gebhart/patrepeval huggingface dataset:
Characterization of dermal dendritic cells obtained from normal human skin reveals phenotypic and functionally distinctive subsets (1994)

The relative contribution of dermal-derived immunocompetent cells to the overall immunologic response in skin has been hampered by the lack of appropriate isolation techniques. In this report, we provide a purification schema that reliably yields highly purified populations of dermal dendritic cells (DDC). These cells are motile, express high levels of class II MHC antigens that decorate their cytoplasmic dendritic processes, and lack numerous B cell, T cell, and natural killer cell antigens. Using a broad panel of 45 different antibodies, an extensive phenotypic analysis was completed, revealing distinctive profiles for subsets of DDC. Despite homogeneous light scatter profile and cytologic appearance, three subsets of DDC could be distinguished by phenotypic and functional criteria. All DDC, but not epidermal Langerhans cells, express factor XIIIa. By triple color cell staining the relative distribution of factor XIIIa positive DDC is as follows: subset 1, 65% to 70% of total DDC express neither CD1a nor CD14; subset 2, 15% to 20% of total DDC express CD1a but not CD14; and subset 3, 10% to 15% of total DDC express CD14 but not CD1a. The CD14-negative subset of DDC were shown to be as potent stimulators of allogeneic mixed lymphocyte reactions as Langerhans cells or blood-derived dendritic cells. However, DDC subsets differed in their ability to support autologous T cell proliferation in response to the mitogenic lectin PHA or bacterial-derived superantigen. In these assays, subsets 1 and 2 were significantly more potent as antigen-presenting cells compared with subset 3. Thus, normal skin contains at least three separate populations of DDC, which have distinctive phenotypic markers and immunologic capabilities.
Synthesis of stereospecific deuterium-labeled homoserines and homoserine lactones (1988)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of stereospecific deuterium-labeled homoserines and homoserine lactonesKondareddiar Ramalingam and Ronald W. WoodardCite this: J. Org. Chem. 1988, 53, 9, 1900–1903Publication Date (Print):April 1, 1988Publication History Published online1 May 2002Published inissue 1 April 1988https://pubs.acs.org/doi/10.1021/jo00244a012https://doi.org/10.1021/jo00244a012research-articleACS PublicationsRequest reuse permissionsArticle Views1970Altmetric-Citations33LEARN 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 optionsGet e-Alertsclose Get e-Alerts
Well‐Defined N‐Heterocyclic Carbene‐Palladium Complexes as Efficient Catalysts for Domino Sonogashira Coupling/Cyclization Reaction and C‐H bond Arylation of Benzothiazole (2019)

Well‐defined and air‐stable PEPPSI (Pyridine Enhanced Precatalyst Preparation Stabilization and Initiation) themed palladium bis ‐N‐heterocyclic carbene complexes have been developed for the domino Sonogashira coupling/cyclization reaction of 2‐iodophenol with a variety of terminal alkynes and C‐H bond arylation of benzothiazole with aryl iodides. The PEPPSI themed palladium complexes, 2a and 2b were synthesized in good yields from the reaction of corresponding imidazolium salts with PdCl 2 and K 2 CO 3 in pyridine. The new air‐stable palladium‐NHC complexes were characterized by NMR spectroscopy, X‐ray crystallography, elemental analysis, and mass spectroscopy studies. The PEPPSI themed palladium(II) bis ‐N‐heterocyclic carbene complexes 2a and 2b exhibited excellent catalytic activities for domino Sonogashira coupling/cyclization reaction of 2‐iodophenol with terminal alkynes yielding benzofuran derivatives. In addition, the palladium complexes, 2a and 2b successfully catalyzed the direct C‐H bond arylation of benzothiazole with aryl iodides as coupling partners in presence of CuI as co‐catalyst.
Synthetic Aperture Imaging with Maneuvers (1972)

A digital processing approach has been devised for performing motion compensation in a high-resolution airborne synthetic aperture radar in the presence of simultaneous longitudinal (speed change), lateral (turn), and vertical (climb or dive) maneuvers. Both side-look and squint are accommodated in a unified scheme, which is validated by various simulation runs reported herein. Present attention is focused on theoretical verification, irrespective of mechanization or specific parameter values.
Optimal transmit signal design for active sonar/radar (2002)

