gebhart/patrepeval huggingface dataset:
Importance of the C-1 Substituent in Classical Cannabinoids to CB<sub>2</sub> Receptor Selectivity:  Synthesis and Characterization of a Series of <i>O</i>,2-Propano-Δ<sup>8</sup>-tetrahydrocannabinol Analogs (1997)

The separation of the mood-altering effects of cannabinoids from their therapeutic effects has been long sought. Results reported here for a series of C-9 analogs of the cyclic ether O,2-propano-delta 8-tetrahydrocannabinol (O,2-propano-delta 8-THC) point to the C-1 position in classical cannabinoids as a position for which CB2 subtype selectivity occurs within the cannabinoid receptors. O,2-Propano-11-delta 8-THC, O,2-propano delta 9,11-THC, O,2-propano-9-oxo-11-nor-hexahydrocannabinol (O,2-propano-9-oxo-11-nor-HHC), and O,2-propano-9 alpha- and O,2-propano-9 beta-OH-11-nor-HHC were synthesized and evaluated in radioligand displacement assays for affinity at the CB1 and CB2 receptors and in the mouse vas deferens in vitro assay and the mouse tetrad in vivo assay for cannabinoid activity. Evaluation of binding affinity at the CB1 and CB2 receptors revealed that each compound possesses a modest increased affinity for the CB2 receptor. Analogs which contained an oxygen attached to C-9 (i.e., oxo and hydroxy derivatives) showed the highest affinity and selectivity for CB2 (for O,2-propano-9-oxo-11-nor-HHC, Ki(CB1) = 90 nM, Ki(CB2) = 23 nM, selectivity ratio 3.9; for O,2-propano-9 beta-OH-11-nor-HHC, Ki(CB1) = 26 nM, Ki(CB2) = 5.8 nM, selectivity ratio 4.5). Each compound was found to produce a dose-dependent inhibition of electrically-evoked contractions of the mouse isolated vas deferens when administered at submicromolar concentrations. This inhibition could readily be prevented by the selective CB1 cannabinoid receptor antagonist SR-141716A. The analogs exhibited unique in vivo profiles with O,2-propano-delta 9,11-THC exhibiting antinociception with reduced activity in three other in vivo measures and O,2-propano-9 beta-OH-HHC exhibiting lack of dose responsiveness in all measures. The CB2 selectivities in the O,2-propano analogs may be due to differences in solvation/desolvation that occur when the ligands enter the CB1 vs CB2 binding site. Alternatively, the CB2 selectivities may be a results of an amino acid change from a hydrogen bond-accepting residue in CB1 to a hydrogen bond-donating residue in CB2.
Further Study on Robust Adaptive Beamforming With Optimum Diagonal Loading (2006)

Significant effort has gone into designing robust adaptive beamforming algorithms to improve robustness against uncertainties in array manifold. These uncertainties may be caused by uncertainty in direction-of-arrival (DOA), imperfect array calibration, near-far effect, mutual coupling, and other mismatch and modeling errors. A diagonal loading technique is obligatory to fulfil the uncertainty constraint where the diagonal loading level is amended to satisfy the constrained value. The major drawback of diagonal loading techniques is that it is not clear how to get the optimum value of diagonal loading level based on the recognized level of uncertainty constraint. In this paper, an alternative realization of the robust adaptive linearly constrained minimum variance beamforming with ellipsoidal uncertainty constraint on the steering vector is developed. The diagonal loading technique is integrated into the adaptive update schemes by means of optimum variable loading technique which provides loading-on-demand mechanism rather than fixed, continuous or ad hoc loading. We additionally enrich the proposed robust adaptive beamformers by imposing a cooperative quadratic constraint on the weight vector norm to overcome noise enhancement at low SNR. Several numerical simulations with DOA mismatch, moving jamming, and mutual coupling are carried out to explore the performance of the proposed schemes and compare their performance with other traditional and robust beamformers
Holey Fibers with 0.4–32-m-Lattice-Constant Photonic Band-Gap Cladding: Fabrication, Characterization, and Nonlinear-Optical Measurements (2001)

