gebhart/patrepeval huggingface dataset:
Design and Synthesis of Tri-Ring P<sub>3</sub> Benzamide-Containing Aminonitriles as Potent, Selective, Orally Effective Inhibitors of Cathepsin K (2005)

We have prepared a series of achiral aminoacetonitriles, bearing tri-ring benzamide moieties and an aminocyclohexanecarboxylate residue at P2. This combination of binding elements resulted in sub-250 pM, reversible, selective, and orally bioavailable cathepsin K inhibitors. Lead compounds displayed single digit nanomolar inhibition in vitro (of rabbit osteoclast-mediated degradation of bovine bone). The best compound in this series, 39n (CRA-013783/L-006235), was orally bioavailable in rats, with a terminal half-life of over 3 h. 39n was dosed orally in ovariectomized rhesus monkeys once per day for 7 days. Collagen breakdown products were reduced by up to 76% dose-dependently. Plasma concentrations of 39n above the bone resorption IC50 after 24 h indicated a correlation between functional cellular and in vivo assays. Inhibition of collagen breakdown by cathepsin K inhibitors suggests this mechanism of action may be useful in osteoporosis and other indications involving bone resorption.
DNASE1L3 enhances antitumor immunity and suppresses tumor progression in colon cancer (2023)

DNASE1L3, an enzyme highly expressed in DCs, is functionally important for regulating autoimmune responses to self-DNA and chromatin. Deficiency of DNASE1L3 leads to development of autoimmune diseases in both humans and mice. However, despite the well-established causal relationship between DNASE1L3 and immunity, little is known about the involvement of DNASE1L3 in regulation of antitumor immunity, the foundation of modern antitumor immunotherapy. In this study, we identify DNASE1L3 as a potentially new regulator of antitumor immunity and a tumor suppressor in colon cancer. In humans, DNASE1L3 is downregulated in tumor-infiltrating DCs, and this downregulation is associated with poor patient prognosis and reduced tumor immune cell infiltration in many cancer types. In mice, Dnase1l3 deficiency in the tumor microenvironment enhances tumor formation and growth in several colon cancer models. Notably, the increased tumor formation and growth in Dnase1l3-deficient mice are associated with impaired antitumor immunity, as evidenced by a substantial reduction of cytotoxic T cells and a unique subset of DCs. Consistently, Dnase1l3-deficient DCs directly modulate cytotoxic T cells in vitro. To our knowledge, our study unveils a previously unknown link between DNASE1L3 and antitumor immunity and further suggests that restoration of DNASE1L3 activity may represent a potential therapeutic approach for anticancer therapy.
The Varieties of Immunological Experience: Of Pathogens, Stress, and Dendritic Cells (2015)

In the 40 years since their discovery, dendritic cells (DCs) have been recognized as central players in immune regulation. DCs sense microbial stimuli through pathogen-recognition receptors (PRRs) and decode, integrate, and present information derived from such stimuli to T cells, thus stimulating immune responses. DCs can also regulate the quality of immune responses. Several functionally specialized subsets of DCs exist, but DCs also display functional plasticity in response to diverse stimuli. In addition to sensing pathogens via PRRs, emerging evidence suggests that DCs can also sense stress signals, such as amino acid starvation, through ancient stress and nutrient sensing pathways, to stimulate adaptive immunity. Here, I discuss these exciting advances in the context of a historic perspective on the discovery of DCs and their role in immune regulation. I conclude with a discussion of emerging areas in DC biology in the systems immunology era and suggest that the impact of DCs on immunity can be usefully contextualized in a hierarchy-of-organization model in which DCs, their receptors and signaling networks, cell-cell interactions, tissue microenvironment, and the host macroenvironment represent different levels of the hierarchy. Immunity or tolerance can then be represented as a complex function of each of these hierarchies.
Assessment of Multi-mycotoxin Adsorption Efficacy of Grape Pomace (2013)

