gebhart/patrepeval huggingface dataset:
Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT<sub>1A</sub> Receptors (1999)

The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none. Incorporation of a fluorine atom in the beta-position to the amino function in the side chain led to analogues that exhibited, in general, enhanced and long-lasting 5-HT1A agonist activity in rats after oral administration. Location of the fluorine atom at the C-4 position of the piperidine ring was the most favorable, and among the various substituents tested, the ability of the fluorine was unique in improving the oral activity of this family of ligands. Thus, the derivatives 39, 46, and 61 bound with higher affinity and selectivity to 5-HT1A receptors (versus dopaminergic D2 and adrenergic alpha1 receptors) and displayed more potent 5-HT1A agonist activity in vitro and in vivo than their C-4 desfluoro analogues. To examine the relationship between the conformation of the pharmacophore and the level of agonistic activity of this type of ligand, we synthesized a series of 3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-(H or CH3)-6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-+ ++methanone derivatives and found that the combination of a 5-methyl and a 6-methylamino substituent on the pyridine ring synergistically affected their 5-HT1A agonist properties. Thus, the 3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-methyl-6-methylamino-pyridin- 2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone 40 behaved as a more potent 5-HT1A receptor agonist in vitro and in vivo than its 5-unsubstituted analogue 38. The antidepressant potential of the lead compounds 40, 45, and 54 was examined by means of the forced swimming test (FST) in rats. The results indicated that, after a single oral administration, these compounds inhibited immobility in the FST more potently and more extensively than the clinically used antidepressant imipramine. Thus, 40, 45, and 54 are potent, orally active 5-HT1A receptor agonists with marked antidepressant potential.
Tethering Metal Ions to Photocatalyst Particulate Surfaces by Bifunctional Molecular Linkers for Efficient Hydrogen Evolution (2014)

A simple and versatile method for the preparation of photocatalyst particulates modified with effective cocatalysts is presented; the method involves the sequential soaking of photocatalyst particulates in solutions containing bifunctional organic linkers and metal ions. The modification of the particulate surfaces is a universal and reproducible method because the molecular linkers utilize strong covalent bonds, which in turn result in modified monolayer with a small but controlled quantity of metals. The photocatalysis results indicated that the CdS with likely photochemically reduced Pd and Ni, which were initially immobilized via ethanedithiol (EDT) as a linker, were highly efficient for photocatalytic hydrogen evolution from Na2S-Na2SO3-containing aqueous solutions. The method developed in this study opens a new synthesis route for the preparation of effective photocatalysts with various combinations of bifunctional linkers, metals, and photocatalyst particulate materials.
Solid‐Phase Synthesis of Sialylglycopeptides through Selective Esterification of the Sialic Acid Residues of an Asn‐Linked Complex‐Type Sialyloligosaccharide (2003)

Egg yolk provided the starting disialylundecasaccharide for a highly efficient chemoenzymatic synthesis of a biantennary complex-type glycopeptide (see picture). Repetitive protection and deprotection steps required in oligosaccharide synthesis were thus avoided, and the desired glycopeptide was rapidly assembled on a solid phase (R=peptide). Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2003/z50572_s.pdf or from the author. 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.
External dye-laser frequency stabilizer (1984)

We describe an external dye-laser frequency stabilizer that combines an acousto-optic frequency shifter with a fast electro-optic phase modulator. A compensating electronic delay line in the crossover network provides a near-ideal transducer response while keeping the voltage across the electro-optic crystal away from the amplifier limits.
Clinical Experience with PEGylated Hyaluronic Acid Fillers: A 3-year Retrospective Study (2021)

