GE11 Peptide as an Active Targeting Agent in Antitumor Therapy: A Minireview

Genta, Ida; Chiesa, Enrica; Colzani, Barbara; Modena, Tiziana; Conti, Bice; Dorati, Rossella

doi:10.3390/pharmaceutics10010002

Cited by 65 publications

(62 citation statements)

References 72 publications

(84 reference statements)

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“…Some of them effectively interact with EGFR, but also exhibit low endocytosis rate [152]. In addition, there is a short peptide GE11used for creating various delivery systems of anticancer agents, which is able to bind with EGFR facilitating internalization of nanoparticles coated with this peptide [153]. Along with antibodies and pep tides utilized as artificial ligands capable of binding to EGFR, there are also aptamers.…”

Section: The Use Of Egfr As a Delivery Systemmentioning

confidence: 99%

Epidermal Growth Factor Receptor: Key to Selective Intracellular Delivery

Rosenkranz

Slastnikova

2020

Biochemistry Moscow

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Epidermal growth factor receptor (EGFR) is an integral surface protein mediating cellular response to a number of growth factors. Its overexpression and increased activation due to mutations is one of the most common traits of many types of cancer. Development and clinical use of the agents, which block EGFR activation, became a prime example of the personalized targeted medicine. However, despite the obvious success in this area, cancer cure remains unattainable in most cases. Because of that, as well as the result of the search for possible ways to overcome the difficulties of treatment, a huge number of new treatment methods relying on the use of EGFR overexpression and its changes to destroy cancer cells. Modern data on the structure, functioning, and intracellular transport of EGFR, its natural ligands, as well as signaling cascades triggered by the EGFR activation, peculiarities of the EGFR expression and activation in oncological disorders, as well as applied therapeutic approaches aimed at blocking EGFR signaling pathway are summarized and analyzed in this review. Approaches to the targeted delivery of various chemotherapeutic agents, radionuclides, immunotoxins, photosensitizers, as well as the prospects for gene therapy aimed at cancer cells with EGFR overexpression are reviewed in detail. It should be noted that increasing attention is being paid nowadays to the development of multifunctional systems, either carrying several different active agents, or possessing several environment-dependent transport functions. Potentials of the systems based on receptor-mediated endocytosis of EGFR and their possible advantages and limitations are discussed.

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Section: The Use Of Egfr As a Delivery Systemmentioning

confidence: 99%

Epidermal Growth Factor Receptor: Key to Selective Intracellular Delivery

Rosenkranz

Slastnikova

2020

Biochemistry Moscow

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“…The polymer conjugate P-GE11-Dy-633 showed the lowest binding affinity. Although GE-11 peptide was previously reported as a targeting ligand for the EGFR [23], in our study, its efficiency to bind to EGFR in vitro was the lowest in comparison to both mAb (cetuximab) and the EGF. Indeed, recently it was published that GE-11 containing systems are significantly internalized by the FaDu cells [13], thus we can conclude that, despite their low binding affinity, the GE11-containing polymers could be internalized significantly in a short time.…”

Section: Binding Affinity Of Polymeric Conjugates To Egfr-positive Cellsmentioning

confidence: 51%

Targeted Polymer-Based Probes for Fluorescence Guided Visualization and Potential Surgery of EGFR-Positive Head-and-Neck Tumors

et al. 2020

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This report describes the design, synthesis and evaluation of tumor-targeted polymer probes to visualize epidermal growth factor receptor (EGFR)-positive malignant tumors for successful resection via fluorescence guided endoscopic surgery. Fluorescent polymer probes of various molecular weights enabling passive accumulation in tumors via enhanced permeability and retention were prepared and evaluated, showing an optimal molecular weight of 200,000 g/mol for passive tumor targeting. Moreover, poly(N-(2-hydroxypropyl)methacrylamide)-based copolymers labeled with fluorescent dyes were targeted with the EGFR-binding oligopeptide GE-11 (YHWYGYTPQNVI), human EGF or anti-EGFR monoclonal antibody cetuximab were all able to actively target the surface of EGFR-positive tumor cells. Nanoprobes targeted with GE-11 and cetuximab showed the best targeting profile but differed in their tumor accumulation kinetics. Cetuximab increased tumor accumulation after 15 min, whereas GE 11 needed at least 4 h. Interestingly, after 4 h, there were no significant differences in tumor targeting, indicating the potential of oligopeptide targeting for fluorescence-navigated surgery. In conclusion, fluorescent polymer probes targeted by oligopeptide GE-11 or whole antibody are excellent tools for surgical navigation during oncological surgery of head and neck squamous cell carcinoma, due to their relatively simple design, synthesis and cost, as well as optimal pharmacokinetics and accumulation in tumors.

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“…GE11 peptide-mediated drug delivery systems including liposomes, polymeric micelle, and viruses have been developed for disease diagnosis and drug delivery. A summary of GE11 peptide-enabled targeted delivery systems has been elaborately discussed in the review of Genta et al (2018) .…”

Section: Functional Enhancement Of Nanoparticles Enabled By Peptidesmentioning

confidence: 99%

Peptide-Enabled Targeted Delivery Systems for Therapeutic Applications

Liu

Fang

Yang

et al. 2021

Front. Bioeng. Biotechnol.

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Receptor-targeting peptides have been extensively pursued for improving binding specificity and effective accumulation of drugs at the site of interest, and have remained challenging for extensive research efforts relating to chemotherapy in cancer treatments. By chemically linking a ligand of interest to drug-loaded nanocarriers, active targeting systems could be constructed. Peptide-functionalized nanostructures have been extensively pursued for biomedical applications, including drug delivery, biological imaging, liquid biopsy, and targeted therapies, and widely recognized as candidates of novel therapeutics due to their high specificity, well biocompatibility, and easy availability. We will endeavor to review a variety of strategies that have been demonstrated for improving receptor-specificity of the drug-loaded nanoscale structures using peptide ligands targeting tumor-related receptors. The effort could illustrate that the synergism of nano-sized structures with receptor-targeting peptides could lead to enrichment of biofunctions of nanostructures.

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GE11 Peptide as an Active Targeting Agent in Antitumor Therapy: A Minireview

Cited by 65 publications

References 72 publications

Epidermal Growth Factor Receptor: Key to Selective Intracellular Delivery

Epidermal Growth Factor Receptor: Key to Selective Intracellular Delivery

Targeted Polymer-Based Probes for Fluorescence Guided Visualization and Potential Surgery of EGFR-Positive Head-and-Neck Tumors

Peptide-Enabled Targeted Delivery Systems for Therapeutic Applications

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