Related Experiment Video

Updated: Mar 29, 2026

Co-immunoprecipitation Assay for Studying Functional Interactions Between Receptors and Enzymes
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Published on: September 28, 2018

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

Krzysztof M Zak1, Radoslaw Kitel2, Sara Przetocka1

  • 1Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Gronostajowa 7, 30-387 Krakow, Poland; Malopolska Centre of Biotechnology, Jagiellonian University, Gronostajowa 7a, 30-387 Krakow, Poland.

Structure (London, England : 1993)
|November 26, 2015
PubMed

Insights

Small-molecule drugs targeting the PD-1/PD-L1 pathway show promise for cancer treatment. This study provides crucial structural insights into the human PD-1/PD-L1 complex, paving the way for new drug development.

Area of Science:

  • Immunology
  • Structural Biology
  • Drug Discovery

Background:

  • Monoclonal antibodies targeting the PD-1/PD-L1 checkpoint have advanced cancer therapy.
  • Development of small-molecule inhibitors is limited by a lack of structural data.

Purpose of the Study:

  • To elucidate the molecular details of the human PD-1/PD-L1 interaction.
  • To provide a structural basis for small-molecule drug design targeting this pathway.

Main Methods:

  • X-ray crystallography of the human PD-1/PD-L1 complex.

Main Results:

  • The study reveals significant receptor plasticity upon ligand binding.
  • A detailed molecular map of the PD-1/PD-L1 interaction surface was generated.

Conclusions:

  • Structural insights into the human PD-1/PD-L1 interaction are crucial for developing small-molecule inhibitors.
  • Specific regions on both PD-1 and PD-L1 are identified as potential targets for small-molecule drugs.

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