gebhart/patrepeval huggingface dataset:
Paclitaxel and ceramide co‐administration in biodegradable polymeric nanoparticulate delivery system to overcome drug resistance in ovarian cancer (2007)

The objective of this study was to overcome drug resistance upon systemic administration of combination paclitaxel (PTX) and the apoptotic signaling molecule C(6)-ceramide (CER) in biodegradable poly(ethylene oxide)-modified poly(epsilon-caprolactone (PEO-PCL) nanoparticles. Subcutaneous sensitive (wild-type) and multidrug resistant (MDR-1 positive) SKOV-3 human ovarian adenocarcinoma xenografts were established in female Nu/Nu mice. PTX and CER were administered intravenously either as a single agent or in combination in aqueous solution and in PEO-PCL nanoparticles to the tumor-bearing mice. There was significant (p< 0.05) tumor growth suppression in both wild-type SKOV-3 and multidrug resistant SKOV-3(TR) models upon single dose co-administration of PTX (20 mg/kg) and CER (100 mg/kg) in nanoparticle formulations as compared to the individual agents and administration in aqueous solutions. For instance, in SKOV-3 wild-type model, more than 4.3-fold increase (p < 0.05) in tumor growth delay and 3.6-fold (p < 0.05) increase in tumor volume doubling time (DT) were observed with the combination treatment in nanoparticles as compared to untreated animals. Similarly, 3-fold increase (p < 0.05) in tumor growth delay and tumor volume DT was observed in SKOV-3(TR) model. Body weight changes and blood cells counts were used as measures of safety and, except for an increase in platelet counts (p < 0.05) in PTX + CER treated animals, there was no difference between various treatment strategies. The results of this study show that combination of PTX and CER in biodegradable polymeric nanoparticles can serve as a very effective therapeutic strategy to overcome drug resistance in ovarian cancer.
Bioconjugate of biological-active proteins with water-soluble polymers for the clinical application. (1995)

Clinical applications of technological proteins has been limited because of their rapid clearance from the blood, due to glomerular filtration, proteolysis, hepatic uptake and immunogenicity. In recent years, chemical modifications of proteins with water-soluble polymers typified by polyethylene glycol (PEG) have been found to effectively overcome these drawbacks. For instance, PEG-modified proteins have been proven to have increased plasma half-lives and stability, and reduced immunogenicity in vivo. These effects are attributed to an increased molecular weight and steric hindrance, both of which are derived from PEG attached to proteins. However, clinical application of modified proteins has been limited yet. This is due to the conflicting effects of chemical modification of proteins ; modified proteins limited the transport from blood to tissues due to the high molecular weight, and sterically inhibited the binding to their receptor, resulting in loss of bioactivity. Nevertheless, an optimal modification-condition, which is a well-balanced tissue transport, receptor-binding, and plasma clearance, must be in existence. For the molecular design of modified proteins applicable to clinical use, the discovery of the optimal modification-condition, which is dominated by the steric hindrance and molecular weight, should be a primary concern. In this review, we indicated that the optimal modification of biological-active protein, such as TNFα, with water-soluble polymer markedly increased its bioavailability and was also reduced its toxic side-effects. This review will provide a fundamental information enabling us to design the modified proteins applicable to therapeutic use.
Nanometer-precision linear sorting with synchronized optofluidic dual barriers (2018)

The past two decades have witnessed the revolutionary development of optical trapping of nanoparticles, most of which deal with trapping stiffness larger than 10<sup>-8</sup> N/m. In this conventional regime, however, it remains a formidable challenge to sort out sub-50-nm nanoparticles with single-nanometer precision, isolating us from a rich flatland with advanced applications of micromanipulation. With an insightfully established roadmap of damping, the synchronization between optical force and flow drag force can be coordinated to attempt the loosely overdamped realm (stiffness, 10<sup>-10</sup> to 10<sup>-8</sup> N/m), which has been challenging. This paper intuitively demonstrates the remarkable functionality to sort out single gold nanoparticles with radii ranging from 30 to 50 nm, as well as 100- and 150-nm polystyrene nanoparticles, with single nanometer precision. The quasi-Bessel optical profile and the loosely overdamped potential wells in the microchannel enable those aforementioned nanoparticles to be separated, positioned, and microscopically oscillated. This work reveals an unprecedentedly meaningful damping scenario that enriches our fundamental understanding of particle kinetics in intriguing optical systems, and offers new opportunities for tumor targeting, intracellular imaging, and sorting small particles such as viruses and DNA.
Supplemental Figure 6 from Short- and Long-Term Effects of CDK4/6 Inhibition on Early-Stage Breast Cancer (2023)

