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As an important chemical biology tool, bioorthogonal reactions have been applied broadly in biomedicine, including bio-labeling, nucleic acid functionalization, drug discovery, drug activation, synthesis of antibody\u2013drug conjugates, and proteolysis-targeting chimeras. Given this, we summarized the basic knowledge, development history, research status, and prospects of bioorthogonal reactions and their biomedical applications. The main purpose of this paper is to furnish an overview of the intriguing bioorthogonal reactions in a variety of biomedical applications and to provide guidance for the design of novel reactions to enrich bioorthogonal chemistry toolkits.<\/jats:p>","DOI":"10.34133\/research.0251","type":"journal-article","created":{"date-parts":[[2023,10,2]],"date-time":"2023-10-02T19:23:03Z","timestamp":1696274583000},"update-policy":"https:\/\/doi.org\/10.34133\/aaas_crossmark_01","source":"Crossref","is-referenced-by-count":23,"title":["Designing Bioorthogonal Reactions for Biomedical Applications"],"prefix":"10.34133","volume":"6","author":[{"given":"Qingfei","family":"Zhang","sequence":"first","affiliation":[{"name":"Wenzhou Institute, \rUniversity of Chinese Academy of Sciences, Wenzhou 325001, China."},{"name":"Beijing National Laboratory for Condensed Matter Physics, Institute of Physics, \rChinese Academy of Sciences, Beijing 100190, China."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gaizhen","family":"Kuang","sequence":"additional","affiliation":[{"name":"Wenzhou Institute, \rUniversity of Chinese Academy of Sciences, Wenzhou 325001, China."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Li","family":"Wang","sequence":"additional","affiliation":[{"name":"Wenzhou Institute, \rUniversity of Chinese Academy of Sciences, Wenzhou 325001, China."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ping","family":"Duan","sequence":"additional","affiliation":[{"name":"Department of Obstetrics and Gynecology, The Second Affiliated Hospital and Yuying Children\u2019s Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5789-1287","authenticated-orcid":true,"given":"Weijian","family":"Sun","sequence":"additional","affiliation":[{"name":"Wenzhou Institute, \rUniversity of Chinese Academy of Sciences, Wenzhou 325001, China."},{"name":"Department of Gastrointestinal Surgery, The Second Affiliated Hospital and Yuying Children\u2019s Hospital of Wenzhou Medical University, Wenzhou, 325027, China."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fangfu","family":"Ye","sequence":"additional","affiliation":[{"name":"Wenzhou Institute, \rUniversity of Chinese Academy of Sciences, Wenzhou 325001, China."},{"name":"Beijing National Laboratory for Condensed Matter Physics, Institute of Physics, \rChinese Academy of Sciences, Beijing 100190, China."}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"221","published-online":{"date-parts":[[2023,12,15]]},"reference":[{"issue":"1","key":"e_1_3_2_2_2","doi-asserted-by":"crossref","first-page":"30","DOI":"10.1038\/s43586-021-00028-z","article-title":"Bioorthogonal chemistry","volume":"1","author":"Scinto SL","year":"2021","unstructured":"Scinto SL, Bilodeau DA, Hincapie R, Lee W, Nguyen SS, Xu M, Am Ende CW, Finn MG, Lang K, Lin Q, et al. 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