BACKGROUND: Hyaluronic acid fillers are the most used worldwide, thanks to the high biocompatibility and safety profile of HA and it is also the only substance that can be “dissolved” due to the hyaluronidase effect. AIM: A retrospective clinical evaluation of the outcomes following PEG cross-linked HA-based filler injection was performed. METHODS: Data were collected from December 2017 to June 2020. A total of 65 patients (12 M, 53 F), age ranging 28–62 year’s old (mean age 42.3), were treated. Exclusion criteria were applied and in accord to treatment plan, were used specific site injections and fillers. Follow-up was evaluated between 6 months and 2 years. RESULTS: A total of 61 treatments using 124 vials of HA filler crosslinked with PEG were performed. CONCLUSION: In conclusion, from 2014, HA fillers having PEG as cross-linker agent have been introduced in the european market. Several papers have been published in order to evaluate the features of these fillers, although, to the best of our knowledge, this is the first clinical paper regarding their use.
Compact wireless antennas using a superstrate dielectric lens (2002)

Today's vehicles have been transformed into sophisticated platforms for transmission and reception of a wide spectrum of electromagnetic waves. These include the traditional AM/FM radio, personal communication services (PCS) like cellular phone and pager systems, remote feature access (RFA) like keyless entry, navigation systems using GPS, and direct satellite radio broadcast. The transmission and reception of electromagnetic waves out of and into the vehicle is conducted through a multitude of vehicular antennas usually in the form of metallic rods protruding out of the vehicle's body. In commercial vehicles, protruding antennas impose aesthetic and mechanical problems and are exposed to vandalism. In military vehicles, they aggravate radar visibility and reduce survivability. This paper is concerned with the development of compact wireless antennas with high radiation efficiency, which offer the capability of multifunction performance on a common platform.
Oncogenic mechanism of soluble Keratin 17 offers potential therapeutic vulnerability in pancreatic cancer (2019)

CLINICAL NEED & OBJECTIVES Our group found that Keratin 17 (K17), an intermediate filament (IF), is a tumor cell‐specific marker of aggressive pancreatic ductal adenocarcinoma (PDAC), and that the detection of K17 by immunohistochemistry level is a more accurate prognostic indicator than transcriptomic subtyping. We determined that K17 can act as an oncoprotein after transitioning from its “insoluble” cytoskeleton form to a “soluble” form that can regulate cell cycle progression. In patients, mice, and PDAC cell lines, the soluble fraction of K17 exists as full length (flK17) and caspase‐cleaved peptide (ccK17), each with potentially unique tumorigenic capacity. Literature suggests that post‐translational modifications (PTMs) are necessary to regulate these and other IF dynamics, though the mechanisms behind K17 solubilization in PDAC are still unclear. Thus, our aims are to 1) determine the mechanisms regulating K17 dynamics, 2) demonstrate inhibited cell cycle progression and tumor growth following disruption of these mechanisms, and 3) verify soluble K17 as a robust negative prognostic biomarker of PDAC. METHODS & RESULTS In a PDAC tumor mouse model, we show, independent of total K17 protein amount, that the percent of soluble ccK17 in tumor cells is negatively prognostic. Work is ongoing to validate this finding in human PDAC samples. We sequenced both the soluble and cytoskeletal insoluble forms of K17 from primary PDACs using liquid chromatography mass spectrometry (LC‐MS) and identified that K17 is phosphorylated on several N‐terminal serine residues. Specifically, we reproducibly identified phosphorylation of a semi‐conserved IF motif that may promote caspase cleavage and solubilization. Ser/Thr phosphatase inhibition in vitro demonstrated that phosphorylation is necessary to trigger K17 solubilization followed by nuclear translocation. Mutagenesis of serine sites is ongoing to determine the specific motifs regulating K17. Using an unbiased kinase inhibitor screen and follow‐up pharmacologic analyses, we identified that polo‐like kinase 1 (PLK1) likely phosphorylates K17. Further studies are underway to validate K17 as a key mediator of PLK1 inhibitor sensitivity in PDAC. CONCLUSION Phosphorylation is an important regulator of K17 dynamics in PDAC, promoting solubilization and, in some cases, caspase cleavage. Our results suggest that soluble K17 may have a functional role in promoting tumor aggression. Inhibiting kinases that phosphorylate K17 could impact tumor growth by blocking K17 solubilization/cleavage and this line of research could accelerate the development of more effective treatments, coupled to soluble K17 testing as a predictive biomarker for PDAC. Support or Funding Information This work was partially supported by the 2018 Pancreatic Cancer Action Network Translational Research Grant (K.R.S.). This abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal .
High fructose syrup production using fructose-selective liquid membranes (1996)

