Chemical synthesis and structural analysis of guanylate cyclase C agonist linaclotide
文献类型：期刊论文
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2018 |
| 卷号 | 29 |
| ISSN号 | 1001-8417 |
| 关键词 | IRRITABLE-BOWEL-SYNDROME RACEMIC PROTEIN CRYSTALLOGRAPHY X-RAY STRUCTURES GASTROINTESTINAL-TRACT PREVALENCE LIGATION PATTERNS IMPACT Linaclotide Guanylyl cyclase Protein chemical synthesis Fmoc solid phase peptide synthesis Racemic crystallization |
| 英文摘要 | Guanylate cyclase C (GC-C) is an important receptor protein expressed by intestinal epithelial cells, and its dysregulation leads to severe intestinal diseases. Linaclotide is a 14-amino acid peptide approved by the FDA for the treatment of irritable bowel syndrome with constipation (IBS-C), which activates guanylate cyclase C to accelerate intestinal transit. Drug molecule design based on structural information plays a crucial role and the activity of linaclotide still need to improve, while the structure of linaclotide remains unknown. In this work, linaclotide and its D-enantiomer were obtained through Fmoc solid phase peptide synthesis method and co-crystalized through racemic crystallization. The crystal structure showed that linaclotide has a tight, three-beta turns structure immobilized by three pairs of disulfide bonds. (C) 2018 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved. |
| 资助项目 | [National Natural Science Foundation of China (NSFC)] ; [Fundamental Research Funds for the Central Universities] |
| 语种 | 英语 |
| CSCD记录号 | CSCD:6275732 |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/63642]  |
| 专题 | 中国科学院合肥物质科学研究院 |
| 推荐引用方式 GB/T 7714 | . Chemical synthesis and structural analysis of guanylate cyclase C agonist linaclotide[J]. CHINESE CHEMICAL LETTERS,2018,29. |
| APA | (2018).Chemical synthesis and structural analysis of guanylate cyclase C agonist linaclotide.CHINESE CHEMICAL LETTERS,29. |
| MLA | "Chemical synthesis and structural analysis of guanylate cyclase C agonist linaclotide".CHINESE CHEMICAL LETTERS 29(2018). |
入库方式： OAI收割
来源：合肥物质科学研究院
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