gebhart/patrepeval huggingface dataset:
Synthesis and Biological Evaluation of Novel <i>N</i><sup>6</sup>-[4-(Substituted)sulfonamidophenylcarbamoyl]adenosine-5‘-uronamides as A<sub>3</sub> Adenosine Receptor Agonists (2004)

A new series of 1-deoxy-1-[(6-(4-(substituted-aminosulfonyl)phenyl)amino)carbonylamino-9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamides (83-102) have been synthesized and tested at the human A3 adenosine receptor subtype. All the derivatives described in this work displayed affinity versus this receptor in the nanomolar range and good selectivity versus A1 adenosine receptor subtype, confirming that the p-sulfonamido moiety positively affected the activity of the molecules. The best substituents at the sulfonamido nucleus were found to be small alkyl groups, like methyl, isopropyl, ethyl, or allyl moieties (compounds 96-100), whereas monosubstitution at the amino group led to a decrease in A3 affinity values. The selectivity versus A1 adenosine receptor subtype is increased when the amino group in the sulfonamido core is represented by a hydrogenated heterocyclic ring like piperidine, morpholine, or pyrroline. Bulky groups, like adamantane and alkyl chains with more than four carbon atoms, are detrimental for the affinity and the selectivity of the A3 adenosine receptor agonists described here.
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 <i>In Vivo</i> (2022)

The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degrader <b>CCT369260</b> to <b>CCT373566</b>, a highly potent probe suitable for sustained depletion of BCL6 <i>in vivo</i>. We observed a sharp degradation SAR, where subtle structural changes conveyed the ability to induce degradation of BCL6. <b>CCT373566</b> showed modest <i>in vivo</i> efficacy in a lymphoma xenograft mouse model following oral dosing.
Quantitative nature of the Prolamin‐box, ACGT and AACA motifs in a rice glutelin gene promoter: minimal <i>cis</i>‐element requirements for endosperm‐specific gene expression (2000)

The -197 bp promoter of the rice seed storage protein gene, GluB-1, is capable of conferring endosperm-specific gene expression. This proximal 5' flanking region contains four motifs, GCN4, AACA, ACGT and Prolamin-box, which are conserved in many seed storage protein genes. We previously showed that multiple copies of GCN4 conferred endosperm expression pattern when fused to the -46 core promoter of CaMV 35S. In this paper we demonstrate, using a similar approach, that tandem repeated copies of any of the other three motifs are unable to direct expression in seeds as well as other tissues of transgenic rice plants. Mutational analysis of individual motifs in the -197 bp promoter resulted in remarkable reductions in promoter activity. These results indicate that the GCN4 motif acts as an essential element determining endosperm-specific expression and that the AACA, ACGT and Prolamin-box are involved in quantitative regulation of the GluB-1 gene. A set of gain-of-function experiments using transgenic rice showed that either the Prolamin-box or AACA, although often coupled with GCN4 in many genes, is insufficient to form a functional promoter unit with GCN4, whereas a combination of GCN4, AACA and ACGT motifs was found sufficient to confer a detectable level of endosperm expression. Taken together, our results provide direct insight into the importance of combinatorial interplay between cis-elements in regulating the expression of seed storage protein genes.
A study of pulsed activation of trapped field magnets: effects of multiple pulsing (2013)

Experimental studies are reported for pulsed activation of trapped field magnets (TFMs), using a sequence of N equal pulses. These experiments are done on low field TFMs for which temperature increase is not yet a dominant limitation. For low and moderate amplitudes of activation pulses heights, BA, the trapped field at any distance r from the TFM centre increases as BT(r,N) ∝ klogN, where k is not a function of N. Thus the increment in trapped field is ∝1/N. Since logN increases without limit as N → ∞, while BT is limited by finite JC, limits are expected on the logN increase. The limiting behaviour is observed at higher values of BT(r,N), and is very well fitted by the multiplicative factor [1 − BT(r,N − 1)/B*(r)]. The resulting phenomenological equation fits the data at essentially all values of N, r, and BA. In this equation, B*(r) plays the role of the limiting value of BT(r) as N → ∞. A study of B*(r) leads to its identification as the trapped field reached in a zero-field-cool activation using a constant field of the same magnitude as the pulsed field.
Carotenoid Extraction from Plants Using a Novel, Environmentally Friendly Solvent (2009)

