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Targets, Volume 1, Issue 1 (September 2023) – 6 articles

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16 pages, 3217 KiB  
Article
Photo-Cleavable Polycations-Wrapped Upconversion Nanoparticles for Efficient siRNA Delivery and Cancer Therapy
by Yuling He, Shuwen Guo, Huangxian Ju and Ying Liu
Targets 2023, 1(1), 63-78; https://doi.org/10.3390/targets1010006 - 12 Sep 2023
Cited by 1 | Viewed by 1178
Abstract
RNA interference (RNAi) therapy is a promising approach for cancer therapy. However, due to the weak binding affinity between a carrier and small interference RNA (siRNA) and complicated tumor environment, efficient loading and release of siRNA still remain challenging. Here, we design photo-cleavable [...] Read more.
RNA interference (RNAi) therapy is a promising approach for cancer therapy. However, due to the weak binding affinity between a carrier and small interference RNA (siRNA) and complicated tumor environment, efficient loading and release of siRNA still remain challenging. Here, we design photo-cleavable polycations-wrapped upconversion nanoparticles (PC-UCNPs) for spatially and temporally controllable siRNA delivery. The PC-UCNPs are synthesized by in situ reversible addition−fragmentation chain transfer (RAFT) polymerization of photo-cleaved 5-(2-(dimethylamino)ethoxy)-2-nitrobenzyl acrylat (MENA) monomer and poly(oligo(ethylene oxide) methyl ether acrylate (OEMA) mononer through a chain transfer agent that anchored on the surface of silica-coated upconversion nanoparticles (UCNPs@SiO2). After reacting with CH3I, siRNA and hyaluronic acid (HA) are adsorbed on the particle surface to prepare PC-UCNPs/siRNA/HA. The reaction with cell-secreted hyaluronidase (HAase) achieves the intracellular delivery of PC-UCNPs/siRNA/HA, and 980 nm laser irradiation causes siRNA release, which effectively improves the gene silencing efficiency in vitro and suppresses tumor growth in vivo; therefore, these processes have a promising potential application in precision medicine. Full article
(This article belongs to the Special Issue Recent Progress in Bioimaging and Targeted Therapy)
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15 pages, 3896 KiB  
Article
The Synthesis of BODIPY-TKI Conjugates and Investigation of Their Ability to Target the Epidermal Growth Factor Receptor
by Simran Dhingra, Prajesh Shrestha, Arpan Chowdhury, Zehua Zhou, Seetharama D. Jois and Maria da Graça H. Vicente
Targets 2023, 1(1), 48-62; https://doi.org/10.3390/targets1010005 - 30 Aug 2023
Viewed by 1070
Abstract
A near-IR BODIPY was covalently conjugated via its isothiocyanate groups to one or two Erlotinib molecules, a known tyrosine kinase inhibitor (TKI), via triethylene glycol spacers, to produce two novel BODIPY-monoTKI and BODIPY-diTKI conjugates. The ability of these conjugates to target the intracellular [...] Read more.
A near-IR BODIPY was covalently conjugated via its isothiocyanate groups to one or two Erlotinib molecules, a known tyrosine kinase inhibitor (TKI), via triethylene glycol spacers, to produce two novel BODIPY-monoTKI and BODIPY-diTKI conjugates. The ability of these conjugates to target the intracellular domain of the epidermal growth factor receptor (EGFR) was investigated using molecular modeling, surface plasma resonance (SPR), EGFR kinase binding assay, time-dependent cellular uptake, and fluorescence microscopy. While both the BODIPY-monoTKI and the BODIPY-diTKI conjugates were shown to bind to the EGFR kinase by SPR and accumulated more efficiently within human HEp2 cells that over-express EGFR than BODIPY alone, only the BODIPY-monoTKI exhibited kinase inhibition activity. This is due to the high hydrophobic character and aggregation behavior of the BODIPY-diTKI in aqueous solutions, as shown by fluorescence quenching. Furthermore, the competition of the two Erlotinibs in the diTKI conjugate for the active site of the kinase, as suggested by computational modeling, might lead to a decrease in binding relative to the monoTKI conjugate. Nevertheless, the efficient cellular uptake and intracellular localization of both conjugates with no observed cytotoxicity suggest that both could be used as near-IR fluorescent markers for cells that over-express EGFR. Full article
(This article belongs to the Special Issue Fluorescence Imaging of Disease Biomarkers)
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14 pages, 8292 KiB  
Article
An Activatable Nanoscintillator Probe for Detecting Telomerase Activity and Screening Inhibitors In Vivo
by Baoliu Chen, Junduan Dai, Sijie Song, Xianzhe Tang, Yuheng Guo, Ting Wu, Mengnan Wu, Chaojie Hao, Xiaofeng Cheng, Xucong Lin, Yijie Bian, Zhaowei Chen and Huanghao Yang
Targets 2023, 1(1), 34-47; https://doi.org/10.3390/targets1010004 - 14 Jun 2023
Cited by 2 | Viewed by 1372
Abstract
Telomerase represents an essential molecular machinery for tumor occurrence and progression and a potential therapeutic target for cancer treatment. Sensitive and reliable analysis of telomerase activity is of significant importance for the diagnosis and treatment of cancer. In this study, we developed a [...] Read more.
