NCp7: targeting a multitasking protein for next-generation anti-HIV drug development part 1: covalent inhibitors.
Identifieur interne : 000C59 ( Main/Exploration ); précédent : 000C58; suivant : 000C60NCp7: targeting a multitasking protein for next-generation anti-HIV drug development part 1: covalent inhibitors.
Auteurs : Luca Sancineto [Pologne] ; Nunzio Iraci [Italie] ; Oriana Tabarrini [Italie] ; Claudio Santi [Italie]Source :
- Drug discovery today [ 1878-5832 ] ; 2018.
Descripteurs français
- KwdFr :
- Agents antiVIH (pharmacologie), Agents antiVIH (usage thérapeutique), Animaux, Découverte de médicament (), Humains, Produits du gène gag du virus de l'immunodéficience humaine (antagonistes et inhibiteurs), Protéines nucléocapside (antagonistes et inhibiteurs), Protéines virales (antagonistes et inhibiteurs), Relation structure-activité.
- MESH :
- antagonistes et inhibiteurs : Produits du gène gag du virus de l'immunodéficience humaine, Protéines nucléocapside, Protéines virales.
- pharmacologie : Agents antiVIH.
- usage thérapeutique : Agents antiVIH.
- Animaux, Découverte de médicament, Humains, Relation structure-activité.
English descriptors
- KwdEn :
- Animals, Anti-HIV Agents (pharmacology), Anti-HIV Agents (therapeutic use), Drug Discovery (methods), Humans, Nucleocapsid Proteins (antagonists & inhibitors), Structure-Activity Relationship, Viral Proteins (antagonists & inhibitors), gag Gene Products, Human Immunodeficiency Virus (antagonists & inhibitors).
- MESH :
- chemical , antagonists & inhibitors : Nucleocapsid Proteins, Viral Proteins, gag Gene Products, Human Immunodeficiency Virus.
- chemical , pharmacology : Anti-HIV Agents.
- chemical , therapeutic use : Anti-HIV Agents.
- methods : Drug Discovery.
- Animals, Humans, Structure-Activity Relationship.
Abstract
The major internal component of the HIV virion core is the nucleocapsid protein 7 (NCp7), a small, highly basic protein that is essential for multiple stages of the viral replicative cycle, and whose structure is preserved in all viral strains, including clinical isolates from therapy-experienced patients. This key protein is recognised as a potential target for an effective next-generation antiretroviral therapy, because it could offer the possibility to develop broad-spectrum agents that are less prone to select for resistant strains. Here, we provide a comprehensive overview of the covalent NCp7 inhibitors that have emerged over the past 25 years of drug discovery campaigns, emphasising, where possible, their structure-activity relationships (SARs) and pharmacophoric features.
DOI: 10.1016/j.drudis.2017.10.017
PubMed: 29107765
Affiliations:
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Le document en format XML
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This key protein is recognised as a potential target for an effective next-generation antiretroviral therapy, because it could offer the possibility to develop broad-spectrum agents that are less prone to select for resistant strains. Here, we provide a comprehensive overview of the covalent NCp7 inhibitors that have emerged over the past 25 years of drug discovery campaigns, emphasising, where possible, their structure-activity relationships (SARs) and pharmacophoric features.</div></front></TEI><affiliations><list><country><li>Italie</li><li>Pologne</li></country></list><tree><country name="Pologne"><noRegion><name sortKey="Sancineto, Luca" sort="Sancineto, Luca" uniqKey="Sancineto L" first="Luca" last="Sancineto">Luca Sancineto</name></noRegion></country><country name="Italie"><noRegion><name sortKey="Iraci, Nunzio" sort="Iraci, Nunzio" uniqKey="Iraci N" first="Nunzio" last="Iraci">Nunzio Iraci</name></noRegion><name sortKey="Santi, Claudio" sort="Santi, Claudio" uniqKey="Santi C" first="Claudio" last="Santi">Claudio Santi</name><name sortKey="Tabarrini, Oriana" sort="Tabarrini, Oriana" uniqKey="Tabarrini O" first="Oriana" last="Tabarrini">Oriana Tabarrini</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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