gebhart/patrepeval huggingface dataset:
Arylaminoheterocycles. II. Arylaminopyrimidines (1944)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTArylaminoheterocycles. II. ArylaminopyrimidinesC. Kenneth BanksCite this: J. Am. Chem. Soc. 1944, 66, 7, 1131Publication Date (Print):July 1, 1944Publication History Published online1 May 2002Published inissue 1 July 1944https://pubs.acs.org/doi/10.1021/ja01235a023https://doi.org/10.1021/ja01235a023research-articleACS PublicationsRequest reuse permissionsArticle Views164Altmetric-Citations11LEARN 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
An enzyme(s) that converts glutaminyl-peptides into pyroglutamyl-peptides. Presence in pituitary, brain, adrenal medulla, and lymphocytes. (1987)

The mechanism for the post-translational conversion of glutamine to pyroglutamic acid on the N terminus of newly synthesized peptides and proteins is unknown. An assay is reported that permits measurement of the rate of conversion of Gln-His-Pro-NH2 to pyroGlu-His-Pro-NH2 (TRH). Using this assay, we demonstrate that the spontaneous cyclization of the N-terminal glutamine of this peptide occurs only slowly under physiological conditions. Furthermore, we describe the presence in rat brain, porcine pituitary, and human B lymphocytes of an enzyme(s) which converts Gln-His-Pro-NH2 into pyroGlu-His-Pro-NH2. The enzyme(s) appears to be a glycoprotein, is maximally active at neutral pH, has a Mr of 55,000, and contains catalytically significant sulfhydryl groups. The product of the enzymatic reaction was confirmed by high resolution fast atom bombardment-mass spectrometry. In preliminary studies, we find that over 90% of the enzyme in bovine adrenal medulla is contained in the soluble chromaffin vesicle fraction. These findings indicate that in vivo the post-translational conversion of a glutaminyl-peptide into a pyroglutamyl-peptide is neither spontaneous nor abiotic as has been previously proposed.
Stimulation of adenylate cyclase activity in cultured endothelial cells subjected to cyclic stretch. (1990)

While vascular endothelial cells are repeatedly stretched by the pulsatile nature of cardiac output, in vitro models traditionally used to study vascular biology involve static culture techniques. We have recently shown that pulsatile stretching of endothelial cells in culture will increase their rates of proliferation and regulate their secretion of macromolecules. The aim of this study was to determine whether membrane adenylate cyclase is involved in intracellular signalling during pulsatile stress. Bovine aortic endothelial cells were seeded on flexible-bottomed culture wells (3 x 10(5) cells/25 mm well) and allowed to attach for 48 hours. The culture wells were placed in a vacuum-operated stress providing instrument and subjected to 0.5 s of 24% strain, 0.5 s relaxation (60 cycles/min) for 0, 1, 3, 5, 7, 10 and 15 minutes (N = 24 wells/time point). Cells were homogenized and a crude membrane preparation (27,000 x g) was assayed for adenylate cyclase under basal and forskolin (100 microM) stimulated conditions. The results indicate that there is a time-dependent increase in both basal and stimulated adenylate cyclase with cyclic deformation and suggest that there may be a "stretch receptor" coupled to adenylate cyclase which can modulate endothelial cell function with hemodynamic changes.
Iterated register coalescing (1996)

An important function of any register allocator is to target registers so as to eliminate copy instructions. Graph-coloring register allocation is an elegant approach to this problem. If the source and destination of a move instruction do not interfere, then their nodes can be coalesced in the interference graph. Chaitin's coalescing heuristic could make a graph uncolorable (i.e., introduce spills); Briggs et al. demonstrated a conservative coalescing heuristic that preserves colorability. But Briggs's algorithm is too conservative and leaves too many move instructions in our programs. We show how to interleave coloring reductions with Briggs's coalescing heuristic, leading to an algorithm that is safe but much more aggressive.
Modulation of lysyl oxidase activity toward peptidyl lysine by vicinal dicarboxylic amino acid residues. Implications for collagen cross-linking. (1994)

