gebhart/patrepeval huggingface dataset:
Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity (2009)

Several 3-acylindoles with high affinity for the CB(2) cannabinoid receptor and selectivity over the CB(1) receptor have been prepared. A variety of 3-acyl substituents were investigated, and the tetramethylcyclopropyl group was found to lead to high affinity CB(2) agonists (5, 16). Substitution at the N1-indole position was then examined. A series of aminoalkylindoles was prepared and several substituted aminoethyl derivatives were active (23-27, 5) at the CB(2) receptor. A study of N1 nonaromatic side chain variants provided potent agonists at the CB(2) receptor (16, 35-41, 44-47, 49-54, and 57-58). Several polar side chains (alcohols, oxazolidinone) were well-tolerated for CB(2) receptor activity (41, 50), while others (amide, acid) led to weaker or inactive compounds (55 and 56). N1 aromatic side chains also afforded several high affinity CB(2) receptor agonists (61, 63, 65, and 69) but were generally less potent in an in vitro CB(2) functional assay than were nonaromatic side chain analogues.
Table S2 from First-in-Human Study of Utomilumab, a 4-1BB/CD137 Agonist, in Combination with Rituximab in Patients with Follicular and Other CD20<sup>+</sup> Non-Hodgkin Lymphomas (2023)

&lt;p&gt;Pharmacokinetic parameters for utomilumab in combination with rituximab (Cycle 1)&lt;/p&gt;
ON THE INFLUENCE OF THE SHAPE OF ANODE VOLTAGE PULSE ON THE OPERATION STABILITY OF SPATIAL- HARMONIC MAGNETRON WITH COLD SECONDARY-EMISSION CATHODE (2018)

One of the main problems faced by developers of modulators for spatial-harmonic magnetrons with the cold secondary-emission cathode is the selection of the correct shape of an anode voltage pulse that will ensure the stable operation of the magnetron. In this paper, the effect of a shape of the anode voltage pulse on the operation of transmitters based on magnetrons with cold secondary-emission cathodes is investigated. It was experimentally studied the influence of different parts of the pulse on such magnetron's parameters as a start cathode current required for stable excitation of cold cathode secondary emission, the stability of operation on the selected mode, and the generation of the maximum power. It is shown that the magnitude of the initial cathode current is primarily determined by the wavefront steepness. Its optimum value is usually about 150 kV/μs. In this case, starting cathode should provide a current of only a few tens of milliamperes, which can significantly increase the device lifetime. The article also shows that the presence of a pulse spike at the beginning of a voltage pulse promotes the premature transition to a non-operable mode. As a result, this leads to a decrease in the output power of the magnetron. The duration of the decay determines the ability of the magnetron to operate at short pulse duration. For very short pulses, the energy expended on the microwave generation can be equal to the energy expended on the formation of the pulse decay. As a result, it was concluded that the usage of spatial-harmonic magnetrons with cold cathode requires a careful refinement of the characteristics of a pulse modulator. The steepness of the front of its output pulse should be about 150 kV/μs and the pulse spike at the beginning of voltage pulse should be as low as possible. When operating at very short pulses it is necessary to provide a longer rate of pulse decay.
Synthesis of the Aziridinomitosene Skeleton by Intramolecular Michael Addition:  α-Lithioaziridines and Nonaromatic Substrates (2004)

The bicyclic pyrrole ketone 16 has been prepared by using an oxaza-Claisen rearrangement, followed by nitrogen deprotection. Coupling with the stannylaziridine mesylate 15a or nosylate 15b affords 17. Conversion to 40 provides a substrate for generation of an α-lithioaziridine 41 by tin lithium exchange. An intramolecular Michael addition pathway for 41 has been demonstrated by the isolation of 46 in 20% yield under conditions where the intermediate enolate 43 is trapped by selenenylation, but competing proton transfer gives 42. The synthetic potential of the process is limited by stability problems at the stage of the enolate 43 or the protonated product 44.
Ligand binding by PDZ domains (2012)