The results of experimental and theoretical studies of the properties of holey fibers are presented. The physical principles of photonic-crystal fibers with a photonic band gap tunable in the visible and near-IR spectral ranges are demonstrated. The fabrication of holey fibers with a pitch of the two-dimensional periodic structure of the cladding less than 500 nm allowed us to experimentally observe a photonic band gap in transmission spectra of holey fibers tunable within the range of 930-1030 nm. It is demonstrated that holey fibers provide an opportunity to considerably increase the efficiency of spectral broadening and phase control of short laser pulses as compared with conventional fibers.
Albumin and a Dialyzable Serum Factor Stimulate Feeding In vitro by Third-Stage Larvae of the Canine Hookworm Ancylostoma caninum (1991)

Previous studies demonstrated that third-stage, developmentally arrested larvae of the canine hookworm Ancylostoma caninum resume feeding in vitro in response to canine serum and hostlike temperature. Experiments to determine the identity of the serum stimulus are described. Serum from several nonhost species stimulated feeding, but to levels lower than canine serum. Heating the serum to 57 C had no effect on its stimulatory ability. Dialysis reduced serum stimulatory activity by 50%, and ultrafiltration through 10- and 30-kDa molecular weight cut-off membranes decreased activity in both the filtrates and retentates similarly. Recombination of the filtrates and retentates restored activity to whole serum control levels. Commercial canine and bovine albumin stimulated feeding to serum control levels at 10 and 50 mg/ml, respectively. These results suggest that albumin and an unidentified low molecular weight compound(s) are capable of inducing in vitro feeding by A. caninum L3.
Single image de-haze based on a new dark channel estimation method (2012)

The image quality is effected dramatically by the weather conditions such as haze, fog and smoke. In surveillance or vehicle systems. In this paper, we propose a novel algorithm to remove haze from a single image. A new dark channel estimation method is employed by subtracting three times variance from mean to approximate the minimum value, which is defined as the dark channel in a local area. To achieve anisotropic local mean and variance, a fast bilateral filter is introduced. Its complexity is a linear function of the size of the image, which makes real-time visibility restoration possible. Compared with existing algorithm based on dark channel prior, the proposed algorithm have better performance by reducing the halos introduced by large patches very well with less computational cost.
The Abelson tyrosine kinase, the Trio GEF and Enabled interact with the Netrin receptor Frazzled in Drosophila (2005)

The attractive Netrin receptor Frazzled (Fra), and the signaling molecules Abelson tyrosine kinase (Abl), the guanine nucleotide-exchange factor Trio, and the Abl substrate Enabled (Ena), all regulate axon pathfinding at the Drosophila embryonic CNS midline. We detect genetic and/or physical interactions between Fra and these effector molecules that suggest that they act in concert to guide axons across the midline. Mutations in Abl and trio dominantly enhance fra and Netrin mutant CNS phenotypes, and fra;Abl and fra;trio double mutants display a dramatic loss of axons in a majority of commissures. Conversely, heterozygosity for ena reduces the severity of the CNS phenotype in fra, Netrin and trio,Abl mutants. Consistent with an in vivo role for these molecules as effectors of Fra signaling, heterozygosity for Abl, trio or ena reduces the number of axons that inappropriately cross the midline in embryos expressing the chimeric Robo-Fra receptor. Fra interacts physically with Abl and Trio in GST-pulldown assays and in co-immunoprecipitation experiments. In addition, tyrosine phosphorylation of Trio and Fra is elevated in S2 cells when Abl levels are increased. Together, these data suggest that Abl, Trio, Ena and Fra are integrated into a complex signaling network that regulates axon guidance at the CNS midline.
Image-based homing (1992)

A system that allows a robot to use a model of its environment to navigate is reported. The system maps the environment as a set of snapshots of the world taken at target locations. The robot uses an image-based local homing algorithm to navigate between neighboring and target locations. The approach has an imaging system that acquires a compact, 360 degrees representation of the environment as an intensity waveform, and an image-based, qualitative homing algorithm that allows the robot to navigate without explicitly inferring three-dimensional structure from the image. The result of an experiment in a typical indoor environment are reported. They show that image-based navigation is a feasible alternative to approaches using 3-D models and more complex model-based vision algorithms.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Improved key rates for quantum key distribution employing soft metrics using Bayesian inference with photon counting detectors (2011)