The substrate specificity of lysyl oxidase has been explored with synthetic oligopeptides. kcat/Km increased with increasing peptide length in Ac-(Gly)n-Lys-(Gly)n-CONH2 (n = 1-5). Using 11-mers as the standard peptide length, Glu immediately N-terminal to Lys increased kcat/Km 8.8-fold over that for the -Lys-Glu- sequence and 4.9-fold over the glutamate-free control. Kinetic constants were significantly less perturbed when Glu was 2 or more residues distant from Lys. Replacement of Glu in -Glu-Lys- with Gln significantly increased Km and lowered kcat/Km. Asp rather than Glu N-terminal to Lys decreased Km similar to that of the -Glu-Lys- 11-mer, although the kcat decreased considerably, indicating that lysyl oxidase responds to the side chain length of vicinal Asp or Glu at this position. -Asp-Glu-Lys- within an 11-mer was not oxidized, although this sequence is oxidized within the N-terminal telopeptide of the alpha 1(I) chain in type I collagen fibrils. Thus, lysyl oxidase exhibits distinct preferences for sequences vicinal to lysine. These results are discussed with respect to a model requiring collagen fibril formation prior to oxidation of lysine in collagen by lysyl oxidase.
Involvement of calcitonin gene-related peptide in migraine: regional cerebral blood flow and blood flow velocity in migraine patients (2008)

Calcitonin gene-related peptide (CGRP)-containing nerves are closely associated with cranial blood vessels. CGRP is the most potent vasodilator known in isolated cerebral blood vessels. CGRP can induce migraine attacks, and two selective CGRP receptor antagonists are effective in the treatment of migraine attacks. It is therefore important to investigate its mechanism of action in patients with migraine. We here investigate the effects of intravenous human alpha-CGRP (halphaCGRP) on intracranial hemodynamics. In a double-blind, cross-over study, the effect of intravenous infusion of halphaCGRP (2 mug/min) or placebo for 20 min was studied in 12 patients with migraine without aura outside attacks. Xenon-133 inhalation SPECT-determined regional cerebral blood flow (rCBF) and transcranial Doppler (TCD)-determined blood velocity (V (mean)) in the middle cerebral artery (MCA), as well as the heart rate and blood pressure, were the outcome parameters. No change of rCBF was observed at the end of infusion [1.2% +/- 1.7 with halphaCGRP, vs. -1.6% +/- 3.1 with placebo (mean +/- SD)] (P = 0.43). V (mean) in MCA decreased to 13.5% +/- 3.6 with halphaCGRP versus 0.6% +/- 1.8 with placebo (P < 0.005). Since rCBF was unchanged, this indicates a dilation of the MCA. halphaCGRP induced a decrease in MAP (12%) (P < 0.005) and an increase in heart rate (58%) (P < 0.0001). CGRP dilates cerebral arteries, but the effect is so small that it is unlikely to be the only mechanism of CGRP-induced migraine.
Adeno-associated virus (AAV) as a vector for gene transfer into glial cells of the human central nervous system. (1994)

To examine the potential of AAV as a vector for gene transfer in glial cells, an established astrocytoma cell line and short-term cultures derived from human oligodendroglioma have been coinfected with AAV and helper adenovirus. The level of AAV replication in glioma cells was high indicating that they express receptors for AAV.
Curcumin and its Derivatives: Their Application in Neuropharmacology and Neuroscience in the 21st Century (2013)

