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Copyright © 2020 Han, Yang, Sun, Liu, Zhou and Li.Among all cancers, lung, breast, and prostate carcinoma are the three most fatal cancers. Although general therapeutic strategies and existent nanomedicine have been applied in relating cancer treatments, the side effects and potential damage induced by the off-target effect greatly lower the therapeutic efficiency. Recently, an increasing number of bioresponsive nanomaterials is recruited in fighting these deadliest cancers. Therefore, these latest bioresponsive nanomedicine are summarized in the current review. More specifically, the various novel nano-agents that could selectively respond to specific bio-conditions in malignant areas (e.g., pH, temperature, enzyme, Redox, elevated copper ion, etc.) are discussed in detail for their applications in cancer imaging (e.g., fluorescence, NIR, and MRI, etc.) and therapy (e.g., antiangiogenesis, chemotherapy, photothermal, and chemodynamic therapy, etc.). The development of next-generation of bioresponsive nanomedicine and challenges involved are further discussed for future design. Copyright © 2020 Mao and Liu.Chiral diketopyrrolopyrrole (DPP)-helicene polymers were synthesized to develop efficient red circularly polarized (CP) light emitters. selleck chemicals These original chiral dyes display intense electronic circular dichroism (ECD) and CP luminescence (CPL) in the far-red spectral region owing to the presence of excitonic coupling between achiral DPPs within the chiral environment of the polymeric structure. This work affords an interesting example illustrating the potential of π-conjugated helical polymers for chiral optoelectronic applications. Copyright © 2020 Dhbaibi, Shen, Jean, Vanthuyne, Roisnel, Górecki, Jamoussi, Favereau and Crassous.Though molecules exhibiting thermally activated delayed fluorescence (TADF) have seen extensive development in organic light-emitting diodes, their incorporation into polymer nanomaterials and thin films has led to a range of applications in sensing and imaging probes. Triplet quenching can be used to probe oxygen concentration, and the reverse intersystem crossing mechanism which gives rise to TADF can also be used to measure temperature. Moreover, the long emission lifetimes of TADF materials allows for noise reduction in time-gated microscopy, making these compounds ideal for time-resolved fluorescence imaging (TRFI). A polymer matrix enables control over energy transfer between molecules, and can be used to modulate TADF behavior, solubility, biocompatibility, or desirable mechanical properties. Additionally, a polymer's oxygen permeability can be tuned to suit imaging applications in a range of media. Here we review the applications of polymer nanoparticles and films exhibiting TADF in sensing and imaging, demonstrating that this class of materials has great potential beyond electroluminescent devices still waiting to be explored. Copyright © 2020 Paisley, Tonge and Hudson.Magnetic and temperature-sensitive solid lipid particles (mag. SLPs) were prepared in the presence of oleic acid-coated iron oxide (IO-OA) nanoparticles with 1-tetradecanol and poly(ethylene oxide)-block-poly(ε-caprolactone) as lipid and stabilizing surfactant-like agents, respectively. The particles, typically ~850 nm in hydrodynamic size, showed heat dissipation under the applied alternating magnetic field. Cytotoxic activity of the mag.SLPs, non-magnetic SLPs, and iron oxide nanoparticles was compared concerning the mammalian cancer cell lines and their drug-resistant counterparts using trypan blue exclusion test and MTT assay. The mag.SLPs exhibited dose-dependent cytotoxicity against human leukemia cell lines growing in suspension (Jurkat and HL-60/wt), as well as the doxorubicin (Dox)- and vincristine-resistant HL-60 sublines. The mag.SLPs showed higher cytotoxicity toward drug-resistant sublines as compared to Dox. The human glioblastoma cell line U251 growing in a monolayer culture was also sensitive ag.SLPs-induced cytotoxicity. Accordingly, hydrogen peroxide and superoxide radical levels in mag.SLPs-treated Jurkat leukemic cells were increased by ~20-40 and ~70%, respectively. In contrast, the non-magnetic SLPs and neat iron oxides did not influence ROS levels significantly. Thus, the developed mag.SLPs can be used for effective killing of human tumor cells, including drug-resistant ones. Copyright © 2020 Świętek, Panchuk, Skorokhyd, Černoch, Finiuk, Klyuchivska, Hrubý, Molčan, Berger, Trousil, Stoika and Horák.Antiapoptotic members of B-cell leukemia/lymphoma-2 (BCL-2) family proteins are one of the overexpressed proteins in cancer cells that are oncogenic targets. As such, targeting of BCL-2 family proteins raises hopes for new therapeutic discoveries. Thus, we used multistep screening and filtering approaches that combine structure and ligand-based drug design to identify new, effective BCL-2 inhibitors from a small molecule database (Specs SC), which includes more than 210,000 compounds. This database is first filtered based on binary "cancer-QSAR" model constructed with 886 training and 167 test set compounds and common 26 toxicity quantitative structure-activity relationships (QSAR) models. Predicted non-toxic compounds are considered for target-driven studies. Here, we applied two different approaches to filter and select hit compounds for further in vitro biological assays and human cell line experiments. In the first approach, a molecular docking and filtering approach is used to rank compounds based on theCL-2. Short MD simulations are performed for the top-docking poses for each compound in complex with BCL-2. The complexes are again ranked based on their MM/GBSA values to select hit molecules for further long MD simulations and in vitro studies. In total, seven molecules are subjected to biological activity tests in various human cancer cell lines as well as Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) assay. Inhibitory concentrations are evaluated, and biological activities and apoptotic potentials are assessed by cell culture studies. Four molecules are found to be limiting the proliferation capacity of cancer cells while increasing the apoptotic cell fractions. Copyright © 2020 Tutumlu, Dogan, Avsar, Orhan, Calis and Durdagi.
Read More: https://www.selleckchem.com/products/merbarone.html
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