Evidence map›Paper›PMID 25899338›Full record

ArticleEuropean journal of medicinal chemistry2015

Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.

Quaovi H Sodji, James R Kornacki, John F McDonald, Milan Mrksich, Adegboyega K Oyelere

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

Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.8field-weighted citation impact, top 15% 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

10 citing papers in PubMed, 32 citations in OpenAlex.

  1. Article
  2. Review
  3. Design, synthesis, biological andBiomedical reports · 2025
    Article
  4. Article
  5. Review
  6. Review
  7. Article
  8. Article
  9. HDACs and HDAC Inhibitors in Cancer Development and Therapy.Cold Spring Harbor perspectives in medicine · 2016
    Review
  10. 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 2 institutions in 1 country.

Quaovi H SodjiSchool of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
James R KornackiDepartment of Chemistry, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208-3113, USA; Department of Biomedical Engineering, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208-3113, USA.
John F McDonaldSchool of Biology, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA; Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
Milan MrksichDepartment of Chemistry, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208-3113, USA; Department of Biomedical Engineering, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208-3113, USA. Electronic address: milan.mrksich@northwestern.edu.
Adegboyega K OyelereSchool of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA; Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA. Electronic address: aoyelere@gatech.edu.
Georgia Institute of Technology · USNorthwestern University · US

Funding

Nonpeptide macrocyclic histone deacetylase (HDAC) inhibitors for targeted lung caR01CA131217 · NCI · GEORGIA INSTITUTE OF TECHNOLOGY · PI OYELERE, ADEGBOYEGA · 2009 to 2013
$1.5M
Peptide Arrays for Understanding Histone BiochemistryR01GM084188 · NIGMS · UNIVERSITY OF CHICAGO · PI MRKSICH, MILAN · 2008 to 2011
$1.2M
NCI NIH HHS R01 CA131217NCI NIH HHS R01CA131217NIGMS NIH HHS R01 GM084188NIGMS NIH HHS R01GM084188
6 · The paper itself

Abstract

Histone deacetylase (HDAC) inhibition has recently emerged as a novel therapeutic approach for the treatment of various pathological conditions including cancer. Currently, two HDAC inhibitors (HDACi) – Vorinostat and Romidepsin – have been approved for the treatment of cutaneous T-cell lymphoma. However, HDACi remain ineffective against solid tumors and are associated with adverse events including cardiotoxicity. Targeted delivery may enhance the therapeutic indices of HDACi and enable them to be efficacious against solid tumors. We showed herein that morphing of folic and pteroic acids into the surface recognition group of HDACi results in hydroxamate and benzamide HDACi which derived tumor homing by targeting folate receptor (FR), a receptor commonly overexpressed in solid tumors. We observed a correlation between the potency of HDAC1 inhibition and cytotoxicity as only the potent pteroate hydroxamates, 11d and 11e, displayed antiproliferative activity against two representative FR-expression cancer cells. Our observation further supports the previous results which suggest that for a drug to be successfully targeted using the FR, it must be extremely potent against its primary target as the FR has a low delivery efficiency.

Indexed as

Drug DesignAntineoplastic AgentsCell Line, TumorCell ProliferationCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorFolic AcidHeLa CellsHistone Deacetylase 1Histone Deacetylase InhibitorsHumansKB CellsModels, MolecularMolecular StructurePterinsAntineoplastic AgentsFolic AcidHDAC1 protein, humanHistone Deacetylase 1Histone Deacetylase InhibitorsPterinspteroic acidReactive Oxygen SpeciesFolateHistone deacetylaseHydroxamic acidPteroic acidTargeted deliveryTubastatin A

Identifiers

PMID25899338
PMCPMC4433810
OpenAlexW1974456689

What OpenQuestion holds

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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.