The postsynaptic density protein-95/disks large/zonula occludens-1 (PDZ) protein domain family is one of the most common protein-protein interaction modules in mammalian cells, with paralogs present in several hundred human proteins. PDZ domains are found in most cell types, but neuronal proteins, for example, are particularly rich in these domains. The general function of PDZ domains is to bring proteins together within the appropriate cellular compartment, thereby facilitating scaffolding, signaling, and trafficking events. The many functions of PDZ domains under normal physiological as well as pathological conditions have been reviewed recently. In this review, we focus on the molecular details of how PDZ domains bind their protein ligands and their potential as drug targets in this context.
Why Do We Need 6G? (2021)

The study and design of 5G seems to have reached its end and 5G communication systems are currently under deployment. In parallel, 5G standardization is as Release 16, which is going to complete the definition and the design guidelines of the 5G radio access network. Because of that, the interest of the scientific and industrial communities has already started focusing on the future 6G communication networks. The preliminary definition of future technology trends towards 2030, given by major standardization bodies, and the flagship 6G projects worldwide have started proposing various visions about what 6G will be. Side by side, various scientific articles, addressing the initial characterisation of 6G, have also been published. However, considering the promises of 5G, can 6G represent a significant technological advancement to justify a so‑called new generation? In fact, now, 5G softwarized networks may just imply continuous network software upgrades (as it happens for the Internet) instead of new generations every ten years. This article starts describing the main characteristics that made 5G a breakthrough in telecommunications, also briefly introducing the network virtualisation and computing paradigms that have reformed telecommunications. Next, by providing rigorous definition of the terminology and a survey of the principal 6G visions proposed, the paper tries to establish important motivations and characteristics that can really justify the need for and the novelty of future 6G communication networks.
Depressive vulnerability is not an independent risk factor for osteoporosis in postmenopausal women (1999)

Major depression has been repeatedly but not consistently reported to be associated with low bone mineral density (BMD) and to an increased risk for fracture in women. We have investigated, in healthy postmenopausal women, whether depressive symptomatology, assessed by the General Health Questionnaire (GHQ), was associated to a significant decrease in BMD, hence supporting the hypothesis of an independent pathogenetic link between the two disorders. We investigated 121 postmenopausal women, aged 48-77 years, spontaneously attending a screening visit for osteoporosis in an outpatient facility. BMD of the spine and the non-dominant hip (total and neck areas) were measured by Dual Energy X-Ray absorptiometry. All subjects completed to the 'General Health Questionnaire' translated and validated in French. No significant correlations were observed between the GHQ score and BMD of the spine (P = 0.54), the total hip area (P = 0.65), or the femoral neck area (P = 0.65). No differences in terms of spinal or femoral BMD were observed between women with GHQ score < 5 or > or = 5. When comparing values of BMD between women within the upper and the lower quartiles for GHQ score, no difference was observed for spine (P = 0.69), total hip (P = 0.80), or femoral neck (P = 0.93). Similarly, GHQ scores were not significantly different when comparing women in the upper and lower quartiles of BMD distribution at the spine or the hip. In conclusion, notwithstanding the clinical pattern of postmenopausal osteoporosis can lead to depression and, on the other hand, hormonal and behavioral disturbances reported in depression might be enhancing factors for accelerated bone loss, our present results do not support the hypothesis that otherwise healthy postmenopausal women with increased depressive complaints are also more prone to exhibit osteoporotic fractures.
Enhanced oxygen storage capacity of cerium oxides in cerium dioxide/lanthanum sesquioxide/alumina containing precious metals (1990)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTEnhanced oxygen storage capacity of cerium oxides in cerium dioxide/lanthanum sesquioxide/alumina containing precious metalsTakeshi. Miki, Takao. Ogawa, Masaaki. Haneda, Noriyoshi. Kakuta, Akifumi. Ueno, Syuji. Tateishi, Shinji. Matsuura, and Masayasu. SatoCite this: J. Phys. Chem. 1990, 94, 16, 6464–6467Publication Date (Print):August 1, 1990Publication History Published online1 May 2002Published inissue 1 August 1990https://pubs.acs.org/doi/10.1021/j100379a056https://doi.org/10.1021/j100379a056research-articleACS PublicationsRequest reuse permissionsArticle Views1081Altmetric-Citations194LEARN 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 options Get e-Alerts
Data from Expression Profiling of Archival Tumors for Long-term Health Studies (2023)

