gebhart/patrepeval huggingface dataset:
Therapeutic Use of Antimelanoma Monoclonal Antibodies (1988)

Monoclonal antibodies (MAb) to tumor‐associated antigens are attracting much attention for tumor therapy. Melanomas belong to the tumors most studied in this respect, and several melanoma‐associated antigens have been studied in great detail. These include the melanoma‐associated glycoprotein p97, the melanoma‐associated proteoglycan, and glycolipid antigens. Although none of the antigens is absolutely specific for tumor, the degree of relative specificity appears to be sufficient to use several of the melanoma antigens as therapeutic “targets”. Antimelanoma MAb can be applied therapeutically in several ways. The most straightforward approach is use of MAb without further modification. MAb which kill melanoma cells in the presence of human serum as the source of complement or mediate antibody‐dependent cellular cytotoxicity with human natural killer (NK) cells or macrophages as effectors are logical choices for this. Some cases of partial or even complete regression of metastatic melanoma have been observed in patients treated with such MAb. Combinations of such MAb with interleukin 2 (IL‐2) or other immunological response modifiers are of great interest. Alternatively, one may use antimelanoma MAb (or fragments prepared from MAb) as carriers of antitumor agents, including radioactive isotopes, toxins, or chemotherapeutic drugs. Although it is premature to make any conclusions about the efficacy of such conjugates, we are optimistic that it will be feasible by using the right combination of MAb and antitumor agent to achieve therapeutic benefit. Another approach is to develop therapeutic “vaccines” for active immunization, once an antigen characterized by using a MAb has proven to have a relatively high level of tumor selectively. Anti‐idiotypic antibodies and live recombinant viruses inducing tumor antigen expression in infected cells provide alternative strategies to this approach.
Modeling and control of a new type of omnidirectional holonomic vehicle (2002)

A new type of omnidirectional holonomic vehicle has been proposed. The vehicle has a pair of driving wheel which configuration has a offset distance between a steering axis and a wheel axis. The wheel of this style is known as a nonholonomic system and is usually used for a caster wheel. In the case of proposed vehicle, a wheel of this style is used as a driving wheel by actuating a wheel axle and a steering axle independently. We first present a concept of the offset steered driving wheel", then describe kinematic models of the single driving wheel and a holonomic vehicle with proposed driving wheels. To avoid the nonholonomic characteristics of the wheel, we have introduced a control method in which an orientation of the wheel is neglected to be controlled. Therefore only translational velocities of the steering axle of the wheel are controlled so as to realize reference velocities. By using proposed wheel mechanism and the control method, the wheel can achieve a reproduction of caster motion. The vehicle with a couple of proposed driving wheels achieves omnidirectional and holonomic movements. Finally, proposed control methodology which based on kinematic models of the driving wheel and the vehicle has tested by a prototype vehicle. Experiments of the prototype vehicle have shown successful performances.
Exogenous nonphysiologic vs physiologic lipids. Divergent mechanisms for correction of permeability barrier dysfunction (1995)

While petrolatum remains restricted to the stratum corneum, physiologic lipid mixtures influence barrier recovery after transport to subjacent, nucleated layers, followed by internalization, apparent transport to the distal Golgi apparatus, and incorporation into nascent lamellar bodies.
Strontium-phosphate hydroxyapatite high-performance liquid chromatography. (1987)

High-performance liquid chromatography using spherical aggregates of strontium-phosphate hydroxyapatite(SrHA) micro-crystals as adsorbent has been developed; preliminary performance tests were carried out by using several types of protein. It can be deduced that, in parallel with the case of usual calcium-phosphate hydroxyapatite(CaHA), with SrHA also, two types of effective surface, vector a (or vector b) and vector c surfaces, appear on the crystal: the same protein molecular generally shows slightly different chromatographic behaviors between the CaHA and the SrHA packed column. Combining the SrHA and the CaHA packed column would lead to an efficient fractionation of a particular molecule from an assembly of molecules with subtle structural differences from one another.
Stereoselective Hydrolysis of Organophosphate Nerve Agents by the Bacterial Phosphotriesterase (2010)

