gebhart/patrepeval huggingface dataset:
Secondary Amides of Sulfonylated 3-Amidinophenylalanine. New Potent and Selective Inhibitors of Matriptase (2006)

Matriptase is an epithelium-derived type II transmembrane serine protease and has been implicated in the activation of substrates such as pro-HGF/SF and pro-uPA, which are likely involved in tumor progression and metastasis. Through screening, we have identified bis-basic secondary amides of sulfonylated 3-amidinophenylalanine as matriptase inhibitors. X-ray analyses of analogues 8 and 31 in complex with matriptase revealed that these inhibitors occupy, in addition to part of the previously described S4-binding site, the cleft formed by the molecular surface and the unique 60 loop of matriptase. Therefore, optimization of the inhibitors included the incorporation of appropriate sulfonyl substituents that could improve binding of these inhibitors into both characteristic matriptase subsites. The most potent derivatives inhibit matriptase highly selective with K(i) values below 5 nM. Molecular modeling revealed that their improved affinity results from interaction with the S4 site of matriptase. Analogues 8 and 59 were studied in an orthotopic xenograft mouse model of prostate cancer. Compared to control, both inhibitors reduced tumor growth, as well as tumor dissemination.
Spectral imaging for brightfield microscopy (2003)

Molecular medicine now requires molecular pathology. While fluorescence has traditionally been used for high-resolution multiplexed molecular imaging, clinical practitioners prefer non-fluorescent multicolor methods. However, in brightfield, typically, only one color is used at a time, which precludes assessment of co-expression on a cell-by-cell basis. Similar constraints apply to brightfield in-situ hybridization techniques. Double- and triple-staining procedures are rarely performed in non-research settings not only because the wet chemistry can be difficult, but also because it can be challenging or impossible to determine visually where and to what extent different chromogens may physically overlap. Spectral imaging can be useful in this context. Two methods of acquiring spectral images are described, along with their application to multicolor immunohistochemistry and transmission in-situ hybridization (TRISH): 1) liquid crystal tunable filters; and 2) a novel, spectrally agile light source. This source emits white light of any desired color temperature, or single 10-nm wavelength bands in the range 420 to 700 nm, or any combination of wavelengths with individual intensity control. Both methods are allied with a grayscale camera and appropriate algorithms to analyze multicolor samples of clinical significance. Spectrally unmixed images clearly separate signals linked to different chromogens, even with spectral and spatial overlap. Intriguing challenges in matching mathematical algorithms to these specific problems remain: how many bands are enough? What are the optimal unmixing procedures? What automated tools can be applied to speed and simplify the procedures?
Impact of Strong Atmospheric Turbulence on Two-Way Optical Time Transfer (2023)

Frequency comb based optical time transfer can provide femtosecond-level timing which will support future clock networks. However, for long-distance terrestrial links, non-reciprocal atmospheric turbulence induces a timing penalty. Here, we quantify this penalty.
A Simple Model of Speech Communication and its Application to Intelligibility Enhancement (2014)

We introduce a model of communication that includes noise inherent in the message production process as well as noise inherent in the message interpretation process. The production and interpretation noise processes have a fixed signal-to-noise ratio. The resulting system is a simple but effective model of human communication. The model naturally leads to a method to enhance the intelligibility of speech rendered in a noisy environment. State-of-the-art experimental results confirm the practical value of the model.
Solvent-Free Patterning of Colloidal Quantum Dot Films Utilizing Shape Memory Polymers (2017)

Colloidal quantum dots (QDs) with properties that can be tuned by size, shape, and composition are promising for the next generation of photonic and electronic devices. However, utilization of these materials in such devices is hindered by the limited compatibility of established semiconductor processing techniques. In this context, patterning of QD films formed from colloidal solutions is a critical challenge and alternative methods are currently being developed for the broader adoption of colloidal QDs in functional devices. Here, we present a solvent-free approach to patterning QD films by utilizing a shape memory polymer (SMP). The high pull-off force of the SMP below glass transition temperature (Tg) in conjunction with the conformal contact at elevated temperatures (above Tg) enables large-area, rate-independent, fine patterning while preserving desired properties of QDs.
Device For Controlling Crystallization Of Protein (1993)

