gebhart/patrepeval huggingface dataset:
The Hydrolysis of Carboxylic Acid Ester Prodrugs (2003)

This chapter contains sections titled: Introduction Prodrugs of Active Carboxylic Acids That Incorporate a Simple or Functionalized Alkyl Pro-Moiety Prodrugs That Incorporate a Simple Alkyl Pro-Moiety Ethyl Ester Other Alkyl Esters Prodrugs That Incorporate an Oxyalkyl, Hydroxyalkyl, or Arylalkyl Pro-Moiety Carboxylic Acid Esters That Incorporate a Carbamoylmethyl, Aminoalkyl, or Amidoalkyl Pro-Moiety Carbamoylmethyl Esters Aminoalkyl Esters Amidoalkyl Esters Quantitative Structure–Metabolism Relationships in Prodrug Design Carboxylic Acid Esters of Acylglycerols and Bis(acyl-amino)propan-2-ols Hybrid Triglycerides Hybrid Pseudolipid Analogues Prodrugs of Active Carboxylic Acids That Incorporate Fragmentable Pro-Moiety Glycolic Acid Esters Prodrugs That Incorporate an (Acyloxy)alkyl or [(Alkoxycarbonyl)oxy]methyl Pro-Moiety (Acyloxy)alkyl Esters [(Alkoxycarbonyl)oxy]methyl Esters Prodrugs That Incorporate an Amidomethyl, an Aminomethyl, or Another Fragmentable Pro-Moiety That Contains an Amino Group Prodrugs That Incorporate an (Oxodioxolyl)methyl Pro-Moiety Prodrugs of Active Carboxylic Acids Esterified with a Phenol or Hydroxylamine Carboxylic Acid Esters of Phenols Carboxylic Acid Esters of Hydroxylamines Prodrugs of Active Alcohols and Phenols Prodrugs That Incorporate an Alkanoyl Pro-Moiety Acetic Acid Esters Unbranched Alkanoic Acid Esters Branched Alkanoic Acid Esters Cycloalkanoic Acid Esters Reactions of Intramolecular Acyl Transfer Prodrugs That Incorporate an Aromatic Acyl Pro-Moiety Prodrugs That Incorporate an Oxygenated Alkanoyl Pro-Moiety Prodrugs That Incorporate an Amino Acyl Pro-Moiety Esters of a-Amino Acids Esters of Other Amino Acids Prodrugs That Incorporate a Fragmentable Acyl Pro-Moiety O-[(Acyloxy)methyl] Derivatives Alkoxycarbonyl Derivatives Carbamic Acid Esters Cyclization-Activated Carboxylic Acid Ester Prodrugs Nucleophilic Attack by a Basic Group Intramolecular Attack by an Anionic N-Atom Intramolecular Attack by a Carboxylate Group Intramolecular Attack by a Hydroxy Group Prodrugs That Incorporate a 1,4-Dihydropyridine Pro-Pro-Moiety Lactones as Prodrugs Prodrugs of Active Amines and Amides Alkyl and Aryl Carbamates (Acyloxy)methyl Carbamates N-[(Acyloxy)methyl] Derivatives Cleavage of the N-(Hydroxymethyl) Intermediate Simple N-[(Acyloxy)methyl] Derivatives Complex N-[(Acyloxy)methyl] Derivatives Cyclization-Activated Double Prodrugs of Amines and Peptides Special Cases Macromolecular Prodrugs
How Thermodynamics Drives Wet-out in Adhesive Bonding: Correcting Common Misconceptions (2008)

The traditional maxim that one should keep the adhesive surface energy below that of the substrate to ensure wet-out is shown to be a false and often counter-productive constraint in designing superior adhesive bonds. The confusion stems from the failure to carefully distinguish the one-substrate problem (coating) from the two-substrate problem (adhesive bonding). When two substrates are bonded the adhesive will almost invariably be driven to wet them out, even if the adhesive is of much higher surface energy than the substrates. The driving force is the elimination of the condensed phase/air interfaces in favor of condensed phase/condensed phase interfaces. Experiments are conducted to demonstrate that high surface energy liquids and adhesives will easily wet low surface energy substrates when sandwiched between them. The standard mathematical formalism for the free energy change of coating, bonding liquid adhesives, and bonding PSA tapes is developed to clarify the thermodynamic distinctions between these very different processes. It is shown that for spontaneous, thermodynamically driven, wet-out the contact angle the adhesive must make with the substrate is <90° for a liquid adhesive and <180° for a pressure sensitive adhesive (PSA) tape. These forgiving criteria are readily met in practice, and are far less stringent than the 0° contact angle required for spontaneous spreading in a coating process.
Transient dynamics during two-wave mixing in photorefractive quantum well diodes using moving gratings (1998)