Telomerase represents an essential molecular machinery for tumor occurrence and progression and a potential therapeutic target for cancer treatment. Sensitive and reliable analysis of telomerase activity is of significant importance for the diagnosis and treatment of cancer. In this study, we developed a telomerase-activated nanoscintillator probe for deep-tissue and background-free imaging of telomerase activity and screening telomerase inhibitors in tumor-bearing living mice models. The probe was constructed by modifying lanthanide-doped nanoscintillators with aptamer-containing DNA anchor strands which hybridized with quencher labelled–oligonucleotide strands and telomerase primers. The X-ray-induced fluorescence of the probe was quenched originally but turned on upon telomerase-catalyzed extension of the primer. Benefiting from exceptional tissue penetrating properties and negligible autofluorescence of X-ray excitation, this probe enabled direct detection of telomerase activity in vivo via fluorescence imaging. Furthermore, with the direct, readable fluorescent signals, the probe enabled the screening of telomerase inhibitors in living cells and whole-animal models in the native states of telomerase. This strategy would inspire the development of low autofluorescence and deep tissue bioimaging probes for disease diagnosis and drug development in high-level living settings. Full article
(This article belongs to the Special Issue Recent Progress in Bioimaging and Targeted Therapy)
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29 pages, 9546 KiB  
Review
Fluorescent Imaging Agents for Brain Diseases
by Feida Che, Xiaoming Zhao, Xin Wang, Ping Li and Bo Tang
Targets 2023, 1(1), 5-33; https://doi.org/10.3390/targets1010003 - 01 Jun 2023
Viewed by 1544
Abstract
The onset of brain diseases has a terrible impact on people’s lives, including brain tumors, Alzheimer’s disease, Parkinson’s disease, depression, and schizophrenia. Thus, the diagnosis and treatment of various brain disorders have been receiving specific attention. The fluorescence imaging technique is useful for [...] Read more.
The onset of brain diseases has a terrible impact on people’s lives, including brain tumors, Alzheimer’s disease, Parkinson’s disease, depression, and schizophrenia. Thus, the diagnosis and treatment of various brain disorders have been receiving specific attention. The fluorescence imaging technique is useful for examining brain diseases because it is intuitive, in situ, and real-time. Therefore, fluorescent imaging has so far been successfully employed to identify molecules associated with brain disease. In this review, the last five years of research advancements in fluorescent imaging agents for the above diseases are summarized, and the creation of pertinent fluorescence probes is described and prospected. Full article
(This article belongs to the Special Issue Fluorescence Imaging of Disease Biomarkers)
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1 pages, 157 KiB  
Editorial
Publisher’s Note: Targets—A New Open Access Journal
by Ioana Craciun
Targets 2023, 1(1), 4; https://doi.org/10.3390/targets1010002 - 27 May 2023
Viewed by 910
Abstract
Targets (ISSN 2813-3137) is a new open-access journal launched under the leadership of Prof [...] Full article
3 pages, 427 KiB  
Editorial
Introducing Targets: A Journal for Bio-Detection and Therapy
by Huangxian Ju and Ying Liu
Targets 2023, 1(1), 1-3; https://doi.org/10.3390/targets1010001 - 18 Aug 2022
Viewed by 1891
Abstract
Targets are the essential elements in bio-detection and therapy [...] Full article
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