NCp7: targeting a multitasking protein for next-generation anti-HIV drug development part 1: covalent inhibitors.
Identifieur interne : 000A67 ( PubMed/Corpus ); précédent : 000A66; suivant : 000A68NCp7: targeting a multitasking protein for next-generation anti-HIV drug development part 1: covalent inhibitors.
Auteurs : Luca Sancineto ; Nunzio Iraci ; Oriana Tabarrini ; Claudio SantiSource :
- Drug discovery today [ 1878-5832 ] ; 2018.
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
Links to Exploration step
pubmed:29107765Le document en format XML
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<author><name sortKey="Sancineto, Luca" sort="Sancineto, Luca" uniqKey="Sancineto L" first="Luca" last="Sancineto">Luca Sancineto</name>
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<author><name sortKey="Iraci, Nunzio" sort="Iraci, Nunzio" uniqKey="Iraci N" first="Nunzio" last="Iraci">Nunzio Iraci</name>
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<front><div type="abstract" xml:lang="en">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.</div>
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<Abstract><AbstractText>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.</AbstractText>
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