This work is concerned with the optimization of an active sonar or radar transmit signal, to maximize the probability of detecting a nonmoving point target in the presence of signal-dependent reverberation and colored ambient noise whose power spectral densities are known. An analytical solution first reported by Kooij is corrected and extended. A simple example for the white ambient noise case is included to provide insight into the transmit signal optimization. This example shows that the effect of the solution is to “pre-emphasize” the transmit signal, which results in the whitening of the signal-dependent reverberation power spectral density.
Preventing invasive breast cancer (2011)

Invasive breast cancer incidence has decreased in the United States since 1998. Widespread excision of preinvasive ductal carcinoma in situ over many years may be a principal cause.
Building Extraction from LIDAR Based Semantic Analysis (2006)

从激光雷达数据的大楼的抽取是最近的年里的一个活跃研究领域。为从激光雷达数据造察觉和重建的一个计划与基于大楼的一个面向对象的方法被介绍“语义规则。二关键步被讨论：怎么组织分离激光雷达点进单个目标并且怎么建立大楼“语义规则。最后，大楼在 3D 形式和三个普通参量的大楼模型被重建(扁平， gabled， hipped ) 被实现。
The Human Cytomegalovirus Gene UL79 Is Required for the Accumulation of Late Viral Transcripts (2011)

In this study, we adopted a conditional protein genetic approach to characterize the role of the human cytomegalovirus (HCMV) gene UL79 during virus infection. We constructed ADddUL79, a recombinant HCMV in which the annotated UL79 open reading frame (ORF) was tagged with the destabilization domain of a highly unstable variant of the human FKBP12 protein (ddFKBP). The ddFKBP domain targets the tagged protein for rapid proteasomal degradation, but the synthetic ligand Shield-1 can stabilize ddFKBP, allowing accumulation of the tagged protein. ADddUL79 failed to replicate without Shield-1, but it grew at wild-type levels with Shield-1 or in human foreskin fibroblasts overexpressing hemagglutinin (HA)-tagged UL79 (HF-UL79HA cells), indicating an essential role of UL79 and the effectiveness of this approach. Without Shield-1, representative immediate-early and early viral proteins as well as viral DNA accumulated normally, but late transcripts and proteins were markedly reduced. UL79 was transcribed with early-late kinetics, which was also regulated via a positive-feedback loop. Using HF-UL79HA cells, we found that the UL79 protein localized to viral replication compartments during HCMV infection. Finally, we created a second UL79 mutant virus (ADinUL79(stop)) in which the UL79 ORF was disrupted by a stop codon mutation and found that ADinUL79(stop) phenocopied ADddUL79 under the destabilizing condition. Taking these results together, we conclude that UL79 acts after viral DNA replication to promote the accumulation of late viral transcripts. Importantly, the comparative analysis of ADddUL79 and ADinUL79(stop) viruses provide additional proof for the power of the protein stability-based conditional approach to dissect the role of viral factors in HCMV biology.
Structure-Activity Relationships of Milrinone Analogs Determined in Vitro in a Rabbit Heart Membrane Ca2+-ATPase Model (1995)

