Herein, BSA-tetraphenylethene derivative conjugates with aggregation-induced emission (AIE) properties were constructed and used as fluorescent probes for label-free detection of protease and α1-antitrypsin. Conjugated AIE probes were formed based on the electrostatic induced assembly between an ammonium cation of quaternized tetraphenylethene salt and carboxyl anion groups of BSA. While water soluble quaternized tetraphenylethene salt showed very low fluorescence in its well-dispersed state, obvious enhancement in the fluorescence of the aggregated tetraphenylethene derivative on the BSA templates was achieved due to the abnormal aggregation-induced emission properties of tetraphenylethene. These BSA-tetraphenylethene derivative conjugates enabled label-free detection of protease. In the presence of trypsin, the BSA templates were enzymatically hydrolyzed and the conjugates decomposed. Therefore the quaternized tetraphenylethene molecules became increasingly isolated from each other. Accordingly, the aggregation to dispersing state change of tetraphenylethene derivative resulted in an obvious decrease in the fluorescence of the conjugates probes and enabled the sensitive and selective detection of trypsin. Furthermore, upon addition of α1-antitrypsin, the enzymatic activity of trypsin was inhibited and the fluorescence was consequently preserved. Sensitive detection of α1-antitrypsin was thus realised. The protein-tetraphenylethene derivative conjugates with aggregation-induced emission properties therefore show great promise for the monitoring of biological processes and cancer diagnostics with simplicity, high sensitivity, and rapid response.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1039/c0an00813c | DOI Listing |
Eur J Nucl Med Mol Imaging
January 2025
Department of Hepatobiliary Surgery and Liver Transplantation Center, The Fifth Affiliated Hospital of Sun Yat-Sen University, 52 Mei Hua East Road, Zhuhai, 519000, China.
Purpose: Cancer-associated fibroblasts (CAFs) are the primary stromal component of the tumor microenvironment in hepatocellular carcinoma (HCC), affecting tumor progression and post-resection recurrence. Fibroblast activation protein (FAP) is a key biomarker of CAFs. However, there is limited evidence on using FAP as a target in near-infrared (NIR) fluorescence imaging for HCC.
View Article and Find Full Text PDFChemMedChem
January 2025
Federal University of Parana: Universidade Federal do Parana, Graduate Program in Pharmaceutical Sciences, BRAZIL.
The breast cancer resistance protein (BCRP/ABCG2) plays a major role in the multidrug resistance of cancers toward chemotherapeutic treatments. It was demonstrated that cholesterol regulates the ABCG2 activity, suggesting that lower levels of membrane cholesterol decrease the ABCG2 activity in mammalian cells. However, the precise mechanism remains unclear.
View Article and Find Full Text PDFInorg Chem
January 2025
Univ. Grenoble Alpes, CNRS, CEA, IRIG, LCBM (UMR 5249), Grenoble F-38000, France.
Lanthanide(III) complexes with two-photon absorbing antennas are attractive for microscopy imaging of live cells because they can be excited in the NIR. We describe the synthesis and luminescence and imaging properties of two Eu complexes, and , with (-carbazolyl)-aryl-alkynyl-picolinamide and (-carbazolyl)-aryl-picolinamide antennas, respectively, conjugated to the TAT cell-penetrating peptides. Contrary to what was previously observed with related Eu complexes with carbazole-based antennas in a mixture of water and organic solvents, these two complexes show very low emission quantum yield (Φ < 0.
View Article and Find Full Text PDFChem Biol Drug Des
January 2025
Research School of Chemistry, Australian National University, Canberra, Australian Capital Territory, Australia.
Drug targeting strategies, such as peptide-drug conjugates (PDCs), have arisen to combat the issue of off-target toxicity that is commonly associated with chemotherapeutic small molecule drugs. Here we investigated the ability of PDCs comprising a human protein-derived cell-penetrating peptide-platelet factor 4-derived internalization peptide (PDIP)-as a targeting strategy to improve the selectivity of camptothecin (CPT), a topoisomerase I inhibitor that suffers from off-target toxicity. The intranuclear target of CPT allowed exploration of PDC design features required for optimal potency.
View Article and Find Full Text PDFHemasphere
January 2025
Children's Cancer Institute, Lowy Cancer Research Centre, School of Clinical Medicine, UNSW Medicine & Health, UNSW Centre for Childhood Cancer Research UNSW Sydney Sydney New South Wales Australia.
Antibody-drug conjugates (ADCs) combining monoclonal antibodies with cytotoxic payloads are a rapidly emerging class of immune-based therapeutics with the potential to improve the treatment of cancer, including children with relapse/refractory acute lymphoblastic leukemia (ALL). CD123, the α subunit of the interleukin-3 receptor, is overexpressed in ALL and is a potential therapeutic target. Here, we show that pivekimab sunirine (PVEK), a recently developed ADC comprising the CD123-targeting antibody, G4723A, and the cytotoxic payload, DGN549, was highly effective in vivo against a large panel of pediatric ALL patient-derived xenograft (PDX) models ( = 39).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!