Evidence map›Paper›PMID 36973833›Full record

ArticleAngewandte Chemie (International ed. in English)2023

Small Molecule Degraders of Protein Tyrosine Phosphatase 1B and T-Cell Protein Tyrosine Phosphatase for Cancer Immunotherapy.

Jiajun Dong, Jinmin Miao, Yiming Miao, Zihan Qu, Sheng Zhang, Peipei Zhu, Florian Wiede, Brenson A Jassim, Yunpeng Bai, Quyen Nguyen and 5 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
8.0field-weighted citation impact, top 2% 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

24 citing papers in PubMed, 52 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Review
  5. Review
  6. Article
  7. Review
  8. Review
  9. Review
  10. Article
  11. Article
  12. Article
  13. Review
  14. Review
  15. Review
  16. Review
  17. Review
  18. Article
  19. Review
  20. 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

15 authors at 2 institutions in 2 countries.

Jiajun DongDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Jinmin MiaoDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Yiming MiaoDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Zihan QuDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Sheng ZhangDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Peipei ZhuDepartment of Biochemistry, Purdue University, West Lafayette, IN 47907, USA.
Florian WiedeMonash Biomedicine Discovery Institute, Monash University, Clayton, Victoria, 3800, Australia.
Brenson A JassimDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Yunpeng BaiDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Quyen NguyenDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Jianping LinDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Lan ChenInstitute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.
Tony TiganisMonash Biomedicine Discovery Institute, Monash University, Clayton, Victoria, 3800, Australia.
W Andy TaoDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Zhong-Yin ZhangDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.ORCID 0000-0001-5527-7910
Purdue University West Lafayette · USDiscovery Institute · US

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI Andrea L Kasinski · 1985 to 2026
$43.4M
Structure/Function of Protein Tyrosine PhosphatasesR01CA069202 · NCI · YESHIVA UNIVERSITY · PI Zhong-Yin Zhang · 1996 to 2026
$7.3M
Dissecting signaling pathways and seeking EV phosphoproteins as novel biomarkers for Alzheimer's DiseaseRF1AG064250 · NIA · PURDUE UNIVERSITY · PI TAO, W. ANDY · 2020 to 2021
$1.7M
NCI NIH HHS P30 CA023168NCI NIH HHS R01 CA069202NIA NIH HHS RF1 AG064250
6 · The paper itself

Abstract

Protein tyrosine phosphatase 1B (PTP1B) and T-cell protein tyrosine phosphatase (TC-PTP) play non-redundant negative regulatory roles in T-cell activation, tumor antigen presentation, insulin and leptin signaling, and are potential targets for several therapeutic applications. Here, we report the development of a highly potent and selective small molecule degrader DU-14 for both PTP1B and TC-PTP. DU-14 mediated PTP1B and TC-PTP degradation requires both target protein(s) and VHL E3 ligase engagement and is also ubiquitination- and proteasome-dependent. DU-14 enhances IFN-γ induced JAK1/2-STAT1 pathway activation and promotes MHC-I expression in tumor cells. DU-14 also activates CD8

Indexed as

NeoplasmsProtein Tyrosine Phosphatase, Non-Receptor Type 2CD8-Positive T-LymphocytesHumansImmunotherapyPhosphorylationProtein Tyrosine Phosphatase, Non-Receptor Type 1Tyramine4-O-(sulfamoyl)-N-tetradecanoyltyramineProtein Tyrosine Phosphatase, Non-Receptor Type 1Protein Tyrosine Phosphatase, Non-Receptor Type 2TyramineImmunotherapyPROTAC DegraderPTP1BTC-PTP

Identifiers

PMID36973833
PMCPMC10196813
OpenAlexW4361191216

What OpenQuestion holds

Textmetadata
LicenceTDM
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 OpenQuestion graph.