Variable sandwich spacer enables optimization of evaporative driving force that governs crystallization of protein from solution. Mechanically more rigid than hanging-drop and sitting-drop devices. Large oscillations and dislodgment of drop of solution in response to vibrations suppressed by glass plates. Other advantages include: suitable for automated delivery, stable handling, and programmable evaporation of protein solution; controlled configuration enables simple and accurate determination of volume of solution without disrupting crystallization; pH and concentration of precipitant controlled dynamically because pH and concentration coupled to rate of evaporation, controllable via adjustment of gap between plates; and enables variation of ratio between surface area and volume of protein solution. Alternative version, plates oriented vertically instead of horizontally.
Embryonic lethality in<i>Dear</i>gene-deficient mice: new player in angiogenesis (2005)

The dual endothelin-1/angiotensin II receptor (Dear) binds endothelin-1 (ET-1) and angiotensin II (ANG II) with equal affinities in the Dahl S/JRHS rat strain. To elucidate its physiological significance within the context of multiple receptor isoforms and diverse ET-1 and ANG II functions spanning blood pressure regulation, tumor proliferation, and angiogenesis, we characterized mouse Dear and Dear-deficient mice. Unlike null mutant models of ET-1, ANG II, and all other ET-1 and ANG II receptors, Dear(-/-) deficiency results in impaired angiogenesis, dysregulated neuroepithelial development, and embryonic lethality by embryonic day 12.5. Interestingly, mouse Dear does not bind ANG II, similar to Dahl R/JRHS rat Dear, but binds ET-1 and vascular endothelial growth factor (VEGF) signal peptide (VEGFsp) with equal affinities, suggesting a putative novel multifunction for VEGFsp and a parsimonious mechanism for coordination of VEGF-induced and Dear-mediated pathways. Consistent with its developmental angiogenic role, Dear inhibition results in decreased tumor growth in B16-F10 melanoma cell-induced subcutaneous tumor in female Dear(+/-)/C57BL6BC10 mice, but not in males (age 3.5 mo), and in 127Cs radiation-induced orthotopic mammary tumors in Sprague-Dawley female rats (age range 3-6.5 mo). Altogether, the data identify Dear as a new player in angiogenesis during development downstream to, and nonredundant with, VEGF-mediated pathways, as well as a putative modulator of tumor angiogenesis acting within a gender-specific paradigm.
Demonstration of Continuous Electrowetting Actuation (2010)

Electrowetting is the change in apparent surface energy of a liquid in an applied electric field. It has shown great promise in diverse applications including lab-on-a-chip and electronic displays. The electrowetting response is typically considered independent of the actuation voltage polarity. This paper describes a new approach that achiees actuation in different directions for positive and negative voltage polarities using the electrochemical characteristics of aluminum electrodes. This paper presents a concept for continuous actuation of a droplet using a single electrode and DC voltage based on this effect. Initial experiments demonstrate that droplet motion is possible. Measurements of voltage drop across aluminum electrodes confirms the polarity-dependent response of the electrodes.
Synchronization of HIFU therapy system with an arbitrary ultrasound imager (2003)

Synchronization for image guided therapy using high intensity focused ultrasound (HIFU) and imaging ultrasound is achieved with a new technique that uses the focused transducer as a receiver that can detect the acoustic pulses created by the imaging probe. Without synchronization, interference from the high intensity source occludes the imager’s display unpredictably, degrading the quality of the system. An imaging probe (Sonosite 180) is registered with a HIFU transducer (d=33 mm, roc=55 mm, f=3.5 MHz) such that the scan line bisects the single element focus. When acoustically coupled through a scattering medium, imaging pulses are passively detected with the HIFU transducer and electronically conditioned into a TTL level trigger. A LabVIEW program uses the trigger to create a pulse width modulated signal that controls the timing of HIFU excitation during treatment. Detection takes less than 1% of the time between displayed images when the imager is running at 20 frames per second. HIFU excitations are programmed to occur such that the single element focus is free of interference when viewed with the imager during treatment. With no electrical connections for this new, simple technique, an arbitrary imager can be selected for synchronized image guided therapy. [Work supported by NSBRI.]
Integrated chip-scale THz technology (2011)

