gebhart/patrepeval huggingface dataset:
Racemization kinetics of free and protein-bound lysinoalanine (LAL) in strong acid media. Isomeric composition of bound LAL in processed proteins (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRacemization kinetics of free and protein-bound lysinoalanine (LAL) in strong acid media. Isomeric composition of bound LAL in processed proteinsRemy Liardon, Mendel Friedman, and Georges PhilippossianCite this: J. Agric. Food Chem. 1991, 39, 3, 531–537Publication Date (Print):March 1, 1991Publication History Published online1 May 2002Published inissue 1 March 1991https://pubs.acs.org/doi/10.1021/jf00003a020https://doi.org/10.1021/jf00003a020research-articleACS PublicationsRequest reuse permissionsArticle Views138Altmetric-Citations31LEARN 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
Design, synthesis and biological evaluation of a sulfonylcyanoguanidine as thromboxane A2 receptor antagonist and thromboxane synthase inhibitor (2001)

The synthesis and the structure of N-isopropyl-N'-[2-(3'-methylphenylamino)-5-nitrobenzenesulfonyl] urea (14) was drawn from two thromboxane A2 receptor antagonists structurally related to torasemide. Compound 14 showed an IC50 value of 22 nM for the thromboxane A2 (TXA2) receptor of human washed platelets. Compound 14 prevented platelet aggregation induced by arachidonic acid (0.6 mM) and U-46619 (1 microM) with an IC50 value of 0.45 and 0.15 microM, respectively. Moreover, 14 relaxed the rat isolated aorta and guinea-pig trachea precontracted by U-46619, a TXA2 agonist. Its efficacy (IC50) was 20.4 and 5.47 nM, respectively. Finally, 14 (1 microM) completely inhibited TXA2 synthase of human platelets. The pKa value and the crystallographic data of 14 were determined and used to propose an interaction model between the TXA2 antagonists related to torasemide and their receptor.
Serotonin improves glucose metabolism by Serotonylation of the small GTPase Rab4 in L6 skeletal muscle cells (2017)

Our data suggest that 5-HT elicits its beneficial effects on Glucose metabolism through serotonylation of Rab4, which likely represents the converging point between the insulin and the 5-HT signalling cascades.
Abstract 9485: Cardiac G Protein-Coupled Receptor Kinase 2 Knockdown Decreases Ischemia/Reperfusion-Induced Injury and Improves Cardiac Function through Anti-Apoptotic Mechanisms (2010)

Background: Studies from our lab have shown that decreasing myocardial G protein-coupled receptor kinase 2 (GRK2) expression or preventing GRK2 activation with an inhibitory peptide (βARKct) can prevent or rescue heart failure after myocardial infarction. In this study we investigated the acute cardiac effects associated with lowered myocyte GRK2 expression in a mouse model of ischemia/reperfusion (I/R) injury. Methods: Cardiomyocyte-specific GRK2 knockout (KO) mice were used with either GRK2 deleted at birth or inducible GRK2 deletion along with appropriate control mice that included GRK2 floxed mice and αMHC-Cre and MerCreMer mice. All mice were subjected to sham or 30 min myocardial ischemia via coronary artery ligation followed by 24 hrs reperfusion. Cardiac function, infarct size, tissue apoptosis (TUNEL and Caspase activity) and changes in the activation state of various signaling molecules (Akt, GSK3β, ERK, p38, JNK and cytochrome C) were analyzed. Results: Echo and hemodynamic measurements showed ...
From phoshines to carbens: synthesis of new coinage metal complexes with applications in bioinorganic chemistry (2012)

