The DOI matches its Crossref record; 37 of the 37 references it cites were found in a registry or an index.
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
Open accessAbstract
Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity. Development of small-molecule PD-1/PD-L1 inhibitors that could overcome these drawbacks is slow because of the incomplete structural information for this pathway. The first chemical PD-1/PD-L1 inhibitors have been recently disclosed by Bristol-Myers Squibb. Here we present NMR and X-ray characterization for the two classes of these inhibitors. The X-ray structures of the PD-L1/inhibitor complexes reveal one inhibitor molecule located at the center of the PD-L1 homodimer, filling a deep hydrophobic channel-like pocket between two PD-L1 molecules. Derivatives of (2-methyl-3-biphenylyl)methanol exhibit the structures capped on one side of the channel, whereas the compounds based on [3-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-methylphenyl]methanol induce an enlarged interaction interface that results in the open "face-back" tunnel through the PD-L1 dimer.
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Metadata
- Authors
- Guzik, K., Zak, K. M., Grudnik, P., Magiera, K., Musielak, B., Törner, R., Skalniak, L., Dömling, A., Dubin, G., & Holak, T. A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2017-06-23
- Volume
- 60
- Issue
- 13
- Pages
- 5857-5867
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2625296602
- Cited by
- 357
- References
- 37
- FWCI
- 10.02
- Type
- journal article
- Language
- en
- Open access
- green
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- Guzik, K., Zak, K. M., Grudnik, P., Magiera, K., Musielak, B., Törner, R., Skalniak, L., Dömling, A., Dubin, G., & Holak, T. A. (2017). 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. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.7b00293
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