gebhart/patrepeval huggingface dataset:
Synthesis and high content cell-based profiling of simplified analogues of the microtubule stabilizer (+)-discodermolide. (2002)

(+)-Discodermolide, a C24:4, trihydroxylated, octamethyl, carbamate-bearing fatty acid lactone originally isolated from a Caribbean sponge, has proven to be the most potent of the microtubule-stabilizing agents. Recent studies suggest that it or its analogues may have advantages over other classes of microtubule-stabilizing agents. (+)-Discodermolide's complex molecular architecture has made structure-activity relationship analysis in this class of compounds a formidable task. The goal of this study was to prepare simplified analogues of (+)-discodermolide and to analyze their biological activities to expand structure-activity relationships. A small library of analogues was prepared wherein the (+)-discodermolide methyl groups at C-14 and C-16 and the C-7 hydroxyl were removed, and the lactone was replaced by simple esters. The library components were analyzed for microtubule-stabilizing actions in vitro, antiproliferative activity against a small panel of human carcinoma cells, and cell signaling, microtubule architecture and mitotic spindle alterations by a multiparameter fluorescence cell-based screening technique. The results show that even drastic structural simplification can lead to analogues with actions related to microtubule targeting and signal transduction, but that these subtle effects were illuminated only through the high information content cell-based screen.
Detection of T790M, the Acquired Resistance EGFR Mutation, by Tumor Biopsy versus Noninvasive Blood-Based Analyses (2015)

Discordant genotypes between tumor biopsy and blood-based analyses may result from technological differences, as well as sampling different tumor cell populations. The use of complementary approaches may provide the most complete assessment of each patient's cancer, which should be validated in predicting response to T790M-targeted inhibitors.
Intraductal Injection for Localized Drug Delivery to the Mouse Mammary Gland (2013)

Herein we describe a protocol to deliver various reagents to the mouse mammary gland via intraductal injections. Localized drug delivery and knock-down of genes within the mammary epithelium has been difficult to achieve due to the lack of appropriate targeting molecules that are independent of developmental stages such as pregnancy and lactation. Herein, we describe a technique for localized delivery of reagents to the mammary gland at any stage in adulthood via intraductal injection into the nipples of mice. The injections can be performed on live mice, under anesthesia, and allow for a non-invasive and localized drug delivery to the mammary gland. Furthermore, the injections can be repeated over several months without damaging the nipple. Vital dyes such as Evans Blue are very helpful to learn the technique. Upon intraductal injection of the blue dye, the entire ductal tree becomes visible to the eye. Furthermore, fluorescently labeled reagents also allow for visualization and distribution within the mammary gland. This technique is adaptable for a variety of compounds including siRNA, chemotherapeutic agents, and small molecules.
PlasmaSources & Sensors ofNearTerahertz Radiation (2005)

Sandia National Labs, POBox5800, MSJ153, Albuquerque, NewMexico 87185-1153 jvrudd@,sandia.gov Abstract: Terahertz radiation fromoptically-induced plasmas onmetal, semiconductor, and dielectric surfaces iscompared toelectron-hole plasma radiation fromGaAsandGe. Electro- optic sampling andelectric-field probes measure radiated field waveforms anddistributions to 0.350 THz. ©2005 Optical Society ofAmerica OCIScodes: (190.71 10)Ultrafast nonlinear optics; (320.2250) Femtosecond phenomena
Characteristics of diffusion in Al-Mg alloys with ultrafine grain sizes (2002)

Abstract Equal-channel angular pressing (ECAP) was used to refine the grain sizes of pure Al and an Al-3 wt% Mg alloy containing minor additions of either Sc or Zr. Following ECAP, the grain sizes were in the ultrafine submicrometre range. Diffusion couples were prepared from the fine-grained material produced by ECAP and from the coarse-grained material without ECAP and these couples were used to measure the interdiffusion coefficients for Mg in an Al lattice. The results show the interdiffusion coefficient is larger in the fine-grained material and the experimental data from this couple agree with predictions from molecular dynamic simulations using the embedded-atom method. An activation energy of about 87 kJ mol−1 is estimated for grain-boundary diffusion of Mg in Al where this value is consistent with the expectations from measurements of the activation energy for lattice diffusion of Mg in Al. There is no evidence for enhanced diffusion in the boundaries produced by ECAP due, it is suggested, to the rapid equilibration of these non-equilibrium boundaries at elevated temperatures.
Preparation and Characterization of Human Rheumatoid Arthritic Synovial Fluid Phospholipase A2 Produced by Recombinant Baculovirus-Infected Insect Cells (1994)