The quantum cascade laser (QCL) is currently the only solid-state source of coherent THz radiation capable of delivering more than 1 mW of average power at frequencies above ~ 2 THz. This power level combined with very good intrinsic frequency definition characteristics make QCLs an extremely appealing solid-state solution as compact sources for THz applications. I will present results on integrating QCLs with passive rectangular waveguides for guiding and controlling the radiation emitted by the QCLs and on the performance of a THz integrated circuit combining a THz QCL with a Schottky diode mixer to form a heterodyne receiver/transceiver.
Tandem organic photodetectors with tunable, broadband response (2012)

Broadband photodetection is achieved by integrating three electron donor materials with complementary absorption into an organic photodetector (OPD). While a single donor-acceptor heterojunction can show broadband response, the spectral tunability is intrinsically limited to the absorption profiles of the active materials. Here, we demonstrate broadband OPDs consisting of multiple bulk heterojunctions arranged in tandem. These OPDs show high responsivity under moderate reverse bias from the ultraviolet to the near-infrared. By combining materials with complementary absorption in a tandem OPD, we demonstrate that the response from each band can be separately tuned with manipulation of the heterojunction thicknesses or composition.
Ketoester methacrylate resin, secondary amine clean-up in the presence of primary amines (2001)

A ketoester resin was developed as the basis for a selective scavenger for primary amines in the presence of secondary amines. The utility of the scavenger was demonstrated with a range of reductive amination chemistries with both mono- and diamines. The resin's specificity is based on the removal of the primary amines via their enamines.
Adaptive Caching Networks With Optimality Guarantees (2018)

We study the optimal placement of content over a network of caches, a problem naturally arising in several networking applications. Given a demand of content request rates and paths followed, we wish to determine the content placement that maximizes the expected caching gain, i.e., the reduction of routing costs due to intermediate caching. The offline version of this problem is NP-hard and, in general, the demand and topology may be a priori unknown. Hence, a distributed, adaptive approximation algorithm for placing contents into caches is desired. We show that path replication, a simple algorithm frequently encountered in literature, can be arbitrarily suboptimal when combined with traditional eviction policies. We propose a distributed, adaptive algorithm that performs stochastic gradient ascent on a concave relaxation of the expected caching gain, and constructs a probabilistic content placement within a 1-1/e factor from the optimal, in expectation. Motivated by our analysis, we also propose a novel greedy eviction policy to be used with path replication, and show through numerical evaluations that both algorithms significantly outperform path replication with traditional eviction policies over a broad array of network topologies.
CD4 molecules with a diversity of mutations encompassing the CDR3 region efficiently support human immunodeficiency virus type 1 envelope glycoprotein-mediated cell fusion (1993)

