gebhart/patrepeval huggingface dataset:
Synthesis of (S)- and (R)-4[(methoxycarbonyl)methyl]-2-azetidinone by chemicoenzymic approach (1981)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of (S)- and (R)-4[(methoxycarbonyl)methyl]-2-azetidinone by chemicoenzymic approachMasaji Ohno, Susumu Kobayashi, Takamasa Iimori, Yi-Fong Wang, and Toshio IzawaCite this: J. Am. Chem. Soc. 1981, 103, 9, 2405–2406Publication Date (Print):May 1, 1981Publication History Published online1 May 2002Published inissue 1 May 1981https://pubs.acs.org/doi/10.1021/ja00399a043https://doi.org/10.1021/ja00399a043research-articleACS PublicationsRequest reuse permissionsArticle Views678Altmetric-Citations117LEARN 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
Characterization of higher avidity monoclonal antibodies produced by murine B-cell hybridoma variants selected for increased antigen binding of membrane Ig. (1988)

Somatic mutation in the Ig genes plays a major role in the increase of antibody affinity observed in secondary immunologic responses. It has been shown that the mechanism responsible for the high rate of somatic mutation in the Ig genes was active not only in normal B lymphocytes but also in B-cell hybridomas secreting mAb. Also, it has been reported that B-cell hybridomas were positive for membrane Ig of the same specificity as the secreted mAb. The presence of membrane Ig suggested that somatic variants secreting mAb of higher affinity could be selected by the increased capacity of these hybridoma cells to bind immobilized Ag. This hypothesis was tested with hybridoma cells secreting an IgM mAb reacting with the A Ag of the ABO blood group system. In two selection experiments, we have isolated several variant cell lines secreting mAb of increased avidity for the A Ag under similar IgM concentrations. Biochemical characterization of one of the variant mAb indicated that the mutation responsible for the increased avidity has occurred in the heavy chain gene. The method developed may have profound implications for the diagnostic and therapeutic use of mAb and will permit the study, in an in vitro system, of the role of somatic mutations in antibody diversity.
Functional Structure of Spontaneous Sleep Slow Oscillation Activity in Humans (2009)

This work gives a quantitative picture of spontaneous SSO activity during NREM sleep: we unveil how SSO features are modulated by sleep stage, site of origin and detection location of the waves. Our measures on SSOs shape indicate that, as in animal models, onsets of silent states are more synchronized than those of neural firing. The differences between sleep stages could be related to the reduction of arousal system activity and to the breakdown of functional connectivity. The frontal SSO prevalence could be related to a greater homeostatic need of the heteromodal association cortices.
Diagnosis of bovine virus diarrhoea by two enzyme-linked immunosorbent assays (1993)

Two enzyme-linked immunosorbent assays (ELISAs) for the diagnosis of bovine virus diarrhoea (BVD) are described: CHEKIT-BVD-VIRUS and CHEKIT-BVD-SERO. The first test detects virus antigen in leucocytes, resulting in identification of persistently-infected animals, while the second detects antibodies to BVD virus (BVDV). It is well known that even persistently-infected animals may have antibodies to heterologous BVDV strains. These animals are still negative to the CHEKIT-BVD-SERO test because of immunotolerance to conserved virus antigens. Data on these two tests are summarised and a scheme is presented for the diagnosis of BVD using a combination of these two tests.
Acetylcholine-Activated Potassium Channel as a Novel Target for AF Treatment (2012)

Atrial fibrillation (AF) is the most frequently encountered cardiac arrhythmia in the clinical practice with prevalence of over 2,200,000 and 1,300,000 in the United States and Japan, respectively. The prevalence of AF is strongly age dependent; less than 1% of individuals aged <60 years, but approximately 5% of those older than 65 years and about 8% of those older than 80 years are affected by AF (Furberg et al., 1994; AF is not lethal arrhythmia but associated with an increased long-term risk of stroke, heart failure, and all-cause mortality One of the most debilitating consequences of AF is the accompanying risk of stroke, which occurs in an estimated 60,000 patients with AF per year in the United States Antiarrhythmic drug therapy remains a cornerstone to restore and maintain sinus rhythm for patient both with paroxysmal and persistent AF. However, conventional drugs such as sodium channel blockers (class I antiarrhythmic drugs) and potassium channel blockers (class III antiarrhythmic drugs) have limited efficacy, especially in persistent AF patients. Clinical studies have shown that the potassium channel blockers can terminate AF in only 30% of cases Sodium channel blockers are more effective than potassium channel blockers, but a potent sodium channel blocker, pilsicainide demonstrated a modest efficacy in converting AF to sinus rhythm, with a conversion rate of 45% within 90 min in patients with recent-onset AF compared with 8.6% on placebo and was ineffective in chronic AF In addition, these conventional drugs have severe problematic risks of ventricular proarrhythmia, such as torsade de pointes (TdP) through excessive delay of ventricular replarization Thus, the development of new antiarrhythmic agents which have more effective and safer profile is highly desirable. These days, the pharmaceutical industry has focused on "atrial-specific antiarrhythmic drug" in the search for safer drugs to terminate or prevent AF The acetylcholine-activated potassium channel (I KACh channel) is one of the most promising targets for atrial-specific antiarrhythmic agent, because the channel is more abundantly expressed in the atrial than ventricle myocytes In this article, the pathophysiolosical roles of I KACh channel in AF are summarized. In
Formal approaches to safety monitoring of clinical trials in life-threatening conditions (2000)