Few environmentally friendly solvents are available to extract carotenoids for use in foods. The most effective known solvents are products of the petroleum industry and toxic for human consumption. Yet carotenoid extracts are desirable for use in dietary supplements and as additives to enhance the health benefits of processed foods. Ethyl lactate is an excellent solvent to extract both trans- and cis-lycopene isomers from dried tomato powder, the extraction efficiency of which is enhanced by the addition of the antioxidants alpha-tocopherol and alpha-lipoic acid, both of which are known to benefit human health. It is also useful to extract lutein and beta-carotene from dried powders prepared from white corn and carrots. Because of its low flammability and its origin as a byproduct of the corn and soybean industries, it is more advantageous than ethyl acetate, which is a petroleum product.
Fire and heat resistant laminating resins based on malemeido and citraconimido substituted 1 -2,4- and -2,6- diaminobenzenes (1987)

A novel class of fire and heat resistant bisimide resins prepared by thermal polymerization of maleimido or citraconimido substituted 1-(dialkox phosphonyl) methyl-2-4 and -2,6-diamino benzenes was presented. The polymer precursors are prepared by reacting 1-(diorgano oxyphosphonyl) methyl-2-4- and -2,6-diamino benzenes with maliec anhydride or citraconic anhydride in a mole ratio 1:2. Chain extension of the monomers is achieved by reacting the mono-N-maleimido derivaties of 1 (diorgano oxyphosphonyl) methyl -2,4- and -2,6-diamino benzenes with aryl tetracarboxylic dianhydrides, such as benzophenone tetracarboxylic dianhydride, or aryl diisocyanates, such as methylene bis(4-phenyl isocyanate), in a mole ratio 2:1. The polymerization of the monomers is studied by diferential scanning calorimetry and the thermal stability of the polymers is ascertained by thermogravimetric analysis.
Photonic arbitrary waveform generator (2002)

We describe a novel photonic method for generating wideband RF waveforms with arbitrary amplitude, frequency, and phase modulation. By eliminating the need for electronic DACs, the photonic arbitrary (electronic) waveform generator (PAWG) promises wideband operation in the millimeter wave region and beyond.
A Package-Integrated Chireix Outphasing RF Switch-Mode High-Power Amplifier (2013)

<?Pub Dtl=""?> This paper describes the design and implementation of a package-integrated Chireix outphasing RF switch-mode power amplifier (PA). The optimum loading conditions, based on class E, and the Chireix compensation elements are provided to the active devices by a dedicated low-loss bondwire-based transformer power combiner that enables a very small form factor and low cost. The realized prototype achieved 70.6-W peak power with 73% peak drain efficiency at 2.3 GHz and 28 V, and up to 81% peak drain efficiency at 2.2 GHz and 20 V. When operated for maximum power at 28 V, it reached 53.5%/43.5% average drain/total efficiency for a 9.6-dB peak-to-average-power-ratio W-CDMA signal at 2.3 GHz with low ACLR1/2 levels ( <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex Notation="TeX">${-}{\hbox{49}}$</tex></formula> / <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex Notation="TeX">${-}{\hbox{56}}$</tex></formula> dBc after memoryless digital predistortion). Moreover, from 2.1 to 2.4 GHz, the realized PA demonstrated more than 50% drain efficiency across <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex Notation="TeX">${>}{\hbox{260}}$</tex></formula> , <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex Notation="TeX">${>}{\hbox{160}}$</tex></formula> , and <formula formulatype="inline" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex Notation="TeX">${>}{\hbox{80}}$</tex></formula> MHz at 6-, 8-, and 10-dB back-off, respectively.
Clinical development of malaria vaccine (2010)

