Small molecule inhibitors against PD-1/PD-L1 immune checkpoints and current methodologies for their development: a review

T cells expanded from renal cell carcinoma display tumor-specific CD137 expression but lack significant IFN-γ, TNF-α or IL-2 production

(2021) Saskia D. van Asten et al.   OncoImmunology

Nanoparticle Conjugation Stabilizes and Multimerizes β-Hairpin Peptides To Effectively Target PD-1/PD-L1 β-Sheet-Rich Interfaces

(2020) Woo-jin Jeong et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Kaempferol and Its Glycoside, Kaempferol 7-O-rhamnoside, Inhibit PD-1/PD-L1 Interaction In Vitro

(2020) Ji Hye Kim et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Innate Activation of IFN-γ—iNOS Axis During Infection With Salmonella Represses the Ability of T Cells to Produce IL-2

(2020) Jitender Yadav et al.   Frontiers in Immunology

Competition NMR for Detection of Hit/Lead Inhibitors of Protein–Protein Interactions

(2020) Bogdan Musielak et al.   MOLECULES

Genetically Encodable Fluorescent and Bioluminescent Biosensors Light Up Signaling Networks

(2020) Xin Zhou et al.   TRENDS IN BIOCHEMICAL SCIENCES

Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint

(2020) Magdalena Konieczny et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy

(2020) Haixia Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY

Revisiting the PD-1 pathway

(2020) Nikolaos Patsoukis et al.   Science Advances

Novel sulphamoylated 2-methoxy estradiol derivatives inhibit breast cancer migration by disrupting microtubule turnover and organization

(2019) Rustelle Janse van Vuuren et al.   Cancer Cell International

Role of the tumor microenvironment in PD-L1/PD-1-mediated tumor immune escape

(2019) Xianjie Jiang et al.   Molecular Cancer

Phenolic compounds from cultivated Glycyrrhiza uralensis and their PD-1/PD-L1 inhibitory activities

(2019) Fang Bao et al.   NATURAL PRODUCT RESEARCH

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

(2019) Hyun Lee et al.   MOLECULES

PD-1/PD-L1 pathway: Basic biology and role in cancer immunotherapy

(2019) Arash Salmaninejad et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Fragment-based screening of programmed death ligand 1 (PD-L1)

(2019) Evan Perry et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of the Inhibitors that Target the PD-1/PD-L1 Interaction—A Brief Look at Progress on Small Molecules, Peptides and Macrocycles

(2019) Guzik et al.   MOLECULES

T-Cell Engagers Based Bioassay for Evaluation of PD-1/PD-L1 Inhibitors Activity

(2019) A. N. Doronin et al.   BIOCHEMISTRY-MOSCOW

T Cell Dysfunction in Cancer Immunity and Immunotherapy

(2019) Anliang Xia et al.   Frontiers in Immunology

Immune checkpoint inhibitors of PD-L1 as cancer therapeutics

(2019) Akintunde Akinleye et al.   Journal of Hematology & Oncology

Outcomes to first-line pembrolizumab in patients with non-small-cell lung cancer and very high PD-L1 expression

(2019) E J Aguilar et al.   ANNALS OF ONCOLOGY

Structure-based derivation and intramolecular cyclization of peptide inhibitors from PD-1/PD-L1 complex interface as immune checkpoint blockade for breast cancer immunotherapy

(2019) Kun Zhou et al.   BIOPHYSICAL CHEMISTRY

Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules

(2019) Xin Lin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Immunotoxicity from checkpoint inhibitor therapy: clinical features and underlying mechanisms

(2019) Petros Fessas et al.   IMMUNOLOGY

Immune Checkpoint PD-1/PD-L1 CTLA-4/CD80 are Blocked by Rhus verniciflua Stokes and its Active Compounds

(2019) Wei Li et al.   MOLECULES

Trends in clinical development for PD-1/PD-L1 inhibitors

(2019) Jia Xin Yu et al.   NATURE REVIEWS DRUG DISCOVERY

Immune Checkpoint Blockade Mediated by a Small‐Molecule Nanoinhibitor Targeting the PD‐1/PD‐L1 Pathway Synergizes with Photodynamic Therapy to Elicit Antitumor Immunity and Antimetastatic Effects on Breast Cancer

