Evidence map›Paper›PMID 27156249›Full record

ArticleBiomaterials2016

KE108-conjugated unimolecular micelles loaded with a novel HDAC inhibitor thailandepsin-A for targeted neuroendocrine cancer therapy.

Guojun Chen, Renata Jaskula-Sztul, April Harrison, Ajitha Dammalapati, Wenjin Xu, Yiqiang Cheng, Herbert Chen, Shaoqin Gong

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Biomaterials, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
4.6field-weighted citation impact, top 4% 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

20 citing papers in PubMed, 47 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Review
  5. Article
  6. Review
  7. SolutolDrug design, development and therapy · 2019
    Article
  8. Review
  9. Article
  10. Review
  11. Article
  12. Article
  13. Tumor-targeted pH/redox dual-sensitive unimolecular nanoparticles for efficient siRNA delivery.Journal of controlled release : official journal of the Controlled Release Society · 2017
    Article
  14. Article
  15. Article
  16. Article
  17. Article
  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

8 authors at 4 institutions in 1 country.

Guojun ChenDepartment of Materials Science and Engineering, University of Wisconsin-Madison, Madison, WI 53715, USA; Wisconsin Institute for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA.
Renata Jaskula-SztulDepartment of Surgery, University of Alabama at Birmingham, Birmingham, AL 35233, USA.
April HarrisonDepartment of Surgery, University of Wisconsin-Madison, WI 53705, USA.
Ajitha DammalapatiDepartment of Surgery, University of Wisconsin-Madison, WI 53705, USA.
Wenjin XuWisconsin Institute for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA; Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53706, USA.
Yiqiang ChengUniversity of Texas Health Sciences Center San Anto-Division, San Antonio, TX 76107, USA.
Herbert ChenDepartment of Surgery, University of Alabama at Birmingham, Birmingham, AL 35233, USA. Electronic address: herbchen@uab.edu.
Shaoqin GongDepartment of Materials Science and Engineering, University of Wisconsin-Madison, Madison, WI 53715, USA; Wisconsin Institute for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA; Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53706, USA. Electronic address: shaoqingong@wisc.edu.
University of Wisconsin–Madison · USUniversity of Alabama at Birmingham · USThe University of Texas Health Science Center at San Antonio · USWisconsin Institutes for Discovery · US

Funding

XRAY CRYSTALLOGRAPHYP30CA013148 · NCI · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI Robert S Welner · 1985 to 2026
$165.9M
GSK3-beta Signaling in Medullary Thyroid CancerR01CA121115 · NCI · UNIVERSITY OF WISCONSIN-MADISON · PI CHEN, HERBERT · 2009 to 2013
$1.5M
Targeted Therapy of Neuroendocrine Cancers Via the Notch Signaling PathwayK25CA166178 · NCI · UNIVERSITY OF WISCONSIN-MADISON · PI GONG, SHAOQIN - · 2013 to 2017
$994k
Targeting Triple Negative Breast Cancer Using Nanoparticles Loaded with the Anti-Cancer Drug AminoflavoneR21CA196653 · NCI · UNIVERSITY OF WISCONSIN-MADISON · PI GONG, SHAOQIN -, XU, WEI · 2016 to 2017
$337k
NCI NIH HHS K25 CA166178NCI NIH HHS P30 CA013148NCI NIH HHS R01 CA121115NCI NIH HHS R21 CA196653
6 · The paper itself

Abstract

Neuroendocrine (NE) cancers can cause significant patient morbidity. Besides surgery, there are no curative treatments for NE cancers and their metastases, emphasizing the need for the development of other forms of therapy. In this study, multifunctional unimolecular micelles were developed for targeted NE cancer therapy. The unimolecular micelles were formed by multi-arm star amphiphilic block copolymer poly(amidoamine)-poly(valerolactone)-poly(ethylene glycol) conjugated with KE108 peptide and Cy5 dye (abbreviated as PAMAM-PVL-PEG-KE108/Cy5). The unimolecular micelles with a spherical core-shell structure exhibited a uniform size distribution and excellent stability. The hydrophobic drug thailandepsin-A (TDP-A), a recently discovered HDAC inhibitor, was physically encapsulated into the hydrophobic core of the micelles. KE108 peptide, a somatostatin analog possessing high affinity for all five subtypes of somatostatin receptors (SSTR 1-5), commonly overexpressed in NE cancer cells, was used for the first time as an NE cancer targeting ligand. KE108 exhibited superior targeting abilities compared to other common somatostatin analogs, such as octreotide, in NE cancer cell lines. The in vitro assays demonstrated that the TDP-A-loaded, KE108-targeted micelles exhibited the best capabilities in suppressing NE cancer cell growth. Moreover, the in vivo near-infrared fluorescence imaging on NE-tumor-bearing nude mice showed that KE108-conjugated micelles exhibited the greatest tumor accumulation due to their passive targeting and active targeting capabilities. Finally, TDP-A-loaded and KE108-conjugated micelles possessed the best anticancer efficacy without detectable systemic toxicity. Thus, these novel TDP-A-loaded and KE108-conjugated unimolecular micelles offer a promising approach for targeted NE cancer therapy.

Indexed as

MicellesMolecular Targeted TherapyAnimalsCell Line, TumorCell ProliferationDepsipeptidesHistone Deacetylase InhibitorsHumansHydrodynamicsMaleMice, NudeNeuroendocrine TumorsParticle SizePeptides, CyclicPolymersProton Magnetic Resonance SpectroscopyDepsipeptidesHistone Deacetylase InhibitorsMicellesPeptides, CyclicPolymersReceptors, Somatostatinthailandepsin ATyr(0)-(cyclo-D-Dab-Arg-Phe-Phe-D-Trp-Lys-Thr-Phe)HDAC inhibitorKE108 peptideNeuroendocrine cancersSomatostatin receptorTargeted drug deliveryUnimolecular micelles

Identifiers

PMID27156249
PMCPMC4882607
OpenAlexW2344582458

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.