gebhart/patrepeval huggingface dataset:
Incorporation of a Bioactive Reverse-Turn Heterocycle into a Peptide Template Using Solid-Phase Synthesis To Probe Melanocortin Receptor Selectivity and Ligand Conformations by 2D <sup>1</sup>H NMR (2011)

By use of a solid-phase synthetic approach, a bioactive reverse turn heterocycle was incorporated into a cyclic peptide template to probe melanocortin receptor potency and ligand structural conformations. The five melanocortin receptor isoforms (MC1R-MC5R) are G-protein-coupled receptors (GPCRs) that are regulated by endogenous agonists and antagonists. This pathway is involved in pigmentation, weight, and energy homeostasis. Herein, we report novel analogues of the chimeric AGRP-melanocortin peptide template integrated with a small molecule moiety to probe the structural and functional consequences of the core His-Phe-Arg-Trp peptide domain using a reverse-turn heterocycle. A series of six compounds are reported that result in inactive to full agonists with nanomolar potency. Biophysical structural analysis [2D (1)H NMR and computer-assisted molecular modeling (CAMM)] were performed on selected analogues, resulting in the identification that these peptide-small molecule hybrids possessed increased flexibility and fewer discrete conformational families compared to the reference peptide and result in a novel template for further structure-function studies.
Decoder for variable number of channel presentation of multidimensional sound fields (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 Mark F. Davis, Craig C. Todd; Decoder for variable number of channel presentation of multidimensional sound fields. J. Acoust. Soc. Am. 1 January 1995; 97 (1): 732. https://doi.org/10.1121/1.413058 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
Compact Single-/Dual-Polarized Filtering Dielectric Resonator Antennas (2018)

A compact single-polarized filtering dielectric resonator (DR) antenna (DRA) with high selectivity is investigated. The DRA is fed by hybrid microstrip line/conformal strip, excited in its fundamental TE <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1δ1</sub> <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">y</sup> mode. Owing to different loading effects of the microstrip stub and conformal strip, the resonance frequency of TE <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1δ1</sub> <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">y</sup> mode excited by the two feed lines is slightly different. Such stepping resonances yield a wide bandwidth of 21.9% and a very flat gain of 5.1 dBi. The hybrid-feeding scheme also establishes a cross-coupled structure in the DRA, which introduces two radiation nulls right near the band edges. A compact wideband filtering DRA (FDRA) with quasi-elliptic bandpass response is, therefore, obtained without requiring any specific filtering circuit. This single-polarized design is also modified to realize a dual-polarized FDRA by adding another orthogonal port with the same feeding scheme. To reduce mutual coupling between the two ports, the microstrip stubs are folded to L shape, and four additional metal posts are inserted into the DR. As a result, the isolation is improved by 14 dB, from 7.2 to 21.2 dB.
High-performance CO<sub>2</sub>-philic graphene oxide membranes under wet-conditions (2014)

Ultrathin graphene oxide (GO) (<5 nm) membranes were prepared by spin-casting onto microporous polymeric support membranes. GO membranes exhibited a highly CO2 permeable character, which is suitable for CO2 separation. In the presence of water vapour, high CO2 selectivity (e.g., CO2/H2, CO2/N2, and CO2/CH4) was achieved by enhanced CO2 sorption.
FRET-based mapping of calmodulin bound to the RyR1 Ca <sup>2+</sup> release channel (2009)