&lt;p&gt;Palbociclib's transcriptomic effects on tumors&lt;/p&gt;
Phase-II study of the new aza-anthracenedione, BBR 2778, in patients with relapsed aggressive non-Hodgkin's lymphomas. (2003)

These results indicate that 85 mg/m2 BBR 2778 in a q1w x 3 schedule is active in elderly and pretreated patients with relapsed aggressive NHL and was generally well tolerated. Thus, we recommend further clinical evaluation of this new compound in phase-III studies for the treatment of NHL.
Application of an Sb Surfactant in InGaAs Nano-ridge Engineering on 300 mm Silicon Substrates (2021)

Nano-ridge engineering (NRE) is a novel heteroepitaxial integration approach for III–V devices on Si substrates. It starts with selective area growth in narrow trenches for misfit defect trapping. Growth is then continued out of the trenches to engineer the nano-ridges (NRs). Different device concepts such as lasers and transistors have been demonstrated using box-shaped NRs. To widen the field of applications, NRE is extended to the alloy In0.53Ga0.47As. The In and Ga incorporation depends strongly on the exposed NR facets; hence, composition fluctuation has to be limited to avoid misfit defect formation. Growth conditions, which typically ensure the formation of a box-shaped NR, result in nonuniform InGaAs NR lines. For the first time, an Sb surfactant was applied in NRE to achieve uniform and box-shaped InGaAs NRs. A detailed structural investigation shows that the presence of Sb improves the In-distribution in the NR but reduces the gliding efficiency of threading dislocations, which is essential for the misfit defect reduction inside the trench. A two-step growth approach was developed to overcome this drawback and to still benefit from the desired impact of a surfactant on the InGaAs box-formation, which ensures InGaAs NRs with high crystal quality.
Atriopeptin stimulates chloride secretion in cultured shark rectal gland cells (1991)

Monolayer cultures of shark rectal gland (SRG) epithelial cells were treated with atriopeptin (AP), and the effects on Cl- secretion and intracellular guanosine 3',5'-cyclic monophosphate (cGMP) accumulation were examined. Basolateral or apical exposure to 10(-7) M AP markedly stimulated (8-fold) Cl(-)-dependent, bumetanide-sensitive, short-circuit current (Isc). The AP-stimulated Isc exhibited transient oscillations before reaching a steady state. This behavior is not observed when Isc is activated by other secretagogues such as vasoactive intestinal peptide, 2-chloroadenosine, forskolin, or ionomycin. Intracellular cGMP was concomitantly elevated (10-fold) by 10(-7) M AP. Both Isc stimulation and cGMP accumulation responses exhibited a similar dose dependency beginning at an AP concentration of 1 nM. The bilateral response to AP suggests the presence of receptors on both apical and basolateral plasma membranes. These results are the first demonstration of a direct effect of AP on Cl(-)-secreting epithelial cells. These data also suggest a role for cGMP in mediating Cl- secretion in these cells.
A design framework for teleoperators with kinesthetic feedback (1989)

The application of a hybrid two-port model to teleoperators with force and velocity sensing at the master and slave is presented. The interfaces between human operator and master, and between environment and slave, are ports through which the teleoperator is designed to exchange energy between the operator and the environment. By computing or measuring the input-output properties of this two-port network, the hybrid two-port model of an actual or simulated teleoperator system can be obtained. It is shown that the hybrid model (as opposed to other two-port forms) leads to an intuitive representation of ideal teleoperator performance and applies to several teleoperator architectures. Thus measured values of the h matrix or values computed from a simulation can be used to compare performance with the ideal. The frequency-dependent h matrix is computed from a detailed SPICE model of an actual system, and the method is applied to a proposed architecture.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Intracortical microstimulation pulse waveform and frequency recruits distinct spatiotemporal patterns of cortical neuron and neuropil activation (2022)

