gebhart/patrepeval huggingface dataset:
Heterocyclic Amides as Kinase Inhibitors (2018)

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTHeterocyclic Amides as Kinase InhibitorsRobert B. Kargbo*Robert B. KargboUsona Institute, 277 Granada Drive, San Luis Obispo, California 93401-7337, United States*E-mail: [email protected]More by Robert B. Kargbohttp://orcid.org/0000-0002-5539-6343Cite this: ACS Med. Chem. Lett. 2018, 9, 12, 1160–1161Publication Date (Web):November 12, 2018Publication History Received3 November 2018Published online12 November 2018Published inissue 13 December 2018https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00528https://doi.org/10.1021/acsmedchemlett.8b00528editorialACS PublicationsCopyright © 2018 American Chemical Society. This publication is available under these Terms of Use. Request reuse permissions This publication is free to access through this site. Learn MoreArticle Views1940Altmetric-Citations-LEARN 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 PDF (397 KB) Get e-AlertscloseSUBJECTS:Apoptosis,Assays,Inflammation,Peptides and proteins,Receptors Get e-Alerts
Effects of a new conjugate drug in a rat model of postmenopausal osteoporosis (2013)

Searchable abstracts of presentations at key conferences on calcified tissues ISSN 2052-1219 (online)
Short-circuit Ring Technics of High Power Asynchronous Traction Motor (2006)

The welding technics of high power asyn- chronous traction motor short-circuit rings is introduced.
Myocardial Fibrosis and Cardiac Decompensation in Aortic Stenosis (2016)

CMR detects ventricular decompensation in aortic stenosis through the identification of myocardial extracellular expansion and replacement fibrosis. This holds major promise in tracking myocardial health in valve disease and for optimizing the timing of valve replacement. (The Role of Myocardial Fibrosis in Patients With Aortic Stenosis; NCT01755936).
Measuring Tempo, Rhythm, Timing, and the Torques that Generate Power in the Golf Swing (2010)

This paper summarizes two previously published technical papers describing what can be learned from measuring the motion of the golf club using two accelerometers. The sensors are mounted at different points along the shaft of the golf club, both sensitive to acceleration along the axis of the shaft. Two distinct signals are resolved. The first signal scales as club speed, which can be used to understand details of tempo, rhythm, and timing. The second measures the acceleration of the hands, which reveals the torques that generate power in the golf swing. A comparative study of twenty-five golfers shows that club speed is generated in the downswing as a two step process. The first phase starts at the top of the swing and involves impulsive acceleration of the hands and club. This is followed by a second phase, the release, where the club is accelerated while the hands decelerate.
An efficient adaptive algorithm for edge detection based on the likelihood ratio test (2002)

Abstract The edge detection problem in blurred and noisy 2‐D signals is dealt with. An adaptive signal processing algorithm is proposed which marks edge points according to an hypothesis test which compares the likelihoods of two models describing the local signal behaviour in the two cases of absence/presence of an edge. The two models are identified by a regularized least squares estimation algorithm, obtaining a numerically efficient procedure, quite robust with respect to additive noise and blurr perturbation. No global thresholding or data prefiltering is required. Copyright © 2002 John Wiley &amp; Sons, Ltd.
Big data and artificial intelligence in healthcare: Ethical and social implications of neonatology (2021)

Summary form only given, as follows. The complete presentation was not made available for publication as part of the conference proceedings. High-speed physiological data are proving to be one of the most untapped resources in healthcare today. Many medical devices produce data streams at frequencies of a reading a second or faster making the effective use of that data a Big Data challenge. A growing body of research studies are demonstrating common physiological patterns for a range of medical conditions at earlier stages in the condition progression paving the way for new artificial intelligence and machine learning based approaches that could also be more reliable. There is great potential for real-time assessment of this physiological data to improve patient outcomes and to do so on an individualized personalized level. Systemic use of Big Data and AI in Healthcare present many ethics and social implications. This keynote will demonstrate how Big Data and AI can be used systemically for new approaches in research and clinical care for differential diagnosis and condition management. Ethical and social implications will be considered within the context of the application of these approaches in neonatology.
New Inorganic-Based Drug Delivery System of Indole-3-Acetic Acid-Layered Metal Hydroxide Nanohybrids with Controlled Release Rate (2007)