Curcumin (diferuloylmethane), a polyphenol extracted from the plant Curcuma longa, is widely used in Southeast Asia, China and India in food preparation and for medicinal purposes. Since the second half of the last century, this traditional medicine has attracted the attention of scientists from multiple disciplines to elucidate its pharmacological properties. Of significant interest is curcumin's role to treat neurodegenerative diseases including Alzheimer's disease (AD), and Parkinson's disease (PD) and malignancy. These diseases all share an inflammatory basis, involving increased cellular reactive oxygen species (ROS) accumulation and oxidative damage to lipids, nucleic acids and proteins. The therapeutic benefits of curcumin for these neurodegenerative diseases appear multifactorial via regulation of transcription factors, cytokines and enzymes associated with (Nuclear factor kappa beta) NFκB activity. This review describes the historical use of curcumin in medicine, its chemistry, stability and biological activities, including curcumin's anti-cancer, anti-microbial, anti-oxidant, and anti-inflammatory properties. The review further discusses the pharmacology of curcumin and provides new perspectives on its therapeutic potential and limitations. Especially, the review focuses in detail on the effectiveness of curcumin and its mechanism of actions in treating neurodegenerative diseases such as Alzheimer's and Parkinson's diseases and brain malignancies.
λgt22, an improved λ vector for the directional cloning of full-length cDNA (1987)

Journal Article λgt22, an improved λ vector for the directional cloning of full-length cDNA Get access Jang H. Han, Jang H. Han Hormone Research Institute and Department of Biochemistry and Biophysics, University of CaliforniaSan Francisco, CA, USA * Present Address: Dept of Virus & Cell Biology, Merck Sharp & Dohme Research Laboratory, West Point, PA 19486 Search for other works by this author on: Oxford Academic PubMed Google Scholar William J. Rutter William J. Rutter Hormone Research Institute and Department of Biochemistry and Biophysics, University of CaliforniaSan Francisco, CA, USA Search for other works by this author on: Oxford Academic PubMed Google Scholar Nucleic Acids Research, Volume 15, Issue 15, 11 August 1987, Page 6304, https://doi.org/10.1093/nar/15.15.6304 Published: 11 August 1987 Article history Received: 24 March 1987 Published: 11 August 1987
[Hepatitis C virus RNA in tumor tissues of Chinese liver cancer patients]. (1994)

A total of 38 specimens of liver cancer and pericancerous tissues from 30 hepatocellular carcinoma patients were studied for hepatitis C virus (HCV) RNA by RT-PCR using primers from the s'non-coding regions of HCV viral genome. Serum anti-HCV of these patients was also assayed as a marker of infection. The results showed that 10/30 (33.3%) hepatocellular carcinoma (HCC) patients were infected by HCV, while 23/30 (76.7%) by hepatitis B virus (HBV). The HCV RNA from liver cancer tissues were characterized by type II and III through restriction enzyme digestion. Sequencing of the 5'-NC regions amplified revealed that this region was conserved. Since 8 of the 10 HCV infected HCC patients were coinfected with HBV, chronic infection caused by HCV and HBV might be one of the factors leading to HCC.
Peptide Aptamers: Specific Inhibitors of Protein Function (2004)

In recent years, peptide aptamers have emerged as novel molecular tools that are useful for both basic and applied aspects of molecular medicine. Due to their ability to specifically bind to and inactivate a given target protein at the intracellular level, they provide a new experimental strategy for functional protein analyses, both in vitro and in vivo. In addition, by using peptide aptamers as "pertubagens", they can be employed for genetic analyses, in order to identify biochemical pathways, and their components, that are associated with the induction of distinct cellular phenotypes. Furthermore, peptide aptamers may be developed into diagnostic tools for the detection of a given target protein or for the generation of high-throughput protein arrays. Finally, the peptide aptamer technology has direct therapeutic implications. Peptide aptamers can be used in order to validate therapeutic targets at the intracellular level. Moreover, the peptide aptamer molecules themselves should possess therapeutic potential, both as lead structures for drug design and as a basis for the development of protein drugs.
Real-time prediction of structural and optical properties of hollow-core photonic bandgap fibers during fabrication (2013)

We formulate a simple model based on mass conservation to accurately predict the structural parameters of hollow-core photonic bandgap fibers from knowledge of the second stage preforms from which they are drawn. We show that combining this model with precalculated property maps can allow real-time prediction of the optical properties of manufactured fibers.
MUI-free receiver for a synchronous DS-CDMA system based on block spreading in the presence of frequency-selective fading (2000)

