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Peptide-based fluorescent probes have found widespread applications in biomedical research, including bio-imaging, disease diagnosis, drug discovery, and image-guided surgery. Their favorable properties-such as small molecular size, low toxicity, minimal immunogenicity, and high targeting specificity-have contributed to their growing utility in both basic research and translational medicine. This review provides a comprehensive overview of recent advances in peptide-based fluorescent probes, emphasizing design strategies, biological targets, and diverse functional applications. Key areas of focus include the integration of molecular targeting with imaging capabilities, the emergence of multimodal imaging techniques, and the development of activatable probes responsive to specific biological stimuli. Applications are discussed in the context of tumor cell membrane recognition, subcellular organelle targeting, non-cancer disease diagnosis, and detection of both metal ions and non-metal ions. Notably, responsive probes for reactive oxygen species (ROS) and other biologically relevant non-metal ions are also highlighted, underscoring their diagnostic and therapeutic potential. The review also addresses key limitations-such as poor in vivo stability, limited targeting accuracy, and delivery efficiency-and outlines future directions including smart peptide probe platforms, self-reporting systems, and high-throughput screening based on peptide libraries to accelerate next-generation probe development.
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http://dx.doi.org/10.2147/IJN.S529323 | DOI Listing |
Int J Nanomedicine
September 2025
Department of Orthopedics, Honghui Hospital, Xi'an Jiaotong University, Xi'an, Shaanxi, People's Republic of China.
Peptide-based fluorescent probes have found widespread applications in biomedical research, including bio-imaging, disease diagnosis, drug discovery, and image-guided surgery. Their favorable properties-such as small molecular size, low toxicity, minimal immunogenicity, and high targeting specificity-have contributed to their growing utility in both basic research and translational medicine. This review provides a comprehensive overview of recent advances in peptide-based fluorescent probes, emphasizing design strategies, biological targets, and diverse functional applications.
View Article and Find Full Text PDFBiology (Basel)
August 2025
The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou 510120, China.
The epidermal growth factor receptor (EGFR) is a key target for both cancer diagnosis and therapeutic interventions. Assessing EGFR expression before therapy has become routine in clinical practice, yet current methods like biopsy and immunohistochemistry (IHC) have significant limitations, including invasiveness, limited repeatability, and lack of real-time, whole-body data. EGFR-targeted imaging has emerged as a promising alternative.
View Article and Find Full Text PDFElife
September 2025
Department of Pharmacology, University of Cambridge, Cambridge, United Kingdom.
E3 ubiquitin ligases engage their substrates via 'degrons' - short linear motifs typically located within intrinsically disordered regions of substrates. As these enzymes are large, multi-subunit complexes that generally lack natural small-molecule ligands and are difficult to inhibit via conventional means, alternative strategies are needed to target them in diseases, and peptide-based inhibitors derived from degrons represent a promising approach. Here we explore peptide inhibitors of Cdc20, a substrate-recognition subunit and activator of the E3 ubiquitin ligase the anaphase-promoting complex/cyclosome (APC/C) that is essential in mitosis and consequently of interest as an anti-cancer target.
View Article and Find Full Text PDFAntibiotics (Basel)
August 2025
Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia-Sede Bogotá, Carrera 45 No 26-85, Building 451, Bogotá D.C. 111321, Colombia.
Palindromic antimicrobial peptides (PAMs) constitute versatile scaffolds for the design and optimization of anticancer agents with applications in therapy, diagnosis, and/or monitoring. In the present study, fluorolabeled peptides derived from the palindromic sequence RWQWRWQWR containing fluorescent probes, such as 2-Aminobenzoyl, 5(6)-Carboxyfluorescein, and Rhodamine B, were obtained. RP-HPLC analysis revealed that the palindromic peptide conjugated to Rhodamine B (RhB-RWQWRWQWR) exhibited the presence of isomers, likely corresponding to the open-ring and spiro-lactam forms of the fluorescent probe.
View Article and Find Full Text PDFLuminescence
August 2025
Precise Synthesis and Function Development Key Laboratory of Sichuan Province, College of Chemistry and Chemical Engineering, China West Normal University, Nanchong, China.
Herein, a new large Stokes shift fluorescent probe DGCA based on dansyl group modified tripeptide molecule (Gly-Cys-Ala-NH) was successfully synthesized. DGCA acts as a promising probe for simultaneous detection of Ag and Cu based on different response modes, which displayed fluorescence enhancement by Ag and fluorescence quenching by Cu in 100% aqueous solution. In addition, DGCA exhibited high sensitivity recognition of Ag and Cu, with the limits of detections (LODs) being 7.
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