gebhart/patrepeval huggingface dataset:
(/sup 11/C)clorgyline and (/sup 11/C)-L-deprenyl and their use in measuring functional monoamine oxidase activity in the brain using positron emission tomography (1986)

This invention involves a new strategy for imaging the activity of the enzyme monoamine oxidase in the living body by using /sup 11/C-labeled enzyme inhibitors which bind irreversibly to an enzyme as a result of catalysis. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography. 2 figs.
The Design and Synthesis of Hard and Impermeable, Yet Flexible, Conformal Organic Coatings (2012)

A new design paradigm for conformal, all-organic coatings that retain their flexibility and chemical functionality while displaying exceptional mechanical hardness and barrier properties is presented. Initiated chemical vapor deposition is used to synthesize a novel alternating copolymer thin film. Upon annealing, films display elastic moduli exceeding 20 GPa, excellent scratch resistance and flexibility, and very low oxygen permeability.
Single-lobe operation of surface-emitting complex-coupled second-order distributed-feedback diode lasers (2002)

We present the first theoretical analysis of surface-emitting, complex-coupled distributed feedback (SE-CC-DFB) lasers with a second-order grating. It is found that lasing operation in a single-lobed, orthonormal far-field radiation pattern as well as in a nearly uniform near-field intensity pattern is fundamentally favored.
Envelope, group and phase velocities in a nested frequency comb (2016)

Fabry–Perot etalons have been traditionally used in a laser cavity to tune the optical frequency. In this work we present the generation of interwoven frequency combs with insertion of an intracavity Fabry–Perot in a mode-locked laser. A high frequency comb is generated by insertion of an uncoated (low finesse) Fabry–Perot inside the laser cavity. The intracavity Fabry–Perot acquires a high finesse from the laser cavity and the velocity of the pulses in the Fabry–Perot is affected by the laser cavity length, gain and losses, with the dielectric group velocity dk/dΩ playing only a minor role. The output characteristics are explained by the condition that the radiation is simultaneously resonant with the etalon and the laser cavity.
Biomechanical Aspects in Implantable Microphones and Hearing Aids and Development of a Concept with a Hydroacoustical Transmission (2001)

The middle ear functions as a sensitive pressure receptor. This implies that it not only transmits sound pressure waves with molecule-sized vibrational amplitudes, but that it also reacts to the million times larger variations of ambient air pressure. This pressure induces movements of the tympanic membrane and of the attached ossicular chain of up to 1,000 microm. Any artificial device that contacts these sound-transporting elements, be it a receiver for an implantable microphone or a transducer for an implantable hearing aid, has to respect these two different modes of biomechanical behavior. A hydroacoustical transmission system has therefore been developed consisting of a water-filled flexible tube, which contacts the ossicular chain with a balloon tip, and which is connected to a piezo-electric transducer at its other end. This soft contact prevents a localized pressure load and does not restrain the free movement of the underlying ossicle during ambient pressure variations. Temporal bone experiments showed that the device transmits vibration energy in good acoustical quality. The device can also be used in a reverse mode, working as a microphone, for example for a totally implantable hearing aid or a cochlear implant. This microphone concept has the advantage that it incorporates the biologic sound receiving components (the tympanic membrane and the ossicular chain micromechanics) into a technical device.
Facile and Selective Cross‐Coupling of Phenols Using Selenium Dioxide (2016)

Nonsymmetric biphenols are important structural motifs in organic chemistry. Therefore, an easy and versatile protocol for oxidative cross‐coupling is essential to generate these so‐called “privileged ligands”. We developed an efficient and selective oxidative pathway to synthesize 2,2′‐biphenols as well as 2,4′‐ and 4,4′‐biphenols. The use of selenium dioxide, a stable, powerful, and commercially available oxidizer, in 1,1,1,3,3,3‐hexafluoroisopropanol allowed the oxidative coupling of alkyl‐, alkoxy‐, and halogen‐substituted phenols.
Identification of Vinca alkaloid acceptors in P388 murine leukemia cells with a photoactive analogue of vinblastine. (1987)

