Design, synthesis, evaluation, and SAR of 4-phenylindoline derivatives, a novel class of small-molecule inhibitors of the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) interaction

Computational methods-guided design of modulators targeting protein-protein interactions (PPIs)

(2020) Yuran Qiu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Emerging roles of allosteric modulators in the regulation of protein‐protein interactions (PPIs): A new paradigm for PPI drug discovery

(2019) Duan Ni et al.   MEDICINAL RESEARCH REVIEWS

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

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

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

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

Immune Checkpoint PD-1/PD-L1: Is There Life Beyond Antibodies?

(2018) Markella Konstantinidou et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structure-function analysis of immune checkpoint receptors to guide emerging anticancer immunotherapy

(2018) Rita Acúrcio et al.   JOURNAL OF MEDICINAL CHEMISTRY

PD-1 Blockade with Cemiplimab in Advanced Cutaneous Squamous-Cell Carcinoma

(2018) Michael R. Migden et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

Immunomodulators targeting the PD-1/PD-L1 protein-protein interaction: From antibodies to small molecules

(2018) Jeffrey Yang et al.   MEDICINAL RESEARCH REVIEWS

A Paradigm Shift in Cancer Immunotherapy: From Enhancement to Normalization

(2018) Miguel F. Sanmamed et al.   CELL

Peptide-based and small synthetic molecule inhibitors on PD-1/PD-L1 pathway: A new choice for immunotherapy?

(2018) Tingkai Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

33rd Annual Meeting & Pre-Conference Programs of the Society for Immunotherapy of Cancer (SITC 2018)

(2018)   Journal for ImmunoTherapy of Cancer

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

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

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

Biomarkers for immunotherapy in bladder cancer: a moving target

(2017) David H. Aggen et al.   Journal for ImmunoTherapy of Cancer

Immune escape to PD-L1/PD-1 blockade: seven steps to success (or failure)

(2016) J. M. Kim et al.   ANNALS OF ONCOLOGY

Immune checkpoint inhibitors: a patent review (2010-2015)

(2016) Matthieu Collin   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Atezolizumab in patients with locally advanced and metastatic urothelial carcinoma who have progressed following treatment with platinum-based chemotherapy: a single-arm, multicentre, phase 2 trial

(2016) Jonathan E Rosenberg et al.   LANCET

Avelumab in patients with chemotherapy-refractory metastatic Merkel cell carcinoma: a multicentre, single-group, open-label, phase 2 trial

(2016) Howard L Kaufman et al.   LANCET ONCOLOGY

Immune Checkpoint Targeting in Cancer Therapy: Toward Combination Strategies with Curative Potential

(2015) Padmanee Sharma et al.   CELL

PD-L1 Expression as a Predictive Biomarker in Cancer Immunotherapy

(2015) S. P. Patel et al.   MOLECULAR CANCER THERAPEUTICS

Nivolumab in Previously Untreated Melanoma without BRAF Mutation

(2015) Caroline Robert et al.   NEW ENGLAND JOURNAL OF MEDICINE

Pembrolizumab for the Treatment of Non–Small-Cell Lung Cancer

(2015) Edward B. Garon et al.   NEW ENGLAND JOURNAL OF MEDICINE