gebhart/patrepeval huggingface dataset:
An efficient and practical total synthesis of (+)-vincamine from L-aspartic acid (1990)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAn efficient and practical total synthesis of (+)-vincamine from L-aspartic acidPeter Gmeiner, Paul L. Feldman, Margaret Y. Chu-Moyer, and Henry RapoportCite this: J. Org. Chem. 1990, 55, 10, 3068–3074Publication Date (Print):May 1, 1990Publication History Published online1 May 2002Published inissue 1 May 1990https://pubs.acs.org/doi/10.1021/jo00297a023https://doi.org/10.1021/jo00297a023research-articleACS PublicationsRequest reuse permissionsArticle Views2910Altmetric-Citations94LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
RILOD: Near Real-Time Incremental Learning for Object Detection at the Edge (2019)

Object detection models shipped with camera-equipped edge devices cannot cover the objects of interest for every user. Therefore, the incremental learning capability is a critical feature for a robust and personalized object detection system that many applications would rely on. In this paper, we present an efficient yet practical system, RILOD, to incrementally train an existing object detection model such that it can detect new object classes without losing its capability to detect old classes. The key component of RILOD is a novel incremental learning algorithm that trains end-to-end for one-stage deep object detection models only using training data of new object classes. Specifically to avoid catastrophic forgetting, the algorithm distills three types of knowledge from the old model to mimic the old model's behavior on object classification, bounding box regression and feature extraction. In addition, since the training data for the new classes may not be available, a real-time dataset construction pipeline is designed to collect training images on-the-fly and automatically label the images with both category and bounding box annotations. We have implemented RILOD under both edge-cloud and edge-only setups. Experiment results show that the proposed system can learn to detect a new object class in just a few minutes, including both dataset construction and model training. In comparison, traditional fine-tuning based method may take a few hours for training, and in most cases would also need a tedious and costly manual dataset labeling step.
ChemInform Abstract: Synthesis and Biological Activity of Novel Nonnucleoside Inhibitors of HIV‐1 Reverse Transcriptase. 2‐Aryl‐Substituted Benzimidazoles. (1998)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Enhanced healing efficacy of an optimized gabapentin-melittin nanoconjugate gel-loaded formulation in excised wounds of diabetic rats (2022)

The present study aimed to design and optimize, a nanoconjugate of gabapentin (GPN)-melittin (MLT) and to evaluate its healing activity in rat diabetic wounds. To explore the wound healing potency of GPN-MLT nanoconjugate, an in vivo study was carried out. Diabetic rats were subjected to excision wounds and received daily topical treatment with conventional formulations of GPN, MLT, GPN-MLT nanoconjugate and a marketed formula. The outcome of the in vivo study showed an expedited wound contraction in GPN-MLT-treated animals. This was confirmed histologically. The nanoconjugate formula exhibited antioxidant activities as evidenced by preventing malondialdehyde (MDA) accumulation and superoxide dismutase (SOD) and glutathione peroxidase (GPx) enzymatic exhaustion. Further, the nanoconjugate showed superior anti-inflammatory activity as it inhibited the expression of interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). This is in addition to enhancement of proliferation as indicated by increased expression of transforming growth factor-β (TGF- β), vascular endothelial growth factor-A (VEGF-A) and platelet-derived growth factor receptor-β (PDGFRB). Also, nanoconjugate enhanced hydroxyproline concentration and mRNA expression of collagen type 1 alpha 1 (Col 1A1). In conclusion, a GPN-MLT nanoconjugate was optimized with respect to particle size. Analysis of pharmacokinetic attributes showed the mean particle size of optimized nanoconjugate as 156.9 nm. The nanoconjugate exhibited potent wound healing activities in diabetic rats. This, at least partly, involve enhanced antioxidant, anti-inflammatory, proliferative and pro-collagen activities. This may help to develop novel formulae that could accelerate wound healing in diabetes.
Structural Diversification of Macrolactones by Substrate‐Flexible Cytochrome P450 Monooxygenases (2005)

