{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,18]],"date-time":"2026-05-18T10:56:54Z","timestamp":1779101814387,"version":"3.51.4"},"reference-count":78,"publisher":"MDPI AG","issue":"21","license":[{"start":{"date-parts":[[2020,11,3]],"date-time":"2020-11-03T00:00:00Z","timestamp":1604361600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"The Ministry of Science and ICT","award":["2020M3E5E2037775, 2019R1F1A1059834, 2019R1A4A1029000, and 2019R1A6A3A01097279"],"award-info":[{"award-number":["2020M3E5E2037775, 2019R1F1A1059834, 2019R1A4A1029000, and 2019R1A6A3A01097279"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>G-protein-coupled receptors (GPCR) transmit extracellular signals into cells to regulate a variety of cellular functions and are closely related to the homeostasis of the human body and the progression of various types of diseases. Great attention has been paid to GPCRs as excellent drug targets, and there are many commercially available small-molecule chemical drugs against GPCRs. Despite this, the development of therapeutic anti-GPCR antibodies has been delayed and is challenging due to the difficulty in preparing active forms of GPCR antigens, resulting from their low cellular expression and complex structures. Here, we focus on anti-GPCR antibodies that have been approved or are subject to clinical trials and present various technologies to prepare active GPCR antigens that enable the isolation of therapeutic antibodies to proceed toward clinical validation.<\/jats:p>","DOI":"10.3390\/ijms21218240","type":"journal-article","created":{"date-parts":[[2020,11,3]],"date-time":"2020-11-03T20:00:29Z","timestamp":1604433629000},"page":"8240","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":17,"title":["Antigen Design for Successful Isolation of Highly Challenging Therapeutic Anti-GPCR Antibodies"],"prefix":"10.3390","volume":"21","author":[{"given":"Man-Seok","family":"Ju","sequence":"first","affiliation":[{"name":"Department of Biomedical Sciences, Korea University College of Medicine, Seoul 02841, Korea"},{"name":"Institute of Human Genetics, Korea University College of Medicine, Seoul 02841, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7217-979X","authenticated-orcid":false,"given":"Sang Taek","family":"Jung","sequence":"additional","affiliation":[{"name":"Department of Biomedical Sciences, Korea University College of Medicine, Seoul 02841, Korea"},{"name":"Institute of Human Genetics, Korea University College of Medicine, Seoul 02841, Korea"},{"name":"Department of Biomedical Sciences, Graduate School, Korea University, Seoul 02841, Korea"},{"name":"BK21 Graduate Program, Department of Biomedical Sciences, Korea University College of Medicine, Seoul 02841, Korea"},{"name":"Biomedical Research Center, Korea University Anam Hospital, Seoul 02841, Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,11,3]]},"reference":[{"key":"ref_1","first-page":"37","article-title":"Dissection of aberrant GPCR signaling in tumorigenesis\u2014A systems biology approach","volume":"9","author":"Wu","year":"2012","journal-title":"Cancer Genom Proteom."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"2","DOI":"10.1186\/1750-2187-2-2","article-title":"Molecular mechanisms mediating the G protein-coupled receptor regulation of cell cycle progression","volume":"2","author":"New","year":"2007","journal-title":"J. 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