The cardiac activity of a series of analogues of the positive inotropic bipyridines amrinone (5-amino-[3,4'-bipyridin]-6(1H)-one) and milrinone (2-methyl-5-cyano-[3,4'-bipyridin]-6(1H)-one) was evaluated in vitro in a rabbit myocardial membrane Mg(2+)-dependent, Ca(2+)-stimulable adenosine triphosphatase (Ca(2+)-ATPase) model and structure-activity relationships were compared for nine closely related derivatives. In the present studies, a 5-bromo analogue of milrinone stimulated myocardial membrane Ca(2+)-ATPase significantly (10(-7) M; P < 0.001 vs control, with 67% of the activity of milrinone), whereas a 2'-methyl-2H-milrinone derivative was inactive. Although amrinone was inactive in this assay, its 2-methyl analogue was stimulatory. However, analogues lacking a 2-substituent (with or without a 5-cyano group) or with the 3-N position blocked by a methyl group did not stimulate myocardial membrane Ca(2+)-ATPase activity. Structural data for these bipyridines show that those with either a 2- or 2'-methyl substituent have a twist conformation, whereas those without are nearly planar. Activity data reveal that those bipyridines with a nonplanar conformation are more active in the Ca(2+)-ATPase assay. Further study of milrinone analogues with a 2'-methyl substituent shows that even though the effect on the twist angle is equivalent to that of 2-methyl substitution, these analogues are less potent. Data for this series reveal that the prerequisites for Ca(2+)-ATPase stimulation include not only a 2-methyl to maintain a twist conformation but also a free 3-N position and a 5-substituent. This model for optimal activity in the myocardial membrane Ca(2+)-ATPase system differs from those proposed for phosphodiesterase enzyme receptor recognition only in the requirement for a nonplanar molecule. We have previously shown that milrinone, but not amrinone, shares structural homology with thyroxine and was able to stimulate myocardial membrane Ca(2+)-ATPase activity in a manner similar to the thyroid hormone. Additionally, milrinone, but not amrinone, was an effective competitor for thyroxine binding to the serum transport protein transthyretin. Analysis of the milrinone-transthyretin crystal complex confirms the structural homology between milrinone and thyroid hormone which is not shared by amrinone. Modeling studies of the binding interactions of milrinone analogues indicate that the 2-desmethylmilrinone analogue, the most inhibitory analogue, lacks the hydrophobic contacts present in milrinone in its transthyretin-bound complex.(ABSTRACT TRUNCATED AT 400 WORDS)
Specific Nucleus as the Transition State for Protein Folding: Evidence from the Lattice Model (1994)

We have studied the folding mechanism of lattice model 36-mer proteins. Using a simulated annealing procedure in sequence space, we have designed sequences to have sufficiently low energy in a given target conformation, which plays the role of the native structure in our study. The sequence design algorithm generated sequences for which the native structures is a pronounced global energy minimum. Then, designed sequences were subjected to lattice Monte Carlo simulations of folding. In each run, starting from a random coil conformation, the chain reached its native structure, which is indicative that the model proteins solve the Levinthal paradox. The folding mechanism involved nucleation growth. Formation of a specific nucleus, which is a particular pattern of contacts, is shown to be a necessary and sufficient condition for subsequent rapid folding to the native state. The nucleus represents a transition state of folding to the molten globule conformation. The search for the nucleus is a rate-limiting step of folding and corresponds to overcoming the major free energy barrier. We also observed a folding pathway that is the approach to the native state after nucleus formation; this stage takes about 1% of the simulation time. The nucleus is a spatially localized substructure of the native state having 8 out of 40 native contacts. However, monomers belonging to the nucleus are scattered along the sequence, so that several nucleus contacts are long-range while other are short-range. A folding nucleus was also found in a longer chain 80-mer, where it also constituted 20% of the native structure. The possible mechanism of folding of designed proteins, as well as the experimental implications of this study is discussed.
Glasses for Photonics (2000)

This book is an introduction to recent progress in the development and application of glass with special photonics properties. Glass has a number of structural and practical advantages over crystalline materials, including excellent homogeneity, variety of form and size, and the potential for doping with a variety of dopant materials. Glasses with photonic properties have great potential and are expected to play a significant role in the next generation of multimedia systems. Fundamentals of glass materials are explained in the first chapter, and the book then proceeds to a discussion of gradient index glass, laser glasses, nonlinear optical glasses and magneto-optical glasses. Beginning with the basic theory, the book discusses actual problems, performance and applications of glasses. The book will be of value to graduate students, researchers and professional engineers working in materials science, chemistry and physics with an interest in photonics and glass with special properties.
Protein kinase activity associated with the nuclear lamina. (1988)

A nuclear lamina-enriched fraction from Ehrlich ascites tumor cells contains a tightly bound protein kinase activity, which phosphorylates in vitro the nuclear lamins, a 52-kilodalton protein, and several unknown minor components. The enzyme(s) is thermolabile, independent of Ca2+ and cAMP, and inhibited by quercetin. After treatment with 4 M urea it remains bound to the nuclear lamina in an active state, but it is irreversibly inactivated in 6 M urea. The lamin proteins are phosphorylated on serine residues. Their two-dimensional phosphopeptide maps show multiple phosphorylation sites and a considerable similarity to the phosphopeptide maps of lamins labeled in vivo. Photoaffinity labeling experiments revealed several polypeptide fractions in the nuclear lamina fraction that are candidates for the protein kinase(s).
Synthesis of a squash-type protease inhibitor by gene engineering and effects of replacements of conserved hydrophobic amino acid residues on its inhibitory activity (1996)