Fructose is separated from a fructose–glucose mixture using a polymer-supported liquid membrane containing a boronic acid carrier; addition of immobilized glucose isomerase to a solution of glucose in the source compartment of a liquid membrane transport cell produces a receiving phase mixture that is more than 80% fructose.
Tensor-Tensor Products for Optimal Representation and Compression (2019)

In this era of big data, data analytics and machine learning, it is imperative to find ways to compress large data sets such that intrinsic features necessary for subsequent analysis are not lost. The traditional workhorse for data dimensionality reduction and feature extraction has been the matrix SVD, which presupposes that the data has been arranged in matrix format. Our main goal in this study is to show that high-dimensional data sets are more compressible when treated as tensors (aka multiway arrays) and compressed via tensor-SVDs under the tensor-tensor product structures in (Kilmer and Martin, 2011; Kernfeld et al., 2015). We begin by proving Eckart Young optimality results for families of tensor-SVDs under two different truncation strategies. As such optimality properties can be proven in both matrix and tensor-based algebras, a fundamental question arises: does the tensor construct subsume the matrix construct in terms of representation efficiency? The answer is yes, as shown when we prove that a tensor-tensor representation of an equal dimensional spanning space can be superior to its matrix counterpart. We then investigate how the compressed representation provided by the truncated tensor-SVD is related both theoretically and in compression performance to its closest tensor-based analogue, truncated HOSVD (De Lathauwer et al., 2000; De Lathauwer and Vandewalle, 2004), thereby showing the potential advantages of our tensor-based algorithms. Finally, we propose new tensor truncated SVD variants, namely multi-way tensor SVDs, provide further approximated representation efficiency and discuss under which conditions they are considered optimal. We conclude with a numerical study demonstrating the utility of the theory.
Microwave whispering-gallery resonator for efficient optical up-conversion (2009)

Conversion of microwave radiation into the optical range has been predicted to reach unity quantum efficiency in whispering-gallery resonators made from an optically nonlinear crystal and supporting microwave and optical modes simultaneously. In this work, we theoretically explore and experimentally demonstrate a resonator geometry that can provide the required phase matching for such a conversion at any desired frequency in the sub-THz range. We show that such a ring-shaped resonator not only allows for the phase matching but also maximizes the overlap of the interacting fields. As a result, unity-efficient conversion is expected in a resonator with feasible parameters.
Smart Programming Playgrounds (2015)

Modern IDEs contain sophisticated components for inferring missing types, correcting bad syntax and completing partial expressions in code, but they are limited to the context that is explicitly defined in a project's configuration. These tools are ill-suited for quick prototyping of incomplete code snippets, such as those found on the Web in Q&A forums or walk-through tutorials, since such code snippets often assume the availability of external dependencies and may even contain implicit references to an execution environment that provides data or compute services. We propose an architecture for smart programming playgrounds that can facilitate rapid prototyping of incomplete code snippets through a semi-automatic context resolution that involves identifying static dependencies, provisioning external resources on the cloud and injecting resource bindings to handles in the original code fragment. Such a system could be potentially useful in a range of different scenarios, from sharing code snippets on the Web to experimenting with new ideas during traditional software development.
Electronic Skin: Electronic Skin: Recent Progress and Future Prospects for Skin‐Attachable Devices for Health Monitoring, Robotics, and Prosthetics (Adv. Mater. 48/2019) (2019)

