磷酸无环核苷前药LAVR-289对痘病毒和非洲猪瘟病毒的抗病毒活性研究

IF 3.8 2区 医学 Q2 CHEMISTRY, MEDICINAL
ACS Infectious Diseases Pub Date : 2025-06-13 Epub Date: 2025-05-22 DOI:10.1021/acsinfecdis.5c00169
Elie Marcheteau, Estelle Mosca, Gaelle Frenois-Veyrat, Sandrine Kappler-Gratias, Laetitia Boutin, Sokunthea Top, Thomas Mathieu, Cyril Colas, Patrick Favetta, Tony Garnier, Peggy Barbe, Mathilde Keck, Daniel Gillet, Alicia Mas, Ali Alejo, Yinyi Yu, Karoly Toth, Getahun Abate, Vincent Roy, Janet Skerry, Kelly S Wetzel, Joshua D Shamblin, Joseph W Golden, Rekha G Panchal, Eric M Mucker, Rajini Mudhasani, Luigi A Agrofoglio, Frederic Iseni, Franck Gallardo
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引用次数: 0

摘要

痘病毒是一种双链DNA病毒,包括相关的人畜共患病原体,具有高发病率和潜在的生物战威胁。虽然非洲猪瘟病毒属于阿斯法病毒科,并没有严格归类为痘病毒科成员,但两者都属于在细胞质中复制的同一类痘病毒。在针对这些病毒的化合物中,无环膦酸核苷(ANP)前药是很有前途的病毒DNA聚合酶抑制剂。然而,与它们的毒性和耐药性的迅速出现有关的一些限制突出了对新的抗病毒分子的需求。在这项研究中,我们测试了一种名为LAVR-289的新型ANP。该产品通过靶向痘病毒DNA聚合酶的特定区域有效抑制病毒复制。使用猴痘病毒模型,皮下或口服给药LAVR-289对受感染动物具有保护作用,且无毒性。LAVR-289的体内半衰期、长货架稳定性和广谱功效使其成为进一步开发和储备的抗dsDNA病毒爆发的药物候选物。LAVR-289可定位于病毒反复流行、生物恐怖主义风险和人群中出现耐药菌株的背景下。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antiviral Activity of the Acyclic Nucleoside Phosphonate Prodrug LAVR-289 against Poxviruses and African Swine Fever Virus.

Poxviruses are double-stranded DNA viruses including relevant zoonotic pathogens with high morbidity and potential biological warfare threats. Although African swine fever virus belongs to the Asfarviridae family and is not strictly classified as a Poxviridae member, both fall within the same class of Pokkesviricetes that replicate in the cytoplasm. Among compounds targeting these viruses, acyclic nucleoside phosphonate (ANP) prodrugs are promising inhibitors of viral DNA polymerases. However, some limitations related to their toxicity and the rapid emergence of resistance highlight the need for new antiviral molecules. In this study, we tested a new ANP called LAVR-289. This product effectively inhibits viral replication by targeting a specific domain in the poxvirus DNA polymerase. Using monkeypox virus models, the subcutaneous or oral administration of LAVR-289 demonstrated protective efficacy in infected animals without toxicity. Its in vivo half-life, long on-the-shelf stability and broad-spectrum efficacy make LAVR-289 a promising candidate for further development and stockpiling as a medical countermeasure against dsDNA virus outbreaks. LAVR-289 can be positioned in the context of recurrent viral epidemics, bioterrorism risk, and the emergence of resistant strains in the population.

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来源期刊
ACS Infectious Diseases
ACS Infectious Diseases CHEMISTRY, MEDICINALINFECTIOUS DISEASES&nb-INFECTIOUS DISEASES
CiteScore
9.70
自引率
3.80%
发文量
213
期刊介绍: ACS Infectious Diseases will be the first journal to highlight chemistry and its role in this multidisciplinary and collaborative research area. The journal will cover a diverse array of topics including, but not limited to: * Discovery and development of new antimicrobial agents — identified through target- or phenotypic-based approaches as well as compounds that induce synergy with antimicrobials. * Characterization and validation of drug target or pathways — use of single target and genome-wide knockdown and knockouts, biochemical studies, structural biology, new technologies to facilitate characterization and prioritization of potential drug targets. * Mechanism of drug resistance — fundamental research that advances our understanding of resistance; strategies to prevent resistance. * Mechanisms of action — use of genetic, metabolomic, and activity- and affinity-based protein profiling to elucidate the mechanism of action of clinical and experimental antimicrobial agents. * Host-pathogen interactions — tools for studying host-pathogen interactions, cellular biochemistry of hosts and pathogens, and molecular interactions of pathogens with host microbiota. * Small molecule vaccine adjuvants for infectious disease. * Viral and bacterial biochemistry and molecular biology.
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