gebhart/patrepeval huggingface dataset:
Laser Diffraction Estimation of Particle Size Distribution of Slightly Water-Soluble Drugs Coexisting with Additives: Application to Solid Dosage Forms. (1992)

A simple and quantitative evaluation method for particle size distribution (fx(r)) of slightly water-soluble drugs dispersed in an aqueous medium together with other water-insoluble additives was developed using a laser diffraction method. The particle size distribution function of the powder mixture, (f(r)), was assumed as f(r) = phi x.fx(r) + phi a.fa(r), where phi is the volume fraction of each component dispersed in a measurement medium and fa(r) is the distribution function of another water-insoluble additive "a". In order to calculate fx(r) from f(r), it is necessary to know the density of drug and additive in the measurement medium, d(x) and d(a), but this is difficult to determine since particles usually swell in the medium. Thus, a method was developed to use their relative value, delta a (= da/dx). As a practical application, oxolinic acids (OA) of three sizes (OA-S (about 2 microns), OA-M (about 7 microns) and OA-L (about 24 microns)) were used as model drugs. delta a values were determined for various additives using the mixture of OA-S and each additive. Then, using delta as, fx(r) of OA-M or OA-L in the mixture containing OA-M or OA-L and additives was calculated from the f(r) experimentally determined for the mixture. They agreed well with their original distributions. The method was applied to some dosage forms, and the results obtained had good correlation with those from turbidity, wet sieving or dissolution test.
Competition between Burkholderia pseudomallei and B. thailandensis (2015)

Taken together, our results indicate that B. pseudomallei inhibits both the growth and motility of its close relative B. thailandensis. The latter phenomenon appears to occur via a previously unreported mechanism involving flagellar processing or degradation.
Synthesis and Properties of Hybrid Organic−Inorganic Materials Containing Covalently Bonded Luminescent Polygermanes (2004)

Covalent binding of arylmethylpolygermanes into hybrid silica materials leads to substantial increases in thermal stability without degrading Ge−Ge σ-conjugation, as determined by UV−vis absorption and fluorescent emission spectroscopy. Poly(methyltrimethoxysilylphenylgermane) was prepared by ruthenium-catalyzed demethanative coupling of dimethyl(trimethoxysilylphenyl)germane, and then hydrolyzed and cured in the presence of either tetraethoxysilane (TEOS) or β-acetoxyethylsilsesquioxane (BAESSQ) to yield hybrid materials containing the polygermane linked to the matrix at every repeat unit. Thermal stability of the bulk hybrid materials was examined by TGA, and films were examined by UV−vis spectroscopy following thermal treatment and photochemical irradiation. Conjugation of the Ge−Ge chains is maintained to 380 °C under nitrogen in the case of the BAESSQ-derived hybrids, but only 200 °C in air. The photolytic stability of the hybrid films is greater than the parent poly(methylphenylgermane), but the gains are less dramatic. A model is proposed in which anchoring each germanium in the polymer chain to the silica matrix reduces mobility of germyl radicals produced by both thermolysis and photolysis, leading to efficient recombination to restore the Ge−Ge chains under nitrogen. On the other hand, germylene intermediates generated only during photolysis are more reactive and can combine irreversibly with Si−O−Si bonds or residual SiOH groups in the silica matrix, leading to faster photolytic degradation of the conjugated Ge−Ge chains, even under nitrogen.
A robust method for computing vehicle ego-motion (2002)

We describe a robust method for computing the ego-motion of the vehicle relative to the road using input from a single camera mounted next to the rear view mirror. Since feature points are unreliable in cluttered scenes we use direct methods where image values in the two images are combined in a global probability function. Combined with the use of probability distribution matrices, this enables the formulation of a robust method that can ignore large number of outliers as one would encounter in real traffic situations. The method has been tested in real world environments and has been shown to be robust to glare, rain and moving objects in the scene.
A regulated, charge-pump CMOS DC/DC converter for low-power applications (1998)

Thesis (M. Eng.)--Massachusetts Institute of Technology, Dept. of Electrical Engineering and Computer Science, 1998.
RETRACTED ARTICLE: MicroRNA expression profile of the hippocampus in a rat model of temporal lobe epilepsy and miR-34a-targeted neuroprotection against hippocampal neurone cell apoptosis post-status epilepticus (2012)

