Evidence map›Paper›PMID 37803138›Full record

ReviewActa pharmacologica Sinica2024

Development of PI3Kγ selective inhibitors: the strategies and application.

Dong-Yan Gu, Meng-Meng Zhang, Jia Li, Yu-Bo Zhou, Rong Sheng

Open access · greenAbstract readReview
In one paragraph

Review in Acta pharmacologica Sinica, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.8field-weighted citation impact, top 27% 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

7 citing papers in PubMed, 5 citations in OpenAlex.

  1. Review
  2. Engineering selective PI3KActa pharmaceutica Sinica. B · 2026
    Article
  3. Review
  4. Review
  5. Evaluation ofMolecules (Basel, Switzerland) · 2025
    Article
  6. Article
  7. 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

5 authors at 3 institutions in 1 country.

Dong-Yan GuCollege of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Meng-Meng ZhangNational Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Jia LiNational Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Yu-Bo ZhouNational Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Rong ShengCollege of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China. shengr@zju.edu.cn.
Shanghai Institute of Materia Medica · CNZhejiang University · CNNational Center for Drug Screening · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The γ isoform of Class I PI3Ks (PI3Kγ) is primarily found in leukocytes and is essential for the function of myeloid cells, as it regulates the migration, differentiation, and activation of myeloid-lineage immune cells. Thus, PI3Kγ has been identified as a promising drug target for the treatment of inflammation, autoimmune disease, and immuno-oncology. Due to the high incidence of serious adverse events (AEs) associated with PI3K inhibitors, in the development of PI3Kγ inhibitors, isoform selectivity was deemed crucial. In this review, an overview of the development of PI3Kγ selective inhibitors in the past years is provided. The isoform selectivity of related drugs was achieved by different strategies, including inducing a specificity pocket by a propeller-shape structure, targeting steric differences in the solvent channel, and modulating the conformation of the Asp-Phe-Gly DFG motif, which have been demonstrated feasible by several successful cases. The insights in this manuscript may provide a potential direction for rational drug design and accelerate the discovery of PI3Kγ selective inhibitors.

Indexed as

Autoimmune DiseasesPhosphatidylinositol 3-KinasesHumansInflammationPhosphoinositide-3 Kinase InhibitorsProtein IsoformsPhosphatidylinositol 3-KinasesPhosphoinositide-3 Kinase InhibitorsProtein Isoformsdrug developmentisoform selectivityPI3KPI3Kγ inhibitorsrational drug design

Identifiers

PMID37803138
PMCPMC10789806
OpenAlexW4387403865

What Socratic holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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 Socratic graph.