gebhart/patrepeval huggingface dataset:
Evaluation criteria: a method to represent and compute technological knowledge in CAPP (2002)

The complexity of research in CAPP is, on the one hand, about the knowledge formalization of the machining expert (knowledge based on scientific models but also on experience) and, on the other hand, about the use of this knowledge to obtain a system of CAPP for general machining (knowledge valuation). The authors' method is based on three tools which allows them to: represent the process plans, describe the knowledge of a machining expert, and imagine process plans. A study of the finished part allows one to conceive many anterior stages of the workpiece and, by successive iterations to obtain raw shapes. This way, technological criteria translate machining expert knowledge, and compute and eliminate non-viable solutions step by step. The graph of representation of process plans, finally obtained, has only a few technologically viable process plans. A global evaluation can then be executed (cost study for example). In this paper, the authors develop the evaluation criteria and the construction of the graph to avoid a combinatorial explosion. The authors' experimental software LURPA-TOUR uses this method on a IBM RISC 6000 computer for turning parts.
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues (2019)

Malaria still affects around 200 million people and is responsible for more than 400,000 deaths per year, mostly children in subequatorial areas. This disease is caused by parasites of the <i>Plasmodium</i> genus. Only a few WHO-recommended treatments are available to prevent or cure plasmodial infections, but genetic mutations in the causal parasites have led to onset of resistance against all commercial antimalarial drugs. New drugs and targets are being investigated to cope with this emerging problem, including enzymes belonging to the main metabolic pathways, while nucleoside and nucleotide analogues are also a promising class of potential drugs. This review highlights the main metabolic pathways targeted for the development of potential antiplasmodial therapies based on nucleos(t)ide analogues, as well as the different series of purine-containing nucleoside and nucleotide derivatives designed to inhibit <i>Plasmodium falciparum</i> purine metabolism.
Supplemental Table 1 from RNA Sequencing of the NCI-60: Integration into CellMiner and CellMiner CDB (2023)

&lt;p&gt;Gene composite transcript levels for 23,826 genes (fragments per kilobase per million reads, FPKM)&lt;/p&gt;
Image-based reconstruction of spatial appearance and geometric detail (2003)

Real-world objects are usually composed of a number of different materials that often show subtle changes even within a single material. Photorealistic rendering of such objects requires accurate measurements of the reflection properties of each material, as well as the spatially varying effects. We present an image-based measuring method that robustly detects the different materials of real objects and fits an average bidirectional reflectance distribution function (BRDF) to each of them. In order to model local changes as well, we project the measured data for each surface point into a basis formed by the recovered BRDFs leading to a truly spatially varying BRDF representation. Real-world objects often also have fine geometric detail that is not represented in an acquired mesh. To increase the detail, we derive normal maps even for non-Lambertian surfaces using our measured BRDFs. A high quality model of a real object can be generated with relatively little input data. The generated model allows for rendering under arbitrary viewing and lighting conditions and realistically reproduces the appearance of the original object.
InsB9-23 Gene Transfer To Hepatocytes-Based Combined Therapy Abrogates Recurrence of Type-1 Diabetes After Islet Transplantation (2020)