We have developed new inorganic-based drug delivery systems through the hybridization of indole-3-acetic acid (IAA) and layered metal hydroxide such as zinc basic hydroxide salt (ZBS) and zinc aluminum layered double hydroxide (ZALDH). A coprecipitation method as well as an ion-exchange route is found to be commonly effective in synthesizing both IAA-ZBS and IAA-ZALDH nanohybrids, in which the tilted bilayers of IAA are stabilized in the interlayer space of layered metal hydroxide lattice. According to the FT-IR spectroscopic analyses, IAA molecules interact more strongly with the ZBS lattice than the ZALDH one, which is due to the formation of coordination bonds between carboxyl groups of the guest species and coordinatively unsaturated Zn(OH)3 units of the host ZBS lattice. Such an interaction gives rise to a slower release of the IAA molecules from the ZBS-based nanohybrid than from the ZALDH-based one. The present results underscore that the layered hydroxydouble salt like ZBS makes it possible to design and develop new efficient drug-delivery systems with the suspended release of guest molecules.
Synthesis of L‐Indospicine. (2002)

Abstract For Abstract see ChemInform Abstract in Full Text.
Bone resorptive activity of side-chain fluoro derivatives of 25-hydroxy- and 1 alpha,25-dihydroxyvitamin D3 in culture. (1981)

Three side-chain fluorinated analogues of vitamin D3 were tested for their bone-resorbing activity on fetal rat forelimb bones in vitro. Two fluoro derivatives of 25-hydroxyvitamin D3 (25-OH-D3), 24,24-difluoro-25-hydroxyvitamin D3 and 25-hydroxy-26,26,26,27,27,27-hexafluorovitamin D3, were compared with 25-OH-D3. The difluoro compound was approximately 7 times more potent than 25-OH-D3, and the hexafluoro analogue was approximately 40 times more potent than 25-OH-D3 in this system. In contrast, the 24,24-difluoro analogue of lα,25-dihydroxyvitamin D3 (lα,25-(OH)2D3) was slightly less potent than lα,25-(OH)2D3. The results indicate that the presence of fluoride groups on carbon atoms immediately adjacent to the 25-hydroxyl group enhances the in vitro bone-resorbing effects of 25-hydroxyvitamin D3. On the other hand, fluorination of the lα-hydroxylated compound on position 24 actually diminished rather than increased bone-resorptive activity.
The quality of nursing care of the frail aged in selected institutions in Eastern Cape and Natal (1990)

An investigation was undertaken to establish standards for the care of the frail aged and to develop an instrument to measure this care. In this process the care in 12 institutions was monitored. In general, the care was found to be of good quality, with an average of 74.3%, but there are residences where the percentage is up to 10% lower. The influence of some internal and external factors on the quality of care were investigated.
Diet and Leukocyte Telomere Length in a Population with Extended Longevity: The Costa Rican Longevity and Healthy Aging Study (CRELES) (2021)

Elderly Costa Ricans have lower mortality rates compared to their counterparts from developed countries. Reasons for this survival advantage are not completely known. In the present study, we aimed to identify dietary factors associated with leukocyte telomere length (LTL), a marker of biologic aging, in the elderly population of Costa Rica. We conducted prospective analysis in 909 participants aged 60+ years from the Costa Rican Longevity and Healthy Aging Study (CRELES). We used a food frequency questionnaire to assess usual diet. We calculated dietary patterns using Principal Component Analysis (PCA). We used generalized linear models to examine the association of dietary patterns and food groups with leukocyte telomere length. We found two major dietary patterns explaining 9.15% and 7.18% of the total variation of food intake, respectively. The first dietary pattern, which represents a traditional Costa Rican rice and beans pattern, was more frequent in rural parts of the country and was positively associated with baseline LTL: β (95% CI) = 42.0 base-pairs (bp) (9.9 bp, 74.1 bp) per one-unit increase of the traditional dietary pattern. In analysis of individual food groups, intake of grains was positively associated with baseline LTL: β (95% CI) = 43.6 bp (13.9 bp, 73.3 bp) per one-serving/day increase of consumption of grains. Our results suggest that dietary factors, in particular a traditional food pattern, are associated with telomere length and may contribute to the extended longevity of elderly Costa Ricans.
Viability states of bacteria—Specific mechanisms of selected probes (2010)

Single cell techniques like flow cytometry combined with viability staining can help to obtain information on viability states of bacteria. Many fluorescent dyes are available for this purpose and can be chosen according to the available excitation source, the species used, and the background of scientific questions and relevant specifications. Within this short overview, we focus on two diverse groups of bacteria: the gram- Escherichia coli and representatives of the gram+ Mycobacterium to demonstrate differences and similarities in dye uptake principles, processing and binding. We call for attention to possible diverse responses of different species to various viability assays. The cell surface structure of bacteria and the chemical properties of fluorescent probes considerably determine the success of a certain staining practice. Particular focus was drawn on analysis of membrane integrity, uptake of substrates and transformation of fluorogenic substrates.
Designer Magnetism in High Entropy Oxides (2021)