熱帯熱マラリアは熱帯・亜熱帯地域を中心に流行し，抜本的な対策としてマラリアワクチンの開発に期待が寄せられているが，いまだ著効を示すワクチン実用化の目処はたっていない．本稿では，世界で実施されてきたマラリアワクチン開発のレヴューとともに，筆者らが発見したマラリア原虫のアキレス腱と考えられるSERA5抗原から開発したSE36マラリアワクチン臨床開発の現状を報告する．また，最近筆者らが見いだした防御エピトープと自然免疫アジュバントの一つであるCpGを組み合わせることにより，より抗原性を改良した第二世代SE36マラリアワクチンの展望について述べる．
An Emerging Screening Method for Interrogating Human Brain Function: Tutorial (2023)

Cognitive decline can be observed due to a myriad of causes. Clinicians would benefit from a noninvasive quantitative tool to screen and monitor brain function based on direct measures of neural features. In this study, we used neuroimaging data from magnetoencephalography (with a whole-head Elekta Neuromag 306 sensor system) to derive a set of features that strongly correlate with brain function. We propose that simple signal characteristics related to peak variability, timing, and abundance can be used by clinicians as a screening tool to investigate cognitive function in at-risk individuals. Using a minimalistic set of features, we were able to perfectly distinguish between participants with normative and nonnormative brain function, and we were also able to successfully predict participants' Mini-Mental Test score (r=0.99; P<.001; mean absolute error=0.413). This set of features can be easily visualized in an analog fashion, providing clinicians with several graded measurements (in comparison to a single binary diagnostic tool) that can be used for screening and monitoring cognitive decline.
Correction: Conversion of landfill gas to liquid fuels through a TriFTS (tri-reforming and Fischer–Tropsch synthesis) process: a feasibility study (2019)

Correction for ‘Conversion of landfill gas to liquid fuels through a TriFTS (tri-reforming and Fischer–Tropsch synthesis) process: a feasibility study’ by Xianhui Zhao <italic>et al.</italic>, <italic>Sustainable Energy Fuels</italic>, 2019, <bold>3</bold>, 539–549.
PLISS: Detecting and Labeling Places Using Online Change-Point Detection (2010)

We present PLISS (Place Labeling through Image Sequence Segmentation), a novel technique for place recognition and categorization from visual cues. PLISS operates on video or image streams and works by segmenting it into pieces corresponding to distinct places in the environment. An online Bayesian change-point detection framework that detects changes to model parameters is used to segment the image stream. Unlike current place recognition methods, in addition to using previously learned place models for labeling, PLISS can also detect and learn a previously unknown place or place category in an online manner. Moreover, since both the inferred boundaries of places (change-points) and the place labels are fully probabilistic, they can indicate when the inference is uncertain. New places and categories are detected using a systematic statistical hypothesis testing framework. We present extensive experiments on a large and difficult image dataset. We validate our claims by comparing results obtained using different types of features and by comparing results from PLISS against the state of the art.
Ranking Causal Anomalies via Temporal and Dynamical Analysis on Vanishing Correlations (2016)

Modern world has witnessed a dramatic increase in our ability to collect, transmit and distribute real-time monitoring and surveillance data from large-scale information systems and cyber-physical systems. Detecting system anomalies thus attracts significant amount of interest in many fields such as security, fault management, and industrial optimization. Recently, invariant network has shown to be a powerful way in characterizing complex system behaviours. In the invariant network, a node represents a system component and an edge indicates a stable, significant interaction between two components. Structures and evolutions of the invariance network, in particular the vanishing correlations, can shed important light on locating causal anomalies and performing diagnosis. However, existing approaches to detect causal anomalies with the invariant network often use the percentage of vanishing correlations to rank possible casual components, which have several limitations: 1) fault propagation in the network is ignored; 2) the root casual anomalies may not always be the nodes with a high-percentage of vanishing correlations; 3) temporal patterns of vanishing correlations are not exploited for robust detection. To address these limitations, in this paper we propose a network diffusion based framework to identify significant causal anomalies and rank them. Our approach can effectively model fault propagation over the entire invariant network, and can perform joint inference on both the structural, and the time-evolving broken invariance patterns. As a result, it can locate high-confidence anomalies that are truly responsible for the vanishing correlations, and can compensate for unstructured measurement noise in the system. Extensive experiments on synthetic datasets, bank information system datasets, and coal plant cyber-physical system datasets demonstrate the effectiveness of our approach.
Magnetic needles and superparamagnetic cells (2007)