This paper investigates the potential improvements that may be obtained in terms of the secret key transmission rate in a Quantum Key Distribution (QKD) scheme whereby photon-counting detectors are used at the receiver. To take full advantage of such detectors, soft information is generated in the form of Log-Likelihood Ratios (LLRs) using a Bayesian estimator of phase of the signal pulse which is used to carry the information. The technique is general in a sense that any optical communication scheme whereby the received mean photon count is relatively small, but not necessarily below one and uses the polarization state of light to transmit the binary data may benefit from the soft information processing proposed, although in this paper, we have focused on the QKD application. We demonstrate using simulations the significant reduction in the residual Bit Error Rate (BER) and Frame Error Rate (FER) that is achievable using the proposed soft information processing scheme for a given Quantum BER (QBER) on the quantum link, after the information reconciliation process using LDPC Forward Error Correction (FEC) coding.
Stability of BaTiO&lt;inf&gt;3&lt;/inf&gt;Ceramics Doped with Dy for High-Voltage Capacitor Use (1977)

For a small-size high-voltage capacitor for power separation filter (PSF) use, corona noises, capacitor characteristics changes, and the life characteristics of Dy-doped BaTiO <inf xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</inf> ceramics have been discussed. Noises caused by corona discharges are sufficiently small to meet the PSF requirement at an applied field below 2 kV/mm. The capacitance change with time for 20 years is estimated to be -5 percent, for use at 0-85°C and below 3 kV/mm. The life of the ceramic is expected to be more than 20 years; under normal temperature and below 2 kV/mm In association with the previously reported result on Dy-doped BaTiO <inf xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</inf> ceramics, the PSF capacitors made from small-grained BaTiO <inf xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</inf> ceramics doped with 0.8 atomic percent Dy will be operated for 20 years with small corona noise, without breakdown, and with a maximum capacitance variation of +7 to -14 percent.
Towards a User-Centric Identity-Usage Monitoring System (2008)

The misuse of identity-related information in cyberspace is one of the biggest concerns among all Internet users. So far several technologies have been proposed and implemented to prevent and detect identity theft and misuse, but none of them are completely successful in terms of privacy, user-centricity and generality. In this paper, we identify the requirements for a user-centric identity-usage monitoring system to solve such problems and propose a monitoring system that runs on a trusted third party. This system can transparently use context information of a request to detect anomalous use of online identity. Finally, we provide a prototypical implementation in an OpenID setting and evaluate it in terms of scalability, performance, user-centricity, and security.
Augmented Reality for Telemaintenance and -inspection in Force-Sensitive Industrial Robot Applications (2015)

Telematic solutions allow fast remote support in industrial robot work cells: Robotic experts can assist the local staff in work process modifications or in tracking down errors without having to actually travel to the remote site. In order to be able to perform such teleinspection and telemaintenance tasks the operator needs to establish a data connection to the robot and get an understanding of the remote work process, as well as of the transmitted data. This contribution introduces a telematic control system developed for remote monitoring and control of an industrial robot performing force-sensitive work applications. An Augmented Reality interface is proposed for intuitive representation of complex robotic data, allowing quick analysis of the current working cycle and process data and altering the robot's program remotely while still having a clear spatial reference to the work environment.
THE PREPARATION OF GUANIDINE FROM UREA, AMMONIUM CHLORIDE, ALUMINUM SULPHATE, AND AMMONIA UNDER PRESSURE (1955)

Guanidine has been synthesized by heating under ammonia pressure an intimate mixture of finely powdered urea, ammonium chloride, and aluminum sulphate. Good yields of guanidine as the hydrochloride salt have been obtained over a wide range of conditions. The mechanism of this synthesis is briefly discussed.
E6-AP/UBE3A Protein Acts as a Ubiquitin Ligase toward SOX9 Protein (2013)