Grape pomace (pulp and skins) was investigated as a new biosorbent for removing mycotoxins from liquid media. In vitro adsorption experiments showed that the pomace obtained from Primitivo grapes is able to sequester rapidly and simultaneously different mycotoxins. Aflatoxin B1 (AFB1) was the most adsorbed mycotoxin followed by zearalenone (ZEA), ochratoxin A (OTA), and fumonisin B1 (FB1), whereas the adsorption of deoxynivalenol (DON) was negligible. AFB1 and ZEA adsorptions were not affected by changing pH values in the pH 3-8 range, whereas OTA and FB1 adsorptions were significantly affected by pH. Equilibrium adsorption isotherms obtained at different temperatures (5-70 °C) and pH values (3 and 7) were modeled and evaluated using the Freundlich, Langmuir, Sips, and Hill models. The goodness of the fits and the parameters involved in the adsorption mechanism were calculated by the nonlinear regression analysis method. The best-fitting models to describe AFB1, ZEA, and OTA adsorption by grape pomace were the Sips, Langmuir, and Freundlich models, respectively. The Langmuir and Sips models were the best models for FB1 adsorption at pH 7 and 3, respectively. The theoretical maximum adsorption capacities (mmol/kg dried pomace) calculated at pH 7 and 3 decreased in the following order: AFB1 (15.0 and 15.1) > ZEA (8.6 and 8.3) > OTA (6.3-6.9) > FB1 (2.2 and 0.4). Single- and multi-mycotoxin adsorption isotherms showed that toxin adsorption is not affected by the simultaneous presence of different mycotoxins in the liquid medium. The profiles of adsorption isotherms obtained at different temperatures and pH and the thermodynamic parameters (ΔG°, ΔH°, ΔS°) suggest that mycotoxin adsorption is an exothermic and spontaneous process, which involves physisorption weak associations. Hydrophobic interactions may be associated with AFB1 and ZEA adsorption, whereas polar noncovalent interactions may be associated with OTA and FB1 adsorption. In conclusion, this study suggests that biosorption of mycotoxins onto grape pomace may be a reasonably low-cost decontamination method.
Polynomial spline signal approximations: filter design and asymptotic equivalence with Shannon's sampling theorem (1992)

The least-squares polynomial spline approximation of a signal g(t) in L/sub 2/(R) is obtained by projecting g(t) on S/sup n/(R) (the space of polynomial splines of order n). It is shown that this process can be linked to the classical problem of cardinal spline interpolation by first convolving g(t) with a B-spline of order n. More specifically, the coefficients of the B-spline interpolation of order 2n+1 of the sampled filtered sequence are identical to the coefficients of the least-squares approximation of g(t) of order n. It is shown that this approximation can be obtained from a succession of three basic operations: prefiltering, sampling, and postfiltering, which confirms the parallel with the classical sampling/reconstruction procedure for bandlimited signals. The frequency responses of these filters are determined for three equivalent spline representations using alternative sets of shift-invariant basis functions of S/sup n/(R): the standard expansion in terms of B-spline coefficients, a representation in terms of sampled signal values, and a representation using orthogonal basis functions.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Cosmetic aspects of orofacial myofunctional therapy (1988)

Introduction: In maxillofacial, craniofacial, plastic and reconstructive surgeries as well as in general orthodontic treatment, one of the principal concerns for patient management is facial esthetic or cosmetic satisfaction. This is manifested by the numerous articles and manuscripts devoted to the topic of cosmesis. Thousands of dollars are paid yearly to practitioners in these and similar disciplines by patients who want a better chin line, less protrusion in the maxillary region, a smaller or less dynamic nose, the elimination of a diastema between the central incisors, fewer wrinkles and numerous additional cosmetic concerns. These professionals generally acknowledge that the need for treatment of many orofacial anomalies may be based on factors other than impairment of physiological functions or the potential loss of function -- namely, cosmetic concern (Tedesco, et al. 1983; Tobiasen, 1987; Kapp-Simon, 1986). The orofacial myologist must share this concern for improvement of cosmesis and seek and use techniques to augment the cosmetic goals of related professionals.
Survival Training for Aircraft Crews and Passengers (1987)

This paper discusses the need for training helicopter pilots to prevent ditching the aircraft over water. The paper describes the settling up of the new Aircrew Survival Training Centre.
Control of Respirable Dust and Crystalline Silica from Breaking Concrete with a Jackhammer (2003)

