gebhart/patrepeval huggingface dataset:
Development of organometallic (organo-transition metal) pharmaceuticals (2005)

This paper is aimed at introducing the organometallic chemist to the fascinating area of organometallic pharmaceuticals. It commences by identifying the properties of organometallic (transition metal) compounds that lend themselves to medical applications. Next, the specialized techniques and methods that are used to assess the medicinal properties of compounds are summarized, and although these techniques are not restricted to organometallic compounds, all examples are concerned with organometallic compounds. The design and evaluation of organometallic compounds for medicinal applications are described in context with the diseases they have been evaluated against, and areas are identified that may have most potential for organometallic pharmaceuticals. Some new results, including the first example of an organo-osmium compound that might exhibit effective anticancer properties, are also described. Copyright © 2005 John Wiley & Sons, Ltd.
Sequence Analysis of a 685-kb Genomic Region on Chromosome 3p22-p21.3 That Is Homozygously Deleted in a Lung Carcinoma Cell Line (1997)

Frequent chromosomal aberrations and/or losses of heterozygosity involving the short arm of chromosome 3 in carcinomas of the lung, kidney and other tissues imply that multiple putative tumor suppressor genes may be present on this chromosomal arm. To search for one of these genes, we determined DNA sequences in the genomic region at 3p22-21.3 where we had previously detected a homozygous deletion in a lung cancer cell line. The DNA sequence results of an about 685-kb region indicated that the size of the homozygously deleted segment was 638,489 bp, in which we identified only four genes including the integrin alpha RLC and the trans-Golgi p230 genes, both reported previously. The predicted amino acid sequences of one of the two novel genes showed high homology to villin, a human cytoskeleton protein; those of the other gene, termed HYA22, revealed significant homology to YA22, a hypothetical protein predicted from DNA sequences of Schizosaccharomyces pombe. The computer programs HEXON or GRAIL were able to predict three-fourths of the exons; the smallest exon predicted by either program was 46 base pairs. Repetitive sequences contained in the genomic region included 151 copies of the Alu sequence (1 copy/every 4.5 kb), 19 copies of the L1 sequence (1 copy/every 36 kb), and 10 copies of the THE sequence.
Mapping of Glutathione and Its Precursor Amino Acids Reveals a Role for GLYT2 in Glycine Uptake in the Lens Core (2007)

The mapping of GSH and its precursor amino acids has shown that an alternative glycine uptake pathway exists in mature fiber cells. Although GLYT1 and -2 are likely to mediate glycine uptake in cortical fiber cells, GLYT2 alone appears responsible for the accumulation of glycine in the center of the lens. Enhancing the delivery of glycine to the core via the sutures may represent a pathway to protect the lens against the protein modifications associated with age-related nuclear cataract.
MicroRNAs: Novel Regulators Involved in the Pathogenesis of Psoriasis? (2007)

MicroRNAs are a recently discovered class of posttranscriptional regulators of gene expression with critical functions in health and disease. Psoriasis is the most prevalent chronic inflammatory skin disease in adults, with a substantial negative impact on the patients' quality of life. Here we show for the first time that psoriasis-affected skin has a specific microRNA expression profile when compared with healthy human skin or with another chronic inflammatory skin disease, atopic eczema. Among the psoriasis-specific microRNAs, we identified leukocyte-derived microRNAs and one keratinocyte-derived microRNA, miR-203. In a panel of 21 different human organs and tissues, miR-203 showed a highly skin-specific expression profile. Among the cellular constituents of the skin, it was exclusively expressed by keratinocytes. The up-regulation of miR-203 in psoriatic plaques was concurrent with the down-regulation of an evolutionary conserved target of miR-203, suppressor of cytokine signaling 3 (SOCS-3), which is involved in inflammatory responses and keratinocyte functions. Our results suggest that microRNA deregulation is involved in the pathogenesis of psoriasis and contributes to the dysfunction of the cross talk between resident and infiltrating cells. Taken together, a new layer of regulatory mechanisms is involved in the pathogenesis of chronic inflammatory skin diseases.
Phosphatidylinositol 4,5-Bisphosphate Induces Actin Stress-Fiber Formation and Inhibits Membrane Ruffling in Cv1 Cells (2001)

