of viral and parasitic diseases |
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| المؤلفون: | Brogi S., Ibba R., Rossi S., Butini S., Calderone V., Gemma S., Campiani G. |
| المساهمون: | Brogi, S., Ibba, R., Rossi, S., Butini, S., Calderone, V., Gemma, S., Campiani, G. |
| سنة النشر: | 2022 |
| المجموعة: | Università degli Studi di Siena: USiena air |
| مصطلحات موضوعية: | covalent inhibition, cysteine/serine/threonine protease, nitrile, protozoan parasite, viru, warhead, Cysteine, Cysteine Proteinase Inhibitor, Drug Discovery, Human, Cysteine Protease, Parasitic Diseases |
| الوصف: | In the field of drug discovery, the nitrile group is well represented among drugs and biologically active compounds. It can form both non-covalent and covalent interactions with diverse biological targets, and it is amenable as an electrophilic warhead for covalent inhibition. The main advantage of the nitrile group as a warhead is mainly due to its milder electrophilic character relative to other more reactive groups (e.g., -CHO), reducing the possibility of unwanted reactions that would hinder the development of safe drugs, coupled to the ease of installation through different synthetic approaches. The covalent inhibition is a well-assessed design approach for serine, threonine, and cysteine protease inhibitors. The mechanism of hydrolysis of these enzymes involves the formation of a covalent acyl intermediate, and this mechanism can be exploited by introducing electrophilic warheads in order to mimic this covalent intermediate. Due to the relevant role played by the cysteine protease in the survival and replication of infective agents, spanning from viruses to protozoan parasites, we will review the most relevant and recent examples of protease inhibitors presenting a nitrile group that have been introduced to form or to facilitate the formation of a covalent bond with the catalytic cysteine active site residue. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | ELETTRONICO |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/35458759; info:eu-repo/semantics/altIdentifier/wos/WOS:000785463200001; volume:27; issue:8; firstpage:1; lastpage:14; numberofpages:14; journal:MOLECULES; https://hdl.handle.net/11365/1205957Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85128802527; https://www.mdpi.com/1420-3049/27/8/2561Test; https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9029279Test/ |
| DOI: | 10.3390/molecules27082561 |
| الإتاحة: | https://doi.org/10.3390/molecules27082561Test https://hdl.handle.net/11365/1205957Test https://www.mdpi.com/1420-3049/27/8/2561Test https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9029279Test/ |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.CCFA49 |
| قاعدة البيانات: | BASE |
| DOI: | 10.3390/molecules27082561 |
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