Calmodulin (CaM) functions as a regulatory subunit of ryanodine receptor (RyR) channels, modulating channel activity in response to changing [Ca(2+)](i). To investigate the structural basis of CaM regulation of the RyR1 isoform, we used site-directed labeling of channel regulatory subunits and fluorescence resonance energy transfer (FRET). Donor fluorophore was targeted to the RyR1 cytoplasmic assembly by preincubating sarcoplasmic reticulum membranes with a fluorescent FK506-binding protein (FKBP), and FRET was determined following incubations in the presence of fluorescent CaMs in which acceptor fluorophore was attached within the N lobe, central linker, or C lobe. Results demonstrated strong FRET to acceptors attached within CaM's N lobe, whereas substantially weaker FRET was observed when acceptor was attached within CaM's central linker or C lobe. Surprisingly, Ca(2+) evoked little change in FRET to any of the 3 CaM domains. Donor-acceptor distances derived from our FRET measurements provide insights into CaM's location and orientation within the RyR1 3D architecture and the conformational switching that underlies CaM regulation of the channel. These results establish a powerful new approach to resolving the structure and function of RyR channels.
Electrically Controlled Catalytic Nanowire Growth from Solution (2009)

Electric-field-induced catalytic growth of cadmium selenide nanowires from solution is demonstrated. Our approach highlights the importance of electric field and surface-charge density for catalytic nanowire growth. In addition, this method is compatible with conventional silicon-based technology, and we demonstrate in situ device fabrication at temperatures below 300 °C. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Synoviocyte-targeted therapy synergizes with TNF inhibition in arthritis reversal (2020)

Fibroblast-like synoviocytes (FLS) are joint-lining cells that promote rheumatoid arthritis (RA) pathology. Current disease-modifying antirheumatic agents (DMARDs) operate through systemic immunosuppression. FLS-targeted approaches could potentially be combined with DMARDs to improve control of RA without increasing immunosuppression. Here, we assessed the potential of immunoglobulin-like domains 1 and 2 (Ig1&2), a decoy protein that activates the receptor tyrosine phosphatase sigma (PTPRS) on FLS, for RA therapy. We report that PTPRS expression is enriched in synovial lining RA FLS and that Ig1&2 reduces migration of RA but not osteoarthritis FLS. Administration of an Fc-fusion Ig1&2 attenuated arthritis in mice without affecting innate or adaptive immunity. Furthermore, PTPRS was down-regulated in FLS by tumor necrosis factor (TNF) via a phosphatidylinositol 3-kinase-mediated pathway, and TNF inhibition enhanced PTPRS expression in arthritic joints. Combination of ineffective doses of TNF inhibitor and Fc-Ig1&2 reversed arthritis in mice, providing an example of synergy between FLS-targeted and immunosuppressive DMARD therapies.
Concept of a 150 krpm bearingless slotless disc drive with combined windings (2013)

In this paper, a concept is developed for a slotless bearingless disc drive with toroidal windings for a rotational speed of 150'000 rpm. The topology and its working principles are explained and an already running prototype for lower speeds is introduced. To reach the high rotational speeds, the mechanical strength and the maximal diameter of the rotor is evaluated. Outgoing form the prototype, scaling laws are examined to identify the challenges for down-scaling of the bearingless motor. 3D FEM Simulations and optimizations are conducted to determine the influence of the magnetic gap length and to find the optimal stator and rotor height. At the end, the geometry of the high speed concept is presented and the performance results are compared to the prototype.
Quantitative Structure−Activity Relationships for the<i>in Vitro</i>Antimycobacterial Activity of Pyrazinoic Acid Esters (1996)

Substituted pyrazinoic acid esters have previously been reported to have in vitro activity against Mycobacterium avium and Mycobacterium kansasii as well as Mycobacterium tuberculosis. Modification of both the pyrazine nucleus and the ester functionality was successful in expanding the antimycobacterial activity associated with pyrazinamide to include M. avium and M. kansasii, organisms usually not susceptible to pyrazinamide. In an attempt to understand the relationship between the activity of the esters with the needed biostability, a quantitative structure-activity relationship has been developed. This derived relationship is consistent with the observation that tert-butyl 5-chloropyrazinoate (13) and 2'-(2'-methyldecyl) 5-chloropyrazinoate (25), compounds which are both 100-fold more active than pyrazinamide against M. tuberculosis and possess a serum stability 900-1000 times greater than the lead compounds in the series.
Design and Preparation of a Multimeric Self-Cleaving Hammerhead Ribozyme (1997)

