Substitution of D-Arginine at Position 11 of & alpha;-RgIA Potently Inhibits & alpha;7 Nicotinic Acetylcholine Receptor
文献类型：期刊论文
| 作者 | Wu, Yong2; Zhang, Junjie2; Ren, Jie2; Zhu, Xiaopeng2; Li, Rui3; Zhangsun, Dongting1,2; Luo, Sulan1,2 |
| 刊名 | MARINE DRUGS
 |
| 出版日期 | 2023-06-01 |
| 卷号 | 21期号:6页码:13 |
| 关键词 | conotoxin peptide synthesis CD structure electrophysiology nicotinic acetylcholine receptors |
| DOI | 10.3390/md21060326 |
| 通讯作者 | Wu, Yong(wuyong@gxu.edu.cn) ; Luo, Sulan(sulan2021@gxu.edu.cn) |
| 英文摘要 | Conotoxins are a class of disulfide-rich peptides found in the venom of cone snails, which have attracted considerable attention in recent years due to their potent activity on ion channels and potential for therapeutics. Among them, & alpha;-conotoxin RgIA, a 13-residue peptide, has shown great promise as a potent inhibitor of & alpha;9 & alpha;10 nAChRs for pain management. In this study, we investigated the effect of substituting the naturally occurring L-type arginine at position 11 of the RgIA sequence with its D-type amino acid. Our results indicate that this substitution abrogated the ability of RgIA to block & alpha;9 & alpha;10 nAChRs, but instead endowed the peptide with the ability to block & alpha;7 nAChR activity. Structural analyses revealed that this substitution induced significant alteration of the secondary structure of RgIA[11r], which consequently affected its activity. Our findings underscore the potential of D-type amino acid substitution as a promising strategy for designing novel conotoxin-based ligands targeting different types of nAChRs. |
| WOS关键词 | ACCURATE DOCKING ; CONOTOXIN ; BLOCKS ; RAT ; ALPHA-4/7-CONOTOXIN ; ALPHA-3-BETA-2 ; DISCOVERY ; GLIDE |
| 资助项目 | National Natural Science Foundation of China[32170534] ; Guangxi Science and Technology Base and Talent Special Project[2021AC19001] ; Guangxi Science and Technology Base amp; Talents Fund[GUIKE AD22035948] ; Major Intergovernmental Joint Research Project of National Key R amp; D Program of China[2022YFE0132700] ; 111 Project[D20010] ; Innovation Project of Guangxi Graduate Education[YCSW2022072] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | MDPI |
| WOS记录号 | WOS:001015280200001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306373]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wu, Yong; Luo, Sulan |
| 作者单位 | 1.Hainan Univ, Key Lab Trop Biol Resources, Minist Educ, Haikou 570228, Peoples R China 2.Guangxi Univ, Sch Med, Nanning 530004, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wu, Yong,Zhang, Junjie,Ren, Jie,et al. Substitution of D-Arginine at Position 11 of & alpha;-RgIA Potently Inhibits & alpha;7 Nicotinic Acetylcholine Receptor[J]. MARINE DRUGS,2023,21(6):13. |
| APA | Wu, Yong.,Zhang, Junjie.,Ren, Jie.,Zhu, Xiaopeng.,Li, Rui.,...&Luo, Sulan.(2023).Substitution of D-Arginine at Position 11 of & alpha;-RgIA Potently Inhibits & alpha;7 Nicotinic Acetylcholine Receptor.MARINE DRUGS,21(6),13. |
| MLA | Wu, Yong,et al."Substitution of D-Arginine at Position 11 of & alpha;-RgIA Potently Inhibits & alpha;7 Nicotinic Acetylcholine Receptor".MARINE DRUGS 21.6(2023):13. |
入库方式： OAI收割
来源：上海药物研究所
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