The third complementarity-determining region (CDR3) within domain 1 of the human CD4 molecule has been suggested to play a critical role in membrane fusion mediated by the interaction of CD4 with the human immunodeficiency virus type 1 (HIV-1) envelope glycoprotein. To analyze in detail the role of CDR3 and adjacent regions in the fusion process, we used cassette mutagenesis to construct a panel of 30 site-directed mutations between residues 79 and 96 of the full-length CD4 molecule. The mutant proteins were transiently expressed by using recombinant vaccinia virus vectors and were analyzed for cell surface expression, recombinant gp120-binding activity, and overall structural integrity as assessed by reactivity with a battery of anti-CD4 monoclonal antibodies. Cells expressing the CD4 mutants were assayed for their ability to form syncytia when mixed with cells expressing the HIV-1 envelope glycoprotein. Surprisingly in view of published data from others, most of the mutations had little effect on syncytium-forming activity. Normal fusion was observed in 21 mutants, including substitution of human residues 85 to 95 with the corresponding sequences from either chimpanzee, rhesus, or mouse CD4; a panel of Ser-Arg double insertions after each residue from 86 to 91; and a number of other charge, hydrophobic, and proline substitutions and insertions within this region. The nine mutants that showed impaired fusion all displayed defective gp120 binding and disruption of overall structural integrity. In further contrast with results of other workers, we observed that transformant human cell lines expressing native chimpanzee or rhesus CD4 efficiently formed syncytia when mixed with cells expressing the HIV-1 envelope glycoprotein. These data refute the conclusion that certain mutations in the CDR3 region of CD4 abolish cell fusion activity, and they suggest that a wide variety of sequences can be functionally tolerated in this region, including those from highly divergent mammalian species. Syncytium formation mediated by several of the CDR3 mutants was partially or completely resistant to inhibition by the CDR3-directed monoclonal antibody L71, suggesting that the corresponding epitope is not directly involved in the fusion process.(ABSTRACT TRUNCATED AT 400 WORDS)
The biphasic intraocular pressure response of rabbits to epinephrine. (1976)

A study has been made of the pupillary and intraocular pressure responses of conscious rabbits to daily topical applications of submaximal doses of epinephrine. On the first day, epinephrine caused rapid pupil dilation which preceded a prolonged -ecrease of intraocular pressure. On the second and subsequent days, the application of the same dose of epinephrine increased the duration of the pupillary response and caused a biphasic pressure response in all treated eyes; an initial increase of intraocular pressure lasting two to four hours followed by decrease of intraocular pressure below the initial value which lasted for more than twenty-four hours. The beta-receptor antagonist, propranolol, and the alpha-receptor antagonist, phenoxybenzamine, caused small and large reductions, respectively, in the hypertensive response to epinephrine. Phenoxybenzamine, but not propranolol, also inhibited the pupil dilation and the hypotensive response to epinephrine. Topical administration of phenoxybenzamine strongly inhibited the hypertensive response to epinephrine but left unaffected the pupillary response.
Radio loudspeaker telephone device capable of automatically preventing howling on execution of calling operation (1995)

Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Twitter Facebook Reddit LinkedIn Tools Icon Tools Reprints and Permissions Cite Icon Cite Search Site Citation Naoki Hirasawa, Yukio Murata; Radio loudspeaker telephone device capable of automatically preventing howling on execution of calling operation. J. Acoust. Soc. Am. 1 October 1995; 98 (4): 1833. https://doi.org/10.1121/1.413404 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAcoustical Society of AmericaThe Journal of the Acoustical Society of America Search Advanced Search |Citation Search
Specific absorption rate reduction in parallel transmission by <i>k</i>‐space adaptive radiofrequency pulse design (2010)

The specific absorption rate (SAR) is an important safety criterion, limiting many MR protocols with respect to the achievable contrast and scan duration. Parallel transmission enables control of the radiofrequency field in space and time and hence allows for SAR management. However, a trade-off exists between radiofrequency pulse performance and SAR reduction. To overcome this problem, in this work, parallel transmit radiofrequency pulses are adapted to the position in sampling k-space. In the central k-space, highly homogeneous but SAR-intensive radiofrequency shim settings are used to achieve optimal performance and contrast. In the outer k-space, the homogeneity requirement is relaxed to reduce the average SAR of the scan. The approach was experimentally verified on phantoms and volunteers using field echo and spin echo sequences. A reduction of the SAR by 25-50% was achieved without compromising image quality.
Preventive and Therapeutic Strategies for Bovine Leukemia Virus: Lessons for HTLV (2011)