The cytotoxic, antimitotic, and growth inhibition properties of a photoactive analogue of vinblastine, N-(p-azidobenzoyl)-N'-beta-aminoethylvindesine (NABV), and vinblastine on P388 murine leukemia cells were compared. After 72-h exposure, the 50% drug-inhibitory concentrations for exponentially growing P388 leukemic cells were 1.2 nM for NABV and 0.6 nM for vinblastine. The ultrastructural effects of NABV and vinblastine on P388 cells were similar: formation of tubulin paracrystals; mitotic arrest (C-mitosis); increased post-C-mitotic multinucleated cells; increased number of annulate lamellae; and the appearance of intracytoplasmic paired cisternae. [3H]NABV was used to identify Vinca alkaloid binding sites in P388 cells by photoaffinity labeling. After irradiation at 302 nm, radioactive Vinca alkaloid binding components were resolved by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and identified in 1-mm gel slices. The most prominent photolabeled species were Mr 44,000, 54,000, and 75,000 polypeptides located in the 100,000 X g supernatant fraction. The Mr 54,000 component was also observed in the membrane fraction. Specific photolabeling of Mr 54,000 and 44,000 polypeptides was blocked in the presence of 20 microM excess of vinblastine and was saturable with half-maximal saturation concentrations of 0.18 and 0.4 microM [3H]NABV, respectively. The Mr 54,000 component was identified as a tubulin subunit by immunoprecipitation with antitubulin monoclonal antibodies. Since NABV and vinblastine have similar pharmacological and biological properties, this photoactive analogue may be useful for identifying important Vinca alkaloid cellular acceptors which may be responsible for drug cytotoxic and antineoplastic activities.
Digital bowel cleansing for computer-aided detection of polyps in fecal-tagging CT colonography (2006)

Digital bowel cleansing (DBC) is an emerging method for segmentation of fecal materials, which are tagged by an X-ray-opaque oral contrast agent in CT colonography (CTC) images, effectively removing them for digital cleansing of the colon. Existing DBC approaches tend to use simple thresholding-based methods for the removal of tagged fecal materials; however, because of the pseudo-enhancement of polyps caused by the surrounding tagged fecal materials, such methods tend erroneously to remove a part of or the entire polyps submerged in these materials. In this study, we developed a novel DBC method that preserves the soft-tissue structures submerged in or partially covered by tagged fecal materials. In our approach, submerged soft-tissue structures are characterized by their local shape signatures that are calculated based on the eigenvalues of a Hessian matrix. A structure-enhancement function is formulated for enhancing of the soft-tissue structures, and the values of the function are integrated into the speed function of a level set method to delineate the submerged soft-tissue structures while removing the tagged fecal materials. In an analysis of 10 submerged polyps, our new DBC method was shown to delineate polyps better than was possible with our previously reported cleansing method based on thresholding. Application of our computer-aided detection (CAD) scheme showed that the use of the new DBS method substantially reduced the number of false-positive detections compared with those of our previous, thresholding-based method.
Decapeptides as effective agonists from L-amino acids biologically equivalent to the luteinizing hormone-releasing hormone. (1986)