(2003). Control of Respirable Dust and Crystalline Silica from Breaking Concrete with a Jackhammer. Applied Occupational and Environmental Hygiene: Vol. 18, No. 7, pp. 491-495.
A primordial and reversible TCA cycle in a facultatively chemolithoautotrophic thermophile (2018)

Inorganic carbon fixation is essential to sustain life on Earth, and the reductive tricarboxylic acid (rTCA) cycle is one of the most ancient carbon fixation metabolisms. A combination of genomic, enzymatic, and metabolomic analyses of a deeply branching chemolithotrophic <i>Thermosulfidibacter takaii</i> ABI70S6<sup>T</sup> revealed a previously unknown reversible TCA cycle whose direction was controlled by the available carbon source(s). Under a chemolithoautotrophic condition, a rTCA cycle occurred with the reverse reaction of citrate synthase (CS) and not with the adenosine 5'-triphosphate-dependent citrate cleavage reactions that had been regarded as essential for the conventional rTCA cycle. Phylometabolic evaluation suggests that the TCA cycle with reversible CS may represent an ancestral mode of the rTCA cycle and raises the possibility of a facultatively chemolithomixotrophic origin of life.
Preparation of Human Immunoglobulin Free of Plasmin and Anticomplement Activities (1977)

Human IgG separated by Cohn fractionation showed variability in the content of aggregates, plasminogen and anticomplement activity. The plasminogen was removed or markedly reduced by affinity chromatography on Sepharose-lysine. Anticomplement activity was reduced by chromatography of Cohn fraction II on DEAE-cellulose. Preparations of IgG obtained by chromatography of intermediates from Cohn fractionation (e.g. Cohn FII + FIII or FII + FIII W) on DEAE-cellulose were devoid of aggregates, plasminogen and exhibited reduced anticomplement activity. The initial levels of specific antibody activity to viral agents were recovered in the IgG fractions. Fragmentation of IgG during storage was prevented or greatly reduced by removal of plasminogen by affinity chromatography on Sepharose-lysine.
Effect of Mulberry Powder on Quality Characteristics and Oxidative Stability of Mayonnaise prepared with Perilla Oil (2014)

This study aimed to investigate the changes in antioxidant activities, quality characteristics, and storage stability of mayonnaise prepared with perilla oil with the addition of mulberry powder ranging from 0 to 5%. The antioxidant activities of perilla oil mayonnaise (PM), as determined by DPPH and ABTS radical scavenging activity, as well as FRAP and total phenolics content were improved by the addition of mulberry powder compared with the control sample. Antioxidant activities were dependent on the amount of mulberry powder added. Lipid oxidation of PM decreased with a higher amount of mulberry powder, based on measurements of peroxide value. The emulsion stability of PM increased with decreases in the amount of mulberry powder level. The a-value in PM color increased with increasing amount of mulberry powder. Sensory evaluation showed that the highest score in overall acceptability of PM was achieved with 4% mulberry.
Lyme Disease (2014)

Erythema migrans at the site of a tick bite is the most common sign of Lyme disease. Antibody testing is generally not helpful in patients with this condition. Treatment with doxycycline, amoxicillin, or cefuroxime is effective for early Lyme disease.
Effective Resistance of a Two Layer Mesh (2011)

The effective resistance of a resistive mesh is a commonly used analogy for various scientific and engineering problems such as voltage drop estimation, distributed control including time synchronization and sensor localization, determining the chemical distance among multiple bonds, and finding the distance between two vertices in a graph. Resistive networks are a commonly used structure in electronics to model different elements of an integrated circuit, such as a physical substrate, an integrated circuit layout, and a power distribution network. On-chip power and ground networks are composed of orthogonal metal lines from different metal layers, and a resistive mesh is typically used to model these networks. A two layer mesh is therefore commonly used to analyze IR voltage drops and decoupling capacitor placement. A closed-form expression is described here for the effective resistance between the intersections of a two layer resistive mesh where the horizontal and vertical unit resistances are different. The physical distance between the nodes of interest and the ratio between the horizontal and vertical resistances are included in the expression. The maximum error of the closed-form expression, as compared with the exact solution, is less than 5% for a wide range of . The error further decreases with greater separation between the nodes of interest.
Highly Birefringent Photonic Crystal Fibre with Enhanced Sensitivity to Hydrostatic Pressure (2006)

