ArticleBioconjugate chemistry2016
Design and Synthesis of Near-Infrared Peptide for in Vivo Molecular Imaging of HER2.
Article in Bioconjugate chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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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.
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Who cites it
24 citing papers in PubMed, 55 citations in OpenAlex.
- Detection of Barrett's neoplasia with a near-infrared fluorescent heterodimeric peptide.Endoscopy · 2022Trial
- Molecularly targeted photoacoustic endoscopy with fiber-scanning side-view probe for in vivo staging of early mucosal tumors.Biosensors & bioelectronics · 2025Article
- Recent Progress in Peptide-Based Fluorescent Probes Biomedical Applications: A Review.International journal of nanomedicine · 2025Review
- Wide-field endoscope accessory for multiplexed fluorescence imaging.Scientific reports · 2023Article
- Flexible fiber cholangioscope for detection of near-infrared fluorescence.VideoGIE : an official video journal of the American Society for Gastrointestinal Endoscopy · 2023Article
- Application of near-infrared fluorescence imaging in theranostics of gastrointestinal tumors.Gastroenterology report · 2023Review
- A Photoacoustic-Fluorescent Imaging Probe for Proteolytic Gingipains Expressed by Porphyromonas gingivalis.Angewandte Chemie (International ed. in English) · 2022Article
- Article
- Dual-modality optical coherence tomography and fluorescence tethered capsule endomicroscopy.Biomedical optics express · 2021Article
- Article
- Light-Emitting Probes for Labeling Peptides.Cell reports. Physical science · 2020Article
- Imaging and monitoring HER2 expression in breast cancer during trastuzumab therapy with a peptide probeEuropean journal of nuclear medicine and molecular imaging · 2020Article
- Sticking to the Problem: Engineering Adhesion in Molecular Endoscopic Imaging.Cellular and molecular bioengineering · 2020Review
- Fluorescence Image-Guided Surgery - a Perspective on Contrast Agent Development.Proceedings of SPIE--the International Society for Optical Engineering · 2020Article
- Multiplexed Imaging Strategy to Distinguish Indeterminant Biliary Strictures: AnWorld journal of gastroenterology, hepatology and endoscopy · 2020Article
- Detection of colonic neoplasia in vivo using near-infrared-labeled peptide targeting cMet.Scientific reports · 2019Article
- Multiplexed Targeting of Barrett's Neoplasia with a Heterobivalent Ligand: Imaging Study on Mouse Xenograft in Vivo and Human Specimens ex Vivo.Journal of medicinal chemistry · 2018Article
- Early-Stage Incorporation Strategy for Regioselective Labeling of Peptides using the 2-Cyanobenzothiazole/1,2-Aminothiol Bioorthogonal Click Reaction.ChemistryOpen · 2018Article
- Molecular imaging of Toll-like receptor 4 detects ischemia-reperfusion injury during intussusception.Oncotarget · 2018Article
- Targeted Optical Imaging Agents in Cancer: Focus on Clinical Applications.Contrast media & molecular imaging · 2018Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
We report the development, characterization, and validation of a peptide specific for the extracellular domain of HER2. This probe chemistry was developed for molecular imaging by using a structural model to select an optimal combination of amino acids that maximize the likelihood for unique hydrophobic and hydrophilic interactions with HER2 domain 3. The sequence KSPNPRF was identified and conjugated with either FITC or Cy5.5 via a GGGSK linker using Fmoc-mediated solid-phase synthesis to demonstrate flexibility for this chemical structure to be labeled with different fluorophores. A scrambled sequence was developed for control by altering the conformationally rigid spacer and moving both hydrophobic and hydrophilic amino acids on the C-terminus. We validated peptide specificity for HER2 in knockdown and competition experiments using human colorectal cancer cells in vitro, and measured a binding affinity of kd = 21 nM and time constant of k = 0.14 min(-1) (7.14 min). We used this peptide with either topical or intravenous administration in a preclinical model of colorectal cancer to demonstrate specific uptake in spontaneous adenomas and to show feasibility for real time in vivo imaging with near-infrared fluorescence. We used this peptide in immunofluorescence studies of human proximal colon specimens to evaluate specificity for sessile serrated and sporadic adenomas. Improved visualization can be used endoscopically to guide tissue biopsy and detect premalignant lesions that would otherwise be missed. Our peptide design for specificity to HER2 is promising for clinical translation in molecular imaging methods for early cancer detection.
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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.