Apparently, no agonist has been found that is comparable in potency to the luteinizing hormone-releasing hormone (LHRH) for release of LH and follicle-stimulating hormone (FSH) without substitutions with unnatural or D forms of natural amino acids. Of 139 known "agonist analogs" of LHRH, two were active in the range of 65%. The four LHRHs known to occur in nature involve a total of six amino acids (Tyr, His, Leu, Trp, Arg, Gln) in positions 5, 7, and 8. There are 16 possible peptides with these six amino acids in positions 5, 7, and 8, of which 4 are the known LHRHs, and 2 more were synthesized. We have synthesized the 10 new peptides and assayed 11 in vivo and in vitro, and we found not only 1 but a total of 5 that have activity equivalent to or greater than that of LHRH for the release of LH and/or FSH under at least one assay condition. These five are as follows: [His5,Trp7,Gln8]LHRH; [His5,Trp7,Leu8]LHRH; [His5,Trp7]LHRH; [Trp7]LHRH; [His5]LHRH. Two of these five agonists variably released relatively more FSH than LH. One or more of these five agonists may occur in nature and one may be follicle-stimulating hormone-releasing hormone. The two peptides with Gln8 and Leu8, if occurring in nature, may have different receptors according to radioreceptor assays and to the ratio of LH/FSH release in vivo. These structures are a basis for the design of antagonists without Arg8 toward avoiding histamine release. Complete inhibition of LH and FSH release in vivo may be induced by joint use of Arg8 and Gln8 or Leu8 antagonists. These potent agonists, related to LHRH, may be therapeutically useful in disorders of reproduction, the central nervous system, and for the control of hormone-dependent carcinomas.
A novel strain of<i>Bacillus thuringiensis</i>(NCIMB 40152) active against coleopteran insects (1991)

A novel Bacillus thuringiensis strain, NCIMB 40152, was isolated from dead Tenebrio molitor L. larvae. The isolate is endowed with specific insecticide activity against the Colorado potato beetle (Leptinotarsa decemlineata (Say), Coleoptera, Crysomelidae), but has no effect against lepidopteran or dipteran insects. During the sporulation process it produces diamond-shaped crystals and small inclusions. Rare flat, square crystals are also produced. The strain can be differentiated from the other reported B. thuringiensis strains active against Coleoptera on the basis of physiological and biochemical tests, flagellar serotype and toxin electrophoretic patterns. NCIMB 40152 toxin is easily extractable from spore/crystal preparations in neutral distilled water without detergents or reducing agents.
The effect of endothelial cells on hESC-derived pancreatic progenitors in a 3D environment (2014)

Generating transplantable β-like-cells from human embryonic stem cells (hESC) could serve as an ideal cell-based therapy for treatment of type 1 diabetes, which is characterized by the destruction of insulin-secreting pancreatic β-cells. There are several protocols for differentiating hESCs into pancreatic or endocrine precursors. However, so far, production of mature, functional β-like-cells has been achieved mainly by transplanting hESC derived pancreatic progenitors (PPs) and allowing several months for maturation to occur in vivo. One approach, believed to have potential in promoting differentiation into β-like-cells prior to transplantation, is culturing PPs alongside blood vessels. Endothelium and blood vessels have been shown to direct pancreatic development during embryogenesis and also induce endocrine differentiation in vitro. Here we designed a three-dimensional (3D) construct utilizing highly porous polymeric scaffolds that mimic natural conditions and provide cells with mechanical support, and used it in the differentiation protocol. Clusters of hESC derived pancreatic precursor cells were embedded within the scaffolds along with human endothelial cells (ECs) and fibroblasts forming vessel-like networks. Culturing these clusters with ECs for one week significantly increased the population of PPs, characterized by co-expression of the pancreatic markers Pdx1 and Nkx6.1 and also highly induced Ngn3 expression which indicates commitment to endocrine fate. The presence of fibroblasts, however, reduced this cell population. Three months upon implantation of constructs containing clusters and ECs or clusters alone, implanted mice retained normal blood glucose levels after treatment with STZ, while un-implanted mice became diabetic. These findings may lay the foundation for creating an optimal tissue-construct that will support PPs' maturation in vitro and enhance graft function upon implantation.
A Segmented Thermometer Coded DAC with Deterministic Dynamic Element Matching for High Resolution ADC Test (2005)