Abstract Background Neural prosthetics often use intracortical microstimulation (ICMS) for sensory restoration. To restore natural and functional feedback, we must first understand how stimulation parameters influence the recruitment of neural populations. ICMS waveform asymmetry modulates the spatial activation of neurons around an electrode at 10 Hz; however, it is unclear how asymmetry may differentially modulate population activity at frequencies typically employed in the clinic (e.g. 100 Hz). Objective We hypothesized that stimulation waveform asymmetry would differentially modulate preferential activation of certain neural populations, and the differential population activity would be frequency-dependent. Methods We quantified how asymmetric stimulation waveforms delivered at 10 Hz or 100 Hz for 30s modulated spatiotemporal activity of cortical layer II/III pyramidal neurons using in vivo two-photon and mesoscale calcium imaging in anesthetized mice. Asymmetry is defined in terms of the ratio of the leading phase to the return phase of charge-balanced cathodal- and anodal-first waveforms. Results Neurons within 40-60μm of the electrode display stable stimulation-induced activity indicative of direct activation, which was independent of waveform asymmetry. The stability of 72% of activated neurons and the preferential activation of 20-90 % of neurons depended on waveform asymmetry. Additionally, this asymmetry-dependent activation of different neural populations was associated with differential progression of population activity. Specifically, neural activity increased over time for some waveforms at 10 Hz, but decreased more at 100 Hz than other waveforms. Conclusion These data demonstrate that at frequencies commonly used for sensory restoration, stimulation waveform alters the pattern of activation of different but overlapping populations of excitatory neurons. The impact of these waveform specific responses on the activation of different subtypes of neurons as well as sensory perception merits further investigation.
A three-million-transistor microprocessor (2003)

Describes a RISC (reduced-instruction-set computer) BiCMOS superscalar microprocessor containing 3.1 M transistors which executes up to three instructions per clock cycle. Clock frequency is 40 MHz with 8 mW dissipation. The chip includes a 32-b integer pipeline (IU), a memory management unit (MMU), a 20-kB instruction cache (I cache), a 16-kB data cache (D cache), an IEEE-compatible double-precision floating-point unit (FU), and a bus interface (BU). The chip supports built-in self-test, internal and JTAG boundary scan, in-circuit emulation for remote symbolic source-code debugging, and hardware to support multiprocessor system architecture. An on-chip phase-locked loop synchronizes external and internal clock edges. The chip is implemented in a 0.8- mu m triple-layer-metal salacided BiCMOS process. The die is 15.98*15.98 mm/sup 2/, with 166 active pins and 127 power/ground pins.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Emergent dynamics of light-induced active colloids probed by XPCS (2022)

Abstract Self-propelled particulate systems manifest certain collective behavior of living matter, which have been the subject of intense research over the past decades. One of the elegant methods for realizing such active motions is by means of custom synthesized Janus particles suspended in a catalytic medium that can be triggered upon illumination by ultraviolet light. In this work, the evolution of the particle dynamics from passive diffusive to active ballistic behavior upon light illumination was probed by multispeckle x-ray photon correlation spectroscopy (XPCS). This technique enables not only studying the emergence of active motions in three dimensions (3D) but also deciphering different contributions to the overall dynamics. Using a combination of homodyne and heterodyne analysis, the ensemble averaged mean velocity, velocity fluctuations and diffusion coefficient of particles were determined in the thermodynamic limit. Results revealed a gradual transition from diffusive to ballistic dynamics with systematic increase of the catalytic activity. At the intermediate region, the dynamics is dominated by Gaussian velocity fluctuations and an enhanced relaxation rate with a weaker wave vector dependence similar to superdiffusive behavior. For the highest activity, the dynamics became purely ballistic with Lorentzian-like distribution of velocity fluctuations. Presented results demonstrate that different aspects of active dynamics can be investigated in 3D over a broad range of Péclet numbers and other control parameters by means of multispeckle XPCS.
Sex-Related Motor Deficits in the Tau-P301L Mouse Model (2021)

