Evidence map›Paper›PMID 34006099›Full record

ArticleJournal of medicinal chemistry2021

Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their

Kalpana Tilekar, Jessica D Hess, Neha Upadhyay, Alessandra Lo Bianco, Markus Schweipert, Antonio Laghezza, Fulvio Loiodice, Franz-Josef Meyer-Almes, Renato J Aguilera, Antonio Lavecchia and 1 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed, 1 pooled it
2.0field-weighted citation impact, top 13% 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

19 citing papers in PubMed, 1 synthesis or guideline pooled it, 37 citations in OpenAlex.

  1. Pooled it
  2. Article
  3. Review
  4. Review
  5. Article
  6. Review
  7. Review
  8. Discovery and Characterization of Novel Non-Hydroxamate HDAC11 Inhibitors.International journal of molecular sciences · 2025
    Article
  9. Review
  10. The ChickenGenes · 2024
    Article
  11. Article
  12. Review
  13. Article
  14. Review
  15. Synthesis and Characterization of Reversible Covalent HDAC4 Inhibitors.Methods in molecular biology (Clifton, N.J.) · 2023
    Article
  16. Review
  17. Article
  18. Article
  19. Review
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

11 authors at 4 institutions in 3 countries.

Kalpana TilekarDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Navi Mumbai- 400614, India.
Jessica D HessCellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, 500 West University Avenue, El Paso, Texas 79968, United States.
Neha UpadhyayDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Navi Mumbai- 400614, India.
Alessandra Lo BiancoDepartment of Pharmacy, "Drug Discovery" Laboratory, University of Napoli "Federico II", Via D. Montesano, 49, 80131 Napoli, Italy.
Markus SchweipertDepartment of Chemical Engineering and Biotechnology, University of Applied Science, Haardtring 100, 64295 Darmstadt, Germany.
Antonio LaghezzaDepartment of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", Via E. Orabona 4, 70126 Bari, Italy.ORCID 0000-0001-6221-6155
Fulvio LoiodiceDepartment of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", Via E. Orabona 4, 70126 Bari, Italy.ORCID 0000-0003-3384-574X
Franz-Josef Meyer-AlmesDepartment of Chemical Engineering and Biotechnology, University of Applied Science, Haardtring 100, 64295 Darmstadt, Germany.ORCID 0000-0002-1001-3249
Renato J AguileraCellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, 500 West University Avenue, El Paso, Texas 79968, United States.
Antonio LavecchiaDepartment of Pharmacy, "Drug Discovery" Laboratory, University of Napoli "Federico II", Via D. Montesano, 49, 80131 Napoli, Italy.ORCID 0000-0002-2181-8026
Ramaa C SDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Navi Mumbai- 400614, India.ORCID 0000-0002-5814-3616
Bharati Vidyapeeth Deemed University · INThe University of Texas at El Paso · USUniversity of Bari Aldo Moro · ITUniversity of Naples Federico II · IT

Funding

UTEP Border Biomedical Research CenterU54MD007592 · NIMHD · UNIVERSITY OF TEXAS EL PASO · PI Gabriel Andrew Frietze · 2019 to 2026
$35.1M
TCCG12MD007592 · NIMHD · UNIVERSITY OF TEXAS EL PASO · PI KIRKEN, ROBERT A. · 2012 to 2018
$19.4M
Characterization of novel compounds with anti-lymphoma activitySC3GM103713 · NIGMS · UNIVERSITY OF TEXAS EL PASO · PI AGUILERA, RENATO J · 2013 to 2016
$453k
NIGMS NIH HHS SC3 GM103713NIMHD NIH HHS G12 MD007592NIMHD NIH HHS U54 MD007592
6 · The paper itself

Abstract

Monotargeting anticancer agents suffer from resistance and target nonspecificity concerns, which can be tackled with a multitargeting approach. The combined treatment with HDAC inhibitors and PPARγ agonists has displayed potential antitumor effects. Based on these observations, this work involves design and synthesis of molecules that can simultaneously target PPARγ and HDAC. Several out of 25 compounds inhibited HDAC4, and six compounds acted as dual-targeting agents. Compound

Indexed as

Drug DesignAnimalsAntineoplastic AgentsApoptosisBinding SitesCell Cycle CheckpointsCell Line, TumorDrug Screening Assays, AntitumorHistone DeacetylasesHumansMiceMice, SCIDMolecular Docking SimulationNeoplasmsPPAR gammaRepressor ProteinsAntineoplastic AgentsHDAC4 protein, humanHDAC8 protein, humanHistone DeacetylasesPPAR gammaRepressor ProteinsThiazolidinediones

Identifiers

PMID34006099
PMCPMC10926851
OpenAlexW3163516767

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.