Our study showed the expression profile of miRNAs in the hippocampus in a rat model of temporal lobe epilepsy and an increase in the expression of the pro-apoptotic miR-34a in post-status epilepticus rats. The results show that miR-34a is up-regulated during seizure-induced neuronal death or apoptosis, and targeting miR-34a is neuroprotective and is associated with an inhibition of an increase in activated caspase-3 protein.
Bis-N,O-diacetylhydroxylamine analog of diaminodiphenyl sulfone possessing antimalarial activity (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTBis-N,O-diacetylhydroxylamine analog of diaminodiphenyl sulfone possessing antimalarial activityBernard Loev, Frederick Dowalo, Vassilios J. Theodorides, and Betty P. VoghCite this: J. Med. Chem. 1973, 16, 2, 161–163Publication Date (Print):February 1, 1973Publication History Published online1 May 2002Published inissue 1 February 1973https://pubs.acs.org/doi/10.1021/jm00260a018https://doi.org/10.1021/jm00260a018research-articleACS PublicationsRequest reuse permissionsArticle Views57Altmetric-Citations8LEARN 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
A high-capacity, anti-jam EHF "bent-pipe" satellite/central-hub system architecture concept (2002)

What has changed with the end of the Cold War? System architects should consciously ask this question to reexamine possibly outdated paradigms and develop new design approaches to meet the challenges of the post-Cold War era. In this context, a new design concept is presented: an EHF 30-/20-GHz "bent-pipe" satellite/central-hub system architecture optimized for major regional conflict (MRC) combat operations and coalition warfare. The concept has the potential to provide higher performance and significant life cycle cost (LCC) savings over current systems. High performance is defined as close-in user-jammer (U-J) standoff distance anti-jam protection, high capacity/throughput, and assured access for MRC combat operations. High performance also includes mobile "comm-on-the-move", broadband aeronautical, and wideband manportable (e.g., direct broadcast) communication services. Implementation of these services follows the pioneering efforts of NASA's EHF 30-/20-GHz ACTS program and the commercial sector's revolutionary trend of introducing high-speed data and videophone services with EHF 30-/20-GHz ultra-small aperture terminals (USAT). The transparency of a bent-pipe satellite and the terminal-to-terminal translation capability of the central hub provide joint and multinational force interoperability for coalition warfare. The trade-off between central hub and onboard processing is discussed, and an alternative perspective suggested. Finally, opportunities for synergism with the emerging EHF 30-/20-GHz commercial satellite communications sector are discussed.
Role of poly(ADP-ribose) synthetase in inflammation and ischaemia–reperfusion (1998)

Oxidative and nitrosative stress can trigger DNA strand breakage, which then activates the nuclear enzyme poly(ADP-ribose) synthetase (PARS). This enzyme has also been termed poly(ADP-ribose) polymerase (PARP) or poly(ADP-ribose) transferase (pADPRT). Rapid activation of the enzyme depletes the intracellular concentration of its substrate, nicotinamide adenine dinucleotide, thus slowing the rate of glycolysis, electron transport and subsequently ATP formation. This process can result in cell dysfunction and cell death. In this article, Csaba Szabó and Valina Dawson overview the impact of pharmacological inhibition or genetic inactivation of PARS on the course of oxidant-induced cell death in vitro, and in inflammation and reperfusion injury in vivo. A major trigger for DNA damage in pathophysiological conditions is peroxynitrite, a cytotoxic oxidant formed by the reaction between the free radicals nitric oxide and superoxide. The pharmacological inhibition of poly(ADP-ribose) synthetase is a novel approach for the experimental therapy of various forms of inflammation and shock, stroke, myocardial and intestinal ischaemia-reperfusion, and diabetes mellitus.
Involvement of FGF-8 in initiation, outgrowth and patterning of the vertebrate limb (1996)