Dynamic element matching (DEM) is an effective way to achieve good average performance in the presence of device mismatch, yet it has not been widely adopted because of the time-local stationarity of the signal path. This paper presents a DEM approach to ADC testing in which low precision DEM DACs are used to generate stimulus signals for the ADCs under test. A deterministic DEM (DDEM) switching scheme is applied to a segmented thermometer coded DAC architecture. Detailed simulation results are presented to verify the expected performance of the proposed testing approach. The new approach is able to accurately test ADCs with linearity that exceeds that of the original DAC used as the signal generator. The new architecture is suitable for production test and built-in-self-test (BIST) environments where high linearity ADCs are difficult to test and characterize.
Pancreatic Tissue Distribution, Pharmacokinetics and Toxicity of Bioactive delta‐tocotrienol, a Potential Anti‐tumor Bioactive Food Component, in Mice (2008)

Tocotrienols are natural vitamin E compounds in foods such as cereal. They have been shown to inhibit cancer cell growth and survival. Recently, we observed that δ‐tocotrienol is the most active tocotrienol against pancreatic cancer. The objective of this study was to determine the oral bioavailability of δ‐tocotrienol in mice pancreas and in the tumor. Mice (4–5 weeks old) were treated orally with vehicle (PBS/ethanol extracted olive oil), 50 mg/kg or 100 mg/kg dose of δ‐tocotrienol. Plasma and tissues were isolated at different time points and δ‐tocotrienol was analyzed by HPLC using fluorescence detection. The results show that the peak plasma concentration (C max ) was 57 μM and the T max was 2 h. The maximum concentration of δ‐Tocotrienol was achieved at 2 h in the liver and at 8 h in the pancreas. The δ‐tocotrienol was cleared from plasma and liver within 24 h but had delayed clearance from the pancreas. Interestingly we found that δ‐tocotrienol was 10‐fold more concentrated in the pancreas than in the tumor tissue. We also observed no toxicity due to δ‐tocotrienol administration as documented by normal weight gain of the mice with no mortality. Our data suggests that δ‐tocotrienol is safe, and orally bioavailable in the pancreatic tissue of mice at levels which predicts bioactivity against neoplastic cells. We conclude that δ‐tocotrienol should be investigated for the prevention and treatment of pancreatic cancer.
A compact planar magic-T junction with aperture-coupled difference port (1997)

The operating principles of a compact planar magic-T junction are described and experimentally validated. The distinguishing feature of this component is the placement of the difference port on a layer separated from the other three ports by a ground plane. Moreover, the two parts of the component are electromagnetically coupled through a slot-aperture in the ground plane. The component is inherently multilayer, i.e., the transition between the circuit layers is a functional part of the device. The tested microstrip prototype performs well over a frequency range of about 40%.
High-gain fiber, optical-parametric, chirped-pulse amplification of femtosecond pulses at 1 μm (2010)

Fiber-based optical-parametric chirped-pulse amplification is reported at 1μm in a microstructured fiber in the femtosecond regime. The signal has been highly stretched by an Öffner triplet and then amplified with an all-fiber, pulsed-pump, fiber optical-parametric amplifier. More than 30dB gain has been achieved over 8.3nm, and the amplified signal has been recompressed.
A Pathogenesis Assay Using <i>Saccharomyces</i> <i>cerevisiae</i> and <i>C</i> <i>aenorhabditis</i> <i>elegans</i> Reveals Novel Roles for Yeast AP-1, Yap1, and Host Dual Oxidase BLI-3 in Fungal Pathogenesis (2009)

Treatment of systemic fungal infections is difficult because of the limited number of antimycotic drugs available. Thus, there is an immediate need for simple and innovative systems to assay the contribution of individual genes to fungal pathogenesis. We have developed a pathogenesis assay using Caenorhabditis elegans, an established model host, with Saccharomyces cerevisiae as the invading fungus. We have found that yeast infects nematodes, causing disease and death. Our data indicate that the host produces reactive oxygen species (ROS) in response to fungal infection. Yeast mutants sod1Delta and yap1Delta, which cannot withstand ROS, fail to cause disease, except in bli-3 worms, which carry a mutation in a dual oxidase gene. Chemical inhibition of the NADPH oxidase activity abolishes ROS production in worms exposed to yeast. This pathogenesis assay is useful for conducting systematic, whole-genome screens to identify fungal virulence factors as alternative targets for drug development and exploration of host responses to fungal infections.
Nanowire Thermocouple Characterization Platform (2013)