Abstract The substrate flexibilities of several cytochrome P450 monooxygenases involved in macrolide biosynthesis were investigated to test their potential for the generation of novel macrolides. PikC hydroxylase in the pikromycin producer Streptomyces venezuelae accepted oleandomycin as an alternative substrate and introduced a hydroxy group at the C‐4 position, which is different from the intrinsic C‐12 hydroxylation position in the natural substrate. This is the first report of C‐4 hydroxylation activity of cytochrome P450 monooxygenase involved in the biosynthesis of 14‐membered macrolides. EryF hydroxylase from the erythromycin biosynthetic pathway of Saccharopolyspora erythraea and OleP oxidase from the oleandomycin biosynthetic pathway of Streptomyces antibioticus also showed a certain degree of plasticity towards alternative substrates. In particular, EryF and OleP were found to oxidize a 12‐membered macrolactone as an alternative substrate. These results demonstrate the potential usefulness of these enzymes to diversify macrolactones by post‐PKS oxidations.
Probe beam deflection study of ion exchange in self-assembled redox polyelectrolyte thin films (2003)

Probe beam deflection during chronoamperometric oxidation-reduction of osmium complex in layer-by-layer self-assembled redox active polyelectrolyte multilayers has shown that the nature of the charge in the topmost layer determines the ion flux that balances the redox charge.
Diarylthiophenes as inhibitors of the pore-forming protein perforin (2015)

Evolution from a furan-containing high-throughput screen (HTS) hit (1) resulted in isobenzofuran-1(3H)-one (2) as a potent inhibitor of the function of both isolated perforin protein and perforin delivered in situ by intact KHYG-1 NK cells. In the current study, structure-activity relationship (SAR) development towards a novel series of diarylthiophene analogues has continued through the use of substituted-benzene and -pyridyl moieties as bioisosteres for 2-thioxoimidazolidin-4-one (A) on a thiophene (B) -isobenzofuranone (C) scaffold. The resulting compounds were tested for their ability to inhibit perforin lytic activity in vitro. Carboxamide (23) shows a 4-fold increase over (2) in lytic activity against isolated perforin and provides good rationale for continued development within this class.
Longitudinal double-spin asymmetry for inclusive jet and dijet production in polarized proton collisions at s=200  GeV (2021)

The authors present the best high-precision measurements of the longitudinal double-spin asymmetry for jet and dijet production in polarized proton collisions, improving on their previous results. The data are sensitive to the gluon helicity distribution and provide new constraints.
A Bottom‐Up Proteomic Approach to Identify Substrate Specificity of Outer‐Membrane Protease OmpT (2017)

Abstract Identifying peptide substrates that are efficiently cleaved by proteases gives insights into substrate recognition and specificity, guides development of inhibitors, and improves assay sensitivity. Peptide arrays and SAMDI mass spectrometry were used to identify a tetrapeptide substrate exhibiting high activity for the bacterial outer‐membrane protease (OmpT). Analysis of protease activity for the preferred residues at the cleavage site (P1, P1′) and nearest‐neighbor positions (P2, P2′) and their positional interdependence revealed FRRV as the optimal peptide with the highest OmpT activity. Substituting FRRV into a fragment of LL37, a natural substrate of OmpT, led to a greater than 400‐fold improvement in OmpT catalytic efficiency, with a k cat / K m value of 6.1×10 6 L mol −1 s −1 . Wild‐type and mutant OmpT displayed significant differences in their substrate specificities, demonstrating that even modest mutants may not be suitable substitutes for the native enzyme.
Theoretical analyses of In incorporation and compositional instability in coherently grown InGaN thin films (2010)

Abstract We performed thermodynamic analyses to calculate the relationship between the input indium molar ratio and solid composition of a coherently grown InGaN thin film that is subjected compressive or tensile stress. The theoretical approach incorporates energy loss of a thin film system due to lattice constraint from the substrate. The results show that the indium composition x of coherently grown InGaN is lower than that of stress‐free InGaN. This represents the composition pulling effect. We also studied stable growth modes under various growth conditions. The results suggest the importance of control of partial pressure of NH 3 to optimize growth conditions of InGaN with a unique composition. (© 2010 WILEY‐VCH Verlag GmbH &amp; Co. KGaA, Weinheim)
Oxidation Behavior of 1,3-Dihydrothieno[3,4-a]HPHAC (2019)

