gebhart/patrepeval huggingface dataset:
(4aS,7S,7aR)-Nepetalactam and (4aS,7S,7aR)-2-[(3R,4R,4aR,7S,7aR)-octahydro-4,7-dimethyl-1-oxocyclopenta[c]pyran-3-yl]nepetalactam. Nitrogen analogs of nepetalactone and nepetalic .psi.-anhydride (1988)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT(4aS,7S,7aR)-Nepetalactam and (4aS,7S,7aR)-2-[(3R,4R,4aR,7S,7aR)-octahydro-4,7-dimethyl-1-oxocyclopenta[c]pyran-3-yl]nepetalactam. Nitrogen analogs of nepetalactone and nepetalic .psi.-anhydrideEdmund J. Eisenbraun, David W. Sullins, Clinton E. Browne, and James N. ShooleryCite this: J. Org. Chem. 1988, 53, 17, 3968–3972Publication Date (Print):August 1, 1988Publication History Published online1 May 2002Published inissue 1 August 1988https://doi.org/10.1021/jo00252a016RIGHTS & PERMISSIONSArticle Views330Altmetric-Citations9LEARN 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 InReddit PDF (690 KB) Get e-Alertsclose Get e-Alerts
Challenges and Key Considerations of the Enhanced Permeability and Retention Effect for Nanomedicine Drug Delivery in Oncology (2013)

Enhanced permeability of the tumor vasculature allows macromolecules to enter the tumor interstitial space, whereas the suppressed lymphatic filtration allows them to stay there. This phenomenon, enhanced permeability and retention (EPR), has been the basis of nanotechnology platforms to deliver drugs to tumors. However, progress in developing effective drugs using this approach has been hampered by heterogeneity of EPR effect in different tumors and limited experimental data from patients on effectiveness of this mechanism as related to enhanced drug accumulation. This report summarizes the workshop discussions on key issues of the EPR effect and major gaps that need to be addressed to effectively advance nanoparticle-based drug delivery.
Effects of bulge composition and flanking sequence on the kinking of DNA by bulged bases (1991)

We recently showed that bulged bases kink duplex DNA, with the degree of kinking increasing in roughly equal increments as the number of bases in the bulge increases from one to four [Hsieh, C.-H., & Griffith, J.D. (1989) Proc. Natl. Acad. Sci. U.S.A. 86, 4833-4837]. Here we have examined the kinking of DNA by single A, C, G, or T bulges with different neighboring base pairs. Synthetic 30 base pair (bp) duplex DNAs containing 2 single-base bulges spaced by 10 bp were ligated head to tail, and their electrophoretic behavior in highly cross-linked gels was examined. All bulge-containing DNAs showed marked electrophoretic retardations as compared to non-bulge-containing DNA. Regardless of the sequence of the flanking base pairs, purine bulges produced greater retardations than pyrimidine bulges. Furthermore, C and T bulges produced the same retardations as did G and A bulges. Bulged DNA containing different flanking base pairs showed marked differences in electrophoretic mobility. For C-bulged DNA, the greatest retardations were observed with G.C neighbors, the least with T.A neighbors, and an intermediate amount with a mixture of neighboring base pairs. For A-bulged DNA, the retardations were greatest with G.C neighbors, less with T.A neighbors, even less with a mixture of neighboring base pairs, and finally least with C.G neighbors. Thus flanking base pairs affect C-bulged DNA and A-bulged DNA differently, and G.C and C.G flanking base pairs were seen to have very different effects. These results imply an important role of base stacking in determining how neighboring base pairs influence the kinking of DNA by a single-base bulge.
Trastuzumab Emtansine in the Treatment of HER-2 -Positive Metastatic Breast Cancer Patients (2013)