Phosphatidylinositol 4,5 bisphosphate (PIP(2)) is widely implicated in cytoskeleton regulation, but the mechanisms by which PIP(2) effect cytoskeletal changes are not defined. We used recombinant adenovirus to infect CV1 cells with the mouse type I phosphatidylinositol phosphate 5-kinase alpha (PIP5KI), and identified the players that modulate the cytoskeleton in response to PIP(2) signaling. PIP5KI overexpression increased PIP(2) and reduced phosphatidylinositol 4 phosphate (PI4P) levels. It promoted robust stress-fiber formation in CV1 cells and blocked PDGF-induced membrane ruffling and nucleated actin assembly. Y-27632, a Rho-dependent serine/threonine protein kinase (ROCK) inhibitor, blocked stress-fiber formation and inhibited PIP(2) and PI4P synthesis in cells. However, Y-27632 had no effect on PIP(2) synthesis in lysates, although it inhibited PI4P synthesis. Thus, ROCK may regulate PIP(2) synthesis by controlling PI4P availability. PIP5KI overexpression decreased gelsolin, profilin, and capping protein binding to actin and increased that of ezrin. These changes can potentially account for the increased stress fiber and nonruffling phenotype. Our results establish the physiological role of PIP(2) in cytoskeletal regulation, clarify the relation between Rho, ROCK, and PIP(2) in the activation of stress-fiber formation, and identify the key players that modulate the actin cytoskeleton in response to PIP(2).
Development of small antenna duplexer using SAW filters for handheld phones (1993)

For smaller handheld telephones, we have developed a small antenna duplexer. This paper describes the fabrication and characteristics of our duplexer. Our package, which comprises two cavities and impedance control circuits with a strip line, has a multilayered structure. The package is made of glass-ceramic of size 7.5×8.5×2.5 mm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> . The conductor patterns of the package are made of Cu. For the SAW filter of the duplexer, we used the ladder type filter composed of one-port SAW resonators. Typical frequency response characteristics of the AMPS specification are 2.5/3.5 dB.(transmitter/receiver) insertion loss at maximum in the 25 MHz passband, and 35/29 dB stopband rejection. We also improved the filter lifetime using a three-layer Al-Cu/Cu/Al-Cu electrode film structure to 300 times the lifetime of a comparable Al-Cu single-layer filter. From the Arrhenius plot, the lifetime was estimated at more than 500000 hours at 120°C for an input power of 1 W
Faster Discovery of Neural Architectures by Searching for Paths in a Large Model (2018)

We propose Efficient Neural Architecture Search (ENAS), a faster and less expensive approach to automated model design than previous methods. In ENAS, a controller learns to discover neural network architectures by searching for an optimal path within a larger model. The controller is trained with policy gradient to select a path that maximizes the expected reward on the validation set. Meanwhile the model corresponding to the selected path is trained to minimize the cross entropy loss. On the Penn Treebank dataset, ENAS can discover a novel architecture thats achieves a test perplexity of 57.8, which is state-of-the-art among automatic model design methods on Penn Treebank. On the CIFAR-10 dataset, ENAS can design novel architectures that achieve a test error of 2.89%, close to the 2.65% achieved by standard NAS (Zoph et al., 2017). Most importantly, our experiments show that ENAS is more than 10x faster and 100x less resource-demanding than NAS.
Ultra-wide band radio: the emergence of an important new technology (2002)

Modern low power UWB (ultra wide band) signaling is the art of reusing previously allocated RF bands by hiding signals under the noise floor. Government regulators are testing UWB emissions to ensure that adequate protection exists to current users of the communications bands, and are on the brink of authorizing its use. The commercial use of UWB is distinct from the radar applications of the 1960s and 70s, and the underlying technology is distinct. Short pulse low power techniques have enabled practical through-the-wall radars, centimeter precision 3D positioning and communication capabilities at the highest spatial capacities as measured in bits/Hz/m/sup 2/.
A High Speed Detection Platform Based on Surface-Enhanced Raman Scattering for Monitoring Antibiotic-Induced Chemical Changes in Bacteria Cell Wall (2009)