Superparamagnetic nanoparticles can be attached in great numbers to pathogenic cells using specific antibodies so that the magnetically-labeled cells themselves become superparamagnets. The cells can then be manipulated and drawn out of biological fluids, as in a biopsy, very selectively using a magnetic needle. We examine the origins and uncertainties in the forces exerted on magnetic nanoparticles by static magnetic fields, leading to a model for trajectories and collection times of dilute superparamagnetic cells in biological fluids. We discuss the design and application of such magnetic needles and the theory of collection times. We compare the mathematical model to measurements in a variety of media including blood. For more information on this article, see medicalphysicsweb.org.
OPERATIONAL CONCEPTS AND IMPLEMENTATION TECHNIQUES FOR VEHICLE-FOLLOWER CONTROL OF AGT SYSTEMS (1979)

This report presents a new baseline approach for the vehicle-follower for the longitudinal control of Automated Guideway Transit (AGT) vehicles. It is shown that for the short headways (0.5 to 3.0 s) contemplated for such systems, a kinematic constraint on the spacing between vehicles exists during speed transit maneuvers. This constraint is a nonlinear function of the service jerk and acceleration limits imposed on vehicle operation and also on the instantaneous values of the state variables of neighboring vehicles. The constraint is explicitly included in an analytical development of the control law, which is then shown to control satisfactorily vehicles during overtaking maneuvers and merging maneuvers up to full line capacity, and to regulate perturbations about nominal operating conditions. Modification of the kinematic constraint is then shown to generalize the approach to the problem of vehicle egress from an off-line station into main line traffic flow, including gap generation. Minimum required station egresslane lengths are then established as a function of headway. The station egress control is shown to be safe and effective even in the event of off-nominal behavior of vehicles in the main line traffic flow. Finally, the implementation requirements for the control are shown to be best satisfied by a smart vehicle control configuration, with state variables for vehicle spacing, velocity, and acceleration transmitted through wayside equipment at intervals of approximately one-fifth operational headway. Other headway-dependent factors determined in the implementation analysis are the permissible time delay for data transmission, the required on-board computation rate, and required levels of digital quantization. Results indicate that the control is compatible with existing microprocessor technology.
Leveraging Multiple GPUs and CPUs for Graphlet Counting in Large Networks (2016)

Massively parallel architectures such as the GPU are becoming increasingly important due to the recent proliferation of data. In this paper, we propose a key class of hybrid parallel graphlet algorithms that leverages multiple CPUs and GPUs simultaneously for computing k-vertex induced subgraph statistics (called graphlets). In addition to the hybrid multi-core CPU-GPU framework, we also investigate single GPU methods (using multiple cores) and multi-GPU methods that leverage all available GPUs simultaneously for computing induced subgraph statistics. Both methods leverage GPU devices only, whereas the hybrid multi-core CPU-GPU framework leverages all available multi-core CPUs and multiple GPUs for computing graphlets in large networks. Compared to recent approaches, our methods are orders of magnitude faster, while also more cost effective enjoying superior performance per capita and per watt. In particular, the methods are up to 300 times faster than a recent state-of-the-art method. To the best of our knowledge, this is the first work to leverage multiple CPUs and GPUs simultaneously for computing induced subgraph statistics.
Intravenous Magnesium Sulphate Relieves Migraine Attacks in Patients with Low Serum Ionized Magnesium Levels: A Pilot Study (1995)

1. We tested the hypothesis that patients with an acute attack of migraine headache and low serum levels (< 0.54 mmol/l) of ionized magnesium are more likely to respond to an intravenous infusion of magnesium sulphate (MgSO4) than patients with higher serum ionized magnesium levels. 2. Serum ionized magnesium levels were drawn immediately before infusion of 1 g of MgSO4 in 40 consecutive patients with an acute migraine headache. 3. Pain reduction of 50% or more as measured on a headache intensity verbal scale of 1 to 10, occurred within 15 min of infusion in 35 patients. In 21 patients, at least this degree of improvement or complete relief persisted for 24h or more. Pain relief lasted at least 24h in 18 of 21 patients (86%) with serum ionized magnesium levels below 0.54 mmol/l, and in 3 of 19 patients (16%) with ionized magnesium levels at or above 0.54 mmol/l (P < 0.001). Mean ionized magnesium levels in patients with relief lasting for at least 24h were significantly lower than in patients with no relief or brief relief (P < 0.01). 4. Measurement of serum ionized magnesium levels may be useful in identifying patients with migraine headaches who may respond to an intravenous infusion of MgSO4.
Biocatalytic conversion of aloeresin A to aloesin (2012)