Bovine leukemia virus (BLV) is a retrovirus closely related to the human T-lymphotropic virus type 1 (HTLV-1). BLV is a major animal health problem worldwide causing important economic losses. A series of attempts were developed to reduce prevalence, chiefly by eradication of infected cattle, segregation of BLV-free animals and vaccination. Although having been instrumental in regions such as the EU, these strategies were unsuccessful elsewhere mainly due to economic costs, management restrictions and lack of an efficient vaccine. This review, which summarizes the different attempts previously developed to decrease seroprevalence of BLV, may be informative for management of HTLV-1 infection. We also propose a new approach based on competitive infection with virus deletants aiming at reducing proviral loads.
Perturbationless calibration of pulse transit time to blood pressure (2012)

Pulse transit time (PTT) often shows strong correlation with blood pressure (BP) and may therefore represent a means for achieving continuous, non-invasive, and cuff-less BP monitoring. However, construction of the subject-specific curve needed to calibrate PTT to BP conventionally requires simultaneous measurements of PTT and BP during an experimental perturbation that varies BP over a significant range. We propose a technique for perturbationless calibration of PTT to BP. This technique constructs the calibration curve from central and peripheral BP waveforms by exploiting the natural pulsatile variation in the waveforms via a nonlinear tube-load model. We conducted initial testing of the technique in animals by applying it to the waveforms during a baseline period and then predicting mean BP during subsequent major hemodynamic interventions via PTT calibrated with the resulting curve. The bias in the mean BP error was 4.9 mmHg, while the precision in this error was 7.6 mmHg.
A parametric evaluation of shear wave speeds estimated with the time-of-flight approach in viscoelastic media (2019)

The time-of-flight approach estimates the shear elasticity in tissue mimicking elastography phantoms and in soft tissue. The time-of-flight approach is effective in elastic phantoms, but the time-of-flight approach tends to overestimate the shear elasticity in viscoelastic phantoms and in viscoelastic soft tissues. To characterize errors in estimated parameters for different values of the shear elasticity and the shear viscosity, three-dimensional (3D) shear wave simulations are evaluated for twelve different parameter combinations. The 3D acoustic radiation force is calculated for an L7-4 transducer using the fast nearfield method and the angular spectrum approach, and then, 3D shear wave propagation in a viscoelastic medium is simulated with Green's functions for a Kelvin-Voigt model. The time-of-flight method is then evaluated within a two-dimensional plane. The results show that the accuracy of the time-of-flight method depends on the values of the shear elasticity and the shear viscosity. In particular, the error in the estimated shear elasticity increases as the shear viscosity increases, where the largest errors are observed when larger values of the shear viscosity are combined with smaller values of the shear elasticity. [Work supported in part by NIH Grants DK092255, EB023051, and EB012079.]
ChemInform Abstract: A COMPARISON OF THE ANTISEROTONIN, ANTIHISTAMINE, AND ANTICHOLINERGIC ACTIVITY OF CYPROHEPTADINE WITH ANALOGS HAVING FURAN NUCLEI FUSED TO THE 10,11‐VINYLENE BRIDGE (1977)

Abstract Die Kondensation der beiden Furane (IIa) und (IIb) mit 10‐Brom‐cyproheptadin (I) liefert die Addukte (IIIa) und (IIIb), die mit Tetraphenylcyclopentadienon (IV) zu (Va) und (Vb) gemäß einer Retro‐Diels‐Alder‐Reaktion reagieren.
A tree-based statistical language model for natural language speech recognition (1989)

The problem of predicting the next word a speaker will say, given the words already spoken; is discussed. Specifically, the problem is to estimate the probability that a given word will be the next word uttered. Algorithms are presented for automatically constructing a binary decision tree designed to estimate these probabilities. At each node of the tree there is a yes/no question relating to the words already spoken, and at each leaf there is a probability distribution over the allowable vocabulary. Ideally, these nodal questions can take the form of arbitrarily complex Boolean expressions, but computationally cheaper alternatives are also discussed. Some results obtained on a 5000-word vocabulary with a tree designed to predict the next word spoken from the preceding 20 words are included. The tree is compared to an equivalent trigram model and shown to be superior.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>