The temporal dynamics of photorefractive and absorptive gains during two-wave mixing in Stark geometry photorefractive quantum wells are investigated using moving gratings to break the symmetry of the photorefractive diodes to achieve nonreciprocal energy transfer between two coherent laser beams.
Implant-protected occlusion. (1994)

Implant-Protected Occlusion is that occlusal scheme which reduces the forces at the crestal bone/implant interface. Biomechanical principles form the basis of this concept. The direction of force, force magnification, and implant position relative to arch or location are blended together for a consistent approach to implant reconstruction. The direction of force demonstrates that angled forces increase the type of forces, alter their point of application, and reduce bone strength. Force magnifiers include cantilevers, offset loads, and monumental forces to the implant body. These magnifiers dramatically increase the among of force applied to a prosthesis. The implant position relative to arch or arch position often determines the density of bone and the amount of force. Adequate surface area of implant bodies considers width, length, and number. The surface area is a primary component in the resistance of force factors. In addition occlusal table width and occlusal contacts contribute to the force amount type and direction and may be modified to reduce crestal loads.
Sparsification and Separation of Deep Learning Layers for Constrained Resource Inference on Wearables (2016)

Deep learning has revolutionized the way sensor data are analyzed and interpreted. The accuracy gains these approaches offer make them attractive for the next generation of mobile, wearable and embedded sensory applications. However, state-of-the-art deep learning algorithms typically require a significant amount of device and processor resources, even just for the inference stages that are used to discriminate high-level classes from low-level data. The limited availability of memory, computation, and energy on mobile and embedded platforms thus pose a significant challenge to the adoption of these powerful learning techniques. In this paper, we propose SparseSep, a new approach that leverages the sparsification of fully connected layers and separation of convolutional kernels to reduce the resource requirements of popular deep learning algorithms. As a result, SparseSep allows large-scale DNNs and CNNs to run efficiently on mobile and embedded hardware with only minimal impact on inference accuracy. We experiment using SparseSep across a variety of common processors such as the Qualcomm Snapdragon 400, ARM Cortex M0 and M3, and Nvidia Tegra K1, and show that it allows inference for various deep models to execute more efficiently; for example, on average requiring 11.3 times less memory and running 13.3 times faster on these representative platforms.
A novel chemical, STF-083010, reverses tamoxifen-related drug resistance in breast cancer by inhibiting IRE1/XBP1 (2015)

Recent studies show that the unfolded protein response (UPR) within the endoplasmic reticulum is correlated with breast cancer drug resistance. In particular, human X-box binding protein-1(XBP1), a transcription factor which participates in UPR stress signaling, is reported to correlate with poor clinical responsiveness to tamoxifen. In this study, we develop a tamoxifen-resistant MCF-7 cell line by treating the cell line with low concentration of tamoxifen, and we find that XBP1 is indeed up-regulated at both the mRNA and protein levels compared to normal MCF-7 cells. STF-083010, a novel inhibitor which specifically blocks the XBP1 splicing, reestablishes tamoxifen sensitivity to resistant MCF-7 cells. Moreover, co-treatment with STF-083010 and tamoxifen can significantly delay breast cancer progression in a xenograft mammary tumor model. We next investigate the expression of XBP1s in over 170 breast cancer patients' samples and the results demonstrate that XBP1s expression level is highly correlated with overall survival in the ER+ subgroup, but not in the ER- subgroup, suggesting a potential therapeutic application of XBP1 inhibitors in ER+breast cancer treatment.
Surface characteristics of human articular cartilage--a scanning electron microscope study. (1971)

