Antigen design for successful isolation of highly challenging therapeutic anti-gpcr antibodies

Man Seok Ju, Sang Taek Jung

Research output: Contribution to journalReview articlepeer-review

10 Citations (Scopus)


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.

Original languageEnglish
Article number8240
Pages (from-to)1-14
Number of pages14
JournalInternational journal of molecular sciences
Issue number21
Publication statusPublished - 2020 Nov 1

Bibliographical note

Funding Information:
This work was supported by grants from the Bio & Medical Technology Development Program (2020M3E5E2037775) and the Basic Science Research Programs (2019R1F1A1059834, 2019R1A4A1029000, and 2019R1A6A3A01097279) through the National Research Foundation of Korea, funded by the Ministry of Science and ICT and by the Ministry of Education, and by a Korea National Institute of Health fund (2020-ER5311-00).

Publisher Copyright:
© 2020 by the authors. Licensee MDPI, Basel, Switzerland.


  • Antigen
  • G protein-coupled receptor
  • Membrane protein
  • Therapeutic antibody

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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