N-heterocyclic carbenes (NHCs) have been extensively investigated for their similarities to phosphines as ligands. Because of their unique electron-donating ability, the lower toxicity and the possibility to tune their structure, NHCs begun to replace phosphines in the development of novel complexes showing cytotoxic properties. In particular, our research group has synthesized new Ag(I) carbene complexes from the precursors {[HB(RImH)3]Br2} (R = Bn, Mes or tBu). Stable trimetallic complexes were obtained with general formula {Ag3[HB(RIm)3]2}Br, which were successfully employed as carbene transfer reagents in the synthesis of related Au(I) complexes. We also reported the first discrete molecules with bis(triazolylidene)borate carbene ligands, Ag2[H2B(BnTz)2]2 and the homoleptic Au2[H2B(BnTz)2]2. These complexes have been recently studied for their antitumor properties. Following this line of research we are recently developing new ligands, modulating the steric and/or electronic properties, and the hydrophilic/lypophilic balance by variation of the azole ring substituents. We have also reported the synthesis of hydrophilic bimetallic complexes of general formula {Na2[H2C(AzR)2]2Ag2} (Az = Im or Tz; R = PrSO3 or EtCOO). Another evolution of this research line involves the chemistry of new water soluble zwitterionic mono-NHC ligands functionalized with hydrophilic side arms. We have synthesized the water soluble carbene ligand precursors{Im1R,3R} (R = PrSO3, CH2COOEt or CH2CONEt2) and the related Cu(I), Ag(I) and Au(I) carbene complexes. They were evaluated for their cytotoxic activity towards a panel of several human tumour cell lines.
Functional signaling pathway analysis of lung adenocarcinomas identifies novel therapeutic targets for <i>KRAS</i> mutant tumors (2015)

Little is known about the complex signaling architecture of KRAS and the interconnected RAS-driven protein-protein interactions, especially as it occurs in human clinical specimens. This study explored the activated and interconnected signaling network of KRAS mutant lung adenocarcinomas (AD) to identify novel therapeutic targets.Thirty-four KRAS mutant (MT) and twenty-four KRAS wild-type (WT) frozen biospecimens were obtained from surgically treated lung ADs. Samples were subjected to Laser Capture Microdissection and Reverse Phase Protein Microarray analysis to explore the expression/activation levels of 150 signaling proteins along with co-activation concordance mapping. An independent set of 90 non-small cell lung cancers (NSCLC) was used to validate selected findings by immunohistochemistry (IHC).Compared to KRAS WT tumors, the signaling architecture of KRAS MT ADs revealed significant interactions between KRAS downstream substrates, the AKT/mTOR pathway, and a number of Receptor Tyrosine Kinases (RTK). Approximately one-third of the KRAS MT tumors had ERK activation greater than the WT counterpart (p<0.01). Notably 18% of the KRAS MT tumors had elevated activation of the Estrogen Receptor alpha (ER-α) (p=0.02).This finding was verified in an independent population by IHC (p=0.03).KRAS MT lung ADs appear to have a more intricate RAS linked signaling network than WT tumors with linkage to many RTKs and to the AKT-mTOR pathway. Combination therapy targeting different nodes of this network may be necessary to treat this group of patients. In addition, for patients with KRAS MT tumors and activation of the ER-α, anti-estrogen therapy may have important clinical implications.
Performance Analysis of Network Composition in Ambient Networks (2007)

Abstract. Currently, resource sharing and service offering remains subject to troublesome, manual configuration and to extensive, previously established agreements. Ambient Networks have emerged to facilitate cooperation between heterogeneous networks, usually among different administrative domains and technologies. This cooperation can be achieved with the adoption of a new key networking concept which is called by composition. The performance of the composition is a key factor for determining the feasibility of Ambient Networks, since it is expected to be extensively used during a typical interaction between a user and the network, itself. This paper presents a network composition simulator and a performance evaluation that uses a voice service aimed for supporting the demands for composition. The obtained results show that, for the scenario which is under consideration, composition does no represent an obstacle when supported by a voice service. 1.
The Biology of Memory: A Forty-Year Perspective (2009)

In the forty years since the Society for Neuroscience was founded, our understanding of the biology of memory has progressed dramatically. From a historical perspective, one can discern four distinct periods of growth in neurobiological research during that time. Here I use that chronology to chart a personalized and selective course through forty years of extraordinary advances in our understanding of the biology of memory storage.
A Study of Somaclonal Variation for Rice Improvement Induced by Three Kinds of Anther-derived Cell Culture Techniques. (1994)

Somaclonal variation in rice induced in three kinds of anther-derived cell culture was morphologically studied.
In Situ Defect Spectroscopy: Probing Dangling Bonds During a-Si: H Film Growth by Subgap Absorption (2006)

