{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T01:16:15Z","timestamp":1760145375932,"version":"build-2065373602"},"reference-count":35,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2024,7,24]],"date-time":"2024-07-24T00:00:00Z","timestamp":1721779200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Key Research and Development Program of China","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"China National Nuclear Corporation","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"Chinese Academy of Sciences","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"Fujian Provincial Natural Fund","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"CAST","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"XIAMEN Autonomously Deployment Project","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"Talent Project of Longyuan (Gansu province)","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]},{"name":"Youth Innovation and Entrepreneurship","award":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"],"award-info":[{"award-number":["YFB3504302","ZDRW-CN-2021-3","E223221YXB","J05101","YESS20210336","GG03","E139222SR0"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>The process of synthesizing radionuclide-coupled drugs, especially shutdown technology that links bipotent chelators with biomolecules, utilizes traditional coupling reactions, including emerging click chemistry; these reactions involve different drawbacks, such as complex and cumbersome reaction steps, long reaction times, and the use of catalysts at various pH values, which can negatively impact the effects of the chelating agent. To address the above problems in this study, This research designed a novel bipotent chelator coupled with peptides. In the present study, dichloromethane was used as a solvent, and the reaction was conducted at room temperature for 12 h. A one-step ring-opening method was employed to introduce the coupling functional group of tridentate amide acid. The coupling materials consisted of the amino active site of the peptide and diethylene glycol anhydride. In this paper, this study explored the reactions between different equivalents of acid anhydride coupled to the peptide (peptide sequence: HLRKLRKR) and determined that the maximum conversion of the peptide feedstock was 87%. To determine the selectivity of the reaction sites in this polypeptide, This study identified the peptide sequence at the reaction site using nuclear magnetic resonance (NMR) and liquid chromatography\u2013mass spectrometry (LC-MS). For the selected peptide, the first reactive site was on the terminal amino group, followed by the amino group on the tetra- and hepta-lysine side chains. The tridentate amic acid framework functions as a chelating agent, capable of binding a range of lanthanide ions. This significantly reduces and optimizes the time and cost associated with synthesizing radionuclide-coupled drugs.<\/jats:p>","DOI":"10.3390\/ph17080981","type":"journal-article","created":{"date-parts":[[2024,7,25]],"date-time":"2024-07-25T08:40:04Z","timestamp":1721896804000},"page":"981","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Development of a Novel, Easy-to-Prepare, and Potentially Valuable Peptide Coupling Technology Utilizing Amide Acid as a Linker"],"prefix":"10.3390","volume":"17","author":[{"given":"Yaling","family":"Wang","sequence":"first","affiliation":[{"name":"College of Chemistry and Materials Science, Fujian Normal University, Fuzhou 350117, China"},{"name":"Xiamen Institute of Rare Earth Materials, Haixi Institute, Chinese Academy of Sciences, Xiamen 361021, China"},{"name":"Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5972-5466","authenticated-orcid":false,"given":"Fan","family":"Yang","sequence":"additional","affiliation":[{"name":"Xiamen Institute of Rare Earth Materials, Haixi Institute, Chinese Academy of Sciences, Xiamen 361021, China"},{"name":"Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China"},{"name":"Fujian Science & Technology Innovation Laboratory for Optoelectronic Information of China, Fuzhou 350108, China"},{"name":"Xiamen Key-Laboratory of Rare Earth Photoelectric Functional Materials, Xiamen 361021, China"},{"name":"Key Laboratory of Rare Earths, Chinese Academy of Sciences, China Rare Earth Group Research Institute, Ganzhou 341000, China"},{"name":"Fujian Province Joint Innovation Key Laboratory of Fuel and Materials in Clean Nuclear Energy System, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China"},{"name":"Key Laboratory of Rare Earths, Ganjiang Innovation Academy, Chinese Academy of Sciences, Ganzhou 341000, China"},{"name":"Xiamen Key Laboratory of Rare Earth Photoelectric Functional Materials, Xiamen Institute of Rare Earth Materials, Haixi Institute, Chinese Academy of Sciences, Xiamen 361021, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hongyan","family":"Li","sequence":"additional","affiliation":[{"name":"Department of Medical Physics, Institute of Modern Physics, Chinese Academy of Sciences, Lanzhou 730000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2024,7,24]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"2001974","DOI":"10.1002\/adhm.202001974","article-title":"Polypeptides\u2013Drug Conjugates for Anticancer Therapy","volume":"10","author":"Zhang","year":"2021","journal-title":"Adv. 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