Journal article
Michael Acceptor-Based Peptidomimetic Inhibitor of Main Protease from Porcine Epidemic Diarrhea Virus
Journal of medicinal chemistry, Vol.60(7), pp.3212-3216
04/13/2017
DOI: 10.1021/acs.jmedchem.7b00103
PMID: 28287727
Abstract
Porcine epidemic diarrhea virus (PEDV) causes high mortality in pigs. PEDV main protease (M
) plays an essential role in viral replication. We solved the structure of PEDV M
complexed with peptidomimetic inhibitor N3 carrying a Michael acceptor warhead, revealing atomic level interactions. We further designed a series of 17 inhibitors with altered side groups. Inhibitors M2 and M17 demonstrated enhanced specificity against PEDV M
. These compounds have potential as future therapeutics to combat PEDV infection.
Details
- Title: Subtitle
- Michael Acceptor-Based Peptidomimetic Inhibitor of Main Protease from Porcine Epidemic Diarrhea Virus
- Creators
- Fenghua Wang - Tianjin UniversityCheng Chen - Tianjin UniversityKailin Yang - Cleveland Clinic Lerner College of MedicineYang Xu - Tianjin International Joint Academy of BiomedicineXiaomei Liu - Tianjin International Joint Academy of BiomedicineFan Gao - Tianjin International Joint Academy of BiomedicineHe Liu - Tianjin International Joint Academy of BiomedicineXia Chen - Tianjin UniversityQi Zhao - Yale UniversityXiang Liu - Tianjin International Joint Academy of BiomedicineYan Cai - Tianjin International Joint Academy of BiomedicineHaitao Yang - Tianjin International Joint Academy of Biomedicine
- Resource Type
- Journal article
- Publication Details
- Journal of medicinal chemistry, Vol.60(7), pp.3212-3216
- DOI
- 10.1021/acs.jmedchem.7b00103
- PMID
- 28287727
- ISSN
- 0022-2623
- eISSN
- 1520-4804
- Language
- English
- Date published
- 04/13/2017
- Academic Unit
- Radiation Oncology
- Record Identifier
- 9984696571002771
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