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Modification: The deterioration inhibition associated with stainless through ferrocene-polyoxometalate cross molecular components : experimental and first concepts studies.
Endocrine therapies in the treatment of early and metastatic estrogen receptor α positive (ERα+) breast cancer (BC) are greatly limited by de novo and acquired resistance. Selective estrogen receptor degraders (SERDs) like fulvestrant provide new strategies for endocrine therapy combinations due to unique mechanisms. Herein, we disclose our structure-based optimization of LSZ102 by replacing 6-hydroxybenzothiophene with 6H-thieno[2,3-e]indazole. Subsequent acrylic acid degron modifications led us to identify compound 40 as the preferred candidate. In general, compound 40 showed much better pharmacological profiles than the lead LSZ102, exhibiting growth inhibition of wild-type or tamoxifen-resistant MCF-7 cells, potent ERα degradation, together with superior pharmacokinetic properties, directional target tissue distribution including the brain, and robust antitumor efficacy in the mice breast cancer xenograft model. Currently, 40 is being evaluated in preclinical trials.In Portugal, fungal symbionts of the ambrosia beetle Platypus cylindrus affect tree vigor of cork oak (Quercus suber) and are linked with the cork oak decline process. Fungal symbionts play crucial roles in the life history of bark and ambrosia beetles and recent work indicates complex interactions on the fungal and plant metabolic level. Colonized trees may respond with an array of currently unknown volatile metabolites being indicative of such interactions, acting as infochemicals with their environment. In this study, we examined volatile organic compounds (VOCs) of cork oak seedlings wound inoculated with strains of three fungal associates of P. cylindrus (Raffaelea montetyi, R. SGC-CBP30 quercina, and Ceratocystiopsis sp. nov.) over a 45-day period by means of thermodesorption gas chromatography-mass spectrometry techniques. Fungal strains induced largely quantitative but species-specific changes among the 58 VOCs characterized. Overall, monoterpenes-the major volatiles of cork oak foliage-were significantly reduced, possibly a result of fungal biotransformation. Acetophenone, sulcatone, and nonanal-volatiles known for mediating ambrosia beetle behavior-increased in response to fungal inoculation. Qualitative VOC profiles of excised tissue of wood lesions (21 VOCs) and pure fungal cultures (60 VOCs) showed little overlap with seedling VOCs, indicating their plant-derived but fungal-induced origin. This chemoecological study expands on the limited knowledge of VOCs as infochemicals emitted from oak trees threatened by oak decline in relation to beetle-vectored ophiostomatoid fungi. It opens new avenues of research to clarify mutualistic or pathogenic aspects of these complex symbiotic interactions and develop new control strategies for P. cylindrus, including its mycobiota.Understanding the level and type of resistance in potato varieties is relevant for integrating varietal resistance into the management of potato late blight. Accordingly, 54 potato varieties were tested for their level and type of resistance to late blight in 2019 and 2020 in Denmark. Spreader rows were artificially inoculated to ensure an even inoculum distribution in the trial. Disease severity was assessed once or twice per week. Cluster analysis (CA) was done based on the weighted mean absolute rate (WMAR), the relative area under the disease progress curve, the onset of disease (Xo), the severity of disease in the middle of the season, the time to reach 1% disease severity, the time to reach final disease severity, and the maximum disease severity. The resistance types were determined by comparing the tested varieties to Bintje (susceptible reference) for Xo and WMAR. The CA ranked the varieties as susceptible, moderately resistant, resistant, and very resistant based on their level of resistance. Except for a few varieties, the expressed resistance levels varied between the years. Several varieties that were susceptible in 2019 were moderately resistant in 2020. Also, the types of resistance that the varieties exhibited varied from year to year. In 2020, most varieties exhibited race-specific resistance, while in 2019 they mostly showed susceptible characteristics. The variation between years for the level and types of resistance of the varieties highlights the importance of regularly monitoring varietal resistance across time and space.A linearly decreasing electric field has been previously proven to be effective for diffusional correction of ions in a varying field drift tube (VFDT) system, leading to higher resolving powers compared to a conventional drift tube due to its capacity to narrow distributions midflight. However, the theoretical predictions in resolving power of the VFDT were much higher than what was observed experimentally. The reason behind this discrepancy has been identified as the difference between the theoretically calculated resolving power (spatial) and the experimental one (time). To match the high spatial resolving power experimentally, a secondary high voltage pulse (HVP) at a properly adjusted time is used to provide the ions with enough momentum to increase their drift velocity and hence their time-resolving power. A series of systematic numerical simulations and experimental tests have been designed to corroborate our theoretical findings. The HVP-VFDT atmospheric pressure portable system improves the resolving power from the maximum expected of 60-80 for a regular drift tube to 250 in just 21 cm in length and 7kV, an unprecedent accomplishment.Balanced charge injection is key to achieving perovskite light-emitting diodes (PeLEDs) with a low efficiency roll-off at a high brightness. The use of zinc oxide (ZnO) with a high electron mobility as the charge transport layers is desirable; however, photoluminescence (PL) quenching of a perovskite on ZnO always occurs. Here, a quasi-two-dimensional perovskite on ZnO is explored to uncover the PL quenching mechanism, mainly ascribed to the deprotonation of ammonium cations on the ZnO film in association with the decomposition of low-dimensional perovskite phases. Surprisingly, crystal plane-dependent PL quenching results indicate that the deprotonation rate strongly correlates with the crystal orientation of the ZnO surface. We developed a strategy for suppressing perovskite PL quenching by incorporating an atomic layer deposited Al2O3 onto the ZnO film. Consequently, an efficient inverted PeLED was achieved with a maximum external quantum efficiency of 17.7% and a less discernible efficiency roll-off at a high current density.The precise arrangement of structural subunits is a key factor for the proper shape and function of natural and artificial supramolecular assemblies. In DNA nanotechnology, the geometrically well-defined double-stranded DNA scaffold serves as an element of spatial control for the precise arrangement of functional groups. Here, we describe the supramolecular assembly of chemically modified DNA hybrids into diverse types of architectures. An amphiphilic DNA duplex serves as the sole structural building element of the nanosized supramolecular structures. The morphology of the assemblies is governed by a single subunit of the building block. The chemical nature of this subunit, i.e., polyethylene glycols of different chain length or a carbohydrate moiety, exerts a dramatic influence on the architecture of the assemblies. Cryo-electron microscopy revealed the arrangement of the individual DNA duplexes within the different constructs. Thus, the morphology changes from vesicles to ribbons with increasing length of a linear polyethylene glycol. Astoundingly, attachment of a N-acetylgalactosamine carbohydrate to the DNA duplex moiety produces an unprecedented type of star-shaped architecture. The novel DNA architectures presented herein imply an extension of the current concept of DNA materials and shed new light on the fast-growing field of DNA nanotechnology.High and sustained renal radioactivity accumulation is a major challenge in peptide-based radionuclide imaging and therapy. However, neutral endopeptidase (NEP)-based enzymatic hydrolysis to release and excrete the radioactive fragments has been proven to be an effective and promising way to reduce renal accumulation. Despite the improvement, the effect is still far from being satisfactory. To further reduce kidney uptake, we studied the relationship between the enzymatic reaction rate and the substrate concentration and came up with a combined probe strategy. Model compounds Boc-MVK-Dde and Boc-MFK-Dde were used for an in vitro enzymatic digestion study. NOTA-Exendin 4 and NOTA-MVK-Exendin 4 were labeled with 64Cu for in vivo dose-dependent micro-positron emission tomography (PET) studies. Groups 1 and 2 were injected with 0.2 and 0.8 nmol of 64Cu-NOTA-Exendin 4, respectively. Groups 3-6 were injected with 0.2, 0.8, 1.0, and 1.4 nmol of 64Cu-NOTA-MVK-Exendin 4, respectively. Groups 7 and 8 were co-injected wy. The enzymatic reaction rate of NEP is dependent on the concentration of the substrates both in vitro and in vivo. The combined probe strategy developed in this study can dramatically reduce the renal accumulation of a peptide radioligand without affecting the tumor uptake, which shows great potential in peptide-based radiotheranostics.Resonances in optical systems are useful for many applications, such as frequency comb generation, optical filtering, and biosensing. However, many of these applications are difficult to implement in optical metasurfaces because traditional approaches for designing multiresonant nanostructures require significant computational and fabrication efforts. To address this challenge, we introduce the concept of Fourier lattice resonances (FLRs) in which multiple desired resonances can be chosen a priori and used to dictate the metasurface design. Because each resonance is supported by a distinct surface lattice mode, each can have a high quality factor. Here, we experimentally demonstrate several metasurfaces with flexibly placed resonances (e.g., at 1310 and 1550 nm) and Q-factors as high as 800 in a plasmonic platform. This flexible procedure requires only the computation of a single Fourier transform for its design, and is based on standard lithographic fabrication methods, allowing one to design and fabricate a metasurface to fit any specific, optical-cavity-based application. This work represents a step toward the complete control over the transmission spectrum of a metasurface.We developed organocatalyst systems to promote the cleavage of stable C-H bonds, such as formyl, α-hydroxy, and benzylic C-H bonds, through a hydrogen atom transfer (HAT) process without the use of exogenous photosensitizers. An electronically tuned thiophosphoric acid, 7,7'-OMe-TPA, was assembled with substrate or co-catalyst N-heteroaromatics through hydrogen bonding and π-π interactions to form electron donor-acceptor (EDA) complexes. Photoirradiation of the EDA complex induced stepwise, sequential single-electron transfer (SET) processes to generate a HAT-active thiyl radical. The first SET was from the electron-rich naphthyl group of 7,7'-OMe-TPA to the protonated N-heteroaromatics and the second proton-coupled SET (PCET) from the thiophosphoric acid moiety of 7,7'-OMe-TPA to the resulting naphthyl radical cation. Spectroscopic studies and theoretical calculations characterized the stepwise SET process mediated by short-lived intermediates. This organocatalytic HAT system was applied to four different carbon-hydrogen (C-H) functionalization reactions, hydroxyalkylation and alkylation of N-heteroaromatics, acceptorless dehydrogenation of alcohols, and benzylation of imines, with high functional group tolerance.
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