Etarfolatide integrates a folate-based motif with a peptide scaffold valuable in ligand-receptor interaction studies. Its heterocyclic assembly offers distinct binding characteristics, enabling investigations of targeted delivery mechanisms. The compound's physicochemical profile aids evaluations of solvent accessibility and structural stability. Broad relevance spans molecular recognition, carrier design, and bioorganic chemistry.
CAT No: R2423
CAS No:479578-27-3
Synonyms/Alias:Folcepri;479578-27-3;EC20 folate peptide;40UB1H6Q6T;EC20;EC 20;UNII-40UB1H6Q6T;EC-20;(2R)-5-(((2S)-2-amino-3-(((2S)-3-carboxy-1-(((1R)-1-carboxy-2-sulfanylethyl)amino)-1-oxopropan-2-yl)amino)-3-oxopropyl)amino)-5-oxo-2-((4-((4-oxo-3H-pteridin-6-yl)methylamino)benzoyl)amino)pentanoic acid;(2R)-5-[[(2S)-2-amino-3-[[(2S)-3-carboxy-1-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-1-oxopropan-2-yl]amino]-3-oxopropyl]amino]-5-oxo-2-[[4-[(4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]amino]pentanoic acid;EC 20 (peptide);SCHEMBL12642924;RKGPQAGUQDVJHG-MHORFTMASA-N;
Etarfolatide is a synthetic peptide-based imaging agent designed to target folate receptor-positive cells, capitalizing on its high affinity for the folate receptor alpha (FRα) frequently overexpressed in various tumor types and activated macrophages. As a conjugated peptide, it incorporates a folate moiety to enable selective binding, making it a valuable tool for molecular imaging and receptor-targeted studies. Its unique biochemical structure allows researchers to investigate cellular processes involving folate transport and receptor-mediated endocytosis, furthering the understanding of disease mechanisms and cellular heterogeneity in complex tissues. The compound's specificity and robust binding properties have established it as a pivotal reagent in the study of folate receptor biology and targeted delivery systems.
Receptor Targeting Studies: Etarfolatide is extensively utilized in receptor targeting research, particularly in the context of folate receptor alpha. By enabling precise localization and quantification of FRα expression on cell surfaces, it supports investigations into receptor distribution patterns across different cell types and tissues. Such studies are critical for elucidating the role of folate receptors in cellular uptake mechanisms, tumor biology, and immune cell activation, thereby informing the design of targeted therapies and diagnostic strategies.
Molecular Imaging Research: The conjugated structure of this peptide compound facilitates its application as a molecular imaging probe. When labeled with suitable radioisotopes or fluorescent tags, it allows for the non-invasive visualization of folate receptor-positive cells in vitro and in vivo. This capability is particularly valuable for preclinical imaging studies, enabling researchers to monitor receptor expression dynamics, assess tissue distribution, and evaluate the efficacy of folate-targeted interventions in real time.
Drug Delivery System Development: Etarfolatide's high affinity for FRα has made it an attractive scaffold for the development of targeted drug delivery systems. By conjugating therapeutic agents or nanoparticles to the peptide backbone, researchers can exploit receptor-mediated endocytosis to achieve selective delivery of payloads to FRα-expressing cells. This approach is instrumental in enhancing the specificity and efficacy of experimental drug candidates, while minimizing off-target effects in non-receptor-expressing tissues.
Cellular Uptake Mechanism Elucidation: The compound serves as a model ligand for studying the molecular mechanisms underlying receptor-mediated endocytosis and intracellular trafficking. By tracking its internalization and subsequent intracellular routing, scientists gain insights into the kinetics and regulatory factors governing folate receptor function. These studies contribute to a deeper understanding of cellular uptake pathways, which are fundamental to both basic cell biology and the rational design of targeted therapeutics.
Tumor Microenvironment Characterization: In the context of cancer research, etarfolatide is applied to characterize the tumor microenvironment by mapping the spatial distribution of FRα-positive cells. Its selective binding properties enable detailed profiling of tumor heterogeneity, facilitating the identification of cellular subpopulations that may influence tumor progression, immune infiltration, or response to experimental treatments. Such applications are essential for advancing personalized approaches in oncology research and for the validation of novel biomarkers in preclinical models.
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