Leaf exudates from Aloe species, such as the Southern African Aloe ferox, are used in traditional medicines for both humans and livestock. This includes aloesin, a skin bleaching product that inhibits the synthesis of melanin. Aloesin, (a C-glycoside-5-methylchromone) can be released from aloeresin A, an ester of aloesin, through hydrolysis. The objective of the current study was to identify an enzymatic hydrolysis method for converting aloeresin A to aloesin, resulting in increased concentrations of aloesin in the aloe bitters extract. More than 70 commercially available hydrolytic enzymes were screened for the conversion of aloeresin A. An esterase (ESL001-02) from Diversa, a lipase (Novozym 388) and a protease (Aspergillus oryzae) preparation were identified during screening as being capable of providing conversion of pure aloeresin A, with the protease giving the best conversion (~100%). It was found that a contaminating enzyme in Novo 388 was responsible for the conversion of aloeresin A to aloesin. This contaminating enzyme, possibly a protease, was able to give almost complete conversion using crude aloe bitters extract, doubling the concentration of aloesin in aloe bitters extract via the hydrolysis of aloeresin A.
Nuclear import, virion incorporation, and cell cycle arrest/differentiation are mediated by distinct functional domains of human immunodeficiency virus type 1 Vpr (1997)

The vpr gene product of human immunodeficiency virus type 1 (HIV-1) is a virion-associated protein that is essential for efficient viral replication in monocytes/macrophages. Vpr is primarily localized in the nucleus when expressed in the absence of other viral proteins. Vpr is packaged efficiently into viral particles through interactions with the p6 domain of the Gag precursor polyprotein p55gag. We developed a panel of expression vectors encoding Vpr molecules mutated in the amino-terminal helical domain, leucine-isoleucine (LR) domain, and carboxy-terminal domain to map the different functional domains and to define the interrelationships between virion incorporation, nuclear localization, cell cycle arrest, and differentiation functions of Vpr. We observed that substitution mutations in the N-terminal domain of Vpr impaired both nuclear localization and virion packaging, suggesting that the helical structure may play a vital role in modulating both of these biological properties. The LR domain was found to be involved in the nuclear localization of Vpr. In contrast, cell cycle arrest appears to be largely controlled by the C-terminal domain of Vpr. The LR and C-terminal domains do not appear to be essential for virion incorporation of Vpr. Interestingly, we found that two Vpr mutants harboring single amino acid substitutions (A30L and G75A) retained the ability to translocate to the nucleus but were impaired in the cell cycle arrest function. In contrast, mutation of Leu68 to Ser resulted in a protein that localizes in the cytoplasm while retaining the ability to arrest host cell proliferation. We speculate that the nuclear localization and cell cycle arrest functions of Vpr are not interrelated and that these functions are mediated by separable putative functional domains of Vpr.
A multiple-input DC-DC converter topology (2003)

A new topology for multiple energy source conversion is presented. The topology is capable of interfacing sources of different voltage-current characteristics to a common load, while achieving a low part count. A fixed frequency switching strategy is investigated and the resulting operating modes are analyzed. The analysis is verified by experimentation. The results show that the converter is an enabling technology for power diversification and optimization.
A Biomimetic Approach to the Rocaglamides Employing Photogeneration of Oxidopyryliums Derived from 3-Hydroxyflavones (2004)

A unified biomimetic approach to the aglain-forbaglin-rocaglamide classes of natural products is reported. The approach involves photogeneration of oxidopyryliums via excited-state intramolecular proton transfer (ESIPT) of 3-hydroxyflavones followed by [3+2] dipolar cycloaddition to the aglain core. An alpha-ketol (acyloin) rearrangement was employed to transform the aglain core to the rocaglamide framework. This approach was successfully used for the synthesis of the natural product (+/-)-methyl rocaglate.