Abstract 1,3-Dihydrothieno[3,4-a]- and 1,3,8,10-tetrahydrodithieno[3,4-a;3′4′-m]-HPHACs were prepared by the successive SNAr reactions of hexafluorobenzene with 1,3-dihydrothieno[3,4-c]pyrrole and 3,4-dihexylpyrrole followed by Scholl oxidation. Oxidation of 1,3-dihydrothieno-fused HPHACs with excess amounts of iodine at room temperature quantitatively gave the corresponding dication bis(triiodide)s. Further dehydrogenative oxidation of the dicationic species with iodine giving a thieno[3,4-a]HPHAC dication was achieved at a higher temperature by removing hydrogen iodide generated during the reaction. Neutral species of thieno[3,4-a]HPHAC could not be isolated.
Amphiphilic oligopeptides grafted to PDMS‐based diblock copolymers for use in antifouling and fouling release coatings (2015)

Amphiphilic surfaces, having both hydrophobic and hydrophilic properties, have been considered for marine antifouling and fouling release applications, as they may provide an environmentally friendly non‐biocidal alternative for surface coating. Here, we report a new class of polymers modified with amphiphilic side chains constructed from non‐natural oligopeptides. These non‐natural amino acids have a diverse array of functionalities and polarities that can be arranged in any sequence to optimize antifouling and fouling release behavior. Because of advances in solid state peptide synthesis, these peptides can be prepared on a multiple gram scale in a short period of time. Different sequences of non‐natural amino acids were synthesized to determine the effect on the physical and antifouling properties of the surface. These oligopeptide sequences were attached to a PS‐ b ‐P(DMS‐ stat ‐MVS) diblock copolymer using thiol‐ene “click” chemistry. The modified polymers were spray coated onto treated glass slides and characterized using water bubble contact angle measurements and near‐edge X‐ray absorption fine structure. The coatings were tested for antifouling and fouling release performance against spores and sporelings (young plants), respectively, of the green seaweed (alga) Ulva linza and also for non‐specific protein absorption. Copyright © 2015 John Wiley &amp; Sons, Ltd.
A mathematical measure for flexibility in communication networks (2019)

For communication networks research, flexibility of network design and networking solutions is considered a competitive advantage. However, this advantage is typically only claimed on an argumentative level and neither formally supported nor thoroughly investigated. To support the claim of flexibility and to make the flexibility of different solutions comparable, its degree must be quantified and thus made measurable. In this work, we propose a mathematical basis to quantify a degree of flexibility achieved by communication networks.We motivate that flexibility can be cast to the "size" of a set of achievable demand changes. Consequently, we propose the use of mathematical measure theory to quantify achieved networking flexibility. We derive several implications on the basic structure of flexibility, extend the insights towards a utility of flexibility and develop systematic approaches for both analytical and empirical measurement of flexibility. We apply the insights to several use-cases, showing that flexibility is in fact not as straight-forward to argue as it seems at first glance.
Pyrroloquinolone PDE5 Inhibitors with Improved Pharmaceutical Profiles for Clinical Studies on Erectile Dysfunction (2004)

