ge11 peptide selectively deliver loading drugs into cancer cells

ge11 peptide GE11 peptide - EGFR targetingpeptide GE11 is a active peptide GE11 Peptide: A Targeted Approach to EGFR-Positive Cancers

GE11 peptidesequence The GE11 peptide has emerged as a significant tool in the fight against cancer, particularly for tumors that overexpress the epidermal growth factor receptor (EGFR).作者:T Hailing·2022·被引用次数:47—GE11 peptideis one of the potent EGFR ligand screened from a phage display peptide library. It is a dodecapeptide that can specifically binds to EGFR with ... This dodecapeptide, identified through phage display, exhibits a remarkable ability to specifically bind to EGFR with high affinity and selectivity.作者:T Hailing·2022·被引用次数:47—GE11 peptideis one of the potent EGFR ligand screened from a phage display peptide library. It is a dodecapeptide that can specifically binds to EGFR with ... Its primary application lies in its capacity to act as a targeting agent, enabling the precise delivery of therapeutic payloads, such as anticancer drugs and imaging agents, directly to cancer cells. This targeted approach holds immense promise for enhancing treatment efficacy while minimizing systemic side effects.

The development and application of GE11 peptide-based strategies have seen considerable research over the past decadeGE11 was identified as a potential EGFR-specific peptidein 2005 by phage display and was shown to bind with a K d of 22.3 ± 0.4 nM to the EGFR.. Its conjugation to various drug delivery systems, including liposomes, micelles, and nanoparticles, has been a key focus. These modified systems are designed to selectively deliver loaded drugs into cancer cells that exhibit high EGFR expression, thereby enhancing therapeutic outcomes.GE11 was identified as a potential EGFR-specific peptidein 2005 by phage display and was shown to bind with a K d of 22.3 ± 0.4 nM to the EGFR. For instance, GE11 peptide-conjugated liposomes have been developed to improve the therapeutic index of anticancer drugs by increasing their accumulation within tumor cells. Similarly, GE11-decorated acidity-responsive micelles can encapsulate drugs like celecoxib, further refining targeted delivery.

Beyond drug delivery, the GE11 peptide also plays a crucial role in cancer diagnostics and imaging. Its ability to bind to EGFR makes it an attractive candidate for developing radioligands for diagnostic imaging techniques like positron emission tomography (PET) and magnetic resonance imaging (MRI). By labeling GE11 with radionuclides, researchers can create agents that visualize EGFR expression in tumors, aiding in early diagnosis and monitoring treatment response. GE11-CSO-SPION micelles, for example, can be utilized as MRI contrast agents to detect hepatocellular carcinoma (HCC) with high EGFR expression, offering reliable data for early diagnosis.Challenges for the application of EGFR-targeting peptide ...

Mechanisms of Action and Binding Affinity

The efficacy of the GE11 peptide stems from its specific interaction with the epidermal growth factor receptor (EGFR)作者:K Li·2021·被引用次数:18—A screened small peptide GE11 by the phage display was demonstrated tohave high affinity against EGFR significantly upregulated cancer cells.. EGFR is a transmembrane protein that plays a critical role in cell growth and proliferation. In many types of cancer, EGFR is overexpressed or mutated, leading to uncontrolled cell division. The GE11 peptide, with its amino acid sequence often cited as YHWYGYTPQNVI, functions as a ligand that binds to the extracellular domain of EGFR. This binding event is highly specific, meaning GE11 preferentially attaches to EGFR over other cellular receptors, a characteristic that underpins its utility in targeted therapies. Studies have demonstrated its binding affinity to EGFR, with dissociation constants (Kd) reported in the nanomolar range, indicating a strong and stable interaction. This high affinity is crucial for effective targeting and subsequent drug delivery or imaging.

Applications in Drug Delivery Systems

The integration of GE11 peptide into various drug delivery platforms has significantly expanded its therapeutic potentialSynthetic GE11 Peptide | ABIN2874272. By conjugating GE11 to nanocarriers, researchers aim to leverage its EGFR-targeting capability to achieve precise drug localization within tumor sites.作者:WW Xu·2017·被引用次数:45—In this study, dual therapeutic-loadedGE11 peptide-conjugated liposomeswere developed and applied to enhance therapeutic efficacies of standard-of-care ...

* Liposomes: GE11 peptide-conjugated liposomes are a prominent example. These liposomes can encapsulate chemotherapeutic agents, and upon administration, the GE11 peptide guides them to EGFR-overexpressing cancer cells. This targeted delivery can lead to higher drug concentrations within the tumor, potentially increasing efficacy and reducing off-target toxicity. Research has explored dual therapeutic-loaded GE11 peptide-conjugated liposomes to amplify therapeutic effects作者:Z Guo·2022·被引用次数:21—We developed an epidermal growth factor receptor-targeted multifunctional micellar nanoplatform (GE11-DOX+CEL-M) by encapsulating celecoxib into polymeric ....