We present three constructions of birefringent photonic crystal fibres with increased sensitivity to hydrostatic pressure. The enhancement of sensitivity was obtained by enlarging diameters of several cladding air-holes or by introducing two air channels located symmetrically in the solid part of the cladding. We used nodal based finite elements method to calculate pressure-induced deformations and stress distribution in the fiber cross-section and hybrid edge/nodal finite elements method with perfectly matched layer to calculate propagation constants of the fiber modes. We calculated the spectral dependence of the phase modal birefringence and its susceptibility to hydrostatic pressure. Our results show that the sensitivity to pressure can be increased several times by optimizing the fiber geometry
Content-addressable and associative memory: alternatives to the ubiquitous RAM (1989)

Content-addressable and associative processing systems are explained, and it is shown that such systems are commercially feasible. Content-based archiving and retrieving are compared with address-based storage methods. The principles, advantages and obstacles of content-addressable storage are examined and associative processing methods and architectures are described. Software for associative systems is also discussed.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Optimal Resource Allocation for OFDMA Downlink Systems (2006)

This paper proposes efficient rate and power allocation algorithms for OFDMA downlink systems where each tone is taken by at most one user. Weighted sum rate maximization (WSRmax) and weighted sum power minimization (WSPmin) problems are considered. Since these resource allocation problems are non-convex, complexity of finding the optimal solutions is prohibitively high. This paper employs the Lagrange dual decomposition method to efficiently solve both optimization problems. Because of their non-convex nature, there is no guarantee for the solution obtained by the dual decomposition method to be optimal. However, it is shown that with practical number of tones, the duality gap is virtually zero and the optimal solutions can be efficiently obtained
Effect of the relative permittivity of oxides on the performance of triboelectric nanogenerators (2017)

The influence of the relative permittivity of dielectric materials on the performance of TENGs, by controlling the positive plate with various oxide materials, has been demonstrated.
Amplified Quenching of a Conjugated Polyelectrolyte by Cyanine Dyes (2004)

The conjugated polyelectrolyte PPESO3 features a poly(phenylene ethynylene) backbone substituted with anionic 3-sulfonatopropyloxy groups. PPESO3 is quenched very efficiently (KSV > 10(6) M(-1)) by cationic energy transfer quenchers in an amplified quenching process. In the present investigation, steady-state and picosecond time-resolved fluorescence spectroscopy are used to examine amplified quenching of PPESO3 by a series of cyanine dyes via singlet-singlet energy transfer. The goal of this work is to understand the mechanism of amplified quenching and to characterize important parameters that govern the amplification process. Steady-state fluorescence quenching of PPESO3 by three cationic oxacarbocyanine dyes in methanol solution shows that the quenching efficiency does not correlate with the Forster radius computed from spectral overlap of the PPESO3 fluorescence with the cyanines' absorption. The quenching efficiency is controlled by the stability of the polymer-dye association complex. When quenching studies are carried out in water where PPESO3 is aggregated, changes observed in the absorption and fluorescence spectra of 1,1',3,3,3',3'-hexamethylindotricarbocyanine iodide (HMIDC) indicate that the polymer templates the formation of a J-aggregate of the dye. The fluorescence dynamics in the PPESO3/HMIDC system were probed by time-resolved upconversion and the results show that PPESO3 to HMIDC energy transfer occurs on two distinctive time scales. At low HMIDC concentration, the dynamics are dominated by an energy transfer pathway with a time scale faster than 4 ps. With increasing HMIDC concentration, an energy pathway with a time scale of 0.1-1 ns is active. The prompt pathway (tau < 4 ps) is attributed to quenching of delocalized PPESO3 excitons created near the HMIDC association site, whereas the slow phase is attributed to intra- and interchain exciton diffusion to the HMIDC.
Prognostic value of human kallikrein 10 expression in epithelial ovarian carcinoma. (2001)

Our results indicate that hK10 is a new, independent, unfavorable prognostic marker, especially for late-stage ovarian cancer.
Distributed and energy efficient self-organization for on-off wireless sensor networks (2005)