This paper describes a novel optical diagnostic that was recently introduced to the field of Si-based thin films for probing defect states such as dangling bonds in a-Si:H. This diagnostic is based on the cavity ringdown spectroscopy (CRDS) technique. When applied in situ or real time during film growth it can provide new insights into the a-Si:H film properties as well as into the fundamental surface processes during growth. In this paper the CRDS technique is described and both the ex situ application on as-deposited a-Si:H films as well as the in situ application during a-Si:H film growth are presented
Homoplastic Keratomileusis for the Correction of Myopia (1985)

ABSTRACT: The authors performed primary homoplastic myopic keratomileusis (MKM) on ten eyes with a minimal followup of three months. The mean preoperative refractive error was -15.13 diopters, Postoperatively, the mean myopia was -0.89 diopter. The surgical accuracy was 93% ± 8.6% with a correlation coefficient of 0.98. Refractive astigmatism was reduced by 0.52 diopter. All patients achieved their preoperative spectacle acuity except for one patient whose vision was reduced from 20/20 to 20/25. The authors conclude that primary homoplastic MKM warrants further investigation as an alternative to autoplastic MKM and myopic epikeratophakia.
Self-aligned silicides or metals for very large scale integrated circuit applications (1986)

The increases in the packing density and the resulting shrinkage of the silicon integrated circuit dimensions led to the investigation and successful application of the deposited refractory silicide layers as the gate and interconnection metallization. The continued shrinking of the device dimensions has now turned attention to further lowering of the resistance at the gate level and to finding a contact metallization for the shallow junctions. Although refractory metals are being considered for the former, self-aligned silicides of cobalt, titanium, platinum, and nickel offer the possibility of satisfying both the gate and interconnection and contact metallization requirements. This paper will review the present status of the refractory silicide and refractory metal technologies and compare them with the upcoming self-aligned silicide technology.
Cervical Sarcoma (1983)

Ninety-six cases of cervical sarcomas have been reviewed. No standard criteria has been used in the diagnosis of these tumors. A variety of therapies has been employed in their management with an overall prognosis which is poor. Thus, this rather complex group of tumors needs better definition with the establishment of rigid criteria for diagnosis in order to evaluate various therapies.
Disposition of ceftazidime in surgical patients with intra-abdominal infection (1988)

The disposition of ceftazidime was assessed in 11 surgical patients with suspected intra-abdominal infection. All patients had normal hepatic function, and creatinine clearances ranged from 43 to 186 ml/min. Patients received 2 g of ceftazidime intravenously every 8 h. Trough and peak concentrations in serum were measured on day 2, and trough and postdose concentrations in serum were determined on 10 samples collected during a dosage interval between days 3 and 6 of therapy. Ceftazidime peak and trough concentrations in serum at steady state determined by high-performance liquid chromatography were 257.4 +/- 122.0 (mean +/- standard deviation) and 13.1 +/- 20.6 mg/liter. The serum-concentration-versus-time profile was multiexponential. The elimination half-life, steady-state volume of distribution, and total body clearance were 2.52 +/- 1.39 h, 0.31 +/- 0.12 liter/kg, and 0.11 +/- 0.05 liter/h per kg, respectively. Total predicted body clearance significantly correlated with the measured values (r = 0.868; P = 0.001). The disposition of ceftazidime is dependent on creatinine clearance and is not significantly altered by surgery or acute infectious processes.
Maximizing precision over extended unambiguous range for TOF range imaging systems (2010)

The maximum unambiguous range for time-of-flight range imaging systems is inversely proportional to the chosen modulation frequency. However, increasing the unambiguous range by decreasing the modulation frequency will generally also degrade the range measurement precision. We describe a technique that significantly extends the range of a time-of-flight imaging system without compromising range precision. This is achieved by employing two modulation frequencies simultaneously. The chosen frequencies can be a combination of high and low frequency, or two similarly high frequencies. In this paper we present experimental results comparing single frequency; dual high and low frequency; and dual high frequency operation and demonstrate that range precision need not be appreciably compromised to achieve an extended unambiguous range.
Dynamic Data Recovery from Damaged CD Media (2005)

Data recovery from damaged CD media is demonstrated on a dynamic spin stand. Types of damage include broken fragments, microwave irradiation, knurling, and sanding. Digital signal processing is used to improve probability of recovery.
Metabolism of 13C-enriched D-fructose in hepatocytes from Goto-Kakizaki rats (2003)