Disorder can have a dominating influence on correlated and quantum materials leading to novel behaviors which have no clean limit counterparts. In magnetic systems, spin and exchange disorder can provide access to quantum criticality, frustration, and spin dynamics, but broad tunability of these responses and a deeper understanding of strong limit disorder is lacking. In this work, we demonstrate that high entropy oxides present an unexplored route to designing quantum materials in which the presence of strong local compositional disorder hosted on a positionally ordered lattice can be used to generate highly tunable emergent magnetic behavior--from macroscopically ordered states to frustration-driven dynamic spin interactions. Single crystal La(Cr0.2Mn0.2Fe0.2Co0.2Ni0.2)O3 films are used as a structurally uniform model system hosting a magnetic sublattice with massive microstate disorder in the form of site-to-site spin and exchange type inhomogeneity. A classical Heisenberg model is found to be sufficient to describe how compositionally disordered systems can paradoxically host long-range magnetic uniformity and demonstrates that balancing the populating elements based on their discrete quantum parameters can be used to give continuous control over ordering types and critical temperatures. Theory-guided experiments show that composite exchange values derived from the complex mix of microstate interactions can be used to design the required compositional parameters for a desired response. These predicted materials are synthesized and found to possess an incipient quantum critical point when magnetic ordering types are designed to be in direct competition; this leads to highly controllable exchange bias sensitivity in the monolithic single crystal films previously accessible only in intentionally designed bilayer heterojunctions.
Higher TNF-Alpha Production Detected in Colorectal Cancer Patients Monocytes (2012)

Many studies have shown that TNF-α is critically involved in tumor promotion and progression. We examined the ability of monocytes from patients with colorectal cancer in different stages of the disease to produce TNF-α after stimulation and the involvement of JNK signal transduction pathway in TNF-α synthesis. Purification of monocytes was done by plastic adherence of PBMC. Monocytes were stimulated with LPS or C3bgp. The involvement of JNK MAP kinase in TNF-α secretion was evaluated by using selective JNK inhibitor SP600125. The quantity determination of TNF-α was performed by ELISA in culture supernatants on 24 h. Monocytes from patients produced significantly higher level of TNF-α in response to LPS stimulation in comparison with monocytes isolated from healthy donors (1926±690 pg/ml vs. 1465±771 pg/ml; p=0.034). Moreover, we observed that LPS-stimulated TNF-α production increased in stage-dependent manner; because monocytes from patients with advanced cancer secreted significantly more TNF-α than monocytes from patients in early stage of the disease (2298±127 pg/ml vs. 1687±780 pg/ml; p=0.041). Inhibition of JNK MAPK led to significant suppression of TNF-α production in both healthy individuals and patients with colorectal cancer. However, even after inhibition of JNK, monocytes from patients produced a greater quantity TNF-α, compared with monocytes from healthy donors. We conclude that monocytes from patients with colorectal cancer are prone to produce higher levels of TNF-α after stimulation and this production is disease stage dependent.
Consideration of operating frequency variation in a constant-on-time synchronous Buck converter (2013)

A constant on-time PWM control with input feed-forward results in ultra-fast transient response while maintaining relatively constant switching frequency over the entire input voltage range. However, in practical design case, the operating frequency is changed by various load conditions. In this paper, variation of the switching frequency in a constant on-time Buck converter was analyzed in details. Experimental results were proposed to verify the characteristics.
Executive Functions and Pilot Characteristics Predict Flight Simulator Performance in General Aviation Pilots (2011)

In general aviation, 85% of the crashes seem to be caused by pilots' errors (Li, Baker, Grabowski, & Rebok, 2001 Li, G., Baker, S., Grabowski, J. and Rebok, G. 2001. Factors associated with pilot error in aviation crashes. Aviation, Space, and Environmental Medicine, 72: 52[PubMed], [Web of Science ®] , [Google Scholar]) and 46% of the crashes occur at airports (Li & Baker, 1999 Li, G. and Baker, S. 1999. Correlates of pilot fatality in general aviation crashes. Aviation, Space, and Environmental Medicine, 70: 305[PubMed], [Web of Science ®] , [Google Scholar]). It is important to determine if the same factors influence the flying performance and the landing decision making and to uncover which factors, among the pilot's cognitive status, personality traits, and experience, are the most predictive. We examined in 24 general aviation pilots the relationship between those factors and the flying performance and weather-related decision-making relevance. The cognitive assessment encompassed the three basic executive functions (Miyake et al., 2000 Miyake, A., Friedman, N. P., Emerson, M. J., Witzki, A. H., Howerter, A. and Wager, T. D. 2000. The unity and diversity of executive functions and their contributions to complex “frontal lobe” tasks: A latent variable analysis. Cognitive Psychology, 41(1): 49–100. [Crossref], [PubMed], [Web of Science ®] , [Google Scholar]), reasoning, and psychomotor velocity. The personal characteristics were age, flight experience, and level of impulsivity. Reasoning, updating in working memory, and flight experience were predictive of the flight performance. In addition, updating in working memory, flight experience, and level of impulsivity were linked with weather-related decision-making relevance.
Granzyme M Mediates a Novel Form of Perforin-dependent Cell Death (2004)