We prepared human rheumatoid arthritic synovial fluid phospholipase A2 (PLA2) [EC 3.1.1.4] from insect cells infected with a recombinant baculovirus. The PLA2 DNA was designed, changing the original codons to those used frequently in the polyhedrin gene. Sixteen oligo-deoxynucleotides ranging from 40 to 70 nucleotides were chemically synthesized and then assembled to form the whole PLA2 gene. The gene thus synthesized was then placed under the control of the polyhedrin promoter of Autographa californica nuclear polyhedrosis virus. The recombinant virus was infected into Spodoptera frugiperda cells. The infected cells secreted protein having PLA2 activity into the culture medium. The enzyme level in the medium reached about 3 mg/liter on day 4 after infection. The secreted protein was purified to a single band of 14,000 Da on SDS-PAGE, by means of cation exchange chromatography and reverse-phase HPLC. N-terminal amino acid sequence analysis revealed that the recombinant protein was recognized and cleaved at the signal sequence in the insect cell. The purified enzyme had almost the same specific enzyme activity, substrate specificity, pH optimum, Ca2+ ion dependency, and kinetic values as those of the natural enzyme.
Estudio clínico comparativo de 15 años de la tasa de supervivencia acumulativa de muñones colados y muñeones de resina, cementados con cemento de resina adhesiva (2011)

Objetivo:el objetivo de este estudio fue comparar las tasas de supervivencia de los munones (TSM) colados y de resina cementados con cemento de resina adhesiva, asi como determinar los factores de riesgo del fracaso de los munones.Materiales y metodos:se incluyeron 991 pacientes (2.124 munones) que recibieron munones colados o de resina, fijados con cemento de resina adhesiva en la Fixed Prosthodontic Clinic of Okayama University Dental Hospital entre abril de 1988 y diciembre de 1991 y cuyo registro estructurado de munones clinicos estaba adecuadamente cumplimentado. El registro de los munones clinicos incluia informacion sobre la edad del paciente, su sexo, el tipo de restauracion, la localizacion del diente, el tipo de diente, la dentina coronal restante y la forma del canal radicular. Las TSM, asi como las causas del fracaso, se analizaron 15 anos postinsercion. Como en 381 pacientes faltaban los datos en cuanto a los factores de prediccion del fracaso del munon, se utilizo una submuestra de 610 pacientes (1.053 munones) para el posterior analisis de los factores de riesgo. Resultados:la TSM acumulativa de los munones de reisna (78, 7%) fue significativamente superior que la de los munones colados (55, 4%; test de log-rank, Pmenor que 0, 0001). La prueba del riesgo proporcional de Cox revelo que el sexo (varones, P menor que 0, 0001), la ausencia de dentina coronal residual (P=0, 0057), el tipo de munon (colado, P=0, 0186) y la edad mas avanzada en el momento de la insercion del nucleo (P=0, 0380) constituyeron factores de prediccion significativos para el fracaso del munon. La incidencia de complicaciones, como el aflojamiento del munon (P=0, 0016) y la extraccion dentaria (P menor que0, 0001) fueron significativamente mayores en los munones metalicos.Conclusiones: los munones colados se asociaron a una TSM significativamente mas baja que los munones de resina y los factores de riesgo significativos para el fracaso del munon fueron el sexo (masculino), la ausencia de dentina coronal residual, el tipo de restauracion del munon (metal fundido) y edad mas avanzada en el momento de la insercion del munon.
Pharmacokinetics of single doses of digoxin administered intravenously to ducks, roosters, and turkeys (1990)