We utilize clustering to achieve energy efficiency for an on-off wireless sensor network, whose member nodes alternate between active and inactive states. In the proposed distributed and energy efficient self-organization (DEESO) scheme, the head election is adjusted adaptively to the energy reserve of local active nodes. Furthermore, we apply adaptive channel assignment to address the on-off topology changes. Simulation results show that DEESO delivers 184% amount of data to the base station compared to LEACH (low energy adaptive clustering hierarchy) for the same amount of dissipation and the effective network lifetime is extended by around 56%.
Quinazoline antifolates inhibiting thymidylate synthase: variation of the N10 substituent (1985)

The synthesis of 12 new 5,8-dideazafolates with isopropyl, cyclopropylmethyl, 2-fluoroethyl, carbamoylmethyl, phenacyl, 3-fluorobenzyl, 5-uracilylmethyl, carboxymethyl, 2-carboxyethyl, 3-cyanopropyl, 3-hydroxypropyl, and cyanomethyl substituents at N10 is described. In general, the synthetic route involved monoalkylation of diethyl N-(4-amino-benzoyl)-L-glutamate, coupling of the resulting secondary amine with 2-amino-6-(bromomethyl)-4-hydroxyquinazoline hydrobromide in N,N-dimethylacetamide with calcium carbonate as the base, and deprotection using mild alkali. The cyanomethyl derivatives was found to be unexpectedly base labile and was therefore prepared by mild acid deprotection of a di-tert-butyl ester. The compounds were tested as inhibitors of purified L1210 thymidylate synthase (TS). Four members of the series were more potent that the N10-hydrogen compound, but none was superior to the previously described N10-propargyl-5,8-dideazafolic acid. Selected compounds were examined as inhibitors of purified L1210 dihydrofolate reductase (DHFR). As desired, N10 substitution in general reduced DHFR inhibitory activity; these results are discussed. As a measure of cytotoxicity, the compounds were examined for their inhibition of the growth of L1210 cells in culture. None of the new substituents conferred enhanced potency relative to N10-propargyl-5,8-dideazafolic acid (ID50 = 5 microM), which, as the best TS inhibitor and a relatively poor DHFR inhibitor, continues to lead this series.
Enhancing es-hyperneat to evolve more complex regular neural networks (2011)

The recently-introduced evolvable-substrate HyperNEAT algorithm (ES-HyperNEAT) demonstrated that the placement and density of hidden nodes in an artificial neural network can be determined based on implicit information in an infinite-resolution pattern of weights, thereby avoiding the need to evolve explicit placement. However, ES-HyperNEAT is computationally expensive because it must search the entire hypercube, and was shown only to match the performance of the original HyperNEAT in a simple benchmark problem. Iterated ES-HyperNEAT, introduced in this paper, helps to reduce computational costs by focusing the search on a sequence of two-dimensional cross-sections of the hypercube and therefore makes possible searching the hypercube at a finer resolution. A series of experiments and an analysis of the evolved networks show for the first time that iterated ES-HyperNEAT not only matches but outperforms original HyperNEAT in more complex domains because ES-HyperNEAT can evolve networks with limited connectivity, elaborate on existing network structure, and compensate for movement of information within the hypercube.
Ultra-Low Power, Emission Gate Driver With Pulse Width Modulation Using Low-Temperature Poly-Si Oxide Thin-Film Transistors (2021)

We report a novel emission gate driver using low- temperature poly-Si oxide (LTPO) thin-film transistors (TFTs). The proposed circuit consists of eight p-type low-temperature poly-Si (LTPS) and four n-type amorphous InGaZnO (a-IGZO) TFTs. The output pulse width is adjustable by changing the position of starting control signal which has constant pulse width without additional clock signals. The emission gate driver releases the output signals with various duty ratios. Excellent gate driving performance is achieved from the LTPO emission gate driver, although the a-IGZO TFTs have the threshold voltage of −5.5 V. In addition, the power consumption is as low as 5.98 mW in case of 80 <inline-formula xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex-math notation="LaTeX">$\boldsymbol {\mu }\text{s}$ </tex-math></inline-formula> pulse, 10 times of gate pulse, at refresh rate of 120 Hz with full high-definition ( <inline-formula xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex-math notation="LaTeX">$1920\times1080$ </tex-math></inline-formula> ) for active-matrix organic light- emitting diode (AMOLED) display.