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Background: Fluorescence-guided molecular imaging may improve colorectal cancer (CRC) patient outcomes by enabling early detection and better surgical treatment, relying on developing targeted fluorescent tracers to highlight tumours. This study investigates visualising primary colon tumours by topically applying EMI-137, a targeted fluorescent tracer designed to bind to c-Met receptor. We introduce a novel viscous formulation to enhance the tracer's performance, aiming for a clear, robust fluorescent signal by improving contact with mucosal surface of ex vivo colon specimens.
Methods: We evaluated fluorescence properties of EMI-137 in phosphate-buffered saline (PBS) and in methylcellulose (m-cellulose) and determined emission spectrum of the tracer in both formulations. Flow cytometry was used to determine EMI-137's specificity for c-Met receptor and its optimal concentration. Live-cell imaging visually confirmed EMI-137's fluorescence signal for the c-Met receptor, highlighting its distinctive characteristics across various solvents. In a prospective cohort study, freshly excised colon cancer specimens were incubated with EMI-137 in PBS or m-cellulose. Specimens underwent a meticulous washing process. Near-infrared fluorescence imaging was performed and compared with histopathological analysis to validate detection accuracy.
Results: Fluorospectrometry showed that m-cellulose enhanced EMI-137's fluorescence intensity compared to PBS. Flow cytometry showed dose-dependent binding of EMI-137 in HT-29 cells, with an optimum at 500 nM. Microscopy confirmed targeting of c-Met receptors. Topical EMI-137 dissolved in m-cellulose visualised colon tumours effectively, resulting in a high tumour-to-background ratio. Histopathological analysis confirmed c-Met expression in these colon tumours.
Conclusion: EMI-137 in a novel viscous vehicle effectively imaged c-Met expressing colon tumors, potentially facilitating fluorescent-guided tumor imaging.
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http://dx.doi.org/10.1007/s11307-025-02042-z | DOI Listing |
Naunyn Schmiedebergs Arch Pharmacol
September 2025
Institute of Pharmacology, West German Heart and Vascular Center, University Duisburg-Essen, Duisburg, Germany.
PLoS One
September 2025
Department of Biomedicine, Health and Life Convergence Sciences, BK21 Four, College of Pharmacy, Mokpo National University, Muan, Republic of Korea.
Non-small cell lung cancer (NSCLC) is one of the leading causes of cancer-related deaths, remaining a significant challenge in terms of early detection, effective treatment, and improving patient survival rates. In this study, we investigated the anticancer mechanism of rubiarbonol B (Ru-B) and its derivative 3-O-acetylrubiarbonol B (ARu-B), a pentacyclic terpenoid in gefitinib (GEF)-sensitive and -resistant NSCLC HCC827 cells. Concentration- and time-dependent cytotoxicity was observed for both Ru-B and ARu-B.
View Article and Find Full Text PDFBioorg Chem
September 2025
Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:
Multi-targeted agents can sequentially act on two or more targets, leading to synergistic and more effective therapeutic effects against several complicated disorders, containing cancer, even with relatively modest action. The TRKs (tropomyosin receptor kinases) are confirmed as promising targets in anti-tumor drug discovery. Over the past 20 years, many small molecules TRK inhibitors have been identified, that some of them are being investigated in various clinical phases.
View Article and Find Full Text PDFThe immune checkpoint molecule B7-H3 is upregulated in many solid tumors, and B7-H3-targeted immunotherapies are in clinical trials. Recently, a growing body of research has highlighted the presence of tumor cell intrinsic while immune cell-independent functions of B7-H3 in tumorigenesis and cancer cell stemness. However, its receptors and mechanisms of action on cancer cells remain poorly understood.
View Article and Find Full Text PDFBMC Cancer
August 2025
Department of Biology, Virginia Commonwealth University, Richmond, VA, 23284, USA.
Background: Glycosphingolipids (GSL) are essential components of the plasma membrane where they are known to play key structural and functional roles and are known to influence molecular processes involved in cancer malignancy, including multi-drug chemoresistance, the epithelial to mesenchymal transition (EMT), and the activation or receptor tyrosine kinases (RTK). Thus, investigating and understanding how GSLs are regulated in cancer and the impact they have on malignancy have important therapeutic potential. In the GSL biosynthetic pathway, one critical regulator of two of the four major branches of GSLs is the gene product of B3GNT5, which produces the precursor for all GSLs in the lactoside and neolactoside series.
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