The activity of a ribozyme can be impaired by additional sequences at the 5' and 3' termini of the catalytic sequence. To approach this problem, a system was designed that minimizes sequences upstream and downstream from active regions of a hammerhead ribozyme and allows delivery of a large number of active molecules. A self-cleavable multimeric molecule was prepared by placing a ribozyme target sequence (derived from the core region of the hepatitis B virus [HBV]) upstream and downstream from the catalytic sequence. This construct was cloned in tandem into in vitro expression vectors. 32P-UTP-labeled transcripts of the multimeric construct, as well as non-self-cleaved monomeric ribozyme controls, and substrate were synthesized. The multimeric ribozyme molecule efficiently self-cleaved to release monomeric ribozymes lacking any extra upstream and downstream sequences. In addition, monomers were substantially more active against the HBV target RNA than the non-self-cleavable ribozymes. Up to 80% degradation of the target RNA was achieved by a tenfold molar excess of a pentameric construct. We conclude that ribozymes can be produced as a multimeric tandem of self-cleavable molecules, the monomers of which are more active than monomeric ribozymes and highly efficient in cleavage of target transcripts.
A Lectin Isolated from Bananas Is a Potent Inhibitor of HIV Replication (2010)

BanLec is a jacalin-related lectin isolated from the fruit of bananas, Musa acuminata. This lectin binds to high mannose carbohydrate structures, including those found on viruses containing glycosylated envelope proteins such as human immunodeficiency virus type-1 (HIV-1). Therefore, we hypothesized that BanLec might inhibit HIV-1 through binding of the glycosylated HIV-1 envelope protein, gp120. We determined that BanLec inhibits primary and laboratory-adapted HIV-1 isolates of different tropisms and subtypes. BanLec possesses potent anti-HIV activity, with IC(50) values in the low nanomolar to picomolar range. The mechanism for BanLec-mediated antiviral activity was investigated by determining if this lectin can directly bind the HIV-1 envelope protein and block entry of the virus into the cell. An enzyme-linked immunosorbent assay confirmed direct binding of BanLec to gp120 and indicated that BanLec can recognize the high mannose structures that are recognized by the monoclonal antibody 2G12. Furthermore, BanLec is able to block HIV-1 cellular entry as indicated by temperature-sensitive viral entry studies and by the decreased levels of the strong-stop product of early reverse transcription seen in the presence of BanLec. Thus, our data indicate that BanLec inhibits HIV-1 infection by binding to the glycosylated viral envelope and blocking cellular entry. The relative anti-HIV activity of BanLec compared favorably to other anti-HIV lectins, such as snowdrop lectin and Griffithsin, and to T-20 and maraviroc, two anti-HIV drugs currently in clinical use. Based on these results, BanLec is a potential component for an anti-viral microbicide that could be used to prevent the sexual transmission of HIV-1.
Design of a neuro-controller for multivariable nonlinear time-varying systems (2010)

This paper presents a controller design method for multi-input multi-output (MIMO) nonlinear time-varying systems using Radial Basis Funtion (RBF) neural network. The developed neuro-controller generates optimal control signals abiding by constraints, if any, on the control signal or on the system output. The proposed controller does not require an explicit knowledge of the states of the system or any apriori knowledge of the structure of nonlinearity of the system. Time based variations in system parameters as well as system nonlinearities are successfully compensated by the neural network. Simulation results for nonlinear time-varying systems are included at the end and controller performance is analyzed.
Whispering-Gallery Mode-Locked Lasers (2003)

Mode-locked lasers of a proposed type would incorporate features of the design and operation of previously demonstrated miniature electro-optical modulators and erbium-doped glass lasers that contain whispering-gallery-mode (WGM) resonators. That is to say, WGM lasers and WGM electro-optical modulators would be integrated into monolithic units that, when suitably excited with pump light and microwaves, would function as mode-locked lasers. The proposed devices are intended to satisfy an anticipated demand for compact, low-power devices that could operate in the optical-communication wavelength band centered at a wavelength of 1.55 m and could generate pulses as short as picoseconds at repetition rates of multiple gigahertz.
Direct Detection of Beryllium on Filters Using the Laser Spark (1985)

