Gold Nanoparticle Aggregates Functionalized with Cyclic RGD Peptides for Targeting and Imaging of Colorectal Cancer Cells
Open accessAbstract
The active targeting strategy has emerged as a promising approach to achieve selectivity in nanobiotechnology applications. Peptides are particularly suited as targeting moieties because the multivalent presentation of these small molecules on a nanoparticle provides high avidity for the target. However, to achieve an efficient targeting activity, the presentation of the peptide on the nanostructure has to be supported by an appropriate design. To optimize the targeting to colorectal cancer cells, we have performed a ligand design study of plasmonic nanostructures covered with a cyclic RGD peptide, a known targeting moiety for the α v β 3 integrin. We find that to achieve a good targeting activity, the RGD peptide has to be linked to plasmonic nanostructures through a long PEG chain and a short oligolysine spacer. When the cyclic RGD peptide is directly linked to the PEG chains of the nanostructures, their targeting ability is lost. Molecular dynamics calculations make possible to understand the difference of the peptide organization in two targeted nanosystems, unveiling an effect of the spacer on the orientation of the active component, which very likely positively affects the targeting properties of the investigated plasmonic nanostructures.
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A long PEG chain (3000 MW) and a short-charged lysine sequence linked to the active peptide are required to obtain high targeting efficiencies, with specificity better than that obtained with a specific monoclonal antibody already used in clinic.
“A long polyethylene glycol (PEG) chain (3000 molecular weight) and a short-charged lysine sequence linked to the active peptide are required to obtain high targeting efficiencies that, in particular for specificity, are found to be also better than those obtained with a specific monoclonal antibody already used in clinic.”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
Split into 2 atoms — 1 confirmed, 0 partially supported, 0 disputed, 0 misattributed, 1 unverifiable. Expand the claim to see per-atom verdicts.
Experimental — accuracy not yet measuredWe developed a methodology for detecting cancer cells based on sub-nanomolar concentration of nanocolloids functionalized with monoclonal antibodies or engineered targeting peptides.
“We developed a methodology for detecting cancer cells based on sub-nanomolar concentration of nanocolloids functionalized with monoclonal antibodies [147,148] or with engineered targeting peptides [172,180,181,182,183].”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
The Synthesis of Nanostructures section reports detecting binding to colorectal cancer cells using SERRS signals from peptide-functionalized gold nanostructures, supporting the engineered-peptide part of the citation. It says cells were exposed to increasing concentrations but does not establish that detection worked at sub-nanomolar concentrations. The monoclonal-antibody branch has separate citations and is not attributed to this paper. (LLM, conf=0.82)
Experimental — accuracy not yet measuredA nanostructured system containing a SERS label and an MRI contrast agent based on Gd3+ produced MRI images of a tumor in mice injected with the nanostructures together with SERS images that easily showed the margin of the tumor.
“MRI images of a tumor were obtained for mice injected with the nanostructures together with SERS images, which easily showed the margin of the tumor [182] (see Figure 17b).”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
The Introduction and Conclusions describe SERRS-labeled gold nanostructures used to assess targeting of colorectal cancer cells. The cited paper does not report a Gd3+-based MRI agent, MRI of tumors in injected mice, or SERS images showing tumor margins; those parts of the claim are unsupported. (LLM, conf=0.84)
Experimental — accuracy not yet measuredWith the engineered peptide approach, sensitivity and specificity larger than 80-90% are obtained.
“With this approach, sensitivity and specificity larger than 80–90% are obtained [171,182] (see Figure 17a).”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
In “Synthesis of Nanostructures” (page unavailable), the optimized peptide-functionalized nanoparticles achieved sensitivity above 88% in Caco2 cells and almost 100% in SW620 cells. The paper does not report a numerical specificity above 80–90%, so it supports the sensitivity portion but not the specificity portion of the claim. (LLM, conf=0.87)
Experimental — accuracy not yet measuredAfter inoculation of nanostructures with SERS signals into mice, SERS signals were easily found in their organs where nanostructures accumulated, or in a tumor, whose margins can be easily obtained with SERS signals.
“After inoculation of nanostructures with SERS signals into mice, we were able to easily find SERS signals in their organs where nanostructures accumulated, or in a tumor, whose margins can be easily obtained with SERS signals.”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
In “Synthesis of Nanostructures” (page unavailable), SERRS signals confirmed that the nanostructures bound to cultured colorectal cancer cells. The paper does not report inoculating mice, detecting signals in their organs or tumors, or using the signals to delineate tumor margins. (LLM, conf=0.84)
Experimental — accuracy not yet measured
Molecular Dynamics calculations show that the presence of the short lysine charged sequence is strategic for obtaining the appropriate exposition of the targeting peptide over the PEG chains collapsed over the NP surface.
“Models for the arrangement of the targeting units on the Au NP surface, obtained with Molecular Dynamics calculations, show that the presence of the short lysine charged sequence is strategic for obtaining the appropriate exposition of the targeting peptide over the PEG chains, collapsed over the NP surface [172,182].”
From Nanoparticles Engineering by Pulsed Laser Ablation in Liquids: Concepts and Applications (2020) · cites this paper as [182]
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- Authors
- Biscaglia, F., Ripani, G., Rajendran, S., Benna, C., Mocellin, S., Bocchinfuso, G., Meneghetti, M., Palleschi, A., & Gobbo, M.
- Affiliations
- University of Padua (IT)
- University of Rome Tor Vergata (IT)
- Department of Surgery Oncology and Gastroenterology, University of Padova, Via Giustiniani 2, 35124 Padova, Italy
- Corresponding author
- Palleschi, Antonio
- Gobbo, Marina
- ORCID
- Venue
- ACS Applied Nano Materials
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-09-18
- Volume
- 2
- Issue
- 10
- Pages
- 6436-6444
- ISSN
- 2574-0970 (ISSN-L)
- OpenAlex
- W2974890122
- Semantic Scholar
- 4035bac4428f0658e9080473b275fc17a2981ca0
- Cited by
- 54
- References
- 71
- Citations by year
- 2026: 5 · 2025: 7 · 2024: 7 · 2023: 8 · 2022: 4 · 2021: 13 · 2020: 9 · 2019: 1
- FWCI
- 2.09
- Type
- journal article
- Language
- en
- Open access
- green
- hdl.handle.net
- Licence
- Locations
- ACS Applied Nano Materials (publishedVersion)
- Cineca Institutional Research Information System (Tor Vergata University) (submittedVersion, other-oa)
- Padua Research Archive (University of Padova) (submittedVersion)
- Funders
- Partnership for Advanced Computing in Europe AISBL (2017174118)
- Associazione Italiana per la Ricerca sul Cancro (Molecular clinical oncology, 5x100 n. 12214)
- Ministero della Salute (GR-2011-02351128)
- Universit?? degli Studi di Padova (#04SID2016, NAMECA - C98C13002740005, #08SID2017)
- Topics
- Physical Sciences › Materials Science › Electronic, Optical and Magnetic Materials › Gold and Silver Nanoparticles Synthesis and Applications
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
- Keywords
- gold nanoparticle aggregates, cyclic RGD peptide, active targeting, colorectal cancer cells, integrin αvβ3, plasmonic nanostructures, PEG spacer, peptide orientation, ligand design, molecular dynamics simulation, cancer cell imaging
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