SUMMARY The articular surfaces of human femoral and acetabular cartilages have been studiedusing the scanningelectron microscope.Surface depressions found on articular cartilage specimens are shown to bedue to the collapse ofthe surface layer into the underlying lacunae. Publishedvalues ofsurface roughness correspond in magnitude to these surface depressions, but theexistence ofthese depressions in vivo has not yet beenestablished beyond dispute. It is suggested that the surface ridges visible in some specimens are artefactscreated bypreparation techniques and that the structure ofthe superficial zone is a fine fibre networkwhich appears orientatedin sometorn surfacesbutwhich generally has arandomappearancein the planeparallel to thearticular surfaces.This work was supported by a Science Research Council Grant no. B/SR/4322and was carried out in the BioEngineering Unit at the University of Strathclyde(Director, Professor R. M. Kenedi) under the supervision of DrP. F. Millington.The author is the
Energy and Environment in Architecture: A Technical Design Guide (2000)

Introduction. Low Energy Strategies. The Provision of Comfort. Heating. Overheating. Day lighting. Ventilation. The Passive Zone Concept. Atria and Sunspaces. Energy Systems. Introduction to the LT Method. How to Use the LT Method. LT Method Worked Examples. LT Curves, Tables and Worksheets. Case Studies. Glossary. Appendices.
Peptides generated from C-reactive protein by a neutrophil membrane protease. Amino acid sequence and effects of peptides on neutrophil oxidative metabolism and chemotaxis. (1990)

We have recently provided evidence that C-reactive protein (CRP) could act as an up-regulatable substrate for membrane-associated neutrophil serine protease(s). The resultant degradation of CRP yielded small soluble bioactive peptides that inhibit many of the proinflammatory functions of activated neutrophils and could oppose the tissue destructive potential of these cells. We report on the reverse phase HPLC separation of the small TCA-soluble peptides obtained when CRP is degraded with nonstimulated or PMA-stimulated neutrophils and purified neutrophil membranes. The amino acid sequence of seven peptides isolated from the CRP digest has been ascertained and synthetic peptides homologous to these sequences have been synthesized. Three of the synthetic peptides corresponding to residues 201-206 (CRP-III), 83-90 (CRP-IV), and 77-82 (CRP-V) of the intact protein were identified to significantly inhibit superoxide production from activated neutrophils at 50 microM whereas CRP-III and CRP-V in addition inhibited neutrophil chemotaxis at this concentration. These peptides act additively and their action likely involves the signal transduction pathways for neutrophil activation.
The physics of proton therapy (2015)

The physics of proton therapy has advanced considerably since it was proposed in 1946. Today analytical equations and numerical simulation methods are available to predict and characterize many aspects of proton therapy. This article reviews the basic aspects of the physics of proton therapy, including proton interaction mechanisms, proton transport calculations, the determination of dose from therapeutic and stray radiations, and shielding design. The article discusses underlying processes as well as selected practical experimental and theoretical methods. We conclude by briefly speculating on possible future areas of research of relevance to the physics of proton therapy.
Effect of training conditions and extended thermal cycling on nitinol two-way shape memory behavior (1995)

Shape memory alloys (SMA) are a class of materials proposed to be used as actuator elements in smart structures. They undergo a reversible martensitic phase transformation during thermal cycling. In this work, 55-nitinol (55% nickel-45% titanium shape memory alloy) was investigated to determine the effect of training conditions, bias stress and extended thermal cycling on the transformational behavior. Thin wires (0.19 mm diameter) were trained using a previously developed methodology to exhibit two-way shape memory (TWSM). The wires were placed in a cryogenically cooled apparatus and heated by electrical resistance while the wire deformation was measured. Several different training schedules were used by varying the amount of prestrain and number of training cycles. The recovery strain and transformation temperatures were measured throughout extended thermal cycling (up to 10000 cycles). A bias stress was also used to enhance the amount of retention of prestrain in the wires. In all cases, stabilization of TWSM behavior occurred within 2000 thermal cycles.
A distinct influenza infection signature in the blood transcriptome of patients with severe community-acquired pneumonia (2012)

The whole-blood expression-profiling data indicate that the host response to influenza pneumonia is distinctly different from that caused by bacterial pathogens. This information may speed the identification of the cause of infection in patients presenting with severe respiratory failure, allowing appropriate patient care to be undertaken more rapidly.
Introduction: The Implication of the Private Securities Reform Act (1998)

I'll offer my observations about key activities at both the federal and state levels in the wake of the Reform Act. I'll conclude by offering my opinion about whether, on the current record, the case for preemption has been made.
Identification of a novel cytokeratin 19 pseudogene that may interfere with reverse transcriptase-polymerase chain reaction assays used to detect micrometastatic tumor cells (1999)

