Design, Synthesis, and Structure–Activity Relationship Study of μ-Conotoxin KIIIA toward Na <sub>V</sub> 1.4
studies confirmed that both [S5R]KA and C4Pen induce potent muscle relaxation. This structure-based optimization combines electrostatic mutagenesis with Pen-mediated stabilization, yielding a promising peptide therapeutic candidate.
Authors
- Guanzhao Wu (ORCID: https://orcid.org/0000-0002-8170-7993)
- YL Zhou (ORCID: https://orcid.org/0009-0001-1491-2479)
- Teng Pan (ORCID: https://orcid.org/0000-0003-1384-9006)
- Na Wang (ORCID: https://orcid.org/0000-0001-9552-0524)
- Zixuan Zhang (ORCID: https://orcid.org/0009-0006-8619-920X)
- Xue Song
- Xiao Li
- Tao Jiang
- Wei Wang
Institutions
- Binzhou Medical University (CN)
- Shandong University of Aeronautics (CN)
- China Pharmaceutical University (CN)
- Peking University (CN)
- Qingdao National Laboratory for Marine Science and Technology (CN)
- Qilu Hospital of Shandong University (CN)
- Ocean University of China (CN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-03-31
- DOI
- https://doi.org/10.1021/acs.jmedchem.5c03142
- Primary Topic
- Nicotinic Acetylcholine Receptors Study
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Qingdao National Laboratory for Marine Science and Technology
- Major Scientific and Technological Innovation Project of Shandong Province
- National Health and Medical Research Council
- Fundamental Research Funds for the Central Universities