The introduction of trastuzumab in the treatment of HER-2-positive metastatic breast cancer patients favorably changed the natural history of this disease. First-line treatment with trastuzumab and taxanes demonstrated a significant improvement in overall survival and progression-free survival compared with taxane alone. Despite such a major advance, HER-2-positive metastatic breast cancer will eventually progress in most patients. Moreover chemotherapy-associated toxicities, such as myelosuppression (docetaxel) and neurotoxicity (paclitaxel), may hamper the possibility to adequately treat metastatic breast cancer and may have a negative effect on patients' quality of life. The need for more effective and better-tolerated therapy for HER-2-positive metastatic breast cancer led to the development of new anti-HER-2 agents. Pertuzumab and trastuzumab emtansine are two of the new agents that will change the approach to the treatment of HER-2-positive metastatic breast cancer. Pertuzumab is a humanized monoclonal antibody that binds HER-2 at a different epitope of the HER-2 extracellular domain (subdomain II) than that at which trastuzumab binds. Trastuzumab emtansine is a HER-2-targeted antibody-drug conjugate, composed of the cytotoxic microtubule polymerization inhibitor DM1 that is conjugated to the monoclonal antibody trastuzumab, able to selectively deliver a cytotoxic agent to HER-2-positive tumor cells. TDM-1 is superior and less toxic than lapatinib plus capecitabine in metastatic breast cancer patients previously treated with trastuzumab and taxanes, and its role as a first-line therapy is currently under investigation.
Ephrin-A Binding and EphA Receptor Expression Delineate the Matrix Compartment of the Striatum (1999)

The striatum integrates limbic and neocortical inputs to regulate sensorimotor and psychomotor behaviors. This function is dependent on the segregation of striatal projection neurons into anatomical and functional components, such as the striosome and matrix compartments. In the present study the association of ephrin-A cell surface ligands and EphA receptor tyrosine kinases (RTKs) with the organization of these compartments was determined in postnatal rats. Ephrin-A1 and ephrin-A4 selectively bind to EphA receptors on neurons restricted to the matrix compartment. Binding is absent from the striosomes, which were identified by mu-opioid receptor immunostaining. In contrast, ephrin-A2, ephrin-A3, and ephrin-A5 exhibit a different mosaic binding pattern that appears to define a subset of matrix neurons. In situ hybridization for EphA RTKs reveals that the two different ligand binding patterns strictly match the mRNA expression patterns of EphA4 and EphA7. Ligand-receptor binding assays indicate that ephrin-A1 and ephrin-A4 selectively bind EphA4 but not EphA7 in the lysates of striatal tissue. Conversely, ephrin-A2, ephrin-A3, and ephrin-A5 bind EphA7 but not EphA4. These observations implicate selective interactions between ephrin-A molecules and EphA RTKs as potential mechanisms for regulating the compartmental organization of the striatum.
Effect of Reduction Protocol of Pd Catalysts on Product Distribution in Furfural Hydrogenation (2017)

Abstract Single step conversion of furfural to ring hydrogenation and decarbonylation products, 2‐methyltetrahydrofuran (2‐MeTHF) and tetrahydrofuran (THF) in high selectivity was achieved by controlling the particle size of Pd/C catalyst. The particle size variation of Pd/C catalysts in the range of 3.8 to 22 nm could be achieved by employing different reducing agents. Of particular interest was the NaBH 4 reduced catalyst (Pd−B/C), which gave the lowest crystallite size of 4.8 nm due to incorporation of B into the inner lattices of Pd−Pd. This phase was evidenced by a characteristic XRD peak of Pd−B at 2θ=38.85 O as well as a shift of (111) peak (40.07 O ) of Pd towards the lower value (39.8 O ). As compared to formaldehyde reduced catalyst (Pd−F/C), Pd−B/C catalyst completely suppressed the formation of furfuryl alcohol to give &gt; 65 % selectivity to 2‐MeTHF and THF. At 180 O C, almost equal distribution of side chain hydrogenation and ring opening products, 2‐MF (45 %) and PeDO (37 %), respectively, was observed while, higher temperature clearly favoured ring hydrogenation and decarbonylation reactions to give 2‐MeTHF and THF.
Information Theoretic Optimization of Audio Features for Multimodal Speaker Detection (2005)

We present a method that exploits an information theoretic framework to extract optimal audio features with respect to the video features. A simple measure of mutual information between the resulting audio features and the video ones allows to detect the active speaker among different candidates. The results show that our method is able to exploit the shared speech information contained in audio and video signals to recover their common source.
Derived amino acid sequence and identification of active site residues of Escherichia coli beta-hydroxydecanoyl thioester dehydrase. (1988)

