ReviewMolecular pharmaceutics2014
Cell-penetrating, guanidinium-rich molecular transporters for overcoming efflux-mediated multidrug resistance.
Review in Molecular pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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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
29 citing papers in PubMed, 63 citations in OpenAlex.
- Guanidinium-rich cell-penetrating peptidomimetic-doxorubicin conjugates show linker-dependent, reduced acute toxicity to cardiomyocytes and normal breast epithelium while retaining activity against a HER2-positive breast cancer model (SKBR3 spheroids).Frontiers in chemistry · 2026Article
- Improving the antimicrobial activity of RP9 peptide through theoretical and experimental investigation.Biochemistry and biophysics reports · 2025Article
- Biguanide-Vancomycin Conjugates are Effective Broad-Spectrum Antibiotics against Actively Growing and Biofilm-Associated Gram-Positive and Gram-Negative ESKAPE Pathogens and Mycobacteria.Journal of the American Chemical Society · 2024Article
- Vancomycin-Polyguanidino Dendrimer Conjugates Inhibit Growth of Antibiotic-Resistant Gram-Positive and Gram-Negative Bacteria and Eradicate Biofilm-AssociatedACS infectious diseases · 2024Article
- Design of pH-responsive antimicrobial peptide melittin analog-camptothecin conjugates for tumor therapy.Asian journal of pharmaceutical sciences · 2024Article
- Chemical biology fluorescent tools forRSC advances · 2023Article
- Role of microRNAs in regulation of doxorubicin and paclitaxel responses in lung tumor cells.Cell division · 2023Review
- Characterization of PGuaMolecular pharmaceutics · 2023Article
- Hemopexin as a Potential Binding Partner of Arginine-Rich Cell-Penetrating Peptides in Serum.ACS pharmacology & translational science · 2022Article
- Effects of self-assembled cell-penetrating peptides and their nano-complexes on ABCB1 expression and activity.Iranian journal of basic medical sciences · 2021Article
- Rapid Access to Dispirocyclic Scaffolds Enabled by Diastereoselective Intramolecular Double Functionalization of Benzene Rings.Chemistry, an Asian journal · 2020Article
- Metal Binding Antimicrobial Peptides in Nanoparticle Bio-functionalization: New Heights in Drug Delivery and Therapy.Probiotics and antimicrobial proteins · 2020Review
- Peptide-Drug Conjugates and Their Targets in Advanced Cancer Therapies.Frontiers in chemistry · 2020Review
- Influence of the Membrane Dye R18 and of DMSO on Cell Penetration of Guanidinium-Rich Peptides.Chemistry & biodiversity · 2018Article
- Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment.Journal of medicinal chemistry · 2018Review
- New tetrahydroisoquinoline-based P-glycoprotein modulators: decoration of the biphenyl core gives selective ligands.MedChemComm · 2018Article
- Deepened cellular/subcellular interface penetration and enhanced antitumor efficacy of cyclic peptidic ligand-decorated accelerating active targeted nanomedicines.International journal of nanomedicine · 2018Article
- On the design principles of peptide-drug conjugates for targeted drug delivery to the malignant tumor site.Beilstein journal of organic chemistry · 2018Review
- Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.ACS medicinal chemistry letters · 2017Article
- Cell-penetrating peptide conjugates to enhance the antitumor effect of paclitaxel on drug-resistant lung cancer.Drug delivery · 2017Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Multidrug resistance (MDR) is a major cause of chemotherapy failure in the clinic. Drugs that were once effective against naïve disease subsequently prove ineffective against recurrent disease, which often exhibits an MDR phenotype. MDR can be attributed to many factors; often dominating among these is the ability of a cell to suppress or block drug entry through upregulation of membrane-bound drug efflux pumps. Efflux pumps exhibit polyspecificity, recognizing and exporting many different types of drugs, especially those whose lipophilic nature contributes to residence in the membrane. We have developed a general strategy to overcome efflux-based resistance. This strategy involves conjugating a known drug that succumbs to efflux-mediated resistance to a cell-penetrating molecular transporter, specifically, the cell-penetrating peptide (CPP), d-octaarginine. The resultant conjugates are discrete single entities (not particle mixtures) and highly water-soluble. They rapidly enter cells, are not substrates for efflux pumps, and release the free drug only after cellular entry at a rate controlled by linker design and favored by target cell chemistry. This general strategy can be applied to many classes of drugs and allows for an exceptionally rapid advance to clinical testing, especially of drugs that succumb to resistance. The efficacy of this strategy has been successfully demonstrated with Taxol in cellular and animal models of resistant cancer and with ex vivo samples from patients with ovarian cancer. Next generation efforts in this area will involve the extension of this strategy to other chemotherapeutics and other MDR-susceptible diseases.
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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.