Rapid and accurate diagnosis for pathogens and their antibiotic susceptibility is critical for controlling bacterial infections. Conventional methods for determining bacterium's sensitivity to antibiotic depend mostly on measuring the change of microbial proliferation in response to the drug. Such "biological assay" inevitably takes time, ranging from days for fast-growing bacteria to weeks for slow-growers. Here, a novel tool has been developed to detect the "chemical features" of bacterial cell wall that enables rapid identification of drug resistant bacteria within hours. The surface-enhanced Raman scattering (SERS) technique based on our newly developed SERS-active substrate was applied to assess the fine structures of the bacterial cell wall. The SERS profiles recorded by such a platform are sensitive and stable, that could readily reflect different bacterial cell walls found in Gram-positive, Gram-negative, or mycobacteria groups. Moreover, characteristic changes in SERS profile were noticed in the drug-sensitive bacteria at the early period (i.e., approximately 1 hr) of antibiotic exposure, which could be used to differentiate them from the drug-resistant ones. The SERS-based diagnosis could be applied to a single bacterium. The high-speed SERS detection represents a novel approach for microbial diagnostics. The single-bacterium detection capability of SERS makes possible analyses directly on clinical specimen instead of pure cultured bacteria.
Radiation tolerant VLSI circuits in standard deep submicron CMOS technologies for the LHC experiments: practical design aspects (1999)

We discuss design issues related to the extensive use of Enclosed Layout Transistors (ELT's) and guard rings in deep submicron CMOS technologies in order to improve radiation tolerance of ASIC's designed for the LHC experiments (the Large Hadron Collider at present under construction at CERN). We present novel aspects related to the use of ELT's: noise measured before and after irradiation up to 100 Mrad (SiO/sub 2/), a model to calculate the W/L ratio and matching properties of these devices. Some conclusions concerning the density and the speed of IC's conceived with this design approach are finally drawn.
Diagnosis and Treatment of Alzheimer Disease and Related Disorders (1997)

Alzheimer disease is the most common disorder causing cognitive decline in old age and exacts a substantial cost on society. Although the diagnosis of AD is often missed or delayed, it is primarily one of inclusion, not exclusion, and usually can be made using standardized clinical criteria. Most cases can be diagnosed and managed in primary care settings, yet some patients with atypical presentations, severe impairment, or complex comorbidity benefit from specialist referral. Alzheimer disease is progressive and irreversible, but pharmacologic therapies for cognitive impairment and nonpharmacologic and pharmacologic treatments for the behavioral problems associated with dementia can enhance quality of life. Psychotherapeutic intervention with family members is often indicated, as nearly half of all caregivers become depressed. Health care delivery to these patients is fragmented and inadequate, and changes in disease management models are adding stresses to the system. New approaches are needed to ensure patients' access to essential resources, and future research should aim to improve diagnostic and therapeutic effectiveness.
Small-molecule inhibitors of HIV-1 entry block receptor-induced conformational changes in the viral envelope glycoproteins (2004)

When interacting with the CD4 receptor, the HIV gp120 envelope glycoprotein undergoes conformational changes that allow binding to the chemokine receptor. Receptor binding is proposed to lead to conformational changes in the gp41 transmembrane envelope glycoprotein involving the creation and/or exposure of a coiled coil consisting of three heptad repeat (HR) sequences. The subsequent interaction of the HR2 region of gp41 with this coiled coil results in the assembly of a six-helix bundle that promotes the fusion of the viral and target cell membranes. Here we show that CD4 binding to gp120 induces the formation and/or exposure of the gp41 HR1 coiled coil in a process that does not involve gp120 shedding and that depends on the proteolytic maturation of the gp160 envelope glycoprotein precursor. Importantly, BMS-806 and related HIV-1 entry inhibitors bind gp120 and block the CD4 induction of HR1 exposure without significantly affecting CD4 binding. Moreover, these compounds do not disrupt gp120-chemokine receptor binding or the HR1-HR2 interaction within gp41. These studies thus define a receptor-induced conformational rearrangement of gp120-gp41 that is important for both CD4-dependent and CD4-independent HIV-1 entry and is susceptible to inhibition by low-molecular-weight compounds.
Regulation of immune cell function and differentiation by the NKG2D receptor (2011)

