Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2

Li, Yihua; Wang, Kun; Sun, Hongmin; Wu, Shuo; Wang, Huiqiang; Shi, Yuanyuan; Li, Xingxing; Yan, Haiyan; Yang, Ge; Wu, Mengyuan; Li, Yihong; Ding, Xiaotian; Si, Shuyi; Jiang, Jian‐Dong; Du, Yu; Li, Yuhuan; Hong, Bin

doi:10.1016/j.antiviral.2023.105606

Cited by 3 publications

(4 citation statements)

References 52 publications

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“…159 Omicsynin B4 was found to inhibit the entry of COVID-19 into host cells by inhibiting CTSL and TMPRSS2. 112 The IC 50 values for CTSL and TMPRSS2 are 0.44 and 380 nM, respectively. The EC 50 to inhibit the entry of SARS-CoV-2 pseudovirus is 640 nM.…”

Section: Dual-target Inhibitors Of Sars-cov-2mentioning

confidence: 97%

“…It has been discovered to exhibit effective antiviral activity against influenza A viruses, HCoV-229E and SARS-CoV-2 . Omicsynin B4 was found to inhibit the entry of COVID-19 into host cells by inhibiting CTSL and TMPRSS2 . The IC 50 values for CTSL and TMPRSS2 are 0.44 and 380 nM, respectively.…”

Section: Dual-target Inhibitors Of Sars-cov-2mentioning

confidence: 99%

“…The EC 50 to inhibit the entry of SARS-CoV-2 pseudovirus is 640 nM. 112 4.3.2. TMPRSS2/Furin Dual Inhibitors.…”

Section: S/d4 Dual Inhibitorsmentioning

confidence: 99%

“…The IC 50 values for CTSL and TMPRSS2 are 0.44 and 380 nM, respectively. The EC 50 to inhibit the entry of SARS-CoV-2 pseudovirus is 640 nM …”

Section: Dual-target Inhibitors Of Sars-cov-2mentioning

confidence: 99%

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New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs

Zhang,

Xiao,

et al. 2024

J. Med. Chem.

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The 2019 coronavirus disease (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has resulted in millions of deaths, posing a serious threat to public health and safety. Rapid mutations of SARS-CoV-2 and complex interactions among multiple targets during infection pose a risk of expiry for small molecule inhibitors. This suggests that the traditional concept of "one bug, one drug" could be ineffective in dealing with the coronavirus. The dual-target drug strategy is expected to be the key to ending coronavirus infections. However, the lack of design method and improper combination of dual-targets poses obstacle to the discovery of new dual-target drugs. In this Perspective, we summarized the profiles concerning drug design methods, structure−activity relationships, and pharmacological parameters of dual-target drugs for the treatment of COVID-19. Importantly, we underscored how target combination and rational drug design illuminate the development of dualtarget drugs for SARS-CoV-2. ■ SIGNIFICANCE• This is the first Perspective on dual-target drugs for treating coronavirus. • Dual-target drugs, acting on multiple pathways, offer enhanced efficacy and can delay resistance compared to single-target treatments. • Drug repurposing for dual-target design can significantly shorten the timeline for clinical trials, addressing urgent medication needs during the early COVID-19 outbreak. • The introduction of covalent warheads can compensate for active site similarity issues, aiding in the development of high-affinity dual-target inhibitors.

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Section: Dual-target Inhibitors Of Sars-cov-2mentioning

confidence: 97%

Section: Dual-target Inhibitors Of Sars-cov-2mentioning

confidence: 99%

See 2 more Smart Citations

New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs

Zhang,

Xiao,

et al. 2024

J. Med. Chem.

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Peptidomimetics as potent dual SARS-CoV-2 cathepsin-L and main protease inhibitors: In silico design, synthesis and pharmacological characterization

Ciaglia,

Vestuto,

Di Sarno

et al. 2024

European Journal of Medicinal Chemistry

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Transplacental Transmission of SARS-CoV-2: A Narrative Review

Bui,

Nguyen Le,

Duong

et al. 2024

Medicina

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Background and Objectives: The study aims to explore the potential for transplacental transmission of SARS-CoV-2, focusing on its pathophysiology, placental defense mechanisms, and the clinical implications for maternal and neonatal health. Materials and Methods: A comprehensive review of the current literature was conducted, analyzing studies on SARS-CoV-2 infection in pregnancy, the expression of key viral receptors (ACE2 and TMPRSS2) in placental cells, and the immune responses involved in placental defense. The review also examined the clinical outcomes related to maternal and neonatal health, including adverse pregnancy outcomes and neonatal infection. Results: The expression of ACE2 and TMPRSS2 in the placenta supports the biological plausibility of SARS-CoV-2 transplacental transmission. Histopathological findings from the infected placentas reveal inflammation, vascular changes, and the evidence of viral particles in placental tissues. Clinical reports indicate an increased risk of preterm birth, intrauterine growth restriction, and neonatal infection in pregnancies affected by COVID-19. However, the frequency and mechanisms of vertical transmission remain variable across studies, highlighting the need for standardized research protocols. Conclusions: SARS-CoV-2 can potentially infect placental cells, leading to adverse pregnancy outcomes and neonatal infection. While evidence of transplacental transmission has been documented, the risk and mechanisms are not fully understood. Ongoing research is essential to clarify these aspects and inform obstetric care practices to improve maternal and neonatal outcomes during the COVID-19 pandemic.

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Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2

Cited by 3 publications

References 52 publications

New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs

New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs

Peptidomimetics as potent dual SARS-CoV-2 cathepsin-L and main protease inhibitors: In silico design, synthesis and pharmacological characterization

Transplacental Transmission of SARS-CoV-2: A Narrative Review

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