ArticleMolecular therapy : the journal of the American Society of Gene Therapy2010
The use of inhibitors to study endocytic pathways of gene carriers: optimization and pitfalls.
Article in Molecular therapy : the journal of the American Society of Gene Therapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 252 papers.
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Who cites it
252 citing papers in PubMed, 670 citations in OpenAlex.
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- Protein Modifications for Cellular Protein Delivery.Chemical reviews · 2026Review
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- Programmable antibody-based chimeric entry receptors for sarbecoviruses.Communications biology · 2026Article
- Zinc-induced exposure of an LxL motif drives clathrin-mediated endocytosis of the zinc transceptor ZIP4.The Journal of biological chemistry · 2026Article
- Using Well-Defined DNA Nanostructures To Study the Influence of DNA Clustering and Presentation on SNA Cellular Uptake.Nano letters · 2026Article
- Endocytosed lipids induce cell aggregation via filopodia retraction in a close relative of animals.EMBO reports · 2026Article
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- The Nanoparticle Delivery Gap in Immune Cell Engineering: From Uptake to Endosomal Escape.International journal of nanomedicine · 2026Review
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- Exploring the Power of Metal-Free Click Transformations toward the Synthesis of Highly Functionalized Dendrimers for Applications in Drug Delivery.ACS applied materials & interfaces · 2025Article
- A genome-wide CRISPR screen in Anopheles mosquito cells identifies fitness and immune cell function-related genes.Nature communications · 2025Article
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- Intracellular redistribution of cell-penetrating peptide p28: A mechanism for enhanced anti-cancer activity.Journal of controlled release : official journal of the Controlled Release Society · 2025Article
192 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
Nonviral gene complexes can enter mammalian cells through different endocytic pathways. For efficient optimization of the gene carrier it is important to profile its cellular uptake, because this largely determines its intracellular processing and subsequent transfection efficiency. Most of the current information on uptake of these gene-delivery vehicles is based on data following the use of chemical inhibitors of endocytic pathways. Here, we have performed a detailed characterization of four commonly used endocytosis inhibitors [chlorpromazine, genistein, methyl-beta-cyclodextrin (MbetaCD), and potassium depletion] on cell viability and endocytosis in five well-described cell lines. We found that chlorpromazine and to a lesser extent MbetaCD significantly decreased cell viability of some cell lines even after short incubation periods and at concentrations that are routinely used to inhibit endocytosis. Through analyzing the uptake and subcellular distribution of two fluorescent endocytic probes transferrin and lactosylceramide (LacCer) that are reported to enter cells via clathrin-dependent (CDE) and clathrin-independent (CIE) mechanisms, respectively, we showed poor specificity of these agents for inhibiting distinct endocytic pathways. Finally, we demonstrate that any inhibitory effects are highly cell line dependent. Overall, the data question the significance of performing endocytosis studies with these agents in the absence of very stringent controls.
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Registered trials
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.