This study aims at assessing the conversion of exogenous D-[1-13C]fructose, D-[2-13C]fructose or D-[6-13C]-fructose (10 mM) to 13C-enriched and either hydrogenated or deuterated D-glucose, L-lactate and L-alanine released by rat liver cells prepared from Goto-Kakizaki rats and incubated for 120 min in the presence of unlabelled D-glucose (also 10 mM) and D2O. The results of this study are relevant to the relative contribution of fructokinase and hexokinase isoenzyme to the phosphorylation of D-fructose, the capacity of D-glucose to confer to glucokinase positive cooperativity towards D-fructose, the circulation of D-fructose 6-phosphate in the pentose phosphate pathway, the regulation of the cytosolic NADD/NADH ratio, the respective fate of D-fructose-derived D-glyceraldehyde and dihydroxyacetone phosphate, the deuteration of fructose-derived glycolytic intermediates at the phosphoglucoisomerase, phosphomannoisomerase, enolase, pyruvate kinase and glutamate-alanine transaminase levels, and the unequal generation of L-[1-13C]lactate by cells exposed to D-[1-13C]fructose or D-[6-13C]fructose versus D-[2-13C]-fructose.
Processing and Properties of Rare Earth Ion-Doped Bismuth Titanate Thin Films by Chemical Solution Deposition method (2003)

Ferroelectric (Bi,R)4Ti3O12 [R: rare earth] thin films were synthesized by the chemical solution deposition (CSD) method. Heat treatment above 600°C was required for the fabrication of crystalline (Bi,R)4Ti3O12 thin films of Bi-layered perovskite structure on Pt/TiOx/SiO2/Si substrates. The orientation of the films prepared at 750°C depended upon the kind of substituent rare earth ions. Bi4.12Ti3O12 (BIT) and Bi3.35La0.75Ti3O12 (BLT) thin films revealed (00l) preferred orientation. On the other hand, Bi3.35Nd0.75Ti3O12 (BNT), Bi3.35Sm0.75Ti3O12 (BST) and Bi3.35Gd0.75Ti3O12 (BGT) thin films showed random orientation with strong (117) reflection. Synthesized (Bi,R)4Ti3O12 films exhibited the typical ferroelectric behavior. The BNT thin film showed Pr of 21.6 µC/cm2, which was higher than the values of the other rare earth-doped BIT thin films.
Thickness Measurements of Silicon Dioxide Films Over Small Geometries (1968)

A simple nondestructive interferometric technique to measure to thickness of transparent films on reflecting substrates in the range of 100–20 000 Å is described. Measurements can be made over areas as small as 0.1 mil in diameter. The method utilizes a microspectrophotometer, operating in the visible region of the spectrum, to measure the intensity of reflected light. The film thickness is calculated by one of two techniques depending upon whether the thickness is greater or less than 3000 Å. The error is less than 50 Å.
Ray tracing over smooth elastic shells of arbitrary shape (1996)

An efficient numerical scheme based on ray theory is developed for the analysis of elastic waves traveling over a fluid-loaded smooth elastic shell of arbitrary shape. The shell’s surface is first discretized into a number of small patches. The local geometry of each patch is then approximated in a parametric form using bi-cubic spline functions. A local curvilinear coordinate frame is defined on each patch. The ray trajectories and ray-tube areas are obtained by solving a set of ordinary differential equations, the ray and transport equations, within each patch. Several numerical tests of the accuracy and efficiency of the scheme were carried out on spherical and ellipsoidal elastic shells. The numerical results for the spherical shell agree well with analytical solutions. The ray trajectories and the ray-tube areas over an ellipsoidal shell with three distinct semiaxes clearly illustrate the inhomogeneous and anisotropic effects due to the variable curvature on the shell’s surface. It is also observed numerically that the magnitude of the ray-tube area along a ray is directly correlated with the stability of its trajectory.
A Phase I Study of the Dolastatin-15 Analogue Tasidotin (ILX651) Administered Intravenously Daily for 5 Consecutive Days Every 3 Weeks in Patients with Advanced Solid Tumors (2005)