The induction of antigen (Ag)-specific tolerance represents a therapeutic option for autoimmune diabetes. We demonstrated that administration of lentiviral vector enabling expression of insulinB9-23 (LV.InsB) in hepatocytes, arrests β cell destruction in pre-diabetic NOD mice, by generating InsB9-23-specific FoxP3+T regulatory cells (Tregs). LV.InsB in combination with a suboptimal dose of anti-CD3 mAb (combined therapy, 1X5µg CT5) reverts diabetes and prevents recurrence of autoimmunity following islets transplantation in ~50% of NOD mice. We investigated whether CT optimization could lead to abrogation of recurrence of autoimmunity. Therefore, allo-islets were transplanted after optimized CT tolerogenic conditioning (1X25µg CT25). Diabetic NOD mice conditioned with CT25 when glycaemia was &lt;500mg/dL, remained normoglycaemic for 100 days after allo-islets transplantation, displayed reduced insulitis, but independently from the graft. Accordingly, cured mice showed T cell unresponsiveness to InsB9-23 stimulation and increased Tregs frequency in islets infiltration and pancreatic LN. Additional studies revealed a complex mechanism of Ag-specific immune regulation driven by CT25, in which both Tregs and PDL1 co-stimulation cooperate to control diabetogenic cells, while transplanted islets play a crucial role, although transient, recruiting diabetogenic cells. Therefore, CT25 before allo-islets transplantation represents an Ag-specific immunotherapy to resolve autoimmune diabetes in the presence of residual endogenous β cell mass.
The Characterization of HRh(CO)2I3- and EtCORh(CO)2I3-: Two Key Intermediates in Rhodium-Catalyzed Carbonylation of Ethylene (1994)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe Characterization of HRh(CO)2I3- and EtCORh(CO)2I3-: Two Key Intermediates in Rhodium-Catalyzed Carbonylation of EthyleneD. Christopher Roe, Robert E. Sheridan, and Emilio E. BunelCite this: J. Am. Chem. Soc. 1994, 116, 3, 1163–1164Publication Date (Print):February 1, 1994Publication History Published online1 May 2002Published inissue 1 February 1994https://pubs.acs.org/doi/10.1021/ja00082a061https://doi.org/10.1021/ja00082a061research-articleACS PublicationsRequest reuse permissionsArticle Views258Altmetric-Citations24LEARN 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
Two Unusual Acetogenins from the Roots of Annona salzmanii (2003)

Two new acetogenins, parisin (1) and salzmanolin (2), were isolated from a MeOH extract of the roots of Annona salzmanii. The structures of 1 and 2 were elucidated by spectroscopic methods including LSI-MS/MS, on both the natural compounds and their acetonide derivatives (1a and 2a). Compounds 1 and 2 showed significant activity against the KB and Vero cell lines.
Effiziente Synthese von Heteroradialenen durch SN′‐Reaktion (1994)

Hervorragende Donor‐Kandidaten für Donor‐Acceptor‐Komplexe sind permethylierte Heteroradialene aufgrund ihrer elektronischen Eigenschaften. Durch bestechend einfache Synthesen konnten die Thiaradialene 1 und 2 sowie das expandierte Thiaradialen 3 hergestellt werden. 1 und 2 wurden photoelektronenspektroskopisch und cyclovoltammetrisch als elektronenreiche π‐Systeme charakterisiert. magnified image
Structure–activity relationships, kinetics, selectivity, and mechanistic studies of synthetic hydraphile channels in bacterial and mammalian cells (2005)

Hydraphile compounds are shown to be cytotoxic to Gram-negative and Gram-positive bacteria, yeast, and mammalian cells. Their cellular toxicity compares favorably with other synthetic ionophores and rivals that potency of natural antibiotics. The effects of structural variations on toxicity are described. The effects of these variations correlate well with previous studies of ion transport in liposomes. Whole cell patch clamping with mammalian cells confirms a channel mechanism in living cells suggesting that this family may comprise novel and flexible pharmacological agents.
Androgen Antagonistic Effect of Estramustine Phosphate (EMP) Metabolites on Wild-Type and Mutated Androgen Receptor (1998)