Cucurbita maxima trypsin inhibitor I (CMTI-I), a member of the squash-type protease inhibitor family, is composed of 29 amino acids and shows strong inhibition of trypsin by its compact structure. To study the structure-function relationship of this inhibitor using protein engineering methods, we constructed an expression system for CMTI-I as a fused protein with porcine adenylate kinase (ADK). A Met residue was introduced into the junction of ADK and CMTI-I to cleave the fusion protein with CNBr, whereas a Met at position 8 of authentic CMTI-I was replaced by Leu. Escherichia coli JM109 transformed with the constructed plasmid expressed the fused protein as an inclusion body. After cleavage of the expressed protein with CNBr, fully reduced species of CMTI-I were purified by reversed-phase HPLC and then oxidized with air by shaking. For efficient refolding of CMTI-I, we used 50 mM NH4HCO3 (pH 7.8) containing 0.1% PEG 6000 at higher protein concentration. Strong inhibitory activity toward trypsin was detected only in the first of three HPLC peaks. The inhibitor constant of CMTI-I thus obtained, in which Met8 was replaced by Leu, was 1.4 x 10(-10) M. The effect of replacement of Met with Leu at position 8 was shown to be small by comparison of the inhibitor constant of authentic CMTI-III bearing Lys at position 9 (8.9 x 10(-11) M) with that of its mutant bearing Leu at position 8 and Lys at position 9 (1.8 x 10(-10) M). To investigate the role of the well conserved hydrophobic residues of CMTI-I in its interaction with trypsin, CMTI-I mutants in which one or all of the four hydrophobic residues were replaced by Ala were prepared. The inhibitor constants of these mutants indicated that those with single replacements were 5-40 times less effective as trypsin inhibitors and that the quadruple mutant was approximately 450 times less effective, suggesting that the hydrophobic residues in CMTI-I contribute to its tight binding with trypsin. However, each mutant was not converted to a temporary inhibitor.
Natural killer (NK) cells as a responder to interleukin 2 (IL 2). I. Proliferative response and establishment of cloned cells. (1983)

The proliferative response of murine natural killer (NK) cells to a T cell growth factor, interleukin 2 (IL 2) was investigated by using the NK-enriched, low-density fractions (F.1) and NK-depleted, T cell-enriched, and high-density fractions (F.3) of normal spleen cells after Percoll-discontinuous density gradient centrifugation. When F.1 and F.3 cells were cultivated with IL 2-containing medium without addition of any other factors, like lectins, feeder layer, or macrophage products, F.1 but not F.3 cells showed an IL 2-dependent proliferative response. Growing populations showed a potent NK activity and consisted largely of cells with a morphology of large granular lymphocyte (LGL) and a surface marker profile characteristic for murine NK cells. By limiting dilution in the liquid culture and colony formation in the soft agar medium, F.1 but not F.3 cells showed a high frequency of clonal replication in IL 2. Almost all growing colonies in either medium showed a typical morphology of LGL. Further, F.1 cells treated with anti-asialo GM1 antibody and C, from which NK cells and cytolytic activity were almost completely abrogated and for which T cells were enriched, conversely formed a few IL 2-dependent colonies. From the colonies in soft agar, 11 clones, all of which showed a typical morphology (LGL), a typical surface profile with the exception of lacking IgG-Fc receptors for NK cells (Thy-1 +/-, Ly-5+, ASGM1+, Lyt-1-, Lyt-2-, Fc gamma R-), and a cytotoxic activity of activated nature, were established and maintained for a period of longer than 1 yr in the medium containing IL 2 alone. These results indicate that a major population in the naive spleens of normal mice that respond directly to IL 2 and clonally replicate without other stimulating factors may be NK cells.
X‐ray structures of Sap1 and Sap5: Structural comparison of the secreted aspartic proteinases from <i>Candida albicans</i> (2008)

