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Review

Molecular Interactions of Antibody Drugs Targeting PD-1, PD-L1, and CTLA-4 in Immuno-Oncology

Department of Chemistry, Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul 05029, Korea
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Author to whom correspondence should be addressed.
Academic Editor: Silvano Geremia
Molecules 2019, 24(6), 1190; https://doi.org/10.3390/molecules24061190
Received: 4 March 2019 / Revised: 22 March 2019 / Accepted: 22 March 2019 / Published: 26 March 2019
(This article belongs to the Special Issue Frontier of Protein Crystallography)
Cancer cells can evade immune surveillance through the molecular interactions of immune checkpoint proteins, including programmed death 1 (PD-1), PD-L1, and cytotoxic T lymphocyte-associated antigen 4 (CTLA-4). Since 2011, the FDA-approved antibody drugs ipilimumab (Yervoy®), nivolumab (Opdivo®), pembrolizumab (Keytruda®), cemiplimab (Libtayo®), atezolizumab (Tecentriq®), durvalumab (Imfinzi®), and avelumab (Bavencio®), which block the immune checkpoint proteins, have brought about a significant breakthrough in the treatment of a wide range of cancers, as they can induce durable therapeutic responses. In recent years, crystal structures of the antibodies against PD-1, PD-L1, and CTLA-4 have been reported. In this review, we describe the latest structural studies of these monoclonal antibodies and their interactions with the immune checkpoint proteins. A comprehensive analysis of the interactions of these immune checkpoint blockers can provide a better understanding of their therapeutic mechanisms of action. The accumulation of these structural studies would provide a basis that is essential for the rational design of next-generation therapies in immuno-oncology. View Full-Text
Keywords: crystal structure; immune checkpoint; PD-1; PD-L1; CTLA-4; cancer; therapeutic antibody crystal structure; immune checkpoint; PD-1; PD-L1; CTLA-4; cancer; therapeutic antibody
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MDPI and ACS Style

Lee, H.T.; Lee, S.H.; Heo, Y.-S. Molecular Interactions of Antibody Drugs Targeting PD-1, PD-L1, and CTLA-4 in Immuno-Oncology. Molecules 2019, 24, 1190. https://doi.org/10.3390/molecules24061190

AMA Style

Lee HT, Lee SH, Heo Y-S. Molecular Interactions of Antibody Drugs Targeting PD-1, PD-L1, and CTLA-4 in Immuno-Oncology. Molecules. 2019; 24(6):1190. https://doi.org/10.3390/molecules24061190

Chicago/Turabian Style

Lee, Hyun T., Sang H. Lee, and Yong-Seok Heo. 2019. "Molecular Interactions of Antibody Drugs Targeting PD-1, PD-L1, and CTLA-4 in Immuno-Oncology" Molecules 24, no. 6: 1190. https://doi.org/10.3390/molecules24061190

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