An electronic skin (e-skin) is a device that mimics the various functions of human skin, such as stretchability, self-healing, and tactile sensitivity. This is a rapidly advancing field, with applications in skin-attachable devices for health monitoring, prosthetics, and robotics. In article number 1904765, recent progress in the e-skin field is reviewed by Zhenan Bao, Steve Park, and co-workers, with a focus on these three applications.
Focus: Querying Large Video Datasets with Low Latency and Low Cost (2018)

Large volumes of videos are continuously recorded from cameras deployed for traffic control and surveillance with the goal of answering "after the fact" queries: identify video frames with objects of certain classes (cars, bags) from many days of recorded video. While advancements in convolutional neural networks (CNNs) have enabled answering such queries with high accuracy, they are too expensive and slow. We build Focus, a system for low-latency and low-cost querying on large video datasets. Focus uses cheap ingestion techniques to index the videos by the objects occurring in them. At ingest-time, it uses compression and video-specific specialization of CNNs. Focus handles the lower accuracy of the cheap CNNs by judiciously leveraging expensive CNNs at query-time. To reduce query time latency, we cluster similar objects and hence avoid redundant processing. Using experiments on video streams from traffic, surveillance and news channels, we see that Focus uses 58X fewer GPU cycles than running expensive ingest processors and is 37X faster than processing all the video at query time.
T cell engineering as therapy for cancer and HIV: our synthetic future (2015)

It is now well established that the immune system can control and eliminate cancer cells. Adoptive T cell transfer has the potential to overcome the significant limitations associated with vaccine-based strategies in patients who are often immune compromised. Application of the emerging discipline of synthetic biology to cancer, which combines elements of genetic engineering and molecular biology to create new biological structures with enhanced functionalities, is the subject of this overview. Various chimeric antigen receptor designs, manufacturing processes and study populations, among other variables, have been tested and reported in recent clinical trials. Many questions remain in the field of engineered T cells, but the encouraging response rates pave a wide road for future investigation into fields as diverse as cancer and chronic infections.
Nail Polish Try-On: Realtime Semantic Segmentation of Small Objects for Native and Browser Smartphone AR Applications (2019)

We provide a system for semantic segmentation of small objects that enables nail polish try-on AR applications to run client-side in realtime in native and web mobile applications. By adjusting input resolution and neural network depth, our model design enables a smooth trade-off of performance and runtime, with the highest performance setting achieving~\num{94.5} mIoU at 29.8ms runtime in native applications on an iPad Pro. We also provide a postprocessing and rendering algorithm for nail polish try-on, which integrates with our semantic segmentation and fingernail base-tip direction predictions.
AutoCaption: Automatic caption generation for personal photos (2014)

AutoCaption is a system that helps a smartphone user generate a caption for their photos. It operates by uploading the photo to a cloud service where a number of parallel modules are applied to recognize a variety of entities and relations. The outputs of the modules are combined to generate a large set of candidate captions, which are returned to the phone. The phone client includes a convenient user interface that allows users to select their favorite caption, reorder, add, or delete words to obtain the grammatical style they prefer. The user can also select from multiple candidates returned by the recognition modules.
Differential Genetic Associations for Systemic Lupus Erythematosus Based on Anti–dsDNA Autoantibody Production (2011)