Thermocouples fabricated out of nanowires possess a high spatial and temporal resolution. Due to their small size, nanowires exhibit different physical properties from their bulk counterparts. One of these properties, the Seebeck coefficient, specifies how well the thermocouple converts a temperature gradient into an open-circuit voltage. We have developed a characterization platform, with which the Seebeck coefficient of nanowires can be measured as required for the calibration of nanowire thermocouples and optimization of their fabrication process.
Encapsulation and Covalent Binding of Molecular Payload in Enzymatically Activated Micellar Nanocarriers (2015)

The high selectivity and often-observed overexpression of specific disease-associated enzymes make them extremely attractive for triggering the release of hydrophobic drug or probe molecules from stimuli-responsive micellar nanocarriers. Here we utilized highly modular amphiphilic polymeric hybrids, composed of a linear hydrophilic polyethylene glycol (PEG) and an esterase-responsive hydrophobic dendron, to prepare and study two diverse strategies for loading of enzyme-responsive micelles. In the first type of micelles, hydrophobic coumarin-derived dyes were encapsulated noncovalently inside the hydrophobic core of the micelle, which was composed of lipophilic enzyme-responsive dendrons. In the second type of micellar nanocarrier the hydrophobic molecular cargo was covalently linked to the end-groups of the dendron through enzyme-cleavable bonds. These amphiphilic hybrids self-assembled into micellar nanocarriers with their cargo covalently encapsulated within the hydrophobic core. Both types of micelles were highly responsive toward the activating enzyme and released their molecular cargo upon enzymatic stimulus. Importantly, while faster release was observed with noncovalent encapsulation, higher loading capacity and slower release rate were achieved with covalent encapsulation. Our results clearly indicate the great potential of enzyme-responsive micellar delivery platforms due to the ability to tune their payload capacities and release rates by adjusting the loading strategy.
The chemical development of selective and specific serotonin S<sub>2</sub>‐antagonists (1986)

Abstract Four types of chemical intermediates were prepared to synthesize novel piperidine derivatives inspired by the butyrophenones benperidol and lenperone and by the diphenylbutyl neuroleptic pimozide. The fist type, comprising benzimidazolone alkyl intermediates, yielded declenperone and milenperone and also the “symmetrical” compound domperidone, which was pharmacologically unusual by its specific peripheral dopamine antagonism. Declenperone was the most potent serotonin antagonist of that series, and replacement of the benzimidazolinonepropyl by the quinazolinedioneethyl moiety led to ketanserin, which was devoid of residual dopamine antagonism. Very potent serotonin S 2 ‐antagonists were also obtained by using intermediates prepared from 2‐aminoaza‐heterocycles. Pirenperone and setoperone had a complex pharmacological profile, including significant dopamine and norepinephrine antagonism. These activity components were absent from the profile of R 56413 and ritanserin, which were obtained by using the fourth intermediate, benzhydrylenepiperidine. R 56413 and ritanserin are the most specific of the presently known serotonin S 2 ‐antagonists.
Linear Feature Space Transformations for Speaker Adaptation (2001)

We extend the well-known technique of constrained Maximum Likelihood Linear Regression (MLLR) to compute a projection (instead of a full rank transformation) on the feature vectors of the adaptation data. We model the projected features with phone-dependent Gaussian distributions and also model the complement of the projected space with a single class-independent, speaker-specific Gaussian distribution. Subsequently, we compute the projection and its complement using maximum likelihood techniques. The resultingML transformation is shown to be equivalent to performing a speaker-dependent heteroscedastic discriminant (or HDA) projection. Our method is in contrast to traditional approaches which use a single speaker-independent projection, and do speaker adaptation in the resulting subspace. Experimental results on Switchboard show a 3% relative improvement in the word error rate over constrained MLLR in the projected subspace only.