&lt;div&gt;Abstract&lt;p&gt;&lt;b&gt;Purpose:&lt;/b&gt; More than 20 million archival tissue samples are stored annually in the United States as formalin-fixed, paraffin-embedded (FFPE) blocks, but RNA degradation during fixation and storage has prevented their use for transcriptional profiling. New and highly sensitive assays for whole-transcriptome microarray analysis of FFPE tissues are now available, but resulting data include noise and variability for which previous expression array methods are inadequate.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Experimental Design:&lt;/b&gt; We present the two largest whole-genome expression studies from FFPE tissues to date, comprising 1,003 colorectal cancer (CRC) and 168 breast cancer samples, combined with a meta-analysis of 14 new and published FFPE microarray datasets. We develop and validate quality control (QC) methods through technical replication, independent samples, comparison to results from fresh-frozen tissue, and recovery of expected associations between gene expression and protein abundance.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Results:&lt;/b&gt; Archival tissues from large, multicenter studies showed a much wider range of transcriptional data quality relative to smaller or frozen tissue studies and required stringent QC for subsequent analysis. We developed novel methods for such QC of archival tissue expression profiles based on sample dynamic range and per-study median profile. This enabled validated identification of gene signatures of microsatellite instability and additional features of CRC, and improved recovery of associations between gene expression and protein abundance of MLH1, FASN, CDX2, MGMT, and SIRT1 in CRC tumors.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Conclusions:&lt;/b&gt; These methods for large-scale QC of FFPE expression profiles enable study of the cancer transcriptome in relation to extensive clinicopathological information, tumor molecular biomarkers, and long-term lifestyle and outcome data. &lt;i&gt;Clin Cancer Res; 18(22); 6136–46. ©2012 AACR&lt;/i&gt;.&lt;/p&gt;&lt;/div&gt;
Molecular Sieves with Encapsulated TiO 2 Clusters: Materials for the Optical Sensing of Reductive Gas Atmospheres (2000)

The reversible redox behavior of intrazeolitic titanium dioxide clusters in reducing and oxidizing atmospheres (H2, CO, O2) is studied by in-situ diffuse reflectance UV/Vis spectroscopy. Clusters of the oxides with only one or up to about ten Ti oxide units have been stabilized in the pores of molecular sieves by chemical vapor deposition (cvd) and subsequent calcination. The nuclearity of the different clusters can be deduced from the blue-shifts of absorption edges in diffuse reflectance UV/Vis spectra and from the behavior towards reduction to TiIII. The response time of hosted mononuclear TiIV Ox species for the registration of H2 is shortened by a factor of about 10 in comparison to bulk TiO2. Changes in the ratio in CO:air mixtures can be monitored with short delay.
Abstract 5348: Single-cell analysis of mutational heterogeneity in acute myeloid leukemia tumors with high-throughput droplet microfluidics (2018)