Systemic lupus erythematosus (SLE) is a clinically heterogeneous, systemic autoimmune disease characterized by autoantibody formation. Previously published genome-wide association studies (GWAS) have investigated SLE as a single phenotype. Therefore, we conducted a GWAS to identify genetic factors associated with anti-dsDNA autoantibody production, a SLE-related autoantibody with diagnostic and clinical importance. Using two independent datasets, over 400,000 single nucleotide polymorphisms (SNPs) were studied in a total of 1,717 SLE cases and 4,813 healthy controls. Anti-dsDNA autoantibody positive (anti-dsDNA +, n = 811) and anti-dsDNA autoantibody negative (anti-dsDNA -, n = 906) SLE cases were compared to healthy controls and to each other to identify SNPs associated specifically with these SLE subtypes. SNPs in the previously identified SLE susceptibility loci STAT4, IRF5, ITGAM, and the major histocompatibility complex were strongly associated with anti-dsDNA + SLE. Far fewer and weaker associations were observed for anti-dsDNA - SLE. For example, rs7574865 in STAT4 had an OR for anti-dsDNA + SLE of 1.77 (95% CI 1.57-1.99, p = 2.0E-20) compared to an OR for anti-dsDNA - SLE of 1.26 (95% CI 1.12-1.41, p = 2.4E-04), with p(heterogeneity)<0.0005. SNPs in the SLE susceptibility loci BANK1, KIAA1542, and UBE2L3 showed evidence of association with anti-dsDNA + SLE and were not associated with anti-dsDNA - SLE. In conclusion, we identified differential genetic associations with SLE based on anti-dsDNA autoantibody production. Many previously identified SLE susceptibility loci may confer disease risk through their role in autoantibody production and be more accurately described as autoantibody propensity loci. Lack of strong SNP associations may suggest that other types of genetic variation or non-genetic factors such as environmental exposures have a greater impact on susceptibility to anti-dsDNA - SLE.
Cloning and characterization of the bovine myostatin promoter (2000)

Myostatin a TGF beta superfamily member has been shown to be present in high levels in the myogenic precursor cells of dermomyotome and in the adult muscle fiber. To identify cis-acting DNA elements involved in myostatin gene expression, we have isolated and sequenced several kilobases of the bovine myostatin promoter region. Sequence analysis of the 1.6 kb immediate upstream region of bovine myostatin revealed several muscle specific transcription factor binding sites such as E-boxes and an MEF2 binding site in this region.
Exploring the effects of cell seeding density on the differentiation of human pluripotent stem cells to brain microvascular endothelial cells (2015)

Brain microvascular-like endothelial cells (BMECs) derived from human pluripotent stem cells (hPSCs) have significant promise as tools for drug screening and studying the structure and function of the BBB in health and disease. The density of hPSCs is a key factor in regulating cell fate and yield during differentiation. Prior reports of hPSC differentiation to BMECs have seeded hPSCs in aggregates, leading to non-uniform cell densities that may result in differentiation heterogeneity. Here we report a singularized-cell seeding approach compatible with hPSC-derived BMEC differentiation protocols and evaluate the effects of initial hPSC seeding density on the subsequent differentiation, yield, and blood–brain barrier (BBB) phenotype. A range of densities of hPSCs was seeded and differentiated, with the resultant endothelial cell yield quantified via VE-cadherin flow cytometry. Barrier phenotype of purified hPSC-derived BMECs was measured via transendothelial electrical resistance (TEER), and purification protocols were subsequently optimized to maximize TEER. Expression of characteristic vascular markers, tight junction proteins, and transporters was confirmed by immunocytochemistry and quantified by flow cytometry. P-glycoprotein and MRP-family transporter activity was assessed by intracellular accumulation assay. The initial hPSC seeding density of approximately 30,000 cells/cm2 served to maximize the yield of VE-cadherin+ BMECs per input hPSC. BMECs displayed the highest TEER (>2,000 Ω × cm2) within this same range of initial seeding densities, although optimization of the BMEC purification method could minimize the seeding density dependence for some lines. Localization and expression levels of tight junction proteins as well as efflux transporter activity were largely independent of hPSC seeding density. Finally, the utility of the singularized-cell seeding approach was demonstrated by scaling the differentiation and purification process down from 6-well to 96-well culture without impacting BBB phenotype. Given the yield and barrier dependence on initial seeding density, the singularized-cell seeding approach reported here should enhance the reproducibility and scalability of hPSC-derived BBB models, particularly for the application to new pluripotent stem cell lines.