We previously reported a series of potent and selective pyrimidinyl pyrroloquinolone PDE5 inhibitors such as 2a for potential use in male erectile dysfunction (MED) (Sui, Z.; Guan, J.; Macielag, M. J.; Jiang, W.; Zhang, S.; Qiu, Y.; Kraft, P., Bhattacharjee, S.; John, T. M.; Craig, E.; Haynes-Johnson, D.; Clancy, J. J. Med. Chem. 2002, 45, 4094-4096). Unfortunately, the low aqueous solubility and poor oral bioavailability rendered them undesirable development candidates. To address this issue, we designed a series of analogues using two approaches: increasing the overall basicity and reducing molecular weight of the lead. Through earlier SAR studies, we discovered that the PDE5 potency of the pyrroloquinolones is insensitive to substitution on the pyrrole nitrogen. Basic functional groups such as pyridines and benzimidazoles were appended via the aromatic ring connected to the pyrrole nitrogen. Several truncated analogues were also designed and synthesized to improve oral absorption. These modifications allowed us to identify analogues with good oral bioavailability in rats, dogs, and monkeys while the high potency against PDE5 and desirable selectivity versus other PDE isozymes were maintained. Compounds R-11e and R-11l were selected as development candidates for MED and other indications.
Biochemical characterization of ADP-ribose polymer metabolism in SLE (1996)

The metabolism of poly(ADP-ribose) in peripheral blood mononuclear (PBM) cells was studied in 13 patients with systemic lupus erythematosus (SLE) and in 12 age and sex matched controls. Poly(ADP-ribose) polymerase activity was measured as the net accumulation of ADP-ribose polymers during the conversion of 32P-NAD to poly(ADP-ribose) in PBM cells in vitro. The control population showed a mean activity of 418 +/- 91(s.d.)pmol ADP-ribose/10 min/10(6) cells. The SLE population was more heterogeneous and showed a lower mean of 225 +/- 147(s.d.)pmol ADP-ribose/10 min/10(6) cells. The mechanism of decreased ADP-ribose polymer accumulation was investigated. Measurements of turnover of the ADP-ribose polymers and its substrate, NAD+, showed that diminished ADP-ribose polymer accumulation in SLE subjects resulted from decreased poly(ADP-ribose) synthesis and not from altered rates of polymer turnover or NAD utilization. Western blot analyses of enzyme protein levels, kinetic studies of poly(ADP-ribose) polymerase activity and analyses of polymer size distribution suggested that the mechanisms of poly(ADP-ribose) synthesis in SLE cells is not altered but that the number of active poly(ADP-ribose) polymerase molecules is reduced.
NF-KB ACTIVATION BY TUMOR NECROSIS FACTOR AND INTERLEUKIN-l (2003)

Tumor necrosis factor (TNF) and interleukin-l (lL-l) are two important proin­ flammatory cytokines with overlapping and often synergizing activities. Both pro­ teins are produced mainly by monocytes/macrophages, but also by other cell types of the immune system in response to inflammation, infection and other stress-inducing factors. Although TNF was originally identified on the basis of its antitumor activity and as a mediator of cachexia, it is a pluripotent cytokine involved in cell growth modulation, inflammation, tumorigenesis, tumor meta­ stasis, viral replication, septic shock and several auto-immune diseases (Aggarwal et al., 2000). IL-l has been found to be one of the most powerful endogenous pyrogens involved in the same physiological phenomena as TNF, except for tumor modulation (Dinarello et al., 2000a-b). The pleiotropic character of TNF and IL-l is reflected by triggering of several signal transduction pathways. Whereas the cytotoxic effects of TNF result from the induction of a cell death program, the proinflammatory function of both TNF and IL-l is the consequence of transcriptional gene activation. TNF- and IL-l-activated mitogen-activated protein kinase (MAPK) p38 and c-Jun NH 2-ter­ minal kinase (JNK) modulate TNF- and IL-l-induced gene expression (Kyriakis & Avruch, 2001). Both cytokines can also activate the IKB kinase (IKK) complex leading to translocation of the transcription factor NF-KB. This chapter will focus on proteins involved in the regulation of TNF- and IL-l-induced signal trans­ duction towards activation of the IKK complex.
Biosensing Using Diffractively Coupled Plasmonic Crystals: the Figure of Merit Revisited (2014)

A refractometric biosensor with a broad range of figure of merit (FoM) is achieved in aqueous media using plasmonic crystals on a CYTOP cladding. Counterintuitively, it is demonstrated that the conventionally defined FoM is not an appropriate benchmark for biosensing performance evaluation due to the divergence of the bulk and surface sensitivities. A new surface sensitivity is thus recommended. As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Active sites in char gasification. First quarterly progress report, September 1983-December 1983 (1983)