ABSTRACT Fibroblast Growth Factors (FGFs) are signaling molecules that are important in patterning and growth control during vertebrate limb development. Beads soaked in FGF-1, FGF-2 and FGF-4 are able to induce additional limbs when applied to the flank of young chick embryos (Cohn, M.J., Izpisua-Belmonte, J-C., Abud, H., Heath, J. K., Tickle, C. (1995) Cell 80, 739-746). However, biochemical and expression studies suggest that none of these FGFs is the endogenous signal that initiates limb development. During chick limb development, Fgf-8 transcripts are detected in the intermediate mesoderm and subsequently in the prelimb field ectoderm prior to the formation of the apical ectodermal ridge, structures required for limb initiation and outgrowth, respectively. Later on, Fgf-8 expression is restricted to the ridge cells and expression disappears when the ridge regresses. Application of FGF-8 protein to the flank induces the development of additional limbs. Moreover, we show that FGF-8 can replace the apical ectodermal ridge to maintain Shh expression and outgrowth and patterning of the developing chick limb. Furthermore, continuous and widespread misexpression of FGF-8 causes limb truncations and skeletal alterations with phocomelic or achondroplasia phenotype. Thus, FGF-8 appears to be a key signal involved in initiation, outgrowth and patterning of the developing vertebrate limb.
Review of Recent Developments in the Molecular Characterization of Recombinant Alfa Interferons on the 40th Anniversary of the Discovery of Interferon (1998)

Recombinant alfa interferons (IFN-alpha s) are approved worldwide for the treatment of a variety of cancers and diseases of virologic origin. A series of recent advances in the molecular characterization of recombinant IFN-alpha s have allowed the determination of the three-dimensional IFN-alpha 2b structure by high-resolution x-ray crystallography. We review here recent developments in our understanding of the molecular and physicochemical properties of recombinant IFN-alpha, including our current state of knowledge of the IFN-alpha gene family and the multiple species of human leukocyte IFN. Based on the reported three-dimensional structure of IFN-alpha 2b, we propose a molecular model for the IFN-alpha 2b receptor complex and predict models for the naturally occurring subtypes IFN-alpha 1 and IFN-alpha 8, as well as the synthetic, non-naturally occurring consensus IFN. Such models provide molecular insights into the mechanism of action of IFN-alpha.
Inhibiting Dickkopf-1 (Dkk1) Removes Suppression of Bone Formation and Prevents the Development of Osteolytic Bone Disease in Multiple Myeloma (2008)

Multiple myeloma (MM) is associated with the development of osteolytic bone disease, mediated by increased osteoclastic bone resorption and impaired osteoblastic bone formation. Dickkopf-1 (Dkk1), a soluble inhibitor of wingless/int (Wnt) signaling and osteoblastogenesis, is elevated in patients with MM and correlates with osteolytic bone disease. In this study, we investigated the effect of inhibiting Dkk1 on the development of osteolytic lesions in the 5T2MM murine model of myeloma. We showed that Dkk1 is expressed by murine 5T2MM myeloma cells. Injection of 5T2MM cells into C57BL/KaLwRij mice resulted in the development of osteolytic bone lesions (p < 0.05), mediated by increased osteoclast numbers (p < 0.001) and a decrease in osteoblast numbers (p < 0.001) and mineralizing surface (p < 0.05). Mice bearing 5T2MM cells were treated with an anti-Dkk1 antibody (BHQ880, 10 mg/kg, IV, twice weekly for 4 wk) from time of paraprotein detection. Anti-Dkk1 treatment prevented 5T2MM-induced suppression of osteoblast numbers (p < 0.001) and surface (p < 0.001). Treatment increased mineralizing surface by 28% and bone formation rate by 25%; however, there was no change in mineral apposition rate. Inhibiting Dkk1 had no effect on osteoclast numbers. muCT analysis showed that anti-Dkk1 treatment significantly protected against 5T2MM-induced trabecular bone loss (p < 0.05) and reduced the development of osteolytic bone lesions (p < 0.05). Treatment had no significant effect on tumor burden. These data suggest that inhibiting Dkk1 prevents the suppression of bone formation and in doing so is effective in preventing the development of osteolytic bone disease in myeloma, offering an effective therapeutic approach to treating this clinically important aspect of myeloma.
Cloud-scale resource management: challenges and techniques (2011)