A method has been developed to spectrochemically analyze beryllium particles on filters using the laser spark. The spark, formed on the filter by a cylindrical lens, is 0.1-mm wide and 4- to 8-mm long. By the rotation of the filter under the spark, a large area can be sampled in only a few minutes. The surface detection limit (SNR = 6) for particles 0.5–5 μm in diameter is 0.45 ng/cm 2 , which corresponds to 3.6 ng total Be mass on the exposed area (32-mm diam.) of a 37-mm-diam. filter. The RSD for replicate sample analysis is 4%. Several methods of calibrating the technique are discussed. The effects of particle size and some contaminants on the analysis are described. The usefulness of this method for monitoring airborne beryllium concentrations is considered.
ChemInform Abstract: Novel 1H‐Benzimidazol‐4‐ols with Potent 5‐Lipoxygenase Inhibitory Activity. (1988)

Abstract The o‐phenylenediamines (I) react with the carboxylic acids (II), yielding the title compounds (III) after deprotection by catalytic dehydrogenation.
The ultrafast response of a scanning tunneling microscope (1995)

Abstract The development of the ultrafast scanning tunneling microscope is reviewed. It is shown that the response of the tunneling gap of a scanning tunneling microscope to excitation by a subpicosecond electrical pulse has a capacitive component, the origin of which is quantum mechanical.
Raman study of the solid-state polymerization of acetylene at high pressure (1988)

The mechanism and kinetics of the pressure-induced polymerization of acetylene were studied by Raman spectroscopy. The polymerization reaction occurred in the orthorhombic phase at room temperature and pressures above 3.5 GPa. Dominant formation of trans-polyacetylene suggested that the monomer underwent trans opening of the triple bond and polymerized along the diagonal of the bc plane of the unit cell. The reaction was described as an idealized one-step and one-dimensional growth process by an Avrami equation with an exponent 1.34.
Regulation of TCL1 expression in B- and T-cell lymphomas and reactive lymphoid tissues. (2000)

Chromosomal rearrangements observed in T-cell prolymphocytic leukemia involve the translocation of one T-cell receptor gene to either chromosome 14q32 or Xq28, deregulating the expression of cellular protooncogenes of unknown function, such as TCL1 or its homologue, MTCP1. In the human hematopoietic system, TCL1 expression is predominantly observed in developing B lymphocytes, whereas its overexpression in T cells causes mature T-cell proliferation in transgenic mice. In this study, using a newly generated monoclonal antibody against recombinant TCL1 protein, we extended our analysis mainly by immunohistochemistry and also by fluorescence-activated cell sorting and Western blot to a large tumor lymphoma data bank including 194 cases of lymphoproliferative disorders of B- and T-cell origin as well as reactive lymphoid tissues. The results obtained show that in reactive lymphoid tissues, TCL1 is strongly expressed by a subset of mantle zone B lymphocytes and is expressed to a lesser extent by follicle center cells and by scattered interfollicular small lymphocytes. In B-cell neoplasia, TCL1 was expressed in the majority of the cases, including lymphoblastic lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, Burkitt lymphoma, diffuse large B-cell lymphoma (60%), and primary cutaneous B cell lymphoma (55%). TCL1 expression was observed in both the cytoplasmic and nuclear compartments, as confirmed by Western blot analysis. Conversely, TCL1 was not expressed in Hodgkin/Reed-Sternberg cells, multiple myelomas, marginal zone B-cell lymphomas, CD30+ anaplastic large cell lymphoma, lymphoblastic T-cell lymphoma, peripheral T-cell lymphoma, and mycosis fungoides. These data indicate that TCL1 is expressed in more differentiated B cells, under both reactive and neoplastic conditions, from antigen committed B cells and in germinal center B cells and is down-regulated in the latest stage of B-cell differentiation.
Zona Incerta: A Role in Central Pain (2009)