Proteolytic activity is an important virulence factor for Candida albicans (C. albicans). It is attributed to the family of the secreted aspartic proteinases (Saps) from C. albicans with a minimum of 10 members. Saps show controlled expression and regulation for the individual stages of the infection process. Distinct isoenzymes can be responsible for adherence and tissue damage of local infections, while others cause systemic diseases. Earlier, only the structures of Sap2 and Sap3 were known. In our research, we have now succeeded in solving the X-ray crystal structures of the apoenzyme of Sap1 and Sap5 in complex with pepstatin A at 2.05 and 2.5 A resolution, respectively. With the structure of Sap1, we have completed the set of structures of isoenzyme subgroup Sap1-3. Of subgroup Sap4-6, the structure of the enzyme Sap5 is the first structure that has been described up to now. This facilitates comparison of structural details as well as inhibitor binding modes among the different subgroup members. Structural analysis reveals a highly conserved overall secondary structure of Sap1-3 and Sap5. However, Sap5 clearly differs from Sap1-3 by its electrostatic overall charge as well as through structural conformation of its entrance to the active site cleft. Design of inhibitors specific for Sap5 should concentrate on the S4 and S3 pockets, which significantly differ from Sap1-3 in size and electrostatic charge. Both Sap1 and Sap5 seem to play a major part in superficial Candida infections. Determination of the isoenzymes' structures can contribute to the development of new Sap-specific inhibitors for the treatment of superficial infections with a structure-based drug design program.
Effects of Fiber Denier, Fiber Cross-Sectional Shape and Fabric Density on Acoustical Behavior of Vertically Lapped Nonwoven Fabrics (2008)

Acoustical insulation and absorption properties of nonwoven fabrics depend on fiber geometry and fiber arrangement within the fabric structure. The different structures of the fibers result in different total surface areas of nonwoven fabrics. Nonwoven fabrics such as vertically lapped fabrics are ideal materials for use as acoustical insulation products, because they have high total surface. Vertically lapped nonwoven technology consists of carding, perpendicular layering of the carded webs, and through-air bonding using synthetic binder fibers. The surface area of the fabric is directly related to the denier and cross-sectional shape of the fibers in the fabric. Smaller deniers yield more fibers per unit weight of the material, higher total fiber surface area, and greater possibilities for a sound wave to interact with the fibers in the fabric structure. The research in the literature uses two methods for measuring acoustical properties of fabric materials: the impedance tube and reverberation room method. Small test samples are in the impedance tube method and sound absorption coefficient is determined at each frequency. Large reverberation rooms and large test samples are used for the reverberation room method. A direct comparative acoustical properties measurement device that was designed and fabricated at Clemson University School of Materials Science & Engineering was used to measure acoustical insulation in this research. This paper provides a description of the measurement devices and acoustical measurement data for vertically lapped nonwoven fabrics made from three different polyester fiber shape and two denier levels.
Conversion of the CPT-11 metabolite APC to SN-38 by rabbit liver carboxylesterase. (1998)

The anticancer drug CPT-11 (7-ethyl-[4(1-piperidino)-1-piperidino]carbonyloxycamptothecin) is a water-soluble derivative of camptothecin. We report here the conversion of APC (7-ethyl-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin), an inactive metabolite of CPT-11, to SN-38 (7-ethyl-10-hydroxycamptothecin), the active metabolite of CPT-11, by a rabbit liver carboxylesterase. This reaction is not catalyzed by any known human enzyme. The formation of SN-38 from APC was characterized by an apparent Km of 37.9 +/- 7.1 microM and a Vmax of 16.9 +/- 0.9 pmol/units/min. SN-38 was confirmed as a reaction product by high-performance liquid chromatography and mass spectrometry. A 24-h incubation of 10 microM APC with 500 units/ml of rabbit carboxylesterase produced 4 microM SN-38. The product of this reaction inhibited the growth of U373 MG human glioblastoma cells in vitro. The IC50 for a 24-h exposure of U373 MG cells to APC in the presence of 50 units/ml of rabbit carboxylesterase was 0.27 +/- 0.08 microM, whereas APC alone demonstrated no inhibition of growth at concentrations up to 1 microM. The IC50 of U373 MG cells transfected with the cDNA encoding the rabbit carboxylesterase (U373pIRESrabbit) and exposed to APC for 24 h was 0.8 +/- 0.1 microM APC, whereas the growth of cells transfected with vector control (U373pIRES) was unaffected by up to 1 microM APC. Because APC is nontoxic to human cells, we are investigating the possibility of using APC/rabbit carboxylesterase in a prodrug/enzyme therapeutic approach.