Managing resources at large scale while providing performance isolation and efficient use of underlying hardware is a key challenge for any cloud management software. Most virtual machine (VM) resource management systems like VMware DRS clusters, Microsoft PRO and Eucalyptus, do not currently scale to the number of hosts and VMs supported by cloud service providers. In addition to scale, other challenges include heterogeneity of systems, compatibility constraints between virtual machines and underlying hardware, islands of resources created due to storage and network connectivity and limited scale of storage resources.In this paper, we shed light on some of the key issues in building cloud-scale resource management systems, based on five years of research and shipping cluster resource management products. Furthermore, we discuss various techniques to provide large scale resource management, along with the pros and cons of each technique. We hope to motivate future research in this area to develop practical solutions to these issues.
Topologically sweeping an arrangement (1986)

Abstract Sweeping a collection of figures in the Euclidean plane with a straight line is one of the novel algorithmic paradigms that have emerged in the field of computational geometry. In this paper we demonstrate the advantages of sweeping with a topological line that is not necessarily straight. We show how an arrangement of n lines in the plane can be swept over in O ( n 2 ) time and O(n) space by a such a line. In the process each element, i.e., vertex, edge, or region, is visited once in a consistent ordering. Our technique makes use of novel data structures which exhibit interesting amortized complexity behavior; the result is an algorithm that improves upon all its predecessors either in the space or the time bounds, as well as being eminently practical. Numerous applications of the technique to problems in computational geometry are given—many through the use of duality transforms. Examples include solving visibility problems, detecting degeneracies in configurations, computing the extremal shadows of convex polytopes, and others. Even though our basic technique solves a planar problem, its applications include several problems in higher dimensions.
Microsyringe-Based Deposition of Two-Dimensional and Three-Dimensional Polymer Scaffolds with a Well-Defined Geometry for Application to Tissue Engineering (2002)

A technique for controlled deposition of biomaterials and cells in specific and complex architectures is described. It employs a highly accurate three-dimensional micropositioning system with a pressure-controlled syringe to deposit biopolymer structures with a lateral resolution of 5 microm. The pressure-activated microsyringe is equipped with a fine-bore exit needle and a wide variety of two- and three-dimensional patterns on which cells to be deposited can adhere. The system has been characterized in terms of deposition parameters such as applied pressure, motor speed, line width and height, and polymer viscosity, and a fluid dynamic model simulating the deposition process has been developed, allowing an accurate prediction of the topological characteristics of the polymer structures.
B Cell Receptor Engagement and T Cell Contact Induce bcl-6 Somatic Hypermutation in Human B Cells: Identity with Ig Hypermutation (2000)

The human bcl-6 proto-oncogene has been found to be mutated in both neoplastic and normal B cells. We used CL-01 cells, our monoclonal model of germinal center differentiation, and normal human B cells to explore the induction requirements and the modalities of bcl-6 hypermutation. As we have previously shown, CL-01 cells are IgM+ IgD+ and effectively mutate the expressed Ig VHDJH and V lambda J lambda genes and switch to IgG, IgA, and IgE upon B cell receptor engagement and contact with CD4+ T cells through CD40:CD154 and CD80:CD28 coengagement. In this paper we showed that the same stimuli induce somatic hypermutation of bcl-6 in CL-01 and normal IgM+ IgD+ B cells. bcl-6 hypermutation was not accompanied by translocation of this proto-oncogene or hypermutation of the beta-actin gene, and it did mimic Ig hypermutation. It was associated with transcription initiation, in that it targeted the first exon and a 696-bp sequence immediately downstream (approximately 0.6 kb) of the transcription initiation site while sparing further downstream (approximately 2.5 kb) and upstream (approximately 0.1 kb) areas. bcl-6 hypermutation displayed an overall rate of 2.2 x 10-4 changes/base/cell division with characteristic nucleotide preferences and showed strand polarity. These findings show that B cell receptor engagement promotes hypermutation in genes other than Ig, and suggest that cis-regulating elements similar to those of the Ig locus exist in bcl-6.
Novel Properties of Human Placental Aromatase as Cytochrome P-450: Purification and Characterization of a Unique Form of Aromatase1 (1988)

