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Both surgeons met personally in Brussels in 1950.1,4-Oxaborines represent an expansion of the current array of heteroborines. Herein, we report a new ladder-type bis(1,4-oxaborine)pentacene (BO-Pen), the backbone of which can be regarded as an isoelectronic structure of pentacene. The synthesis begins with a two-fold nucleophilic aromatic substitution followed by a ring-closing reaction. The structure was confirmed by X-ray crystallographic analysis. Compound BO-Pen is stable (even after 160 h) under ambient condition and exhibits very different electronic properties as compared to its all-carbon pentacene analogue (Pen-M). Particularly, it shows bright photoluminescence (73 % relative quantum yield) in both solution and in solid state.The dynamics of cortical neuronal activity plays important roles in controlling body movement and is regulated by connection weights between neurons in a cortex-basal ganglia-thalamus (BGCT) loop. Beta-band oscillation of cortical activity is closely associated with the movement disorder of Parkinson's disease, which is caused by an imbalance in the connection weights of direct and indirect pathways in the BGCT loop. In this study, the authors investigate how the dynamics of cortical activity are modulated by connection weights of direct and indirect pathways in the BGCT loop under low dopamine levels through bifurcation analyses and potential landscapes. The results reveal that cortical activity displays rich dynamics under different connection weights, including one, two, or three stable steady states, one or two stable limit cycles, and the coexistence of one stable limit cycle with one stable steady state or two stable ones. For a low dopamine level, cortical activity exhibits oscillation for larger connection weights of direct and indirect pathways. The stability of these stable dynamics is explored by the potential landscapes.Interactions between glycans and glycan-binding proteins (GBPs) consist of weak, noncovalent, and transient binding events, making them difficult to study in live cells void of a static, isolated system. Furthermore, the glycans are often presented as protein glycoconjugates, but there are limited efforts to identify these proteins. Proximity labeling permits covalent tagging of the glycoprotein interactors to query GBP in live cells. Coupled with high-resolution mass spectrometry, it facilitates determination of the proteins bearing the interacting glycans. In this method, fusion protein constructs of a GBP of interest with a peroxidase enzyme allows for in situ spatiotemporal radical-mediated tagging of interacting glycoproteins in living cells that can be enriched for identification. selleck chemicals llc Using this method, the capture and study of glycan-GBP interactions no longer relies on weak, transient interactions, and results in robust capture and identification of the interactome of a GBP while preserving the native cellular environment. This protocol focuses on (1) expression and characterization of a recombinant fusion protein consisting of a peroxidase and the GBP galectin-3, (2) corresponding in situ labeling and visualization of interactors, (3) and proteomic workflow and analysis of captured proteins for robust identification using mass spectrometry. © 2021 Wiley Periodicals LLC. Basic Protocol 1 Expression, purification, and characterization of recombinant fusion protein Alternate Protocol 1 Manual Ni-NTA purification of recombinant fusion protein Basic Protocol 2 In situ proximity labeling and evaluation by fluorescence microscopy Alternate Protocol 2 Western blot analysis of in situ proximity labeling Basic Protocol 3 Proximity labeling of cells for quantitative MS-based proteomics with tandem mass tags.A novel series of tacrine based cyclopentapyranopyridine- and tetrahydropyranoquinoline-kojic acid derivatives were designed, synthesized, and evaluated as anti-cholinesterase agents. The chemical structures of all target compounds were characterized by 1 H-NMR, 13 C-NMR, and elemental analyses. The synthesized compounds mostly inhibited acetylcholinesterase enzyme (AChE) with IC50 values of 4.18-48.71 μM rather than butyrylcholinesterase enzyme (BChE) with IC50 values of >100 μM. Among them, cyclopentapyranopyridine-kojic acid derivatives showed slightly better AChE inhibitory activity compared to tetrahydropyranoquinoline-kojic acid. The compound 10-amino-2-(hydroxymethyl)-11-(4-isopropylphenyl)-7,8,9,11-tetrahydro-4H-cyclopenta[b]pyrano[2',3' 5,6]pyrano[3,2-e]pyridin-4-one (6f) bearing 4-isopropylphenyl moiety and cyclopentane ring exhibited the highest anti-AChE activity with IC50 value of 4.18 μM. The kinetic study indicated that the compound 6f acts as a mixed inhibitor and the molecular docking studies also illustrated that the compound 6f binds to both the catalytic site (CS) and peripheral anionic site (PAS) of AChE. The compound 6f showed moderate neuroprotective properties against H2 O2 -induced cytotoxicity in PC12 cells. The theoretical ADME study also predicted good drug-likeness for the compound 6f. Based on these results, the compound 6f seems to be a very promising AChE inhibitor for the treatment of Alzheimer's disease.
Black Americans are disproportionately affected by cancer and chronic diseases. Black patients with cancer and their family caregivers may concurrently experience symptoms that influence their wellbeing. This study investigates the influence of mental and physical symptom distress on quality of life (QOL) among Black Americans with cancer and their family caregivers from a dyadic perspective.
One hundred and fifty-one dyads comprised of a Black American with breast, colorectal, lung or prostate cancer and a Black family caregiver were included in this secondary analysis of pooled baseline data from three studies. Self-reports of problems managing 13 symptoms were used to measure mental and physical symptom distress. Descriptive statistics and the actor-partner interdependence model were used to examine symptom prevalence and the influence of each person's symptom distress on their own and each other's QOL.
Fatigue, sleep problems, pain and mental distress were prevalent. Patients and caregivers reported similar levels of mental distress; however, patients reported higher physical distress.