We discuss a synchronous direct-sequence code division multiple-access (DS-CDMA) system based on block spreading in the presence of frequency-selective fading. Note that block spreading, which is also known as chip interleaving, refers to a spreading of a data block sequence, which is obtained by dividing a data symbol sequence into consecutive blocks. For such a system, we develop a simple new receiver that completely removes the multiuser interference (MUI) without using any channel information. The MUI-free operation is obtained by the use of a shift-orthogonal set of code sequences on which this receiver is based. Within the framework of the MUI-free receiver, we further present a subspace deterministic blind single-user channel estimation algorithm. As a benchmark for the MUI-free receiver and the corresponding subspace deterministic blind single-user channel estimation algorithm, we consider the linear multiuser equalizer and the corresponding subspace deterministic blind multiuser channel estimation algorithm developed by Liu and Xu (1996) for a standard synchronous DS-CDMA system in the presence of frequency-selective fading. We show that the complexity of the MUI-free receiver using the corresponding subspace deterministic blind single-user channel estimation algorithm is much smaller than the complexity of the linear multiuser equalizer using the corresponding subspace deterministic blind multiuser channel estimation algorithm. We further show that the performance of the MUI-free receiver is comparable with the performance of the linear multiuser equalizer. This is for the case in which the channels are known as well as for the case in which the channels are estimated with the corresponding subspace deterministic blind channel estimation algorithm.
A novel regulatory mechanism for whey acidic protein gene expression. (1989)

When primary mouse mammary epithelial cells (PMME) are cultured on a basement membrane type matrix, they undergo extensive morphogenesis leading to the formation of 3-dimensional alveoli-like spherical structures surrounding a closed lumen. We show for the first time that cells cultured on basement membrane-type matrix express high levels of whey acidic protein (WAP) mRNA and secrete the protein into the lumen. The expression of WAP appears to be dependent upon the formation of the alveoli-like spheres: prevention of sphere formation by fixation or drying of the matrix abolishes the expression of WAP. Co-culturing PMME on native and fixed basement membrane matrix indicates that the suppression of WAP expression is dominant, thereby revealing the existence of a diffusible inhibitor(s). The inhibitory activity is present in the conditioned medium of PMME cultured on plastic surface and floating collagen gels, substrata that do not form alveoli and do not allow WAP expression. These findings are consistent with the model that the synthesis, or the action, of the WAP inhibitory factor is regulated by the tissue-like multicellular organization of mammary cells. When PMME do not have correct 3-dimensional structures, one (or more) inhibitor is secreted into the medium which suppresses WAP expression by an autocrine or paracrine mechanism. Nuclear run-on experiments suggest that the suppression of WAP expression is posttranscriptional. These results have obvious bearings on the understanding of the mechanisms by which cell-cell and cell-extracellular matrix interaction regulate tissue specific gene expressions.
Inhibiting Immune Checkpoints for the Treatment of Bladder Cancer (2016)

Immune checkpoint blockade is an exciting cancer treatment modality which is demonstrating impressive clinical results across multiple tumour types. For UC, anti-PD directed therapy represents a much needed treatment in the metastatic, post chemotherapy context. Potential for these agents to have clinical utility in non-metastatic UC is still to be assessed.
Acceptor Specificity and Inhibition of the Bacterial Cell‐Wall Glycosyltransferase MurG (2003)

A continuous fluorescence coupled enzyme assay was developed to study the acceptor specificity of the glycosyltransferase MurG toward different lipid I analogues with various substituents replacing the undecaprenyl moiety. It was found that most lipid I analogues are accepted as substrates and, amongst these, the saturated C14 analogue exhibits the best activity. This substrate was used to evaluate the inhibition activity of such antibiotics as moenomycin, vancomycin, and two chlorobiphenyl vancomycin derivatives. A vancomycin derivative with a chlorobiphenyl moiety on the aglycon section was identified as a potent inhibitor of MurG.
Cavity ringdown spectroscopy with widely tunable swept-frequency lasers (2006)