This report reviews the background and motivation for this work, and discusses some initial scoping studies on chars similar to the model compounds to be used in later phases of the work. Some preliminary synthetic methodologies for model compounds are presented. 69 references.
Efficient Implementation on Low-Cost SoC-FPGAs of TLSv1.2 Protocol with ECC_AES Support for Secure IoT Coordinators (2019)

Security management for IoT applications is a critical research field, especially when taking into account the performance variation over the very different IoT devices. In this paper, we present high-performance client/server coordinators on low-cost SoC-FPGA devices for secure IoT data collection. Security is ensured by using the Transport Layer Security (TLS) protocol based on the TLS_ECDHE_ECDSA_WITH_AES_128_CBC_SHA256 cipher suite. The hardware architecture of the proposed coordinators is based on SW/HW co-design, implementing within the hardware accelerator core Elliptic Curve Scalar Multiplication (ECSM), which is the core operation of Elliptic Curve Cryptosystems (ECC). Meanwhile, the control of the overall TLS scheme is performed in software by an ARM Cortex-A9 microprocessor. In fact, the implementation of the ECC accelerator core around an ARM microprocessor allows not only the improvement of ECSM execution but also the performance enhancement of the overall cryptosystem. The integration of the ARM processor enables to exploit the possibility of embedded Linux features for high system flexibility. As a result, the proposed ECC accelerator requires limited area, with only 3395 LUTs on the Zynq device used to perform high-speed, 233-bit ECSMs in 413 µs, with a 50 MHz clock. Moreover, the generation of a 384-bit TLS handshake secret key between client and server coordinators requires 67.5 ms on a low cost Zynq 7Z007S device.
Selective mapping based RF watermark technique for robust data transmission in ATSC system (2018)

In the Advanced Television Systems Committee (ATSC) digital television (DTV) systems, RF watermark technique was introduced to analyze interference among DTV transmitters for single frequency networks (SFN). Recently, there is an increasing interest in employing RF watermark technique for additional data transmission. This paper proposes a selective mapping based RF watermark technique for robust data transmission. Laboratory test results demonstrate that the proposed technique can achieve an enhanced data transmission capability with backward compatibility to legacy DTV receiver.
Combining QD-FRET and Microfluidics to Monitor DNA Nanocomplex Self-Assembly in Real-Time (2009)

Advances in genomics continue to fuel the development of therapeutics that can target pathogenesis at the cellular and molecular level. Typically functional inside the cell, nucleic acid-based therapeutics require an efficient intracellular delivery system. One widely adopted approach is to complex DNA with a gene carrier to form nanocomplexes via electrostatic self-assembly, facilitating cellular uptake of DNA while protecting it against degradation. The challenge lies in the rational design of efficient gene carriers, since premature dissociation or overly stable binding would be detrimental to the cellular uptake and therapeutic efficacy. Nanocomplexes synthesized by bulk mixing showed a diverse range of intracellular unpacking and trafficking behavior, which was attributed to the heterogeneity in size and stability of nanocomplexes. Such heterogeneity hinders the accurate assessment of the self-assembly kinetics and adds to the difficulty in correlating their physical properties to transfection efficiencies or bioactivities. We present a novel convergence of nanophotonics (i.e. QD-FRET) and microfluidics to characterize the real-time kinetics of the nanocomplex self-assembly under laminar flow. QD-FRET provides a highly sensitive indication of the onset of molecular interactions and quantitative measure throughout the synthesis process, whereas microfluidics offers a well-controlled microenvironment to spatially analyze the process with high temporal resolution (~milliseconds). For the model system of polymeric nanocomplexes, two distinct stages in the self-assembly process were captured by this analytic platform. The kinetic aspect of the self-assembly process obtained at the microscale would be particularly valuable for microreactor-based reactions which are relevant to many micro- and nano-scale applications. Further, nanocomplexes may be customized through proper design of microfludic devices, and the resulting QD-FRET polymeric DNA nanocomplexes could be readily applied for establishing structure-function relationships.