A single dose of digoxin was injected, IV, into 5 mature male turkeys (0.066 mg/kg of body weight), 8 male ducks (0.066 mg/kg), and 6 roosters (0.33 mg/kg). Twenty-three serial venous blood samples were collected before (baseline) and after the administration of digoxin to turkeys, ducks, and roosters. Plasma concentrations of digoxin were determined in duplicate by a radioimmunoassay that was validated for avian species. The plasma concentrations were best fitted by a 3 (turkeys, ducks)- and 2 (roosters)-compartment open model, with first-order elimination from the central compartment. Significant (P less than 0.05) kinetic differences were determined among species. Mean half-life (t1/2) for ducks, roosters, and turkeys were 8.30 +/- 2.70 (mean +/- SD), 6.67 +/- 3.50, and 23.7 +/- 4.8 hours, respectively. The volume of distribution at steady state (Vss) was 14.7 +/- 2.9, 3.13 +/- 0.49, and 2.27 +/- 0.36 L/kg, and total body clearance (CL) of drug was 1.54 +/- 0.43, 0.461 +/- 0.187, and 0.136 +/- 0.022 L/h/kg for ducks, roosters, and turkeys, respectively. The mean residence time was 10.3 +/- 3.9, 8.37 +/- 4.97, and 16.8 +/- 2.2 hours, respectively. Volume of distribution at steady state and CL in ducks were several fold higher than that in turkeys. The terminal half-life of digoxin determined for ducks and roosters in this study was considerably shorter than those previously reported for several mammalian species.
Nitric-oxide generating hydrogels inhibit intimal thickening and promote endothelial cell proliferation (2003)

Nitric oxide-generating hydrogels have been shown to inhibit smooth muscle cell proliferation and platelet adhesion, as well as promote endothelial cell proliferation; for this reason these hydrogels should be useful in preventing restenosis, or vessel re-occlusion, following balloon angioplasty. Over 600,000 percutaneous transluminal coronary angioplasty (PTCA) procedures are performed annually in the U.S.; unfortunately. 30-40% of patients treated with PTCA experience failure due to restenosis. We have developed nitric oxide (NO)-generating hydrogels that release NO over a period of days to weeks, depending on material design. They are able to significantly reduce platelet adhesion to collagen and inhibit smooth muscle cell proliferation in vitro. In addition, we have covalently grafted a cell adhesion peptide into the NO-generating hdrogels and assessed the ability of endothelial cells (EC) to proliferate on the surface. ECs owed significantly higher rates of proliferation on the NO-generating hydrogels as compared to controls. The perivascular application of NO-generating, hydrogels significantly reduced neointimal formation in an experimental balloon angioplasty model as compared to controls. The combined effects of these NO-generating hydrogels make them well suited for incorporation into blood-contacting devices and for use as a stent coating or stent replacement to prevent restenosis following balloon angioplasty.
Letter: corticosteroid use alongside tofacitinib in OCTAVE Open. Authors' reply (2020)

LINKED CONTENT This article is linked to Sands et al and Peng et al papers. To view these articles, visit https://doi.org/10.1111/apt.15555 and https://doi.org/10.1111/apt.15674 .
A combined electromagnetic and thermal optimisation of an aerospace electric motor (2010)

An innovative design strategy has been set up which is capable of optimising both the electromagnetic as well as the thermal design of permanent magnet synchronous machines (PMSM) for aerospace actuation systems. This has been achieved by linking up the electromagnetic design process and motor housing design process for an overall minimum mass. A validation process was initially performed on a PMSM to ensure the correct functionality of the thermal model. Tests were carried out to calibrate the model with experimental data. This paper further describes the adopted optimisation procedure of a 12.75Nm - 2000rpm, horizontally mounted, 12 slot 14 pole Aerospace Permanent Magnet Synchronous motor and highlights the significant weight and volume saving capabilities.
Multicore EDFA for Space Division Multiplexing by Utilizing Cladding-pumped Technology (2013)

Get PDF Email Share Share with Facebook Tweet This Post on reddit Share with LinkedIn Add to CiteULike Add to Mendeley Add to BibSonomy Get Citation Copy Citation Text Y. Tsuchida, H. Matsuura, M. Tadakuma, and R. Sugizaki, "Multicore EDFA for Space Division Multiplexing by Utilizing Cladding-pumped Technology," in Asia Communications and Photonics Conference 2013, OSA Technical Digest (online) (Optica Publishing Group, 2013), paper AF1D.6. Export Citation BibTex Endnote (RIS) HTML Plain Text Citation alert Save article
Bio-inspired UAV routing, source localization, and acoustic signature classification for persistent surveillance (2011)