In many recent publications, it has been claimed that reverse transcriptase-polymerase chain reaction (RT-PCR) assays involving genes with tissue-restricted expression can be used for specific and sensitive detection of cancer cells in blood, bone marrow and lymph nodes. Many different target mRNAs have been evaluated for such purposes. One of the most extensively studied genes, CK19, is predominantly expressed in cells of epithelial origin and normally not at detectable levels in hematopoietic or lymphatic tissues. Based on previous reports on CK19 we wanted to establish a useful assay for detection of micrometastatic cells. RNA and DNA specimens extracted from peripheral blood nucleated cells of healthy volunteers, as well as cell lines positive and negative for CK19 expression, were used in nested RT-PCR assays. Using previously published primers, we found a novel pseudogene that shows a high degree of identity with the CK19 gene sequence, except for differences caused by 3 small deletions and a number of point mutations, resulting in termination codons and frameshifts. The gene has therefore no coding potential. Importantly, published primer sequences and reaction conditions used by several other groups to detect CK19 mRNA may have led to the amplification of this pseudogene. The data illustrate one of the problems that must be addressed in validating RT-PCR assays for micrometastasis detection, and it is suggested that previous work using CK19 as a marker should be reassessed in view of the present finding.
Nuclear Factor of Activated T-cells (NFAT) Rescues Osteoclastogenesis in Precursors Lacking c-Fos (2004)

Osteoclasts are specialized macrophages that resorb bone. Mice lacking the AP-1 component c-Fos are osteopetrotic because of a lack of osteoclast differentiation and show an increased number of macrophages. The nature of the critical function of c-Fos in osteoclast differentiation is not known. Microarray analysis revealed that Nfatc1, another key regulator of osteoclastogenesis, was down-regulated in Fos(-/-) osteoclast precursors. Chromatin immunoprecipitation assay showed that c-Fos bound to the Nfatc1 and Acp5 promoters in osteoclasts. In vitro promoter analyses identified nuclear factor of activated T-cells (NFAT)/AP-1 sites in the osteoclast-specific Acp5 and Calcr promoters. Moreover, in Fos(-/-) precursors gene transfer of an active form of NFAT restored transcription of osteoclast-specific genes in the presence of receptor activator of the NF-kappaB ligand (RANKL), rescuing bone resorption. In the absence of RANKL, however, Fos(-/-) precursors were insensitive to NFAT-induced osteoclastogenesis unlike wild-type precursors. These data indicate that lack of Nfatc1 expression is the cause of the differentiation block in Fos(-/-) osteoclast precursors and that transcriptional induction of Nfatc1 is a major function of c-Fos in osteoclast differentiation.
Microstrip-Fed Semi-Elliptical Dipole Antennas for Ultrawideband Communications (2008)

A microstrip-fed semi-elliptical dipole antenna (MFSEDA) is proposed and designed for ultrawideband (UWB) communications. The antenna has large bandwidth covering the frequency band from 3.1 to 10.6 GHz, radiation patterns similar to those of a conventional dipole antenna, and small size with the dimension of only about one third of the wavelength instead of half wavelength for the lower frequency. With simple and proper modification of the radiation patches, a frequency-notched antenna based on the MFSEDA is also designed and good band-notched performance from 5.0 to 6.0 GHz can be obtained. Measured results show that these MFSEDAs are suitable for UWB applications due to their high performances.
A dynamical formalism for an arbitrary number of interconnected rigid bodies, with reference to the problem of satellite attitude control. (1966)

Dynamical formalism for arbitrary number of interconnected rigid bodies analyzed with reference to passive attitude stabilization of satellites
Managing Access Control for Presence-Based Services (2005)

This paper presents an approach for managing access to services over presence-based communications based on the context of the situation. This paper addresses two technical challenges. The first is to form a communication group based on an association such as physical location. The second is to dynamically create and enforce a security policy by using service description and the user association. We validate this approach by implementing a prototype based on the IETF SIP/SIMPLE presence protocol for observing a user's context to form an association group. In addition the security policy is dynamically created and enforced on a packet filtering firewall for blocking unauthorized access.
Spread spectrum pulse position modulation-a simple approach for Shannon's limit- (1992)