Central pain syndrome (CPS) is a debilitating condition that affects a large number of patients with a primary lesion or dysfunction in the CNS. Despite its discovery over a century ago, the pathophysiological processes underlying the development and maintenance of CPS are poorly understood. We recently demonstrated that activity in the posterior thalamus (PO) is tightly regulated by inhibitory inputs from zona incerta (ZI). Here we test the hypothesis that CPS is associated with abnormal inhibitory regulation of PO by ZI. We recorded single units from ZI and PO in animals with CPS resulting from spinal cord lesions. Consistent with our hypothesis, the spontaneous firing rate and somatosensory evoked responses of ZI neurons were lower in lesioned animals compared with sham-operated controls. In PO, neurons recorded from lesioned rats exhibited significantly higher spontaneous firing rates and greater responses to noxious and innocuous stimuli applied to the hindpaw and to the face. These changes were not associated with increased afferent drive from the spinal trigeminal nucleus or changes in the ventroposterior thalamus. Thus CPS can result from suppressed inputs from the inhibitory nucleus zona incerta to the posterior thalamus.
Source localization in reverberant environments using sparse optimization (2013)

In this paper, we demonstrate that recently-developed sparse recovery algorithms can be used to improve source localization in reverberant environments. By formulating the localization problem in the frequency domain, we are able to efficiently incorporate information that exploits the reverberation instead of considering it a nuisance to be eliminated. In this formulation, localization becomes a joint-sparsity support recovery problem which can be solved using model-based methods. We also develop a location model which further improves performance. Using our approach, we are able to recover more sources that the number of sensors. In contrast to conventional wisdom, we demonstrate that reverberation is beneficial in source localization, as long as it known and properly accounted for.
A novel method for the isolation of extracellular vesicles and RNA from urine (2017)

The discovery of urinary extracellular biomarkers has been impeded by the lack of efficient methods for the isolation of extracellular vesicles (EVs: exosomes and microvesicles) and extracellular nucleic acid (RNA and DNA) from urine. Ultracentrifugation (UC), considered the gold standard for vesicle isolation from many biofluids, is efficacious but laborious, and, like most commercially available methods, is unable to isolate enough material from small volumes for protein or RNA-based biomarker discovery. We have developed a novel precipitation method for the isolation of EVs and nucleic acids from urine. The method, which is now commercially available, takes less than 30 min and does not require polyethylene glycol. Transmission electron microscopy and Nanosight particle analysis confirm that the method isolates intact vesicles with a similar size, shape, and number to UC. Immunoblot analysis of preparations made from a variety of urine samples demonstrates that the method isolates multiple vesicle protein markers more efficiently than other commercial kits, especially from more diluted samples. Bioanalyzer, quantitative reverse transcription polymerase chain reaction, and array analysis show that the method is extremely efficient at the isolation of extracellular miRNAs. The Ymir Genomics EV and Extracellular RNA Isolation Kits offer an efficient and rapid alternative to UC and other commercial kits.
Neuroimmunophilin Ligands Accelerate and Promote Nerve Regeneration in the Rat Peripheral Nerve and Spinal Cord (2003)

Neuroimmunophilins refer to the binding targets for immunosuppressant drugs (FK506, rapamycin, and cyclosporin A) present in the nervous system. Neuroimmunophilin ligand, the compounds that bind to them, have great potential for significantly advancing the practice of clinical neurology. The ability to separate the nerve regenerative and immunosuppressant properties of FK506 (tacrolimus) was a fundamental step in the development of clinically useful neuroimmunophilin ligands for nerve regeneration. This discovery was made independently by the Snyder/Guilford and Gold laboratories (1–3) who demonstrated that nonimmunosuppressant (noncalcineurin inhibitor) FK506 derivatives (e.g., GPI-1046 and V-10, 367, respectively) retain the nerve regenerative property of FK506 and are orally active (4, 5), the latter finding being unprecedented.