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Published on: March 24, 2017
[Development of peptidic MERS-CoV entry inhibitors]
Abstract:
In 2012, a new SARS-like coronavirus emerged in the Middle East, namely the Middle East respiratory syndrome coronavirus (MERS-CoV). It has caused outbreaks with high mortality. During infection of target cell, MERS-CoV S protein S1 subunit binds to the cellular receptor (DPP4), and its S2 subunit HR1 and HR2 regions intact with each other to form a stable six-helix bundle to mediate the fusion between virus and target cell membranes. Hence, blocking the process of six-helix bundle formation can effectively inhibit MERS-CoV entry into the target cells. This review focuses on the recent advance in the development of peptidic entry inhibitors targeting the MERS-CoV S2 subunit.
Insights
Middle East respiratory syndrome coronavirus (MERS-CoV) entry into cells involves S protein binding to DPP4 and forming a six-helix bundle. Peptidic inhibitors targeting the MERS-CoV S2 subunit show promise in blocking viral entry.
Area of Science:
- Virology
- Infectious Diseases
- Drug Discovery
Background:
- Middle East respiratory syndrome coronavirus (MERS-CoV), a SARS-like virus, emerged in 2012 and has caused high-mortality outbreaks.
- MERS-CoV infection relies on its S protein; the S1 subunit binds the DPP4 receptor, while the S2 subunit mediates membrane fusion via a six-helix bundle.
Purpose of the Study:
- To review recent advancements in developing peptidic entry inhibitors.
- To focus on inhibitors targeting the MERS-CoV S2 subunit's six-helix bundle formation.
Main Methods:
- Literature review of recent research on MERS-CoV entry inhibitors.
- Analysis of studies focusing on peptidic inhibitors targeting the MERS-CoV S2 subunit.
Main Results:
- The formation of a stable six-helix bundle by the MERS-CoV S2 subunit's HR1 and HR2 regions is crucial for viral entry.
- Blocking this six-helix bundle formation is a viable strategy to inhibit MERS-CoV cell entry.
- Recent progress has been made in developing peptidic inhibitors targeting this mechanism.
Conclusions:
- Peptidic inhibitors targeting the MERS-CoV S2 subunit represent a promising therapeutic strategy.
- Inhibition of the six-helix bundle formation effectively blocks MERS-CoV entry into host cells.
- Further research into these peptidic inhibitors could lead to effective treatments for MERS-CoV infections.
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