Evidence map›Paper›PMID 34199417›Full record

ArticleMolecules (Basel, Switzerland)2021

Discovery of Novel Small-Molecule Inhibitors of PD-1/PD-L1 Interaction via Structural Simplification Strategy.

Hongbo Zhang, Yu Xia, Chunqiu Yu, Huijie Du, Jinchang Liu, Hui Li, Shihui Huang, Qihua Zhu, Yungen Xu, Yi Zou

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
2.1field-weighted citation impact, top 10% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

18 citing papers in PubMed, 24 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Novel PD-L1 Small-Molecule Inhibitors Advancing Cancer Immunotherapy.Anti-cancer agents in medicinal chemistry · 2026
    Review
  5. Article
  6. Article
  7. Article
  8. Review
  9. Review
  10. Review
  11. Review
  12. Review
  13. Review
  14. Review
  15. Generation, secretion and degradation of cancer immunotherapy target PD-L1.Cellular and molecular life sciences : CMLS · 2022
    Review
  16. Article
  17. Review
  18. PD-L1 Inhibitors: Different Classes, Activities, and Mechanisms of Action.International journal of molecular sciences · 2021
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 1 institution in 1 country.

Hongbo ZhangState Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Yu XiaJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Chunqiu YuJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Huijie DuJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Jinchang LiuJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Hui LiJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Shihui HuangJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Qihua ZhuState Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Yungen XuState Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Yi ZouJiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
China Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Blockade of the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction is currently the focus in the field of cancer immunotherapy, and so far, several monoclonal antibodies (mAbs) have achieved encouraging outcomes in cancer treatment. Despite this achievement, mAbs-based therapies are struggling with limitations including poor tissue and tumor penetration, long half-life time, poor oral bioavailability, and expensive production costs, which prompted a shift towards the development of the small-molecule inhibitors of PD-1/PD-L1 pathways. Even though many small-molecule inhibitors targeting PD-1/PD-L1 interaction have been reported, their development lags behind the corresponding mAb, partly due to the challenges of developing drug-like small molecules. Herein, we report the discovery of a series of novel inhibitors targeting PD-1/PD-L1 interaction via structural simplification strategy by using BMS-1058 as a starting point. Among them, compound

Indexed as

B7-H1 AntigenCell LineCrystallography, X-RayHumansInterferon-gammaModels, MolecularMolecular Docking SimulationMolecular StructurePrimary Cell CultureProgrammed Cell Death 1 ReceptorProtein BindingSmall Molecule LibrariesStructure-Activity RelationshipT-LymphocytesB7-H1 AntigenCD274 protein, humanIFNG protein, humanInterferon-gammaPDCD1 protein, humanProgrammed Cell Death 1 ReceptorSmall Molecule LibrariesPD-1/PD-L1small molecule PD-1/PD-L1 inhibitorstructural simplification strategy

Identifiers

PMID34199417
PMCPMC8199613
OpenAlexW3169107069

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.