The nucleotide sequence of the fabA gene encoding beta-hydroxydecanoyl thioester dehydrase, a key enzyme of the unsaturated fatty acid synthesis pathway of Escherichia coli, has been determined by the dideoxynucleotide sequencing technique. Most of the sequence was obtained by sequencing intragenic insertions of the transposon, Tn1000, isolated in vivo. A synthetic primer complementary to a portion of the inverted repeat sequences at the ends of the transposon was used to prime DNA synthesis into the flanking fabA sequences. The gene is composed of 516 nucleotides (171 amino acid residues) encoding a protein with a molecular weight of 18,800. Approximately half of the derived amino acid sequence was confirmed by automated Edman sequencing of peptides obtained by cyanogen bromide cleavage. The active site histidine residue (His-70) has been identified by analysis of the peptides labeled by reaction with 14C-labeled 3-decynoyl-N-acetylcysteamine, a specific mechanism-activated inhibitor. A cysteine residue (Cys-69) adjacent to the active site histidine may play the role in catalysis previously assigned to a tyrosine residue. We also report a simplified purification process for the dehydrase beginning with extracts of a brain which greatly overproduces the enzyme.
Angiopellosis as an Alternative Mechanism of Cell Extravasation (2016)

Stem cells possess the ability to home in and travel to damaged tissue when injected intravenously. For the cells to exert their therapeutic effect, they must cross the blood vessel wall and enter the surrounding tissues. The mechanism of extravasation injected stem cells employ for exit has yet to be characterized. Using intravital microscopy and a transgenic zebrafish line Tg(fli1a:egpf) with GFP-expressing vasculature, we documented the detailed extravasation processes in vivo for injected stem cells in comparison to white blood cells (WBCs). While WBCs left the blood vessels by the standard diapedesis process, injected cardiac and mesenchymal stem cells underwent a distinct method of extravasation that was markedly different from diapedesis. Here, the vascular wall undergoes an extensive remodeling to allow the cell to exit the lumen, while the injected cell remains distinctively passive in activity. We termed this process Angio-pello-sis, which represents an alternative mechanism of cell extravasation to the prevailing theory of diapedesis. Stem Cells 2017;35:170-180 Video Highlight: https://youtu.be/i5EI-ZvhBps.
A divide and conquer approach to least-squares estimation (1990)

The problem of estimating parameters theta which determine the mean mu ( theta ) of a Gaussian-distributed observation X is considered. It is noted that the maximum-likelihood (ML) estimate, in this case the least-squares estimate, has desirable statistical properties but can be difficult to compute when mu ( theta ) is a nonlinear function of theta . An estimate formed by combining ML estimates based on subsections of the data vector X is proposed as a computationally inexpensive alternative. The main result is that this alternative estimate, termed here the divide-and-conquer (DAC) estimate, has ML performance in the small-error region when X is appropriately subdivided. As an example application, an inexpensive range-difference-based position estimator is derived and shown by means of Monte-Carlo simulation to have small-error-region mean-square error equal to the Cramer-Rao lower bound.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Mobility Management Strategy Based on User Mobility Patterns in Wireless Networks (2007)

Mobility management plays an important role in wireless communication networks in effectively delivering services to users on the move. Many schemes have been proposed and investigated extensively in the past to improve performance. Profile-based scheme (PBS) is one of them, which uses the user routine information stored in the user profile to reduce location update signaling traffic. To improve PBS performance, in this paper, a new location management scheme called the mobility-pattern-based scheme (MPBS) is proposed, which incorporates the time information in the user profile so that a user's current location can be determined by his/her movement state and the current system time. Extensive simulations have been carried out, and the results show that the MPBS scheme can mitigate the signaling traffic load significantly while reducing paging delay at the same time
Revisiting the Role of Fat Mass in the Life Extension Induced by Caloric Restriction (1999)

