ArticleMolecular pharmaceutics2014
Enhanced cellular entry and efficacy of tat conjugates by rational design of the auxiliary segment.
Article in Molecular pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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.
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.
Who cites it
23 citing papers in PubMed, 59 citations in OpenAlex.
- Exploring CPP Enhanced Hypoxia Targeting: An Approach Using Radiolabeled 2-nitroimidazole TAT Conjugate.Drug development research · 2026Article
- PCFT-Independent Cellular Uptake of Cyclic Cell-Penetrating Peptide-Conjugated Folic Acid.Chembiochem : a European journal of chemical biology · 2025Article
- Palmitoylation in cancer: decoding its roles in signal transduction, tumor immunity, and emerging therapeutic opportunities.Frontiers in immunology · 2025Review
- Peptide Amphiphiles as Biodegradable Adjuvants for Efficient Retroviral Gene Delivery.Advanced healthcare materials · 2024Article
- Deciphering variations in the endocytic uptake of a cell-penetrating peptide: the crucial role of cell culture protocols.Cytotechnology · 2023Article
- Development of Hydrophobic Cell-Penetrating Stapled Peptides as Drug Carriers.International journal of molecular sciences · 2023Article
- Smart Delivery Systems Responsive to Cathepsin B Activity for Cancer Treatment.Pharmaceutics · 2023Review
- The Balance between Hydrophobicity/Aromaticity and Positively Charged Residues May Influence the Cell Penetration Ability.Pharmaceutics · 2023Article
- Membrane Internalization Mechanisms and Design Strategies of Arginine-Rich Cell-Penetrating Peptides.International journal of molecular sciences · 2022Review
- Construction of a Multifunctional Nano-Scale Metal-Organic Framework-Based Drug Delivery System for Targeted Cancer Therapy.Pharmaceutics · 2021Article
- Enhanced Live-Cell Delivery of Synthetic Proteins Assisted by Cell-Penetrating Peptides Fused to DABCYL.Angewandte Chemie (International ed. in English) · 2021Article
- Self-assembling prodrug nanotherapeutics for synergistic tumor targeted drug delivery.Acta biomaterialia · 2020Review
- Article
- Novel tool to quantify cell wall porosity relates wall structure to cell growth and drug uptake.The Journal of cell biology · 2019Article
- Nanomedicines for Malaria Chemotherapy: Encapsulation vs. Polymer Therapeutics.Pharmaceutical research · 2018Review
- Self-assembling prodrugs.Chemical Society reviews · 2017Review
- Supramolecular biofunctional materials.Biomaterials · 2017Review
- Peptide-drug conjugates as effective prodrug strategies for targeted delivery.Advanced drug delivery reviews · 2017Review
- Self-assembling peptide-based building blocks in medical applications.Advanced drug delivery reviews · 2017Review
- Fabrication of functional hollow microspheres constructed from MOF shells: Promising drug delivery systems with high loading capacity and targeted transport.Scientific reports · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Conjugation with a cell penetrating peptide such as Tat presents an effective approach to improve the intracellular accumulation of molecules with low membrane permeability. This strategy, however, leads to a reduced cellular entry of molecules that can cross cell membrane effectively. We report here that covalent linkage of an additional hydrophobic unit that mimics a hydrophobic domain near the Tat sequence can further improve the cellular uptake of the parental conjugate into cancer cells regardless of the membrane permeability of the unconjugated molecule. Both fluorescent imaging and flow cytometry measurements confirmed the effect of palmitoylation on the increased internalization of the Tat conjugates with either 5-carboxyfluorescein (5-FAM), a nonmembrane penetrating dye, or doxorubicin, an anticancer cancer drug that can readily diffuse across cell membranes. In the case of the Tat-doxorubicin conjugate, palmitoylation improves the conjugate's anticancer activity in both drug sensitive and resistant cervical cancer cell lines. We further demonstrate that modification of a Tat-5-FAM conjugate with a hydrophobic quencher could not only efficiently quench the fluorescence outside of cancer cell but also facilitate its entry into MCF-7 breast cancer cells. These results highlight the importance of rational molecular design of using peptide conjugation chemistry in cancer therapeutics and diagnostics.
Indexed as
Identifiers
What OpenQuestion holds
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.