The maximum tolerated dose and recommended phase II dose for tasidotin when administered on this schedule was 27.3 mg/m(2)/d. The favorable toxicity profile of tasidotin compared with other antitubulin agents (particularly the lack of severe cumulative neuropathy, peripheral edema, and fatigue), the observed antitumor activity of tasidotin, and its novel mechanism of action support further disease-directed evaluations of this agent on this 5-day schedule every 3 weeks.
Formation of adenosine triphosphate from Pi and adenosine diphosphate by purified Ca-2+-adenosine triphosphatase. (1975)

Ca-2+-ATPase purified from sarcoplasmic reticulum of rabbit muscle forms a phsophoeznyme when exposed to inorganic phosphate in the presence of Mg-2+. On addition of ADP and Ca-2+ virtually all of the phosphate bound to the enzyme is transferred to form ATP. It has been shown previously and confirmed by us that (a) the purified ATPase contains one major polypeptide and about 30% phospholipids; (b) on removal of residual detergent by passage through Sephadex the enzyme forms vesicular membranes; and (c) these vesicles are leaky and incapable of accumulating Ca-2+. Our findings therefore indicate that we have observed ATP generation from ADP and P-i without the formation of an ion gradient across a membrane. We propose that the energy derived from ion-protein interaction drives the formation of ATP.
Hypervolemic short-time hemodilution: Longtime observation of hemorheological parameters (1988)

In a series 43 patients suffering from cerebral or peripheral diseases were investigated over a period of 3 days after a single hypervolemic hemodilution with 500ml low molecular weight dextran (Rheomacrodex ® ) applied within 3 hours. Changes in hematocrit, visco-elasticity of whole blood and plasma viscosity were studied. 18 to 36 hours after onset of infusion a significant increase in plasma viscosity ( <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" overflow="scroll"> <mml:mi mathvariant="italic">p</mml:mi> <mml:mo>⩽</mml:mo> <mml:mn>0.001</mml:mn> </mml:math> ) and elasticity ( <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" overflow="scroll"> <mml:mi mathvariant="italic">p</mml:mi> <mml:mo>⩽</mml:mo> <mml:mn>0.01</mml:mn> </mml:math> ) could be observed. Furthermore, there was a tendency towards higher hematocrit and whole blood viscosity levels. However, after 60 hours a second lower numerical peak for hematocrit and viscosity of whole blood could be seen, which was yet above starting values.
The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins (2015)

The long term side effects of any newly introduced drug is a subject of intense research, and often raging controversies. One such example is the dipeptidyl peptidase-IV (DPP4) inhibitor used for treating type 2 diabetes, which is inconclusively implicated in increased susceptibility to acute pancreatitis. Previously, based on a computational analysis of the spatial and electrostatic properties of active site residues, we have demonstrated that phosphoinositide-specific phospholipase C (PI-PLC) from Bacillus cereus is a prolyl peptidase using in vivo experiments. In the current work, we first report the inhibition of the native activity of PI-PLC by two DPP4 inhibitors - vildagliptin (LAF-237) and K-579. While vildagliptin inhibited PI-PLC at micromolar concentrations, K-579 was a potent inhibitor even at nanomolar concentrations. Subsequently, we queried a comprehensive, non-redundant set of 5000 human proteins (50% similarity cutoff) with known structures using serine protease (SPASE) motifs derived from trypsin and DPP4. A pancreatic lipase and a gastric lipase are among the proteins that are identified as proteins having promiscuous SPASE scaffolds that could interact with DPP4 inhibitors. The presence of such scaffolds in human lipases is expected since they share the same catalytic mechanism with PI-PLC. However our methodology also detects other proteins, often with a completely different enzymatic mechanism, that have significantly congruent domains with the SPASE motifs. The reported elevated levels of serum lipase, although contested, could be rationalized by inhibition of lipases reported here. In an effort to further our understanding of the spatial and electrostatic basis of DPP4 inhibitors, we have also done a comprehensive analysis of all 76 known DPP4 structures liganded to inhibitors till date. Also, the methodology presented here can be easily adopted for other drugs, and provide the first line of filtering in the identification of pathways that might be inadvertently affected due to promiscuous scaffolds in proteins.