NKG2D is one of the most intensively studied immune receptors of the past decade. Its unique binding and signaling properties, expression pattern, and functions have been attracting much interest within the field due to its potent antiviral and anti-tumor properties. As an activating receptor, NKG2D is expressed on cells of the innate and adaptive immune system. It recognizes stress-induced MHC class I-like ligands and acts as a molecular sensor for cells jeopardized by viral infections or DNA damage. Although the activating functions of NKG2D have been well documented, recent analysis of NKG2D-deficient mice suggests that this receptor may have a regulatory role during NK cell development. In this review, we will revisit known aspects of NKG2D functions and present new insights in the proposed influence of this molecule on hematopoietic differentiation.
Antimalarial phenathrene amino alcohols. 1. Fluorine-containing 3- and 6-substituted 9-phenanthrenemethanols (1971)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAntimalarial phenathrene amino alcohols. 1. Fluorine-containing 3- and 6-substituted 9-phenanthrenemethanolsEdward A. Nodiff, Keiichi Tanabe, Christoph Seyfried, Shin Matsuura, Yasuaki Kondo, Eugene H. Chen, and Mahesh P. TyagiCite this: J. Med. Chem. 1971, 14, 10, 921–925Publication Date (Print):October 1, 1971Publication History Published online1 May 2002Published inissue 1 October 1971https://pubs.acs.org/doi/10.1021/jm00292a007https://doi.org/10.1021/jm00292a007research-articleACS PublicationsRequest reuse permissionsArticle Views267Altmetric-Citations32LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Multi-functional universal device using a band-engineered vertical structure (2011)

A multi-functional universal device based on a vertical channel is demonstrated as a total device solution. Four different operation modes: conventional MOSFET, steep slope FET, multi-faceted volatile memory (1T-DRAM and 1T-SRAM), and non-volatile memory are implemented in a single transistor. The steep slope FET and volatile memory are boosted by a vertically inhomogeneous doped channel for spatial energyband-engineering, and non-volatile memory capable of high performance and reliable operation is obtained via tunneling bandgap-engineering.
Bit-Interleaved LDPC-Coded Modulation with Iterative Demapping and Decoding (2009)

Bit-interleaved coded modulation (BICM) is a sub- optimal scheme from the average mutual information (AMI) point of view due to independent demapping. However, this AMI loss can be neglected for signal constellations with Gray mapping at high coding rates. AMI of amplitude-phase shift keying (APSK) constrained additive white Gaussian noise (AWGN) channel is provided in this paper, which shows that the BICM scheme has considerable loss with APSK constellations since no Gray mapping exists. Bit-interleaved low-density parity-check (LDPC) coded modulation (BILCM) is an excellent scheme and has been employed in many broadcasting and communication systems, however, such scheme also suffers from the independent demapping loss. Therefore, BILCM with iterative demapping and decoding (BILCM-ID) is proposed in this paper to overcome such loss. Simulation results show that the BILCM-ID scheme outweighs BILCM scheme by about 0.5 and 0.3 dB over AWGN channel for 32-APSK constellation at coding rates 2/3 and 4/5, respectively.
Copper‐Promoted Trifluoromethylation of Primary and Secondary Alkylboronic Acids (2012)

New couple: The Cu-promoted trifluoromethylation of primary and secondary alkylboronic acids with TMSCF(3) extends the scope of transition-metal-catalyzed trifluoromethylation reactions to sp(3)-hybridized carbon centers. It also represents one of the first examples for Cu-catalyzed C-C cross-coupling reactions of alkylboronic acid derivatives.
Immunologic Parameters in Cord Blood Indicating Early-Onset Sepsis (1996)