Cell death is mediated by cytotoxic lymphocytes through various granule serine proteases released with perforin. The unique protease activity, restricted expression, and distinct gene locus of granzyme M suggested this enzyme might have a novel biological function or trigger a novel form of cell death. Herein, we demonstrate that in the presence of perforin, the protease activity of granzyme M rapidly and effectively induces target cell death. In contrast to granzyme B, cell death induced by granzyme M does not feature obvious DNA fragmentation, occurs independently of caspases, caspase activation, and perturbation of mitochondria and is not inhibited by overexpression of Bcl-2. These data raise the likelihood that granzyme M represents a third major and specialized perforin-dependent cell death pathway that plays a significant role in death mediated by NK cells.
Effects of n-3 fatty acids on cartilage metabolism (2006)

An abstract is not available for this content. As you have access to this content, full HTML content is provided on this page. A PDF of this content is also available in through the ‘Save PDF’ action button.
Better than real: Complex-valued neural nets for MRI fingerprinting (2017)

The task of MRI fingerprinting is to identify tissue parameters from complex-valued MRI signals. The prevalent approach is dictionary based, where a test MRI signal is compared to stored MRI signals with known tissue parameters and the most similar signals and tissue parameters retrieved. Such an approach does not scale with the number of parameters and is rather slow when the tissue parameter space is large. Our first novel contribution is to use deep learning as an efficient nonlinear inverse mapping approach. We generate synthetic (tissue, MRI) data from an MRI simulator, and use them to train a deep net to map the MRI signal to the tissue parameters directly. Our second novel contribution is to develop a complex-valued neural network with new cardioid activation functions. Our results demonstrate that complex-valued neural nets could be much more accurate than real-valued neural nets at complex-valued MRI fingerprinting.
Spinning-disk self-referencing interferometry of antigen–antibody recognition (2004)

A gold ridge microstructure fabricated to a height of lambda/8 on a high-reflectivity substrate behaves as a wave-front-splitting self-referencing interferometer in phase quadrature when illuminated by a Gaussian laser beam and observed in the far field along the optic axis. When immuno-gammaglobulin (IgG) antibodies are selectively immobilized on the gold microstructure, they recognize and bind to a specific antigen, which shifts the relative optical phase of the interferometer and modifies the far-field diffracted intensity. We detect bound antigen interferometrically on spinning disks at a sampling rate of 100 kHz and verify the interferometric nature of the signal by using two quadratures of opposite sign to rule out effects of dynamic light scattering. Strong molecular recognition is demonstrated by the absence of binding to nontarget molecules but strong signal change in response to a specific antigen. This BioCD has the potential to be applied as a spinning-disk interferometric immunoassay and biosensor.
A process for asynchronous software inspection (2002)

Although there exists a multitude of different inspection processes, the basis process has remained unchanged since it was first defined by Fagan in 1976. The process has as its central component an inspection meeting which all participants attend. But is this meeting cost effective? Recent work suggests this is not the case. An inspection model that dispenses totally with the need for the inspectors to be in the same place at the same time is presented. It replaces the meeting with further individual inspections combined with asynchronous communication between inspectors. A prototype tool has been developed that supports the asynchronous model. In contrast to a previously developed asynchronous inspection tool, it uses electronic mail as the basis for communication and the reasons for this approach are discussed. The inspection model is evaluated in comparison with the traditional, meeting-oriented approach on a number of criteria. An initial attempt was made to gain quantitive data by carrying out a small-scale experiment, but whilst encouraging results being obtained, the number of subjects was too low for any significant conclusions to be drawn. Larger scale experiments are planned for the future to obtain more data.
Greatly Enhanced Fluorescence by Increasing the Structural Rigidity of an Imine: Enantioselective Recognition of 1,2‐Cyclohexanediamine by a Chiral Aldehyde (2016)

An aldehyde that is not fluorescent responsive toward a chiral diamine has been converted to a sensitive fluorescence enhancement sensor through incorporation of an additional hydrogen bonding unit to increase the structural rigidity of the reaction product of the aldehyde with the diamine. This new chiral aldehyde is synthesized in one step from the reaction of (S)-3-formylBINOL with salicyl chloride. When treated with trans-1,2-cyclohexanediamine in ethanol, it shows greatly enhanced fluorescence at λ=410 nm with good enantioselectivity. NMR and mass spectroscopic methods are used to investigate the reaction of the chiral aldehyde with the diamine. This study has revealed a two-stage reaction mechanism including a fast imine formation and a slow ester cleavage.