Abstract To make possible the routine characterization of genetic diversity within cancer cell populations, we developed a novel two-step microfluidic droplet workflow that enables efficient and massively-parallel single-cell PCR-based genomic barcoding for single-cell DNA sequencing applications. We demonstrate that the two-step microfluidic approach is required for robust DNA amplification on thousands of individual cells per run with high coverage uniformity and low allelic dropout of targeted genomic loci. To apply our single-cell sequencing technology to human tumor samples, we developed a targeted panel to partially sequence 26 genes frequently mutated in acute myeloid leukemia (AML) including TP53, DNMT3A, FLT3, NPM1, NRAS, IDH1 and IDH2. Using this panel, we were able to sensitively identify SNV and indel-defined clones within AML samples and assess their distribution at the time of diagnosis, remission and relapse. We also used single cell SNVs to monitor host and donor cell populations during bone marrow transplantation (BMT), which allowed us to accurately evaluate engraftment and disease relapse. Collectively, our single-cell data indicates that clonal populations inferred from VAFs obtained from bulk sequencing data may not fully resolve the heterogeneity within tumors; moreover, the single-cell nature of our approach enabled the unambiguous identification of multiple co-occurring mutations within subclones that is not possible with bulk measurements. Collectively, our results show a greater degree of heterogeneity in AML tumor samples than is commonly appreciated with traditional sequencing paradigms and demonstrate the value of single-cell analysis for AML. Citation Format: Dennis J. Eastburn, Maurizio Pellegrino, Adam Sciambi, Sebastian Treusch, Liwen Xu, Robert Durruthy-Durruthy, Kaustubh Gokhale, Jose Jacob, Tina X. Chen, William Oldham, Jairo Matthews, Hagop Kantarjian, Andrew Futreal, Keyur Patel, Keith W. Jones, James L. Zehnder, Koichi Takahashi. Single-cell analysis of mutational heterogeneity in acute myeloid leukemia tumors with high-throughput droplet microfluidics [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 5348.
Transcellular activation of the human immunodeficiency virus type 1 long terminal repeat in T lymphocytes requires CD4-gp120 binding (1992)

Cells expressing human immunodeficiency virus type 1 (HIV-1) tat can transactivate the HIV-1 long terminal repeat (LTR) in cocultured T lymphocytes. In this report, we describe the molecular requirements for transcellular activation of the LTR in Jurkat cells. An analysis with deletion mutants and blocking antibodies demonstrated a requirement for env expression in addition to tat expression for transcellular activation to occur. The results suggest that the transient association of CD4 and gp120 in cocultured cells is required for tat-mediated transcellular activation. The events that follow CD4-gp120 binding in transactivation, however, do not require the gp120-neutralizing domain, in contrast to HIV-mediated fusion and infection. The consequences of this interaction on cellular function are currently under investigation.
Computer analysis of lighting style in fine art: steps towards inter-artist studies (2011)

Stylometry in visual art-the mathematical description of artists' styles - has been based on a number of properties of works, such as color, brush stroke shape, visual texture, and measures of contours' curvatures. We introduce the concept of quantitative measures of lighting, such as statistical descriptions of spatial coherence, diuseness, and so forth, as properties of artistic style. Some artists of the high Renaissance, such as Leonardo, worked from nature and strove to render illumination "faithfully" photorealists, such as Richard Estes, worked from photographs and duplicated the "physics based" lighting accurately. As such, each had dierent motivations, methodologies, stagings, and "accuracies" in rendering lighting clues. Perceptual studies show that observers are poor judges of properties of lighting in photographs such as consistency (and thus by extension in paintings as well); computer methods such as rigorous cast-shadow analysis, occluding-contour analysis and spherical harmonic based estimation of light fields can be quite accurate. For this reasons, computer lighting analysis can provide a new tools for art historical studies. We review lighting analysis in paintings such as Vermeer's Girl with a pearl earring, de la Tour's Christ in the carpenter's studio, Caravaggio's Magdalen with the smoking flame and Calling of St. Matthew) and extend our corpus to works where lighting coherence is of interest to art historians, such as Caravaggio's Adoration of the Shepherds or Nativity (1609) in the Capuchin church of Santa Maria degli Angeli. Our measure of lighting coherence may help reveal the working methods of some artists and in diachronic studies of individual artists. We speculate on artists and art historical questions that may ultimately profit from future renements to these new computational tools.
Supplementary Figures 1 - 3 from Reducing CD73 Expression by IL1β-Programmed Th17 Cells Improves Immunotherapeutic Control of Tumors (2023)