Organophosphorus compounds include many synthetic, neurotoxic substances that are commonly used as insecticides. The toxicity of these compounds is due to their ability to inhibit the enzyme acetylcholine esterase. Some of the most toxic organophosphates have been adapted for use as chemical warfare agents; the most well-known are GA, GB, GD, GF, VX, and VR. All of these compounds contain a chiral phosphorus center, with the S(P) enantiomers being significantly more toxic than the R(P) enantiomers. Phosphotriesterase (PTE) is an enzyme capable of detoxifying these agents, but the stereochemical preference of the wild-type enzyme is for the R(P) enantiomers. A series of enantiomerically pure chiral nerve agent analogues containing the relevant phosphoryl centers found in GB, GD, GF, VX, and VR has been developed. Wild-type and mutant forms of PTE have been tested for their ability to hydrolyze this series of compounds. Mutant forms of PTE with significantly enhanced, as well as relaxed or reversed, stereoselectivity have been identified. A number of variants exhibited dramatically improved kinetic constants for the catalytic hydrolysis of the more toxic S(P) enantiomers. Improvements of up to 3 orders of magnitude relative to the value of the wild-type enzyme were observed. Some of these mutants were tested against racemic mixtures of GB and GD. The kinetic constants obtained with the chiral nerve agent analogues accurately predict the improved activity and stereoselectivity against the authentic nerve agents used in this study.
A cylindrical bender acoustic transducer (1985)

An acoustic transducer having hollow cylinder geometry has been developed for generation of compressional waves in fluid or solid media or of shear waves in solid media using the bender concept of a two-layered piezoelectric ceramic transducer element. The device can be constructed with either two active piezoelectric layers or with one active piezoelectric layer and one passive layer. The latter configuration allows construction of a cylindrical transducer with a relatively thick metal exterior shell for electrical shielding. The active ceramic can be either monolithic or a mosaic of small elements. Mechanical details of several transducers that have been constructed will be presented with their operational parameters. Low resonance frequency, small size, rugged construction, excellent electrical shielding, and electrically switchable modes of operation are a few of the positive attributes of the transducer design. [Work supported by U.S. Department of the Interior, Bureau of Mines.]
Optimization of waveguide photodetector with thin absorbing layer and large responsivity (2020)

We present optimized structure of waveguide photodetector (WGPD) having large responsivity in spite that its absorption layer is thin. Through beam-propagation method simulations, spot-size converter integrated WGPD is found to be able to have larger responsivity with thinner absorbing layer. Calculated responsivity and polarization dependent loss of the optimized design are 0.83 A/W and 0.13 dB with 150-nm-thick and 25-μm-long absorber.
Virtual Airway Pressure and Lung Temperature Sensors in a Total Liquid Ventilation Connector (2014)

Total liquid ventilation (TLV) is an experimental mechanical ventilation technique where the lungs are completely filled with a perfluorocarbon liquid (PFC). It can be used to implement moderate therapeutic hypothermia (MTH) and treat severe respiratory problems. During TLV, the airway pressure must be monitored adequately to avoid overpressure and airway collapses. On the thermodynamic level, rectal, esophageal or tympanic temperature measurements are not suitable (long time constant) to avoid lowering the heart below 30°C. The objective was to design a Y connector positioned at the mouth which integrates the virtual sensors, used by controllers. The first estimates the airway pressure and the second provides the core body temperature. Pressure and RTD sensors were installed in the connector to implement the virtual measurements. In-vitro experiments were done to validate the virtual sensors. In-vivo experiments (on newborn lambs) confirm the accuracy of the airway pressure estimation and of the systemic arterial temperature.
The kinetics of plasminogen activation by thrombin-cleaved pro- urokinase and promotion of its activity by fibrin fragment E-2 and by tissue plasminogen activator (1993)