* Nanoparticles: Various types of nanoparticles have been modified with GE11 peptide.作者:D Hu·2016·被引用次数:63—GE11 peptidemodified and reduction-responsive hyaluronic acid-based nanoparticles induced higher efficacy of doxorubicin for breast ... These include reduction-responsive hyaluronic acid-based nanoparticles and PLGA/TPGS nanoparticlesSynthesis of a novel 99m Tc labeled GE11 peptide for .... These systems are engineered to release their therapeutic cargo under specific conditions within the tumor microenvironment, further enhancing targeted action. For instance, GE11-modified nanoparticles have shown higher efficacy in delivering doxorubicin for breast cancer treatment.

* Micelles: GE11 peptide-decorated micelles offer another avenue for targeted drug delivery.Store at 2 to 4°C before hydration and at -70°C after rehydration. Most peptides are stable for approximately 3-6 month after rehydration. Typically, any ... These systems can encapsulate hydrophobic drugs and are designed to respond to stimuli like tumor acidity. This allows for controlled release of the drug at the tumor site after GE11-mediated targeting.

Role in Diagnostics and Imaging

The GE11 peptide's specific affinity for EGFR also makes it a valuable tool for diagnostic applications, particularly in visualizing EGFR expression in tumors作者:MA Yuanzheng·2020—In the past 15 years, more systematic and in-depth studies on theEGFR-targeted GE11 peptidehave been carried out in the prevention, diagnosis ....

* Radiolabeling for PET and SPECT: GE11 peptide can be radiolabeled with isotopes such as Technetium-99m (99mTc) or Fluorine-18 (18F).GE11 was identified as a potential EGFR-specific peptidein 2005 by phage display and was shown to bind with a K d of 22.3 ± 0.4 nM to the EGFR. These radiolabeled peptides can then be used as tracers in Positron Emission Tomography (PET) or Single-Photon Emission Computed Tomography (SPECT) scans作者:B Judmann·2022·被引用次数:5—In conclusion, a monovalentGE11 peptideor a low number of GE11 peptide units per radiotracer molecule appears to be of limited utility to .... These imaging techniques allow for the quantification of EGFR expression in vivo, which can aid in patient selection for EGFR-targeted therapies and in monitoring treatment response. Studies have focused on optimizing labeling approaches to ensure the stability and targeting efficiency of these radiotracers.

* MRI Contrast Agents: GE11 peptide has also been incorporated into MRI contrast agents, such as GE11-CSO-SPION micelles. These agents can enhance the visibility of tumors with high EGFR expression in MRI scans, contributing to more accurate diagnosis and staging of cancers like HCC.作者:F Striese·2018·被引用次数:25—The peptideYHWYGYTPQNVI (GE11) has been reported to bind the receptor with high specificity and affinity.

Challenges and Future Directions

Despite the significant progress in GE11 peptide research, several challenges remain. One challenge is the potential for EGFR receptor activation by the GE11 peptide itself, which could complicate therapeutic outcomes.作者:Z Guo·2022·被引用次数:21—We developed an epidermal growth factor receptor-targeted multifunctional micellar nanoplatform (GE11-DOX+CEL-M) by encapsulating celecoxib into polymeric ... Additionally, the affinity of a single GE11 molecule for EGFR may sometimes be insufficient for optimal targeting, necessitating the use of multiple GE11 units per molecule or conjugate.GE11 Peptide as an Active Targeting Agent in Antitumor ... The stability and shelf-life of GE11 peptide, especially after rehydration, also require careful consideration for practical clinical applications. Storage conditions, typically at 2-4°C before hydration and -70°C after rehydration, are recommended to maintain peptide integrity for approximately 3-6 months.

Future research is likely to focus on overcoming these challenges by developing more robust and efficient GE11-based delivery systems, exploring novel modifications to enhance binding affinity and reduce off-target effects, and further refining radiolabeling techniques for improved diagnostic imaging. The continued exploration of GE11 peptide's potential in combination therapies and its application against a broader spectrum of EGFR-expressing cancers will also be critical作者:T Hailing·2022·被引用次数:45—GE11 has been widely used in the diagnosis and targeted delivery of drugsfor radiotherapy, genetherapy and chemotherpy against EGFR positive .... The development of bispecific peptide conjugates incorporating GE11 could also offer new therapeutic strategies. Ultimately, the GE11 peptide represents a vital component in the evolving landscape of precision oncology, offering targeted solutions for a range of challenging diseases.作者:T Hailing·2022·被引用次数:45—GE11 has been widely used in the diagnosis and targeted delivery of drugsfor radiotherapy, genetherapy and chemotherpy against EGFR positive ...

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