&lt;p&gt;Supplementary Figure 1: Differential cytolytic potential and activation of Th17IL-1β cells in culture. Supplementary figure 2: Ectonucleotidase expression and persistence of different Th17 cells. Supplementary figure 3: Schematic summary highlighting the effect of different Th17 programming conditions on anti-tumor function.&lt;/p&gt;
High velocity lamb waves in LiTaO3 thin plate for high frequency filters (2016)

First anti-symmetric (A <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> ) mode Lamb wave propagating in a LiTaO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> thin plate at an Euler angle around (0°, 45°, 0°) has a high velocity. Both phase velocity and electromechanical coupling factor have been evaluated at different propagation angles (0°, 45°, ψ°). A <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> mode Lamb wave at (0°, 45°, 0°) offers the highest velocity and largest electromechanical coupling factor, thus proving suitable for high frequency devices. Leaky Lamb waves' velocities have been measured for A <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> and zero-th symmetric (S <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ) modes at different propagation angles by ultrasonic microscopy and are almost similar to the calculated Lamb wave velocities. Whereas Ai mode Lamb wave response has been evaluated at (0°, 42°, 0°), (0°, 42°, 45°) and (0°, 42°, 90°) using a network analyzer. The influence of Al-interdigital transducers' (IDT) thickness on the reflection coefficient has been evaluated for thin (0°, 39°, 0°) LiTaO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> . An IDT's thickness larger than 0.03λ (λ is the wavelength) is needed to fabricate A <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> mode Lamb wave resonators.
HYPERTHERMIE WÄHREND DER HÄMODIALYSEBEHANDLUNG - MODELLBASIERTE ANALYSE DER PATHOPHYSIOLOGIE (2000)

Article HYPERTHERMIE WÄHREND DER HÄMODIALYSEBEHANDLUNG - MODELLBASIERTE ANALYSE DER PATHOPHYSIOLOGIE was published on January 1, 2000 in the journal Biomedical Engineering / Biomedizinische Technik (volume 45, issue s1).
Provisioning Schemes Accounting for ROADM Add/Drop Constraints in GMPLS-based WSON (2011)

Provisioning schemes exploiting the recently introduced GMPLS extensions for add/drop in WSONs are proposed to effectively handle different ROADM structures and provide a preference on the utilization of add/drop resources with limited flexibility.
Microstructure of ionic liquid (EAN)-rich and oil-rich microemulsions studied by SANS (2018)

In a previous study we investigated the phase behavior of microemulsions consisting of the ionic liquid ethylammonium nitrate (EAN), an n-alkane and a nonionic alkyl polyglycolether (CiEj). We found the same general trends as for the aqueous counterparts, i.e. a transition from an oil-in-EAN microemulsion via a bicontinuous microemulsion to an EAN-in-oil microemulsion with increasing temperature. However, unlike what happens in the corresponding aqueous systems, in EAN-in-oil microemulsions only a very small amount of EAN was detected by NMR-measurements. This is why we investigated the phase behavior and microstructure of EAN-rich n-dodecane-in-EAN microemulsions and oil-rich EAN-in-n-octane microemulsions. We found that the ionic liquid emulsification failure boundary has an extraordinarily small slope, which suggests that the amphiphilic film loses its ability to solubilize EAN with an increase in temperature by only a few degrees. The analysis of the small angle neutron scattering (SANS) curves unambiguously shows that this behavior is due to the fact that the EAN molecules form a substructure with a characteristic length scale of Λ ≈ 8 Å inside the EAN-in-oil droplets. In more detail, the analysis of the SANS data with the GIFT method revealed a transition from spherical to cylindrical structures approaching the respective critical endpoint temperatures. By using the respective form factors and combining them with a Gaussian spatial intensity distribution to account for the EAN sub-structure we were able to describe the scattering curves nearly quantitatively.