PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action

Targeting the programmed cell death protein 1/programmed cell death 1 ligand 1 (PD-1/PD-L1) interaction has become an established strategy for cancer immunotherapy. Although hundreds of small-molecule, peptide, and peptidomimetic inhibitors have been proposed in recent years, only a limited number o...

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Autores principales:	Ewa Surmiak, Katarzyna Magiera-Mularz, Bogdan Musielak, Damian Muszak, Justyna Kocik-Krol, Radoslaw Kitel, Jacek Plewka, Tad A. Holak, Lukasz Skalniak
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	PD-L1 inhibitor immune checkpoint blockade immunotherapy Biology (General) QH301-705.5 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/6efcefd2a67a44adbb40e6a90dc13b84
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id	oai:doaj.org-article:6efcefd2a67a44adbb40e6a90dc13b84
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spelling	oai:doaj.org-article:6efcefd2a67a44adbb40e6a90dc13b842021-11-11T17:14:37ZPD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action10.3390/ijms2221117971422-00671661-6596https://doaj.org/article/6efcefd2a67a44adbb40e6a90dc13b842021-10-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/21/11797https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Targeting the programmed cell death protein 1/programmed cell death 1 ligand 1 (PD-1/PD-L1) interaction has become an established strategy for cancer immunotherapy. Although hundreds of small-molecule, peptide, and peptidomimetic inhibitors have been proposed in recent years, only a limited number of drug candidates show good PD-1/PD-L1 blocking activity in cell-based assays. In this article, we compare representative molecules from different classes in terms of their PD-1/PD-L1 dissociation capacity measured by HTRF and in vitro bioactivity determined by the immune checkpoint blockade (ICB) co-culture assay. We point to recent discoveries that underscore important differences in the mechanisms of action of these molecules and also indicate one principal feature that needs to be considered, which is the eventual human PD-L1 specificity.Ewa SurmiakKatarzyna Magiera-MularzBogdan MusielakDamian MuszakJustyna Kocik-KrolRadoslaw KitelJacek PlewkaTad A. HolakLukasz SkalniakMDPI AGarticlePD-L1 inhibitorimmune checkpoint blockadeimmunotherapyBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 11797, p 11797 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	PD-L1 inhibitor immune checkpoint blockade immunotherapy Biology (General) QH301-705.5 Chemistry QD1-999
spellingShingle	PD-L1 inhibitor immune checkpoint blockade immunotherapy Biology (General) QH301-705.5 Chemistry QD1-999 Ewa Surmiak Katarzyna Magiera-Mularz Bogdan Musielak Damian Muszak Justyna Kocik-Krol Radoslaw Kitel Jacek Plewka Tad A. Holak Lukasz Skalniak PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
description	Targeting the programmed cell death protein 1/programmed cell death 1 ligand 1 (PD-1/PD-L1) interaction has become an established strategy for cancer immunotherapy. Although hundreds of small-molecule, peptide, and peptidomimetic inhibitors have been proposed in recent years, only a limited number of drug candidates show good PD-1/PD-L1 blocking activity in cell-based assays. In this article, we compare representative molecules from different classes in terms of their PD-1/PD-L1 dissociation capacity measured by HTRF and in vitro bioactivity determined by the immune checkpoint blockade (ICB) co-culture assay. We point to recent discoveries that underscore important differences in the mechanisms of action of these molecules and also indicate one principal feature that needs to be considered, which is the eventual human PD-L1 specificity.
format	article
author	Ewa Surmiak Katarzyna Magiera-Mularz Bogdan Musielak Damian Muszak Justyna Kocik-Krol Radoslaw Kitel Jacek Plewka Tad A. Holak Lukasz Skalniak
author_facet	Ewa Surmiak Katarzyna Magiera-Mularz Bogdan Musielak Damian Muszak Justyna Kocik-Krol Radoslaw Kitel Jacek Plewka Tad A. Holak Lukasz Skalniak
author_sort	Ewa Surmiak
title	PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
title_short	PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
title_full	PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
title_fullStr	PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
title_full_unstemmed	PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action
title_sort	pd-l1 inhibitors: different classes, activities, and mechanisms of action
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/6efcefd2a67a44adbb40e6a90dc13b84
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PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action

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