Thrombin hydrolyzes the Arg156-Phe157 bond in pro-urokinase (pro-UK), two residues from the activation site, generating a two-chain form (thromb-UK) believed to have little activity and that is resistant to plasmin activation. The kinetic constants for thromb-UK against synthetic substrate (S2444) were found to be essentially identical to pro-UK. Against native plasminogen, thromb-UK had a lower Michaelis constant (KM) and a higher (2-fold) catalytic efficiency. However, this difference with pro-UK was nullified by carboxypeptidase B (CpB) treatment of thromb-UK to remove the C-terminal arginine on the A- chain. Plasminogen activation by thromb-UK was substantially promoted by fibrin fragment E-2 but not by other fibrin derivatives, a phenomenon previously observed with pro-UK. Similarly, clot lysis by thromb-UK was promoted by tissue plasminogen activator because their combined effect was synergistic. Fibrinogenolysis in plasma occurred at 80-fold the concentration of thromb-UK as pro-UK, reflecting the 90- fold greater plasmin resistance of thromb-UK. Addition of a CpB inhibitor to the plasma enhanced fibrinogenolysis by thromb-UK and pro- UK by approximately 16%, consistent with the promotion of both forms by certain C-terminal lysines. In conclusion, CpB-thromb-UK corresponds functionally to a plasmin resistant form of pro-UK, indicating that the catalytic site of the single-chain pro-UK is unaffected by thrombin cleavage. The effect of CpB indicates that the C-terminal Arg of thromb- UK slightly enhances its affinity for plasminogen. Thromb-UK has potential plasminogen-activating activity at surfaces where C-terminal lysines, functionally comparable to fragment E-2, are found.
54.3: <i>Invited Paper:</i> Surface Control of LC Alignment for Creation of Liquid Crystal Lenses Arrays (2022)

New photosensitive alignment materials, capable to obtain pretilt angle from 90 to 0 degree in single technological process of UV exposure, are developed. The novel technological method for fabrication LC lens and LC lenses arrays has been developed based on new pretilt angle gradient alignment materials. Laboratory samples of voltage tunable LC lens and LC lenses arrays are obtained and characterized. The developed low cost fabrication technology of tunable micro‐lenses arrays based on photosensitive alignment materials has low complexity and is perspective for light field technology applications.
Multilayer Aperture Ring Frequency Selective Surface Modelling (2005)

This paper describes the design of a low loss quasi-optical beam splitter, which is required to provide efficient diplexing of the bands 316.5-325.5 GHz and 349.5-358.5 GHz with at least 20 dB of isolation. To minimise the filter insertion loss, frequency selective surfaces (FSS) that consists of freestanding resonant shorted ring elements is proposed. In addition, to achieve the stringent isolation a two layer FSS structure is required. Two commercial electromagnetic modelling tools, a time domain finite integral method (FIT) and a finite element method (FEM) solver are used to obtain the specified transmission response. The FIT solver was used to generate fast design information at normal incidence while the FEM was only used to obtain the final design of the FSS at 45/spl deg/ due to its substantially increased run times.
Lithium–Sulfur Capacitors (2017)

Although many existing hybrid energy storage systems demonstrate promising electrochemical performances, imbalances between the energies and kinetics of the two electrodes must be resolved to allow their widespread commercialization. As such, the development of a new class of energy storage systems is a particular challenge, since future systems will require a single device to provide both a high gravimetric energy and a high power density. In this context, we herein report the design of novel lithium-sulfur capacitors. The resulting asymmetric systems exhibited energy densities of 23.9-236.4 Wh kg<sup>-1</sup> and power densities of 72.2-4097.3 W kg<sup>-1</sup>, which are the highest reported values for an asymmetric system to date. This approach involved the use of a prelithiated anode and a hybrid cathode material exhibiting anion adsorption-desorption in addition to the electrochemical reduction and oxidation of sulfur at almost identical rates. This novel strategy yielded both high energy and power densities, and therefore establishes a new benchmark for hybrid systems.
Ruthenium‐Catalyzed <i>trans</i>‐Selective Hydrostannation of Alkynes (2014)

Abstract In contrast to all other transition‐metal‐catalyzed hydrostannation reactions documented in the literature, the addition of Bu 3 SnH across various types of alkynes proceeds with excellent trans selectivity, provided the reaction is catalyzed by [Cp*Ru]‐based complexes. This method is distinguished by a broad substrate scope and a remarkable compatibility with functional groups, including various substituents that would neither survive under the conditions of established Lewis acid mediated trans hydrostannations nor withstand free‐radical reactions. In case of unsymmetrical alkynes, a cooperative effect between the proper catalyst and protic functionality in the substrate allows outstanding levels of regioselectivity to be secured as well.
Distal Cationic Poly(Ethylene Glycol) Lipid Conjugates in Large Unilamellar Vesicles Prepared by Extrusion Enhance Liposomal Cellular Uptake (2004)