(2019) Rui Zhang et al.   Small

Comprehensive in vitro characterization of PD-L1 small molecule inhibitors

(2019) Aravindhan Ganesan et al.   Scientific Reports

PD-1/PD-L1 inhibitor screening of caffeoylquinic acid compounds using surface plasmon resonance spectroscopy

(2018) Ya Han et al.   ANALYTICAL BIOCHEMISTRY

A versatile T cell-based assay to assess therapeutic antigen-specific PD-1-targeted approaches

(2018) Maarten Versteven et al.   Oncotarget

Tumor cells versus host immune cells: whose PD-L1 contributes to PD-1/PD-L1 blockade mediated cancer immunotherapy?

(2018) Fei Tang et al.   Cell and Bioscience

Macrocyclic Compounds from Ansamycin Antibiotic Class as Inhibitors of PD1–PDL1 Protein–Protein Interaction

(2018) Sachin P. Patil et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

A patent review on PD-1/PD-L1 antagonists: small molecules, peptides, and macrocycles (2015-2018)

(2018) Shabnam Shaabani et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Adipose PD-L1 Modulates PD-1/PD-L1 Checkpoint Blockade Immunotherapy Efficacy in Breast Cancer

(2018) Bogang Wu et al.   OncoImmunology

Analysis of PD-1 related immune transcriptional profile in different cancer types

(2018) Jun Shang et al.   Cancer Cell International

Small molecules as PD-1/PD-L1 pathway modulators for cancer immunotherapy

(2018) Peifu Jiao et al.   CURRENT PHARMACEUTICAL DESIGN

Clinical applications of PD-L1 bioassays for cancer immunotherapy

(2017) Delong Liu et al.   Journal of Hematology & Oncology

Characterization of FcγRIIIA effector cells used in in vitro ADCC bioassay: Comparison of primary NK cells with engineered NK-92 and Jurkat T cells

(2017) Yao-Te Hsieh et al.   JOURNAL OF IMMUNOLOGICAL METHODS

Cancer, checkpoint inhibitors, and confusion

(2017) Michael Fernandes et al.   LANCET ONCOLOGY

PD1 signal transduction pathways in T cells

(2017) Hugo Arasanz et al.   Oncotarget

PD-1 and PD-L1 Checkpoint Signaling Inhibition for Cancer Immunotherapy: Mechanism, Combinations, and Clinical Outcome

(2017) Hashem O. Alsaab et al.   Frontiers in Pharmacology

PD-1 expression on tumor-specific T cells: Friend or foe for immunotherapy?

(2017) Sylvain Simon et al.   OncoImmunology

PD-1/PD-L1 binding studies using microscale thermophoresis

(2017) Romain Magnez et al.   Scientific Reports

Green fluorescent protein-based assays for high-throughput functional characterization and ligand-binding studies of biotin protein ligase

(2016) Samuel P. Askin et al.   Analytical Methods

Cancer immunotherapy: the beginning of the end of cancer?

(2016) Sofia Farkona et al.   BMC Medicine

From monoclonal antibodies to small molecules: the development of inhibitors targeting the PD-1/PD-L1 pathway

(2016) Mei-Miao Zhan et al.   DRUG DISCOVERY TODAY

Safety and Efficacy of Durvalumab (MEDI4736), an Anti–Programmed Cell Death Ligand-1 Immune Checkpoint Inhibitor, in Patients With Advanced Urothelial Bladder Cancer

(2016) Christophe Massard et al.   JOURNAL OF CLINICAL ONCOLOGY

Genetic and Epigenetic Regulation of PD-1 Expression

(2016) Alexander P. R. Bally et al.   JOURNAL OF IMMUNOLOGY

Structure and Dynamics of PD-L1 and an Ultra-High-Affinity PD-1 Receptor Mutant

(2016) Roberta Pascolutti et al.   STRUCTURE

Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)

(2016) Krzysztof M. Zak et al.   Oncotarget

Anti–PD-1/PD-L1 therapy of human cancer: past, present, and future

(2015) Lieping Chen et al.   JOURNAL OF CLINICAL INVESTIGATION

Safety and Antitumor Activity of Anti–PD-1 Antibody, Nivolumab, in Patients With Platinum-Resistant Ovarian Cancer