Estramustine phosphate is used frequently, alone or in combination with other antitumor agents, for the treatment of hormone-refractory prostate cancer. Estramustine phosphate is metabolically activated in vivo, and its metabolites, estramustine, estromustine, estrone, and beta-estradiol inhibit the assembly of microtubules [for review see: Kreis W, In: Concepts, Mechanisms, and New Targets for Chemotherapy (Ed. Muggia FM), pp. 163-184. Kluwer Academic Publishers, Boston, 1995]. We investigated, by displacement of [3H]methyltrienolone in the presence of 2.5 mM of triamcinolone acetonide, the binding of estramustine phosphate and its metabolites, estramustine, estromustine, estrone, and beta-estradiol, as well as other antiandrogen agents including alpha-estradiol, bicalutamide, and hydroxyflutamide, to the mutated androgen receptor (m-AR) in LNCaP cells and to the wild-type androgen receptor in wild-type AR cDNA expression plasmid (w-pAR0) cDNA-transfected HeLa cells. Analogous to the antiandrogens, bicalutamide and hydroxyflutamide, binding of estramustine phosphate metabolites to the androgen receptor was observed. The EC50 values (in microM) were: estramustine phosphate, > 10; estramustine, 3.129 +/- 0.312; estromustine; 2.612 +/- 0.584; estrone, 0.800 +/- 0.090; alpha-estradiol, 1.051 +/- 0.096; beta-estradiol, 0.523 +/- 0.028; bicalutamide, 4.920 +/- 0.361; and hydroxyflutamide, 0.254 +/- 0.012. The transactivation assay demonstrated that, analogous to bicalutamide, estramustine could not induce luciferase activity in either w-pAR0 or m-pARL transfected HeLa cells. In contrast, a strong induction of the reporter activity by dihydrotestosterone was observed. Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor. Exposure of LNCaP cells to estramustine for 24 hr caused transcriptional inhibition of PSA in a concentration-dependent manner. The levels of PSA mRNA decreased 56 and 90% when LNCaP cells were treated with 5 and 10 microM of estramustine, respectively (IC50 = 10.97 +/- 1.68 microM). Binding of hydroxyflutamide to m-AR in LNCaP cells resulted in a concentration-dependent stimulation of PSA expression, suggesting that hydroxyflutamide acted as an agonist of the m-AR. Our data indicate that estramustine phosphate metabolites perform as androgen antagonists of AR, an additional mechanism involved in the therapeutic effect of estramustine phosphate in patients with prostate cancer.
Renal Organic Solute Transporters: Relation to Serum (2010)

Hyperuricemia is associated with an increased risk of developing gout, hypertension, cardiovascular diseases such as myocardial infarction and stroke, and renal diseases such as acute urate nephropathy and nephrolithiasis, despite its beneficial role, e.g. antioxidative activity. The urate transport system of the kidney is an important determinant of the serum urate level, but clarification of its molecular mechanism remains incomplete. In 2002, our group identified URAT1, a kidney-specific urate transporter, leading to the accumulation of information concerning individual molecules involved in urate transport in the kidney. In 2008, we functionally characterized facilitatory glucose transporter family member GLUT9 as a voltage-driven urate efflux transporter URATv1 and analysis of a renal hypouricemia patient with a genetic defect in URATv1/GLUT9 gene SLC2A9 have established the main route of the urate reabsorption pathway, where urate in the urinary lumen is taken up via URAT1 and intracellular urate exits from the cell to the interstitium/blood space via GLUT9. Therapeutics designed to modify urate transport activities of these proteins might be useful in treating pathologies associated with hyperuricemia. In this review, recent findings concerning these molecules are presented.
A quantitative high-throughput screen identifies compounds that lower expression of the SCA2-and ALS-associated gene ATXN2 (2022)

CAG repeat expansions in the ATXN2 (ataxin-2) gene can cause the autosomal dominant disorder spinocerebellar ataxia type 2 (SCA2) as well as increase the risk of ALS. Abnormal molecular, motor, and neurophysiological phenotypes in SCA2 mouse models are normalized by lowering ATXN2 transcription, and reduction of nonmutant Atxn2 expression has been shown to increase the life span of mice overexpressing the TDP-43 (transactive response DNA-binding protein 43 kDa) ALS protein, demonstrating the potential benefits of targeting ATXN2 transcription in humans. Here, we describe a quantitative high-throughput screen to identify compounds that lower ATXN2 transcription. We screened 428,759 compounds in a multiplexed assay using an ATXN2-luciferase reporter in human embryonic kidney 293 (HEK-293) cells and identified a diverse set of compounds capable of lowering ATXN2 transcription. We observed dose-dependent reductions of endogenous ATXN2 in HEK-293 cells treated with procillaridin A, 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG), and heat shock protein 990 (HSP990), known inhibitors of HSP90 and Na<sup>+</sup>/K<sup>+</sup>-ATPases. Furthermore, HEK-293 cells expressing polyglutamine-expanded ATXN2-Q58 treated with 17-DMAG had minimally detectable ATXN2, as well as normalized markers of autophagy and endoplasmic reticulum stress, including STAU1 (Staufen 1), molecular target of rapamycin, p62, LC3-II (microtubule-associated protein 1A/1B-light chain 3II), CHOP (C/EBP homologous protein), and phospho-eIF2α (eukaryotic initiation factor 2α). Finally, bacterial artificial chromosome ATXN2-Q22 mice treated with 17-DMAG or HSP990 exhibited highly reduced ATXN2 protein abundance in the cerebellum. Taken together, our study demonstrates inhibition of HSP90 or Na<sup>+</sup>/K<sup>+</sup>-ATPases as potentially effective therapeutic strategies for treating SCA2 and ALS.
4-Fluoro-2-(phosphonomethyl)benzenesulfonic acid monohydrate (2000)

