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Introduction
Molecular and cellular functions of CTLA-4 pathway
Roles of PD-1/PD-L1 pathway: signaling, cancer, and beyond
Discovery of new immune checkpoints: family grows up
Mechanisms of resistance to checkpoint blockade therapy
Molecular events behind adverse effects
Rational discovery of response biomarkers
Spatiotemporal changes in checkpoint molecule expression
Functions of checkpoint molecules beyond immune evasion
Genetic alterations and checkpoint expression
Regulations on messenger RNA: wires and nodes
Folded or degraded in endoplasmic reticulum
Mono- and poly-ubiquitination: tags for fates
Lysosome as the black hole for checkpoint molecules
Phosphorylation: a fast switch for checkpoint signalling
Palmitoylation as a signal for delivery
Checkpoints under traffic control: from and to organelles
Exosome and secretion: action on?
Macromolecules and antibody-based drugs
Mechanisms inspired targeting peptides
Small molecular inhibitors
Therapeutic development of immune checkpoint blockers
Concluding remarks.

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