Aromatase has been purified to homogeneity from human placental microsomes based on detection of its catalytic activities in the eluates from columns of octylamino-Sepharose 4B, hydroxylapatite, Mono S, hydroxylapatite HCA, and Mono Q. The purified preparation shows only one band corresponding to the apparent subunit molecular weight of 51,000 daltons on sodium dodecyl sulfate-polyacrylamide gel. The aromatase in the presence of NADPH and NADPH-cytochrome P-450 reductase converts testosterone to 17β-estradiol with the high specific activity of 103 nmol/min/mg of protein. However, whether the preparation is reduced by sodium dithionate chemically or by NADPH and the reductase enzymatically, its reduced, CO-difference spectrum has no peak at about 450 nm and has only a small peak at about 420 nm, probably due to its inactivation in spite of the catalytically full activity in the same preparation. The absolute spectrum of the aromatase exhibits a Soret peak at 423 nm in the absence of testosterone and addition of testosterone to the aromatase sample makes its absorption peak shift gradually from 423 to 393 nm (high spin type peak), which is a usual characteristic in the spectrum of cytochrome P-450. The reconstituted aromatase system efficiently catalyzes aromatization of 4-androstenedione, 19-hydroxy-4-androstenedione as well as testosterone. 16α-Hydroxy-4-androstenedione and 16α-hydroxytestosterone are also aromatized less efficiently and 19-nortestosterone is aromatized least efficiently. The reconstituted aromatase could scarcely oxidize various xenobiotics examined, suggesting a strict and narrow substrate specificity of this enzyme. The antibody against the purified aromatase inhibits the aromatization of testosterone in human placental microsomes by more than 80%. Western blotting analysis indicated that human placental microsomes possess only one immunoreactive protein which has the same molecular weight (51,000 daltons) as the purified aromatase, and its content in placental microsomes is 2–4 μg/mg of protein. These results suggest that the purified aromatase may be a unique form different from the aromatase cytochrome P-450 (55,000 daltons) reported recently by several groups.
A model for insulin binding to the insulin receptor (1994)

The affinities of a number of insulin analogues for the human insulin receptor, a truncated soluble form of the insulin receptor, and the human insulin-like growth factor 1 receptor were determined. Insulin analogues with substitutions in the A13 or B17 positions were shown to have anomalous binding properties. This suggests that these positions, which are located in the hexamer-forming surface on the opposite side of the molecule from the classical binding site, constitute a second domain of the molecule important for receptor binding. In the present work, a model is proposed where each of the two alpha subunits of the insulin receptor contributes with a different binding region to the formation of the high-affinity binding site. Subsequently, a second molecule of insulin is able to bind to a low-affinity site involving only one of the alpha subunits, thus accounting for the curvilinear Scatchard plot. The affinity of the low-affinity site could be estimated using a high-affinity insulin analogue as the tracer. The model also provides the framework for a molecular explanation of the negative cooperativity phenomenon.
Combined treatment with interferon alpha‐2b and ribavirin for chronic hepatitis C in patients with a previous non‐response or non‐sustained response to interferon alone (1995)

Ten patients with chronic hepatitis C, six of whom had not responded and four of whom had responded in a non-sustained fashion to interferon-alpha treatment alone, were given interferon alpha-2b and ribavirin in combination during 24 weeks. Interferon alpha-2b was given subcutaneously, at a dose of 3 MU thrice weekly, together with ribavirin orally, at a dose of 1,000-1,200 mg/day. All four patients with a prior non-sustained response to interferon alone had normal alanine aminotransferase (ALT) levels at the end of treatment as well as during follow-up (> or = 24 weeks post treatment). Furthermore, all four lost serum HCV-RNA at the end of treatment and three continued to be negative during follow-up. Among patients with a prior non-response to interferon alone three of six had normal ALT levels at the end of treatment and one at follow-up. Two of six became HCV-RNA negative at cessation of treatment, one of whom was negative also at follow-up. All former non-sustained responders and one of six non-responder patients thus showed a sustained biochemical response with eradication of HCV-RNA from serum in all cases but one. It is concluded that combination therapy with interferon alpha-2b and ribavirin offers a chance of sustained biochemical response with eradication of the viremia in patients who have not shown a persistent response to interferon-alpha alone.