One of the most robust observations in the biology of aging is that caloric restriction (CR) extends life in a variety of species. Although CR results in a severalfold decrease in fat mass (FM), the role of fat on life extension was considered to be minimal. Two main reasons accounted for this belief. First, although increased FM is associated with changes in substrate oxidation and in glucose homeostasis, in part through the effects of free fatty acids (FFA) and glycerol, several studies have suggested that longevity is determined independent of FM. Second, CR has systemic effects on a range of functions including neurological, endocrine, reproductive, immunological and antineoplastic, none of which have been historically linked to fat. In the last few years, an explosion of evidence has demonstrated that fat tissue is a very active endocrine gland which secretes a variety of peptides (such as leptin and plasminogen activating inhibitor-1), cytokines (such as tumor necrosis factor), and complement factors (such as D, C3, and B). This is in addition to the presence of substrates, such as glycerol and FFA, which are stored and released by fat cells and are known to have a major role in hepatic and peripheral glucose metabolism. We propose that many of the systemic effects of CR can now be explained by the chronic effects related to decreased plasma levels of peptides, cytokines, complement factors, and substrates. In fact, all of the benefits of CR on the neuroendocrine system and those related to the improvement in glucose homeostasis can be attributed to decrease in adipose cells and their products. Other evidence from epidemiological data in human obesity supports the role of fat mass and its body distribution as a risk factor for morbidity and mortality in humans due to impaired glucose metabolism (similar to rodents), for cancer (similar to rodents), and for the development of atherosclerotic vascular disease (in humans). If all or most of the life-extending benefits of CR can be attributed to decreased fat stores, the expression of specific candidate proteins may be explored and manipulated in the search for the most powerful adipose-dependent signals that modulate life expectancy.
Production of ferulic acid and coniferyl alcohol by conversion of eugenol using a recombinant strain of Saccharomyces cerevisiae (2013)

ABSTRACT We isolated an industrial strain of Saccharomyces cerevisiae 92411 able to convert coniferyl alcohol (2 g/l) into ferulic acid (1.8 g/l). To use eugenol as a substrate for the synthesis of natural ferulic acid, an optimized sequence of the Penicillium simplicissimum vaoA gene, encoding the flavoenzyme vanillyl‐alcohol oxidase (VAO), was expressed in the yeast 92411. To obtain a strong and stable expression of vaoA , an expression cassette flanked by Ty1 homologous sequences was constructed so the sequence encoding VAO could be integrated into various Ty1 loci of the host genome. The recombinant S. cerevisiae strain produced VAO. It synthesized ferulic acid directly from eugenol due to expression of the VAO activity and the natural ability of the strain to convert coniferyl alcohol into ferulic acid. In fermentation experiments, the strain produced up to 16.9 g/l of ferulic acid after 136 h. These results open new perspectives for the use of yeast biocatalysts in the biotechnological production of aromatic flavour from eugenol. Copyright © 2013 John Wiley &amp; Sons, Ltd.
Fc-dependent expression of CD137 on human NK cells: insights into “agonistic” effects of anti-CD137 monoclonal antibodies (2008)

CD137 (4-1BB) is a costimulatory molecule that can be manipulated for the treatment of cancer and autoimmune disease. Although it is known that agonistic antibodies (mAbs) against CD137 enhance the rejection of murine tumors in a natural killer (NK) cell- and T cell-dependent fashion, the mechanism for NK dependence is poorly understood. In this study, we evaluated the ability of 2 different glycoforms of a chimerized antihuman CD137 mAb, an aglycosylated (GA) and a low fucose form (GG), to react with human NK cells. Both mAbs bound similarly to CD137 and partially blocked the interaction between CD137 and CD137 ligand. However, unlike GA mAb, immobilized GG mAb activated NK cells and enhanced CD137 expression. These effects were seemingly dependent on Fc interaction with putative Fc receptors on the NK-cell surface, as only the immobilized Fc-fragment of GG was required for CD137 expression. Furthermore, CD137 expression could be enhanced with antibodies directed against non-CD137 epitopes, and the expression levels directly correlated with patterns of Fc-glycosylation recognized to improve Fc interaction with Fc gamma receptors. Our data suggest that CD137 can be enhanced on NK cells in an Fc-dependent fashion and that expression correlates with phenotypic and functional parameters of activation.
Modeling Coverage for Neural Machine Translation (2016)