A team consisting of Teledyne Scientific Company, the University of California at Santa Barbara and the Army Research Laboratory* is developing technologies in support of automated data exfiltration from heterogeneous battlefield sensor networks to enhance situational awareness for dismounts and command echelons. Unmanned aerial vehicles (UAV) provide an effective means to autonomously collect data from a sparse network of unattended ground sensors (UGSs) that cannot communicate with each other. UAVs are used to reduce the system reaction time by generating autonomous collection routes that are data-driven. Bio-inspired techniques for search provide a novel strategy to detect, capture and fuse data. A fast and accurate method has been developed to localize an event by fusing data from a sparse number of UGSs. This technique uses a bio-inspired algorithm based on chemotaxis or the motion of bacteria seeking nutrients in their environment. A unique acoustic event classification algorithm was also developed based on using swarm optimization. Additional studies addressed the problem of routing multiple UAVs, optimally placing sensors in the field and locating the source of gunfire at helicopters. A field test was conducted in November of 2009 at Camp Roberts, CA. The field test results showed that a system controlled by bio-inspired software algorithms can autonomously detect and locate the source of an acoustic event with very high accuracy and visually verify the event. In nine independent test runs of a UAV, the system autonomously located the position of an explosion nine times with an average accuracy of 3 meters. The time required to perform source localization using the UAV was on the order of a few minutes based on UAV flight times. In June 2011, additional field tests of the system will be performed and will include multiple acoustic events, optimal sensor placement based on acoustic phenomenology and the use of the International Technology Alliance (ITA) Sensor Network Fabric (IBM).
Targeted Drug Delivery in Covalent Organic Nanosheets (CONs) via Sequential Postsynthetic Modification (2017)

Covalent organic nanosheets (CONs) have emerged as a new class of functional two-dimensional (2D) porous organic polymeric materials with a high accessible surface, diverse functionality, and chemical stability. They could become versatile candidates for targeted drug delivery. Despite their many advantages, there are limitations to their use for target specific drug delivery. We anticipated that these drawbacks could be overturned by judicious postsynthetic modification steps to use CONs for targeted drug delivery. The postsynthetic modification would not only produce the desired functionality, it would also help to exfoliate to CONs as well. In order to meet this requirement, we have developed a facile, salt-mediated synthesis of covalent organic frameworks (COFs) in the presence of p-toluenesulfonic acid (PTSA). The COFs were subjected to sequential postsynthetic modifications to yield functionalized targeted CONs for targeted delivery of 5-fluorouracil to breast cancer cells. This postsynthetic modification resulted in simultaneous chemical delamination and functionalization to targeted CONs. Targeted CONs showed sustained release of the drug to the cancer cells through receptor-mediated endocytosis, which led to cancer cell death via apoptosis. Considering the easy and facile COF synthesis, functionality based postsynthetic modifications, and chemical delamination to CONs for potential advantageous targeted drug delivery, this process can have a significant impact in biomedical applications.
Dynamic memory management methodology applied to embedded telecom network systems (2002)

Presents a new methodology for dynamic memory management of embedded telecom network systems. This methodology enables the designer to further raise the abstraction level of the initial system specification and to achieve optimized embedded system designs. This methodology is well suited for systems characterized by a set of concurrent and dynamic processes, very high-bit-rate data streams, and intensive data transfer and storage, as encountered in telecom network applications. Up to now, it has been successfully applied to four telecom network systems. This methodology can be easily integrated into any C++-based system synthesis approach that bridges the gap between a concurrent process-level system specification and an optimized (for area, performance, or power) embedded implementation of communicating hardware/software processors. This is in contrast to current system design practice, where VHDL/C is derived without room for exploration, refinement, and verification, leading to expensive late design iterations. In this paper, the main focus lies on the system-level specification model and the dynamic memory management applied to two real-life telecom network systems.
Prediction of a Ligand‐Binding Niche within a Human Olfactory Receptor by Combining Site‐Directed Mutagenesis with Dynamic Homology Modeling (2011)