The paper reports an efficient way to record a single cavity ringdown (CRD) spectroscopy data point per FSR in real time, by measuring the time interval for the CRD decay to drop from one preset level to another. Registering a data point for each build-up and decay event, without logging the full CRD waveform at each laser frequency, imposes much less demand on digitizer memory depth and data processing. Data-acquisition schemes of this type are able to generate characteristic spectroscopic signatures for key gas-sensing applications, such as security screening for airborne chemical agents.
A rough introduction (1992)

You did the groundwork for this section of your project when you decided on your reasons for studying a topic and thought about your aims. In addition, while you were transcribing your spoken material or looking over your written material, you will have gained some idea of the areas in which some interesting features occurred. What you need to do now is to put this information together in the form of a few paragraphs. An important consideration from the outset is to convey interest and enthusiasm about your project. The introduction need not be long. In fact, it is often better if it is brief and succinct, so that you can quickly get down to the meat of the project — the analysis.
Bioengineered tissues in wound healing: a progress report (2011)

An extensive number of bioengineered tissues have been studied and published in the medical literature. Due to the number of released data for these biologics, the purpose and utility often becomes ambiguous. Despite this difficulty, the therapeutic options continue to be advantageous for the practicing clinicians and can regularly provide manageable outcomes for acute, chronic and difficult-to-heal wounds. The purpose of this article is to review the many biologics that have been studied or released over the past decade and comment on data supporting or refuting their use.
Design and implementation of MaRS: a routing testbed (1992)

This paper presents the design and implementation of MaRS, a discrete-event simulation testbed for developing routing algorithms for wide-area computer networks. MaRS allows the user to define a network configuration consisting of physical network, routing algorithm and workload. The user can control its simulation, log the values of selected parameters, and save, load and modify network configurations. To accomodate a variety of network configurations and performance measures, MaRS is structured in two parts: a simulation engine, which manages the event list and user interface; and a set of components for modeling the network configuration and handling certain simulation functions. We have used MaRS to evaluate and compare several next-hop routing algorithms.
Facile methods for generating human somatic cell gene knockouts using recombinant adeno-associated viruses (2004)

Emerging evidence suggests that recombinant adeno-associated viral (rAAV) vectors can be used for specific gene targeting in human somatic cells. We have developed an rAAV vector construction procedure employing fusion PCR and a single cloning step that considerably simplifies the knockout process. We demonstrate its utility by disrupting genes at specific positions within human colon cancer cells as well as within immortalized normal epithelial cells. This technology should be broadly applicable to in vitro studies that require the manipulation of the human genome.
Disruption of ADAM3 Impairs the Migration of Sperm into Oviduct in Mouse1 (2009)

Sperm from four different gene-disrupted mouse lines (calmegin [Clgn], Adam1a, Adam2, and Ace) are known to have defective zona-binding ability. Moreover, it is also reported that the sperm from all of these mouse lines exhibit another common phenotype of impaired migration into oviduct despite the large number of sperm found in uterus after coitus. On the other hand, the sperm from the Adam3-disrupted mouse line was reported to have defects in binding ability to zona, but were able to move into the oviduct. In order to clarify the difference, we investigated the migration of ADAM3-null sperm into oviduct precisely by visualizing the sperm by using acrosin-green fluorescent protein as a tag. As a result, in contrast to previous observations, it was demonstrated that the Adam3-disrupted sperm were unable to migrate into the oviduct after coitus. It was ultimately shown that, in five out of five different gene-disrupted mouse lines, the phenotype of impaired sperm binding to zona pellucida was accompanied by the loss of ability of sperm to migrate into the oviduct. This indicates a close relationship between the two phenomena, and also that sperm migration into the oviduct is a crucial step for fertilization.
Preparation of Collagen–Glycosaminoglycan Copolymers for Tissue Regeneration (2003)

Certain analogs of the extracellular matrix (ECM) have been shown to possess surprising morphogenetic activity during healing of lesions in various anatomical sites. This chapter describes methods for synthesis of the two ECM analogs that have been studied most extensively. The reader is referred to descriptions of these methods in the original literature (1-3). The biological activity of ECM analogs has been reviewed elsewhere (4).