Cationic poly(ethylene glycol)-lipid conjugates (CPLs), a class of lipid designed to enhance the interaction of liposomes with cells, possess the following architectural features: 1) a hydrophobic lipid anchor of distearoylphosphatidylethanolamine (DSPE); 2) a hydrophilic spacer of poly(ethylene glycol); and 3) a cationic head group prepared with 0, 1, 3, or 7 lysine residues located at the distal end of the PEG chain, giving rise to CPL possessing 1, 2, 4, or 8 positive charges, respectively (CPL1 to CPL8). Previously we have described the synthesis of CPL, have characterized the postinsertion of CPL into PEG-containing LUVs and SPLP (stabilized plasmid-lipid particles), have shown significant increases in the binding of CPL-LUV to cells, and have observed dramatically enhanced transfection (up to a million-fold) of cells with CPL-SPLP in the presence of calcium [Chen et al. (2000) Bioconjugate Chem. 11, 433-437; Fenske et al. (2001) Biochim. Biophys. Acta 1512, 259-272; Palmer et al. (2003) Biochim. Biophys. Acta 1611, 204-216]. In the present study, we examine a variety of CPL properties (such as polarity and CMC) and characterize CPL-vesicular systems formed by extrusion and examine their interaction with cells. While CPL polarity was observed to increase dramatically with increasing charge number, CMC values were all found to be low, in the range of other PEGylated lipids, and exhibited only a small increase, going from CPL1 (1.3 microM) to CPL8 (2 microM). The CPLs were almost quantitatively incorporated into large unilamellar vesicles (LUVs) prepared by the extrusion method and were evenly distributed across the lipid bilayer. Lower levels of incorporation were obtained when CPLs were incubated with preformed liposomes (DSPC/Chol, 55:45) at 60 degrees C. The binding of CPL-LUVs to BHK cells in vitro was found to be dependent on the distal charge density of the CPL rather than total surface charge. Liposomes possessing CPL4 or CPL8 were observed to bind efficiently to cell surfaces and enhance cellular uptake in BHK cells (as observed with both lipid and aqueous content markers), whereas those possessing CPL1 or CPL2 exhibited little or no binding. These results suggest new directions for the design of liposomal systems capable of in vivo delivery of both conventional and genetic (plasmid and antisense) drugs.
Output frequencies of nonlinear systems (1997)

An explicit expression for the output frequency range of nonlinear systems for general inputs is derived. This reveals the relationship between the input and output frequency ranges of a nonlinear system and extends the well-known concept in linear systems where the output frequency range is exactly the same as that of the corresponding input. The new results provide an important and basic relationship that can be applied in nonlinear system frequency domain analysis and design.
E-Ring Modified Steroids as Novel Potent Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (2005)

17β-Hydroxysteroid dehydrogenases (17β-HSDs) are an important class of steroidogenic enzymes that regulate the bioavailability of active estrogens and androgens and are as yet a relatively unexploited therapeutic target. Based on our investigations and those of others, E-ring modified steroids were identified as a useful template for the design of inhibitors of 17β-HSD type 1, an enzyme involved in the conversion of estrone into estradiol. The synthesis and biological evaluation of a new series of N- and C-substituted 1,3,5(10)-estratrien-[17,16-c]-pyrazoles and the corresponding SAR are discussed. Among the N-alkylated analogues, the most potent inhibitor was the 1‘-methoxyethyl derivative, 41, with an IC50 of 530 nM in T47-D human breast cancer cells. The X-ray crystal structure of the 1‘-isobutyl derivative, 37, was determined. Further optimization of the template using parallel synthesis resulted in a library of C5‘-linked amides from which 73 emerged. This pyridylethyl amide had an IC50 of 300 nM and its activity, with that of 41, suggests the importance of hydrogen bond acceptor groups in the pyrazole side chain. Both 41 and 73 displayed selectivity over 17β-HSD type 2, and preliminary investigations showed 41 to be nonestrogenic in vitro in a luciferase reporter gene assay in contrast to the parent pyrazole 25. Molecular modeling studies, which support these findings, and a QSAR, the predictive power of which was demonstrated, are also presented.
Nanocluster-Containing Mesoporous Magnetoceramics from Hyperbranched Organometallic Polymer Precursors (2000)