(2015) Junzo Hamanishi et al.   JOURNAL OF CLINICAL ONCOLOGY

PD-L1 expression as a potential predictive biomarker

(2015) Alberto Fusi et al.   LANCET ONCOLOGY

Cancer immunotherapy: Strategies for personalization and combinatorial approaches

(2015) Vishwanath Sathyanarayanan et al.   Molecular Oncology

Immune-checkpoint proteins VISTA and PD-1 nonredundantly regulate murine T-cell responses

(2015) Jun Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Human cancer immunotherapy with antibodies to the PD-1 and PD-L1 pathway

(2015) Kim C. Ohaegbulam et al.   TRENDS IN MOLECULAR MEDICINE

Current advances in T-cell-based cancer immunotherapy

(2014) Mingjun Wang et al.   Immunotherapy

Presence of Suppressor HIV-Specific CD8+ T Cells Is Associated with Increased PD-1 Expression on Effector CD8+ T Cells

(2014) M. Elrefaei et al.   JOURNAL OF IMMUNOLOGY

Immune checkpoint blockade immunotherapy to activate anti-tumour T-cell immunity

(2013) Alan G. Ramsay   BRITISH JOURNAL OF HAEMATOLOGY

The PD-1/PD-L1 axis contributes to T-cell dysfunction in chronic lymphocytic leukemia

(2013) D. Brusa et al.   HAEMATOLOGICA

Adoptive T Cell Transfer for Cancer Immunotherapy in the Era of Synthetic Biology

(2013) Michael Kalos et al.   IMMUNITY

Structure and Interactions of the Human Programmed Cell Death 1 Receptor

(2013) Xiaoxiao Cheng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Role of the PD-1 Pathway in the Immune Response

(2012) L. V. Riella et al.   AMERICAN JOURNAL OF TRANSPLANTATION

The PD-1/PD-L1 Pathway in Human Pathology

(2012) M. Saresella et al.   CURRENT MOLECULAR MEDICINE

Targeting the PD-1/B7-H1(PD-L1) pathway to activate anti-tumor immunity

(2012) Suzanne L Topalian et al.   CURRENT OPINION IN IMMUNOLOGY

Targeting PD-1/PD-L1 interactions for cancer immunotherapy

(2012) Laurence Zitvogel et al.   OncoImmunology

Molecular Interaction Studies Using Microscale Thermophoresis

(2011) Moran Jerabek-Willemsen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Applications of isothermal titration calorimetry in pure and applied research-survey of the literature from 2010

(2011) Rajesh Ghai et al.   JOURNAL OF MOLECULAR RECOGNITION

Fluorescence polarization assays in small molecule screening

(2010) Wendy A Lea et al.   Expert Opinion on Drug Discovery

The PD-1 pathway in tolerance and autoimmunity

(2010) Loise M. Francisco et al.   IMMUNOLOGICAL REVIEWS

Putting the brakes on BTLA in T cell–mediated cancer immunotherapy

(2010) Chrystal M. Paulos et al.   JOURNAL OF CLINICAL INVESTIGATION

High expression of PD-L1 in lung cancer may contribute to poor prognosis and tumor cells immune escape through suppressing tumor infiltrating dendritic cells maturation

(2010) Chuan-Yong Mu et al.   MEDICAL ONCOLOGY

Protein-binding assays in biological liquids using microscale thermophoresis

(2010) Christoph J. Wienken et al.   Nature Communications

Development of a homogeneous immunoassay for the detection of angiotensin I in plasma using AlphaLISA acceptor beads technology

(2009) Elizabeth Cauchon et al.   ANALYTICAL BIOCHEMISTRY

Label-Free Detection of Biomolecular Interactions Using BioLayer Interferometry for Kinetic Characterization

(2009) Joy Concepcion et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Interactions between PD-1 and PD-L1 promote tolerance by blocking the TCR–induced stop signal

(2009) Brian T Fife et al.   NATURE IMMUNOLOGY

PD-1 and Its Ligands in Tolerance and Immunity

(2008) Mary E. Keir et al.   Annual Review of Immunology

High-field solution NMR spectroscopy as a tool for assessing protein interactions with small molecule ligands

(2008) Andria L. Skinner et al.   JOURNAL OF PHARMACEUTICAL SCIENCES