The contribution of mouse models for basic and translational research at different levels is important to understand neurodegenerative diseases, including tauopathies, by studying the alterations in the corresponding mouse models in detail. Moreover, several studies demonstrated that pathological as well as behavioral changes are influenced by the sex. For this purpose, we performed an in-depth characterization of the behavioral alterations in the transgenic Tau-P301L mouse model. Sex-matched wild type and homozygous Tau-P301L mice were tested in a battery of behavioral tests at different ages. Tau-P301L male mice showed olfactory and motor deficits as well as increased Tau pathology, which was not observed in Tau-P301L female mice. Both Tau-P301L male and female mice had phenotypic alterations in the SHIRPA test battery and cognitive deficits in the novel object recognition test. This study demonstrated that Tau-P301L mice have phenotypic alterations, which are in line with the histological changes and with a sex-dependent performance in those tests. Summarized, the Tau-P301L mouse model shows phenotypic alterations due to the presence of neurofibrillary tangles in the brain.
Using chromatic confocal apparatus for in situ rolling thickness measurement in hot embossing process (2010)

The in-situ measurements for continuously rolling optical films by the chromatic confocal apparatus have been successfully achieved by the authors. The apparatus presented here consists of chromatic confocal to avoid the vibrations caused by the roller machine while working. Without the need of the vertical z axis scan, chromatic confocal can give instant thickness measurements. Therefore, the apparatus possesses the characters of high resolution and fast response. We believe that this system can highly monitor and improve the yield rate in production lines.
Room-Temperature $\lambda\approx 2.7~\mu{\rm m}$ Quantum Cascade Laser Sources Based on Intracavity Second-Harmonic Generation (2011)

We present experimental results on a short-wavelength quantum cascade laser based on intracavity second-harmonic generation. Our devices consist of an injectorless quantum cascade laser, which serves as a pump, and a transversely integrated passive two-well nonlinear section. The presented devices demonstrate above 1 mW output power at 2.65 μm emission wavelength with a record high peak conversion efficiency of 278 mW/W <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> at 80 K and still around 10 μW at 2.73 μm emission wavelength with 770 μW/W <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> conversion efficiency at room temperature. Experimental threshold current densities are demonstrated to be as low as 1.5 kA/cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> at room temperature.
Massively Multidimensional Diffusion-Relaxation Correlation MRI (2022)

Diverse approaches such as oscillating gradients, tensor-valued encoding, and diffusion-relaxation correlation have been used to study microstructure and heterogeneity in healthy and pathological biological tissues. Recently, acquisition schemes with free gradient waveforms exploring both the frequency-dependent and tensorial aspects of the encoding spectrum b ( ω ) have enabled estimation of nonparametric distributions of frequency-dependent diffusion tensors. These “ D ( ω )-distributions” allow investigation of restricted diffusion for each distinct component resolved in the diffusion tensor trace, anisotropy, and orientation dimensions. Likewise, multidimensional methods combining longitudinal and transverse relaxation rates, R 1 and R 2, with ( ω -independent) D -distributions capitalize on the component resolution offered by the diffusion dimensions to investigate subtle differences in relaxation properties of sub-voxel water populations in the living human brain, for instance nerve fiber bundles with different orientations. By measurements on an ex vivo rat brain, we here demonstrate a “massively multidimensional” diffusion-relaxation correlation protocol joining all the approaches mentioned above. Images acquired as a function of the magnitude, normalized anisotropy, orientation, and frequency content of b ( ω ), as well as the repetition time and echo time, yield nonparametric D ( ω )- R 1 - R 2 -distributions via a Monte Carlo data inversion algorithm. The obtained per-voxel distributions are converted to parameter maps commonly associated with conventional lower-dimensional methods as well as unique statistical descriptors reporting on the correlations between restriction, anisotropy, and relaxation.
Enhancing the Sensitivity of the Virus BioResistor by Overoxidation: Detecting IgG Antibodies (2021)

