新的三环扩展精氨酸核化物具有泛病毒活性
Céline Martin-Ghoteimi1, Kyle A Davis1, Rayane Ghoteimi1
1Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, Baltimore, MD 21250, USA.
Bioorganic & medicinal chemistry
|September 12, 2025
概括
新型的硫扩增核酸原药显示出强大的,广泛的抗病毒活性,对多个病毒家族,包括冠状病毒和黄病毒,具有低毒性. 这些有前途的化合物有可能成为新的抗病毒疗法.
科学领域:
- 药用化学 医学化学
- 病毒学 病毒学
- 药物发现 药物发现 药物发现
背景情况:
- 新型抗病毒疗法的开发对于新出现的病毒威胁至关重要.
- 核类类似物是抗病毒药物的关键类别.
- 提奥芬扩增三环核化物代表了抗病毒研究的新型结构类.
研究的目的:
- 合成和评估新型硫扩展三环核化物及其抗病毒活性前药物.
- 探索糖和核基基修改对抗病毒疗效的影响.
- 识别具有针对大流行相关病毒的广泛活性的化合物.
主要方法:
- 硫扩展三环核酸及其前物的化学合成.
- 对各种病毒家族进行抗病毒活性查.
- 确定EC50值和评估细胞毒性.
- 改性类似物及其前药物的比较分析.
主要成果:
- CEM-007显示出有前途的初始抗病毒活性.
- CEM-024,一种2'-修饰的类似物,显示出有限的抗病毒作用.
- 几种CEM-024的前药物 (CEM-042,CEM-052,CEM-053,CEM-054,CEM-055) 显示出强大的,广泛的抗病毒活性.
- 这些活性前药物对病毒,菲洛病毒和冠状病毒具有有效性,具有低微分子EC50值和最小毒性.
结论:
- 新型硫扩增三环核酸原药具有显著的广泛抗病毒潜力.
- 特定的前药物修改增强了抗病毒活性和输送.
- 这些化合物代表了作为抗病毒疗法对抗具有挑战性的病毒感染进一步开发的有希望的候选人.
相关概念视频
Subviral Agents
534
Subviral agents are infectious entities that resemble viruses but lack one or more viral components, such as a capsid or essential replication machinery. These agents include viroids, prions, and satellites, each possessing distinct structural and functional characteristics that influence their mode of infection and replication.Viroids are the simplest subviral agents, consisting of circular, single-stranded RNA molecules without a protein coat. They exclusively infect plants, relying entirely...
534
Retroviruses
14.6K
Retroviruses and retrotransposons both insert copies of their genetic elements into the genome of the host cell. Thus, the viral genes are passed on when the host genome is replicated or translated. A typical retroviral DNA sequence contains 3-4 genes that encode the different proteins required for its structural assembly and function as a molecular parasite. This DNA is transcribed into a single mRNA, which is very similar in structure to conventional mRNAs, i.e., it is capped at the 5’...
14.6K
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
597
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy. SP binds and activates...
597