A spread spectrum pulse position modulation (SS-PPM) system is proposed and its basic performances are described. In many direct sequence spread spectrum (DS-SS) systems, each demodulator is desired to use an only pseudonoise (PN) matched filter for simple structure and low cost. Such systems as on-off keying (SS-OOK) or differential phase-shift keying (SS-DPSK) systems have been conventionally used. The present authors propose the spread spectrum pulse position modulation (SS-PPM) system as one of such systems, and show that the SS-PPM system has the following advantages: (1) higher data rate (about 4 times higher than the other conventional SS systems under the same bandwidth and the same code length), (2) superior performance of bit error rate (BER) to the other systems (BER characteristics of the SS-PPM system improves with increasing the number of chip slot of the SS-PPM system, and it approaches Shannon's limit). Furthermore they evaluate asynchronous CDMA performance of the SS-PPM system by theory and computer simulation.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
The complete genome of <i>Bacillus subtilis</i>: from sequence annotation to data management and analysis (1998)

The completion of the entire 4.2-Mb genome sequence of the gram-positive bacterium Bacillus subtilis has been a milestone for biological studies on this model organism. This paper describes bioinformatics work related to this joint European and Japanese project: methods and strategies for gene annotation and detection of sequencing errors, using an integrated cooperative computer environment (Imagene); construction of a specialized database for data management and a WWW server for data retrieval (SubtiList); DNA sequence analysis, yielding striking results on oligonucleotide bias, repeated sequences, and codon usage, all landmarks of evolutionary events shaping the B. subtilis genome.
Effective Darcy‐scale contact angles in porous media imbibing solutions of various surface tensions (2009)

Surface tensions of high‐salinity solutions are significantly different from those of pure water. Our objective was to develop and test a methodology to determine whether these surface tension effects predictably alter imbibition into dry and moist porous media. Static and dynamic experiments were performed using four grades of quartz sand to determine the effects of solution salinity on imbibition. Results were quantified as apparent contact angles between the sand and three solutions (pure water, 5 molal NaNO 3 , and n‐hexane). Contact angles determined using a static method in initially air dried sand ranged from 23° to 31°, with the same values found for both water and the NaNO 3 solution. Effective contact angles determined for the air‐dried sand using a dynamic method based on a modified version of the Green and Ampt model were about twice those found using the static method, averaging 45° and 62° for water and the NaNO 3 solution, respectively. In prewetted sands, the dynamic imbibition data yielded apparent contact angles of 2° and 21° for water and the NaNO 3 solution, respectively, with the latter value comparing well to a predicted value of 25° for the NaNO 3 solution solely on the basis of surface tension contrast. The results of this study indicate that on the Darcy scale, saline solutions appear to follow the relationship of nonzero contact angles with other miscible fluids of different surface tensions used to prewet the sand grains, in agreement with the macroscale infiltration results of Weisbrod et al. (2004).
Structural and functional analysis of Utp23, a yeast ribosome synthesis factor with degenerate PIN domain (2013)

During synthesis of yeast ribosome, a large complex, called the 90S pre-ribosome or the small subunit processome, is assembled on the nascent precursor rRNA and mediates early processing of 18S rRNA. The Utp23 protein and snR30 H/ACA snoRNA are two conserved components of 90S pre-ribosomes. Utp23 contains a degenerate PIN nuclease domain followed by a long C-terminal tail and associates specifically with snR30. Here, we report the crystal structure of the Utp23 PIN domain at 2.5-Å resolution. The structure reveals a conserved core fold of PIN domain with degenerate active site residues, a unique CCHC Zn-finger motif, and two terminal extension elements. Functional sites of Utp23 have been examined with conservation analysis, mutagenesis, and in vivo and in vitro assays. Mutations in each of three cysteine ligands of zinc, although not the histidine ligand, were lethal or strongly inhibitory to yeast growth, indicating that the Zn-finger motif is required for Utp23 structure or function. The N-terminal helix extension harbors many highly conserved basic residues that mostly are critical for growth and in vitro RNA-binding activity of Utp23. Deletion of the C-terminal tail, which contains a short functionally important sequence motif, disrupted the interaction of Utp23 with snR30 and perturbed the pre-ribosomal association of Utp23. Our data establish a structural framework for dissecting Utp23 function in the assembly and dynamics of 90S pre-ribosomes.