Insights into non-peptide small-molecule inhibitors of the PD-1/PD-L1 interaction: Development and perspective

Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1

(2020) Binbin Cheng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

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

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

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

(2019) Hyun Lee et al.   MOLECULES

Discovery of [1,2,4]Triazolo[4,3-a]pyridines as Potent Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction

(2019) Mingze Qin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, Evaluation, and Structural Studies of C2-Symmetric Small Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein–Protein Interaction

(2019) Subhadwip Basu et al.   JOURNAL OF MEDICINAL CHEMISTRY

CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not?

(2019) Bogdan Musielak et al.   MOLECULES

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

(2019) William Farnaby et al.   Nature Chemical Biology

In Vitro Assessment of Putative PD-1/PD-L1 Inhibitors: Suggestions of an Alternative Mode of Action

(2019) Derek J. Blevins et al.   ACS Medicinal Chemistry Letters

Discovery of the programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing an indoline scaffold

(2019) Mingze Qin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Promising approaches in cancer immunotherapy

(2019) Nima Taefehshokr et al.   IMMUNOBIOLOGY

Comprehensive in vitro characterization of PD-L1 small molecule inhibitors

(2019) Aravindhan Ganesan et al.   Scientific Reports

Lessons learned from the blockade of immune checkpoints in cancer immunotherapy

(2018) Xiaolei Li et al.   Journal of Hematology & Oncology

Nivolumab plus Ipilimumab in Lung Cancer with a High Tumor Mutational Burden

(2018) Matthew D. Hellmann et al.   NEW ENGLAND JOURNAL OF MEDICINE

Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-ligand 1 Signaling Pathway

(2018) Tianyu Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

STAT3 Induces Immunosuppression by Upregulating PD-1/PD-L1 in HNSCC

(2017) L.L. Bu et al.   JOURNAL OF DENTAL RESEARCH

Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1

(2017) Katarzyna Guzik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

COX2/mPGES1/PGE2pathway regulates PD-L1 expression in tumor-associated macrophages and myeloid-derived suppressor cells

(2017) Victor Prima et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2

(2017) Krzysztof M. Zak et al.   STRUCTURE

Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells

(2017) Lukasz Skalniak et al.   Oncotarget

Immunotherapy of cancer: from monoclonal to oligoclonal cocktails of anti-cancer antibodies: IUPHAR Review 18

(2016) Silvia Carvalho et al.   BRITISH JOURNAL OF PHARMACOLOGY

Mutational Landscape and Sensitivity to Immune Checkpoint Blockers

(2016) R. M. Chabanon et al.   CLINICAL CANCER RESEARCH

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted Therapy and Checkpoint Immunotherapy Combinations for the Treatment of Cancer

(2016) Paul E. Hughes et al.   TRENDS IN IMMUNOLOGY

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

(2016) Krzysztof M. Zak et al.   Oncotarget

Immune Checkpoint Blockade: A Common Denominator Approach to Cancer Therapy

(2015) Suzanne L. Topalian et al.   CANCER CELL

Control of PD-L1 Expression by Oncogenic Activation of the AKT–mTOR Pathway in Non–Small Cell Lung Cancer

(2015) Kristin J. Lastwika et al.   CANCER RESEARCH

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1

(2015) Krzysztof M. Zak et al.   STRUCTURE

Inducible but Not Constitutive Expression of PD-L1 in Human Melanoma Cells Is Dependent on Activation of NF-κB

(2015) Kavitha Gowrishankar et al.   PLoS One

Paclitaxel Induced B7-H1 Expression in Cancer Cells via the MAPK Pathway

(2014) Wenrong Gong et al.   JOURNAL OF CHEMOTHERAPY

PD-L1 is a novel direct target of HIF-1α, and its blockade under hypoxia enhanced MDSC-mediated T cell activation

(2014) Muhammad Zaeem Noman et al.   JOURNAL OF EXPERIMENTAL MEDICINE

The role of PD-1 and PD-L1 in T-cell immune suppression in patients with hematological malignancies

(2013) Li Shi et al.   Journal of Hematology & Oncology

Anti-TIM3 Antibody Promotes T Cell IFN- -Mediated Antitumor Immunity and Suppresses Established Tumors

(2011) S. F. Ngiow et al.   CANCER RESEARCH

Immune Inhibitory Molecules LAG-3 and PD-1 Synergistically Regulate T-cell Function to Promote Tumoral Immune Escape

(2011) S.-R. Woo et al.   CANCER RESEARCH

Cancer immunotherapy comes of age

(2011) Ira Mellman et al.   NATURE

Ipilimumab

(2011) Vernon K. Sondak et al.   NATURE REVIEWS DRUG DISCOVERY

Disrupting protein–protein interactions with non-peptidic, small molecule α-helix mimetics

(2010) Christopher G Cummings et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

A dimeric structure of PD-L1: functional units or evolutionary relics?

(2010) Yong Chen et al.   Protein & Cell

PD-1 and Its Ligands in Tolerance and Immunity

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

The PD-1/PD-L1 complex resembles the antigen-binding Fv domains of antibodies and T cell receptors

(2008) D. Y.-w. Lin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA