Evidence map›Paper›PMID 19806436›Full record

ArticlePharmaceutical research2009

Leucine-Aspartic Acid-Valine sequence as targeting ligand and drug carrier for doxorubicin delivery to melanoma cells: in vitro cellular uptake and cytotoxicity studies.

Sha Zhong, Shiladitya Bhattacharya, William Chan, Bhaskara Jasti, Xiaoling Li

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Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
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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

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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

3 citing papers in PubMed.

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4 · The record

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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.

Sha ZhongDepartment of Pharmaceutics and Medicinal Chemistry, Thomas J. Long School of Pharmacy and Health Sciences, University of the Pacific, Stockton, CA 95211, USA.
Shiladitya Bhattacharya
William Chan
Bhaskara Jasti
Xiaoling Li

Funding

Poly (amino acid) as an Integrin Targeted Drug CarrierR15CA100182 · NCI · UNIVERSITY OF THE PACIFIC-STOCKTON · PI LI, XIAOLING · 2005 to 2005
$174k
NCI NIH HHS 1R15CA100182-01A2
6 · The paper itself

Abstract

purposeTo study the feasibility of Leucine-Aspartic Acid-Valine (LDV) as targeting ligand and drug carrier for targeted delivery to integrin alpha(4)beta(1) over-expressing cancer cells.

methodsPoly(L,D,V) was randomly copolymerized using N-carboxyanhydrides of leucine, beta-benzyl-aspartic acid, and valine. Oligo(LDV), consisting of 2-6 LDV units, were synthesized by solid phase protein synthesis (SPPS) method. Binding of Leu-Asp-Val, Val-Asp-Leu, and Leu-Asn-Val, and internalization of FITC labeled LDV by wild-type and integrin alpha(4) knock-down A375 cells were studied. Cytotoxicity of poly(L,D,V)-Dox, oligo(LDV)-Dox, and doxorubicin (Dox) was also determined on wild-type, integrin alpha(4) knock-down A375 cells, and normal human epithelial keratinocytes (NHEK).

resultsLDV was essential for the specific binding and internalization by cells expressing integrin alpha(4)beta(1). Cytotoxicity of poly(L,D,V)-Dox and oligo(LDV)-Dox was integrin alpha(4)-dependent, while free Dox did not show this differential effect. No observable cytotoxicity trend was found when increasing LDV repeating unit. Poly(L,D,V) was relatively more effective than oligo(LDV) for the delivery of Dox to A375.

conclusionLDV containing moieties bind specifically to integrin alpha(4)beta(1) expressing cancer cells. The binding, internalization, and cytotoxicity depend on the level of integrin alpha(4)beta(1) expression. Poly(L,D,V) and oligo(LDV) were both effective in the in vitro targeted delivery of Dox to integrin alpha(4)beta(1) over-expressing A375 cells.

Indexed as

Drug CarriersDrug Delivery SystemsOligopeptidesAntineoplastic AgentsBlotting, WesternCell Line, TumorDoxorubicinHumansInhibitory Concentration 50Integrin alpha4beta1LigandsMelanomaMolecular StructurePolymerase Chain ReactionAntineoplastic AgentsDoxorubicinDrug CarriersIntegrin alpha4beta1leucyl-aspartyl-valineLigandsOligopeptides

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Registered trials

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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.