The title compound, C7H8FO6PS·H2O, contains both phospho­nic and sulfonic acid functionalities. An extensive network of O—H⋯O hydrogen bonds is present in the crystal structure. The three acidic protons are associated with the phospho­nate group. Two protons experience typical hydrogen-bond contacts with the sulfonate-O atoms, while the third has a longer covalent bond of 1.05 (3) Å to the phospho­nate-O atom and a short hydrogen-bond contact of 1.38 (3) Å to the water O atom (all O—H⋯O angles are in the range 162–175°). The sulfonate group is positioned so that one S—O bond is nearly coplanar with the phenyl ring [torsion angle O—S—C—C −8.6 (2)°]. The phospho­nate group is oriented approximately perpendicular to the ring [torsion angle P—C—C—C 99.2 (2)°] with one P—O bond anti to the benzyl C—C bond. The mol­ecules pack in layers in the b–c plane with the water mol­ecules in between adjacent pairs of inverted layers.
Expression of FKBP12 and ryanodine receptors (RyRs) in the spinal cord of MND patients (2005)

We investigated the FKBP12 and ryanodine receptor (RyR) immunoreactivity (IR) in the spinal cords of neurological controls and patients with motor neuron disease (MND). In the neurological controls, the cytoplasm of the spinal anterior horn neurons was stained with anti-FKBP12 antibodies and anti-RyR (type 1 and type 2) antibodies. In the MND cases, the residual neurons in the anterior horn of the spinal cord showed IR for RyR (type 1 and 2) antibodies, while weak IR for anti-FKBP12 antibodies was comparable to that of controls. The numbers of neurons recognized with the anti-FKBP 12 or anti-RyR (type 1 and 2) antibodies were counted in the anterior horn of spinal cords from the MND cases and neurological controls. Frequency of neurons stained with anti-FKBP 12 antibody was significantly decreased in the MND cases compared to that in controls (48.7+/-23.2%, 71.0+/-18.5%, respectively, mean+/-SD, p<0.0005). In the MND cases, numbers of normal-appearing, chromatolytic neurons showing IR to anti-FKBP12 (N19) antibody were significantly decreased compared to those in the controls. Immunoreactivities to anti-RyR antibodies (type 1and 2) in MND cases were present and there was no difference compared to those of the controls. Neurons in the spinal cord anterior horn of Kii-ALS cases with prolonged clinical duration were immunostained with both anti-FKBP12 and anti-RyR (type 1 and 2) antibodies similar to that in the controls. The anterior horn neurons of MND cases of short clinical duration showed absent IR to FKBP 12 antibody but present IR to RyR (type 1 and 2) antibodies. The present result suggests that FKBP12 IR was decreased in the MND cases with short clinical duration. RyR (type 1 and 2) is a major component of the intracellular calcium channel, which mediates calcium-induced calcium release. FKBP12, which is an endogenous ligand for RyR, stabilizes the calcium channels preventing calcium leakage in the absence of receptor activation. Imbalance between FKBP12 and RyR IR may play an important role in degeneration due to MND. Further study of the correlation between RyR and FKBP12 should contribute to clarifying the mechanisms of neurodegeneration in MND, including calcium-induced neuronal loss.
Diclo fenac in the treatment of osteoarthritis (2013)

Diclo fenac is a nonselective NSAID that, in its oral form, has been used for decades in the treatment of osteoarthritis. More recently, topical formulations have been developed to decrease the significant systemic exposure associated with oral diclo fenac. Several formulations of both oral and topical diclo fenac are now approved for the treatment of osteoarthritis in the USA and Europe. Although diclo fenac has generally been shown to be relatively safe, some significant safety risks have been observed. For instance, oral diclo fenac displays the classic gastrointestinal and cardiovascular effects of the NSAID class; however, topical formulations of the drug show a reduced incidence of these effects. Diclo fenac is, thus, well established as an effective and relatively safe option for the treatment for osteoarthritis.
From Lean to Extreme-Lean Well Profile: Field Experience in the Mediterranean Sea (2008)