SOX9 is a transcription factor that acts as a key regulator at various stages of cartilage differentiation. There is ample evidence that intracellular SOX9 protein levels are tightly regulated both by sumoylation and by degradation through the ubiquitin-proteasome pathway. Using a proteomics approach, here we report the identification of a SOX9-binding protein, E6-AP/UBE3A, that may act as a ubiquitin ligase toward Sox9. E6-AP bound SOX9 through the region consisting mostly of its high mobility group domain in vitro. In nuclear lysates, FLAG-tagged E6-AP coprecipitated with Sox9 and its high mobility group domain. This finding was estimated using nuclear lysates from a chondrocytic cell line that endogenously expresses E6-AP and SOX9. Accordingly, ectopically expressed E6-AP and SOX9 colocalized in the nucleus. We show that E6-AP ubiquitinates SOX9 in vitro and in vivo and that SOX9 levels are enhanced after addition of the proteasome inhibitor bortezomib. Similar, siRNA knockdown of E6-AP and the E2 ligase Ubc9 increased cellular SOX9 amounts, supporting the notion that SOX9 may be ubiquitinated in hypertrophic chondrocytes by E6-AP and degraded by proteasomes. This is in accordance with the distribution of SOX9 levels, which are high in proliferating and prehypertrophic chondrocytes but low in hypertrophic chondrocytes, whereas E6-AP levels are high in hypertrophic chondrocytes and low in prehypertrophic chondrocytes. Furthermore, E6-AP-deficient mice showed SOX9 accumulation in chondrocytes and the brain. These findings support the concept that E6-AP regulates SOX9 levels in developing cartilage by acting as a ubiquitin ligase.
Structure and Expression of the Human SM22  Gene, Assignment of the Gene to Chromosome 11, and Repression of the Promoter Activity by Cytosine DNA Methylation (1997)

To investigate the molecular mechanisms that control expression of smooth muscle cell (SMC) differentiation genes, we have isolated the human SM22a gene, which is composed of five exons and four introns, spanning an approximately 6-kilobase (kb) genomic DNA at chromosome region 11q23.2. Expression of the SM22a messenger RNA was detected in serum-stimulated cell cultures including SMC, undifferentiated skeletal muscle-lineage cells, and fibroblasts, and it was down-regulated in SMC of balloon-injured atheromatous human vessels. A major transcription start site of the SM22alpha gene is located at 75 base-pairs (bp) upstream of the ATG start codon. Analysis of the 2.6 kb 5'-upstream sequence demonstrated that two CArG/SRF-boxes and two GC-box/Sp1-binding sites were present at bp -147 and -274, and at bp -233 and -1635, respectively. The nucleotide sequences of the two CArG/SRF-boxes and the proximal GC-box/Sp1 binding site are 100% conserved with those of the murine SM22alpha genes [Solway, J., Seltzer, J., Samaha, F.F., Kim, S., Alger, L.E., Niu, Q., Morriesey, E.E., Ip, H.S., and Parmacek, M.S. (1995) J. Biol. Chem. 270, 13460-13469; Kemp, P.R., Osbourn, J.K., Grainger, D.J., and Metcalf, C. (1995) Biochem. J. 310, 1037-1043]. Cell transfection assays using a luciferase reporter gene construct containing the 455-bp 5'-flanking region (positions -26 to -480) showed that methylation of the CpG dinucleotides within this segment reduces its transcriptional activity. The results imply a novel mechanism for transcriptional control of the SMC differentiation-specific gene promoter.
The role of IFNγ nuclear localization sequence in intracellular function (2003)

Intracellularly expressed interferon gamma (IFNgamma) has been reported to possess biological activity similar to that of IFNgamma added to cells. This study addresses the mechanisms for such similar biological effects. Adenoviral vectors were used to express a non-secreted form of human IFNgamma or a non-secreted mutant form in which a previously demonstrated nuclear localization sequence (NLS), 128KTGKRKR134, was replaced with alanines at K and R positions. With the vector expressing non-secreted wild-type IFNgamma, biological responses normally associated with extracellular IFNgamma, such as antiviral activity and MHC class I upregulation, were observed, although the mutant IFNgamma did not possess biological activity. Intracellular human IFNgamma possessed biological activity in mouse L cells, which do not recognize extracellularly added human IFNgamma. Thus, the biological activity was not due to leakage of IFNgamma to the surroundings and subsequent interaction with the receptor on the cell surface. Biological function was associated with activation of STAT1alpha and nuclear translocation of IFNgamma, IFNGR1 and STAT1alpha. Immunoprecipitation of cellular extracts with antibody to the nuclear transporter NPI-1 showed the formation of a complex with IFNgamma-IFNGR1-STAT1alpha. To provide the physiological basis for these effects we show that extracellularly added IFNgamma possesses intracellular signaling activity that is NLS dependent, as suggested by our previous studies, and that this activity occurs via the receptor-mediated endocytosis of IFNgamma. The data are consistent with previous observations that the NLS of extracellularly added IFNgamma plays a role in IFNgamma signaling.
Ultrasonic sensors in air (1994)