Pyrolysis of hyperbranched poly[1,1‘-ferrocenylene(methyl)silyne] (5) yields mesoporous, conductive, and magnetic ceramics (6). Sintering at high temperatures (1000−1200 °C) under nitrogen and argon converts 5 to 6N and 6A, respectively, in ∼48−62% yields. The ceramization yields of 5 are higher than that (∼36%) of its linear counterpart poly[1,1‘-ferrocenylene(dimethyl)silylene] (1), revealing that the hyperbranched polymer is superior to the linear one as a ceramic precursor. The ceramic products 6 are characterized by SEM, XPS, EDX, XRD, and SQUID. It is found that the ceramics are electrically conductive and possess a mesoporous architecture constructed of tortuously interconnected nanoclusters. The iron contents of 6 estimated by EDX are 36−43%, much higher than that (11%) of the ceramic 2 prepared from the linear precursor 1. The nanocrystals in 6N are mainly α-Fe2O3 whereas those in 6A are mainly Fe3Si. When magnetized by an external field at room temperature, 6A exhibits a high-saturation magnetization (Ms ∼ 49 emu/g) and near-zero remanence and coercivity; that is, 6A is an excellent soft ferromagnetic material with an extremely low hysteresis loss.
Cloning and molecular dissection of the 8.8 kb pig uroplakin II promoter using transgenic mice and RT4 cells (2006)

Uroplakin II (UPII) gene expression is highly tissue and cell specific, with mRNA present in the suprabasal cell layers of the bladder and urethra. Previous reports described the mouse UPII (mUPII) promoter as primarily urothelium selective. However, ectopic expression of a transgene under the 3.6 kb mUPII promoter was also detected in brain, kidney, and testis in some transgenic mouse lines. Here, we have cloned an 8.8 kb pig UPII (pUPII) promoter region and investigated which cells within the bladder and urethra express a transgene consisting of the pUPII promoter fused to human erythropoietin (hEPO) or a luciferase gene. pUPII-luciferase expression vectors with various deletions of the promoter region were introduced into mouse fibroblast (NIH3T3), Chinese hamster ovary (CHO), and human bladder transitional carcinoma (RT4). A 2.1 kb pUPII promoter fragment displayed high levels of luciferase activity in transiently transfected RT4 cells, whereas the 8.8 kb pUPII promoter region displayed only low levels of activity. The pUPII-hEPO expression vector was injected into the pronucleus of zygotes to make transgenic mice. To elucidate the in vivo molecular mechanisms controlling the tissue- and cell-specific expression of the pUPII promoter gene, transgenic mice containing 2.1 and 8.8 kb pUPII promoter fragments linked to the genomic hEPO gene were generated. An erythropoietin (EPO) assay showed that all nine transgenic lines carrying the 8.8 kb construct expressed recombinant human erythropoietin (rhEPO) only in their urethra and bladder, whereas two transgenic lines carrying the 2.1 kb pUPII promoter displayed hEPO expression in several organs including bladder, kidney, spleen, heart, and brain. These studies demonstrate that the 2.1 kb promoter contains the DNA elements necessary for high levels of expression, but lacks critical sequences necessary for tissue-specific expression. We compared binding sites in the 2.1 and 8.8 kb promoter sequences and found five peroxisome proliferator responsive elements (PPREs) in the 8.8 kb promoter. Our data demonstrated that proliferator-activated receptor (PPAR)-gamma activator treatment in RT4 cells induced the elevated expression of hEPO mRNA under the control of the 8.8 kb pUPII promoter, but not the 2.1 kb promoter. Collectively, our data suggested that all the major trans-regulatory elements required for bladder- and urethra-specific transcription are located in the 8.8 kb upstream region and that it may enhance tissue-specific protein production and be of interest to clinicians who are searching for therapeutic modalities with high efficacy and low toxicity.
Pulsed Excitation in Magnetic Particle Imaging (2019)

Magnetic particle imaging (MPI) is a promising new tracer-based imaging modality. The steady-state, nonlinear magnetization physics most fundamental to MPI typically predicts improving resolution with increasing tracer magnetic core size. For larger tracers, and given typical excitation slew rates, this steady-state prediction is compromised by dynamic processes that induce a significant secondary blur and prevent us from achieving high resolution using larger tracers. Here, we propose a new method of excitation and signal encoding in MPI we call pulsed MPI to overcome this phenomenon. Pulsed MPI allows us to directly encode the steady-state magnetic physics into the time-domain signal. This in turn gives rise to a simple reconstruction algorithm to obtain images free of secondary relaxation-induced blur. Here, we provide a detailed description of our approach in 1D, discuss how it compares with alternative approaches, and show experimental data demonstrating better than 500- [Formula: see text] resolution (at 7 T/m) with large tracers. Finally, we show experimental images from a 2D implementation.