Reprogramming a smell receptor: The ligand-binding niche within a three-dimensional model of a human olfactory receptor has been predicted by dynamic homology modeling and confirmed experimentally by functional studies of site-directed receptor mutants. Even a proposed reprogramming of the receptor's binding and activation properties was experimentally confirmed. Detailed facts of importance to specialist readers are published as "Supporting Information". Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
ChemInform Abstract: A General, Enantioselective Synthesis of β‐ and γ‐Fluoroamines. (2013)

Abstract An efficient enantioselective conversion of different aldehydes (I) to β‐fluoro alcohols is developed as well as conversion of these products to enantioenriched β‐ and γ‐fluoroamines.
A local roughness measure for 3D meshes and its application to visual masking (2009)

3D models are subject to a wide variety of processing operations such as compression, simplification or watermarking, which may introduce some geometric artifacts on the shape. The main issue is to maximize the compression/simplification ratio or the watermark strength while minimizing these visual degradations. However few algorithms exploit the human visual system to hide these degradations, while perceptual attributes could be quite relevant for this task. Particularly, the masking effect defines the fact that one visual pattern can hide the visibility of another. In this context we introduce an algorithm for estimating the roughness of a 3D mesh, as a local measure of geometric noise on the surface. Indeed, a textured (or rough ) region is able to hide geometric distortions much better than a smooth one. Our measure is based on curvature analysis on local windows of the mesh and is independent of the resolution/connectivity of the object. The accuracy and the robustness of our measure, together with its relevance regarding visual masking have been demonstrated through extensive comparisons with state-of-the-art and subjective experiment. Two applications are also presented, in which the roughness is used to lead (and improve) respectively compression and watermarking algorithms.
Comparison of a novel 450-nm laser with Ho:YAG (2100 nm), Tm fiber (1940 nm), and KTP (532 nm) lasers for soft-tissue ablation (2018)

Three lasers were directly compared, including the Ho:YAG laser (&lambda; = 2100 nm), Tm fiber laser (&lambda; = 1940 nm) operating in 3 different modes (CW, regular pulse, and super pulse), and blue diode laser (&lambda; = 442 nm) for vaporization and coagulation efficiency for treating blood-rich soft tissues, ex vivo, in a porcine kidney model at quasi-contact cutting in water. In addition, experimental results were compared with published data on performance of KTP laser (&lambda; = 532 nm) at similar experimental settings (Power = 60 W and cutting speed = 2 mm/s). Tm fiber laser in pulsed mode and blue laser produced highest vaporization rates of 3.7 and 3.4 mm<sup>3</sup>/s, respectively. Tm fiber laser (in both CW and pulsed modes) also produced the largest coagulation zone among the laser sources tested. A carbonization zone was observed for Tm fiber laser in CW and pulsed modes, as well as for the blue diode laser. Tm fiber laser in super-pulse mode and Ho:YAG laser both resulted in irregular coagulation zones without carbonization. Comparison with known data for KTP laser revealed that tissue effects of the blue laser are similar to that of the KTP laser. These results suggest that the combination of the two lasers (Tm fiber and blue diode) in one system may achieve high cutting efficiency and optimal coagulation for hemostasis during surgical treatment. Ex vivo testing of the combined system revealed feasibility of this approach. The combination of the CW Tm fiber laser (120W) and the blue diode laser (60W) emitting through a combination tip were compared with CW 120 W Tm fiber laser alone and 120 W Ho:YAG laser. Vaporization rates measured 34, 28, and 6 mm<sup>3</sup>/s, and coagulation zones measured 0.6, 1.3, and 1.7 mm, respectively. A carbonization zone was only observed with CW Tm fiber laser. The vaporization rate of combined CW Tm fiber laser / blue diode laser was comparable to published data for KTP laser for equivalent total power. Thus, high-power blue diode laser, Tm fiber laser, and their combination may provide an alternative to conventional Ho:YAG and KTP lasers for applications in urology and other surgical fields.