Ultrasonic sensors in air are intelligent sensors, which use wave-propagation phenomena in air to measure physical or chemical variables. With accordance to the influence principle, two main types of ultrasonic sensors can be differentiated. Propagation-path sensors decode changes on propagation to obtain a fast measurement of temperature, pressure variations or gas concentration. Most important are ultrasonic flow sensor e.g. for engine intake air or for air/gas measurement. Distance sensors detect echoes from objects and evaluate their propagation time and amplitude. Examples are distance meters and presence detectors. By intelligent algorithms based on signal theory models or heuristic approaches (synthetic aperture, pulse holography, fuzzy or neural network etc.) the resolution and detection range were increased, the radial and lateral resolution significantly enhanced and objects recognized. With piezoelectric PVDF-foils efficient and versatile transducers arrays were realized. Robust transducers for operation in adverse environment (dirt, moisture, abrasion) were developed using rugged matching layers or a special composite-transducer technology
Bis-Acridines as Lead Antiparasitic Agents: Structure-Activity Analysis of a Discrete Compound Library In Vitro (2007)

Parasitic diseases are of enormous public health significance in developing countries-a situation compounded by the toxicity of and resistance to many current chemotherapeutics. We investigated a focused library of 18 structurally diverse bis-acridine compounds for in vitro bioactivity against seven protozoan and one helminth parasite species and compared the bioactivities and the cytotoxicities of these compounds toward various mammalian cell lines. Structure-activity relationships demonstrated the influence of both the bis-acridine linker structure and the terminal acridine heterocycle on potency and cytotoxicity. The bioactivity of polyamine-linked acridines required a minimum linker length of approximately 10 A. Increasing linker length resulted in bioactivity against most parasites but also cytotoxicity toward mammalian cells. N alkylation, but less so N acylation, of the polyamine linker ameliorated cytotoxicity while retaining bioactivity with 50% effective concentration (EC(50)) values similar to or better than those measured for standard drugs. Substitution of the polyamine for either an alkyl or a polyether linker maintained bioactivity and further alleviated cytotoxicity. Polyamine-linked compounds in which the terminal acridine heterocycle had been replaced with an aza-acridine also maintained acceptable therapeutic indices. The most potent compounds recorded low- to mid-nanomolar EC(50) values against Plasmodium falciparum and Trypanosoma brucei; otherwise, low-micromolar potencies were measured. Importantly, the bioactivity of the library was independent of P. falciparum resistance to chloroquine. Compound bioactivity was a function of neither the potential to bis-intercalate DNA nor the inhibition of trypanothione reductase, an important drug target in trypanosomatid parasites. Our approach illustrates the usefulness of screening focused compound libraries against multiple parasite targets. Some of the bis-acridines identified here may represent useful starting points for further lead optimization.
Determination of lattice polarity for growth of GaN bulk single crystals and epitaxial layers (1996)

The polarity of the lattice of bulk single GaN crystals and the polarity of homoepitaxial and heteroepitaxial-on-sapphire GaN thin films has been studied using convergent beam electron diffraction. Diffraction patterns obtained at 200 kV for the 〈1–100〉 projection of GaN were matched with calculated patterns. The lattice orientations of two commonly observed bulk single-crystal facets were identified. It is shown that the smooth facets in single crystals correspond to the (0001), Ga-terminated, lattice planes, whereas the rough facets correspond to the (0001̄), N-terminated, planes. It is also shown that metalorganic chemical vapor deposition epitaxy retains the polarity of the substrate, i.e., no inversion boundaries were observed. Heteroepitaxy on sapphire is shown to grow in the (0001), Ga-terminated orientation.