The Virus BioResistor (VBR) is a biosensor capable of rapid and sensitive detection of small protein disease markers using a simple dip-and-read modality. For example, the bladder cancer-associated protein DJ-1 (22 kDa) can be detected in human urine within 1.0 min with a limit of detection (LOD) of 10 pM. The VBR uses engineered virus particles as receptors to recognize and selectively bind the protein of interest. These virus particles are entrained in a conductive poly(3,4-ethylenedioxythiophene) or PEDOT channel. The electrical impedance of the channel increases when the target protein is bound by the virus particles. But VBRs exhibit a sensitivity that is inversely related to the molecular weight of the protein target. Thus, large proteins, such as IgG antibodies (150 kDa), can be undetectable even at high concentrations. We demonstrate that the electrochemical overoxidation of the VBR's PEDOT channel increases its electrical impedance, conferring enhanced sensitivity for both small and large proteins. Overoxidation makes possible the detection of two antibodies, undetectable at a normal VBR, with a limit of detection of 40 ng/mL (250 pM), and a dynamic range for quantitation extending to 600 ng/mL.
Grigory Yakovlevich Kogan: Director of the Leningrad Pharmaceutical Institute in 1938-1941 (2020)

On the basis of archival and little-known documents, the biography of a specialist in pharmaceutical chemistry in the field of galena drugs technology, was reconstructed in the article. Grigory Yakovlevich Kogan (1889-1956), D.Sc. in Pharmaceutical Sciences, Professo held senior positions in the 1920s and 1930s in the leading pharmaceutical institutions: the Leningrad Military-Medical Preparations Plant, the Leningrad Scientific and Pharmaceutical Society. In 1938-1941 G. Kogan was the Director of theLeningrad Pharmaceutical Institute (now Saint Petersburg State Chemical Pharmaceutical University), after the war, he headed the Department of Technology of Medicinal Forms and Galena Drugs at the Moscow Pharmaceutical Institute (now I.M.Sechenov First Moscow State Medical University). Based on the analysis of his scientific and pedagogical activities, his contribution to the development of national and world pharmacy and training of specialists in the USSR has been revealed.
Synthesis of 3-Aminomethyl-3-fluoropiperidines (2009)

A synthetic route toward new 1-alkyl-3-aminomethyl-3-fluoropiperidines, which are of high interest as building blocks in medicinal chemistry, is described. The Successful approach consists of the fluorination of ethyl 3-chloropropyl-2-cyanoacetate with N-fluorodibenzenesulfonimide (NFSI) and transformation of the ester moiety into different amides, yielding N-alkyl-5-chloro-2-cyano-2-fluoropentanamides. Ring closure was achieved under basic conditions, yielding 1-alkyl-3-fluoro-2-oxopiperidine-3-carbonitriles. After reduction of the obtained lactams with borane, the desired 3-aminomethyl-3-fluoropiperidines were obtained in good yields.
An N,N-Bis(benzimidazolylpicolinoyl)piperazine (BT-11): A Novel Lanthionine Synthetase C-Like 2-Based Therapeutic for Inflammatory Bowel Disease (2016)

Lanthionine synthetase C-like 2 (LANCL2), a novel therapeutic target for inflammatory and autoimmune diseases and diabetes, exerts anti-inflammatory and insulin-sensitizing effects. This study reports the first LANCL2-based therapeutics for inflammatory bowel disease (IBD). Analogues of 1 (ABA) and 2 (NSC61610) were screened by molecular docking, then synthesized and analyzed for binding to LANCL2 by surface plasmon resonance. Piperazine-1,4-diylbis(6-benzo[d]imidazole-2-yl)pyridine-2-yl)methanone, 7, was identified as the lead LANCL2-binding compound for treating IBD. The oral treatment with 7 (8 mg/kg/d) in a mouse model of IBD resulted in lowering the disease activity index, decreasing colonic inflammatory lesions by 4-fold, and suppressing inflammatory markers (e.g., TNF-α, and interferon-γ) in the gut. Furthermore, studies in LANCL2-/- mice demonstrated that loss of LANCL2 abrogated beneficial actions of 7, suggesting high selectivity for the target. In conclusion, 7 merits continued development as a LANCL2-based, first-in-class orally active therapeutic for IBD.
ChemInform Abstract: 4‐Nitrophenyltriflate and 4‐Nitrophenylnonaflate as New Perfluoroalkanesulfonyl Transfer Agents: Experimental and Computational Studies. (2000)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Measurement and modelling of dark current decay transients in perovskite solar cells (2016)

The current decay in response to a sudden change of applied bias up to 1 V has been measured on a methylammonium lead triiodide perovskite solar cell, for temperatures between 258 and 308 K.