Abstract The main subject of this paper will be to outline the field experience achieved with a new type of well profile and directional drilling system. Reducing the cost of well construction has been a driver for many new technologies. The lean casing profile introduced by Eni about a decade ago was a successful step towards lowering the drilling and completion cost in the vertical, top hole section. Automated vertical drilling tools have been the technical enabler of such concept. Recently Eni has moved further towards an even more radical "Extreme Lean Well Profile". This paper gives a brief insight into the well design concept and the enabling technology behind it. The drilling technology is based on the well-known automated vertical drilling system, which has been enhanced by the capability to drill an enlarged hole size below a casing, without compromising the verticality and hole quality. In the main part of the paper two field applications, in the Mediterannean Sea offshore Egypt, are described. The paper will also cover the lessons learned especially from the second of the first two field applications. The extreme lean well profile and automated vertical reaming technology can provide value to several drilling campaigns not only through the reduction of well construction cost. Another major benefit is the ability to run an intermediate casing string, if required because of difficult well conditions, and still arrive at the same diameter of casing in the reservoir. The completion concept as well the enabling tool technology is very unique and has not been available to the industry until recently.
Thrombelastographic method to quantify the contribution of factor XIII to coagulation kinetics (2007)

Factor XIII (FXIII) plays a critical role in clot strength, and FXIII deficiency or excess is associated with hemorrhage or thrombosis, respectively. Our goal was to design a thrombelastography-based method to characterize the effects of FXIII on plasma clot strength. Normal human plasma was exposed to 0 or 200 mug/ml anti-FXIII antibodies for 20 min prior to celite activation and calcium addition. Other plasma had addition of fibrinogen (625 mg/dl)/FXIII (2 U/ml) or 30% dilution with hydroxyethyl starch before exposure to 0 or 200 mug/ml anti-FXIII antibodies. Thromboelastography was performed and data were collected until stable clot strength was observed. The exposure of normal plasma to anti-FXIII antibodies resulted in a significant (P < 0.05) decrease in clot strength (63%) compared with plasma without antibodies. Further samples exposed to anti-FXIII antibodies had clot strength no different from FXIII-deficient plasma. The FXIII-mediated clot strength varied between 44 and 50% in hypercoagulable and hypocoagulable plasma, respectively. In conclusion, the present investigation successfully demonstrated a novel method to detect the impact of FXIII activity in plasma samples. Further actuarial investigation will be required to determine the utility of this approach in the diagnosis and treatment of patients with either acquired FXIII deficiency or excess and concordant coagulopathy.
Multichip assembly with flipped integrated circuits (1989)

A multichip module process has been developed using flipped-chip interconnection. The process uses plated copper bumps for superior thermal transport characteristics, active silicon as a substrate material for matched expansion properties, on-chip interconnection metallization that allows bumps to be placed over the active circuitry, and conventional wafer fabrication facilities for low-cost production. For successful design and fabrication of multichip assemblies, an organized methodology similar to that which has proved successful in design and assembly of single VLSI circuits was used. This approach involves: computer-aided modeling of the circuit and package for electrical, thermal, and mechanical simulation; test chips for process development and failure mechanism testing; and fabrication of actual demonstration circuits. Verification of function and reliability was then made through temperature cycle testing (-65 degrees C to 150 degrees C), exposure to accelerated moisture environments, and measure of heat dissipation properties. This approach and an example of its application to a multichip module that demonstrated successful performance on the first design pass are described.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Focus control system for laser welding (1997)

We describe a focus control system for Nd:YAG laser welding based on an optical sensor incorporated into the fiber delivery system to detect light generated by the process. This broadband light is separated into two wavelength bands, and simple electronic processing gives a signal proportional to focal error as a result of chromatic aberrations in the optical delivery system. Focus control is demonstrated for bead-on-plate welds in different thicknesses of titanium alloy, aluminum alloy, mild steel, and stainless steel. The control system works for both pulsed and continuous laser radiation.