Different immunologic parameters were measured in cord blood to test their usefulness in the early diagnosis of early onset sepsis. Cord blood levels of circulating intercellular adhesion molecule-1 (cICAM-1), interleukin-6 (IL-6) and interleukin-8 (IL-8) were significantly elevated in septic compared to nonseptic neonates. No significant difference between either population was seen for cord blood C3a and elastase-alpha 1-proteinase inhibitor complex (E alpha 1 PI). Measured concentrations of cICAM-1, IL-6 and IL-8 in fetal and maternal blood did not correlate, indicating that the neonate's response to sepsis is clearly different from the mother. Our data suggest that cord blood measurements of cICAM-1, IL-6 and IL-8 might be useful in identifying neonates with early-onset sepsis.
Hypercupremia associated with a monoclonal immunoglobulin. (1976)

Although copper is an essential constituent of many physiologic systems, most human diseases effect minimal changes in copper homeostasis. Therefore, the association of marked hypercupremia with copper deposition in the ocular media and with a circulating immunoglobulin G in an apparently healthy woman prompted our interest. Balance and radioisotopic studies suggest a normal gastrointestinal and renal threshold for copper but a specific and tight binding between the serum copper and the anomalous protein, the probable result of a preclinical myeloma. Because the response of the hypercupremia to chelation therapy was limited, the multiple myeloma was treated with cytoxic drugs.
<title>Visual Performance And Image Coding</title> (1976)

Sample spacing and quantization levels are usually chosen for digitizing images such that the eye should not see degradations due to either process. Sample spacing is chosen based on the resolution (or high frequency) limit of the eye and quantization is based on perception of low contrast differences at lower frequencies. This process results in about 8 bit/pixel, 20 pixel/mm digitization, but, being based on two different visual limits, the total number of bits is an overestimate of the information perceived by the eye. The visual MTF can be interpreted in terms of perceptible levels as a function of spatial frequency. We show by this interpretation that the total information perceived by the eye is much less than 8 bits times the number of pixels. We consider the classic halftone as an image coding process, yielding 1 bit/ pixel. This approach indicates that halftones approximate the proper distribution of levels as a function of spatial frequency; therefore we have a possible explanation of why halftone images retain most of the visual quality of the original.
Origin and Mechanisms of Ca2+ Waves in Smooth Muscle as Revealed by Localized Photolysis of Caged Inositol 1,4,5-Trisphosphate (2004)

The cytosolic Ca(2+) concentration ([Ca(2+)](c)) controls diverse cellular events via various Ca(2+) signaling patterns; the latter are influenced by the method of cell activation. Here, in single-voltage clamped smooth muscle cells, sarcolemma depolarization generated uniform increases in [Ca(2+)](c) throughout the cell entirely by Ca(2+) influx. On the other hand, the Ca(2+) signal produced by InsP(3)-generating agonists was a propagated wave. Using localized uncaged InsP(3), the forward movement of the Ca(2+) wave arose from Ca(2+)-induced Ca(2+) release at the InsP(3) receptor (InsP(3)R) without ryanodine receptor involvement. The decline in [Ca(2+)](c) (the back of the wave) occurred from a functional compartmentalization of the store, which rendered the site of InsP(3)-mediated Ca(2+) release, and only this site, refractory to the phosphoinositide. The functional compartmentalization arose by a localized feedback deactivation of InsP(3) receptors produced by an increased [Ca(2+)](c) rather than a reduced luminal [Ca(2+)] or an increased cytoplasmic [InsP(3)]. The deactivation of the InsP(3) receptor was delayed in onset, compared with the time of the rise in [Ca(2+)](c), persisted (>30 s) even when [Ca(2+)](c) had regained resting levels, and was not prevented by kinase or phosphatase inhibitors. Thus different forms of cell activation generate distinct Ca(2+) signaling patterns in smooth muscle. Sarcolemma Ca(2+) entry increases [Ca(2+)](c) uniformly; agonists activate InsP(3)R and produce Ca(2+) waves. Waves progress by Ca(2+)-induced Ca(2+) release at InsP(3)R, and persistent Ca(2+)-dependent inhibition of InsP(3)R accounts for the decline in [Ca(2+)](c) at the back of the wave.