Attention mechanism has enhanced state-of-the-art Neural Machine Translation (NMT) by jointly learning to align and translate. It tends to ignore past alignment information, however, which often leads to over-translation and under-translation. To address this problem, we propose coverage-based NMT in this paper. We maintain a coverage vector to keep track of the attention history. The coverage vector is fed to the attention model to help adjust future attention, which lets NMT system to consider more about untranslated source words. Experiments show that the proposed approach significantly improves both translation quality and alignment quality over standard attention-based NMT.
Potential Regulatory Function of Human Dendritic Cells Expressing Indoleamine 2,3-Dioxygenase (2002)

Antigen-presenting cells (APCs) can induce tolerance or immunity. We describe a subset of human APCs that express indoleamine 2,3-dioxygenase (IDO) and inhibit T cell proliferation in vitro. IDO-positive APCs constituted a discrete subset identified by coexpression of the cell-surface markers CD123 and CCR6. In the dendritic cell (DC) lineage, IDO-mediated suppressor activity was present in fully mature as well as immature CD123+ DCs. IDO+ DCs could also be readily detected in vivo, which suggests that these cells may represent a regulatory subset of APCs in humans.
Polymyxin acylase: Purification and characterization, with special reference to broad substrate specificity. (1989)

Polymyxin acylase, which produces deacylated polymyxins by hydrolyzing only the fattyacyl groups of polymyxin antibiotics without affecting the peptide moiety, was purified from acetone-dried cell powder of Pseudomonas sp. M-6-3. The cell-free enzyme, solubilized by Triton X-100, was further purified on successive DEAE-cellulose, hydroxyapatite, and Sephacryl S-300 columns to a homogeneous state. This purified enzyme (Type I) had a single band with an MW of 62, 000 in SDS-polyacrylamide gel electrophoresis. Gel filtration on a calibrated Sephacryl S-300 column also gave an estimated MW of 62, 000. The isoelectric point of the enzyme was 5.7. Enzyme activity was optimal at pH 9.0 for colistin A (polymyxin E1) and was stable up to 50°C for 24 hr. The observed Vmax and Km values were 1750nmol/min/mg and 3.85 mM, respectively. This enzyme was almost not affected by metal chelators and various thiol-enzyme inhibitors (other than p-chloromercuribenzoate), and showed high tolerance for organic modifiers; for example, half of the activity remained in 50% ethylene glycol buffer. This enzyme deacylated not only polymyxins but also various N-fattyacyl compounds (peptides and amino acids). Among several fattyacyl groups (C2-C16) of N-acyl DL-methionines, the caprinoyl (C10) group was most easily liberated, and the benzyloxycarbonyl (Z) group was also slightly susceptible. When the enzyme was solubilized in 0.2 M KCl-containing buffer by Triton X-100, the enzyme (Type II) showed a slightly different substrate specificity and an increased activity for some Z-derivatives. With this enzyme, it is possible to remove the Z group from several Z-peptides under mild conditions.
Chronic prenatal restraint stress induced memory impairment in passive avoidance task in post weaned male and female Wistar rats. (2009)

With a view to examine the effect of chronic maternal stress on cognitive function in the offspring during young age, pregnant Wistar rats were subjected to restraint stress from embryonic day 11 till delivery. Male and female pups born to these stressed rats were subjected to passive avoidance test on postnatal day 30 and 31. Results were compared with rats of the same age and sex born to control mothers, which were not stressed. The results showed that prenatal maternal restraint stress impairs the memory retention during young age in both sexes. The memory retention deficit induced by maternal restraint stress was evident in the decreased latency to enter the dark compartment of passive avoidance apparatus by the rats born to stressed mothers. The observed behavioral deficit may be due to the insult of stress on the developing hippocampus, a structure of the brain concerned with learning and memory. The results suggest that prolonged prenatal stress leads to long lasting malfunction in the behavioral development during young age in both male and female young rats. However when compared to their respective stress naïve controls, it seems evident that prenatal restraint stress has a less effect on females which could be due to their oesterogenic effects. These data reinforce the view that prenatal stress affects cognitive development in a sex-specific manner.