Large clinical trials in life-threatening conditions are usually conducted under the surveillance of a Data and Safety Monitoring Board (DSMB), whose remit is to protect the ethical and safety interests of the patients. The purpose of this paper is to describe a formal approach to safety monitoring, using a sequential safety procedure to aid the decisions made by the DSMB. This procedure is designed to recommend termination of the study as soon as evidence that the experimental treatment is worse than the control in terms of the primary safety response is so strong that it is unethical to proceed. The use of this formal sequential procedure enables probabilities of the study stopping erroneously and stopping correctly, under various degrees of experimental treatment disadvantage, to be examined. Also scenarios depicting data sets which lead to continuing or stopping can be presented. Such explorations are useful in encouraging all DSMB members to consider carefully, prior to the start of a study, the conditions under which they would seriously wish to consider termination. The implementation of these methods is described for three recently completed trials in which it has been used. Finally, our current recommendations for the design of these procedures, arising from these and other similar experiences, are given.
Public Schools: Make Them Private (1997)

A voucher system that would enable parents to choose freely the schools that their children attend is the most feasible way to improve elementary and secondary education in the US. Such a voucher system will encourage privatization of a sizeable fraction of educational services. That will unleash the drive, imagination and energy of competitive free enterprise to revolutionize the education process. The competition will froce goverment schools to improve in order to retain thier clientele. Except for a small group who have a vested interest in the present system, everyone would win: parents, students, teachers, taxpayers, private entrepreneurs and, above all, the residents of the central cities.
Synthesis, biological activity and structural study of new benzotriazole-based protein kinase CK2 inhibitors (2015)

A new series of TBB-derivatives was synthesized and characterized as CK2 inhibitors. Crystallographic analysis and docking studies were used to understand the mode of binding.
Monoclonal Antibodies to Six-Transmembrane Epithelial Antigen of the Prostate-1 Inhibit Intercellular Communication <i>In vitro</i> and Growth of Human Tumor Xenografts <i>In vivo</i> (2007)

Six-transmembrane epithelial antigen of the prostate-1 (STEAP-1) is a novel cell surface protein highly expressed in primary prostate cancer, with restricted expression in normal tissues. In this report, we show STEAP-1 expression in prostate metastases to lymph node and bone and in the majority of human lung and bladder carcinomas. We identify STEAP-1 function in mediating the transfer of small molecules between adjacent cells in culture, indicating its potential role in tumor cell intercellular communication. The successful generation of two monoclonal antibodies (mAb) that bind to cell surface STEAP-1 epitopes provided the tools to study STEAP-1 susceptibility to naked antibody therapy. Both mAbs inhibited STEAP-1-induced intercellular communication in a dose-dependent manner. Furthermore, both mAbs significantly inhibited tumor growth in mouse models using patient-derived LAPC-9 prostate cancer xenografts and established UM-UC-3 bladder tumors. These studies validate STEAP-1 as an attractive target for antibody therapy in multiple solid tumors and provide a putative mechanism for mAb-induced tumor growth inhibition.
Organs from mice deleted for NRH:quinone oxidoreductase 2 are deprived of the melatonin binding site <i>MT</i><sub>3</sub> (2004)

Two melatonin receptors (MT1 and MT2) have been cloned. A third melatonin binding site, MT3, is known with remarkable and distinct pharmacological properties. We previously reported the purification of MT3 and identified it as the enzyme dihydronicotinamide riboside:quinone reductase 2 (NQO2). To investigate the relationship between NQO2 and MT3, we generated a NQO2-/- mouse strain. These mice no longer present MT3 binding sites as measured with 2-[125I]-iodo, 5-methoxycarbonylamino-N-acetyltryptamine, the specific MT3 radioligand. These data establish NQO2 as part of the MT3 binding sites in vivo and resolve the matter of the nature of the third melatonin binding site.
Measurement of gamma-ray emission probabilities using a combination of activation and oscillation techniques: applications to <sup>171</sup>Er, <sup>181</sup>Hf, <sup>233</sup>Pa and <sup>243</sup>Pu (2007)

Emission probabilities of -rays are one of the most important decay parameters and reduction of their uncertainty is required in many fields of nuclear physics. For some radionuclides, a direct measurement of these parameters is not achievable with a sufficient accuracy due to the limitations of the usual experimental techniques. In this paper, an innovating method for measuring some -ray emission probabilities is proposed. It is based on the combination of oscillation and activation techniques. On one hand, the oscillation measurements provide an accurate estimation of the integral absorption cross sections of the studied isotope. On the other hand, the integral capture cross sections are also determined by -ray spectrometry using the relevant -rays of the capture product. The comparison of those independent results gives a direct and accurate assessment of the -ray emission probabilities. The combined method is fully described, as well for instruments and conditions as for the control of the uncertainties. It is applied to the cases of 171 Er, 181 Hf, 233 Pa and 243 Pu. The study enlightens an overestimation of (19.1 20.5)%, (28.6 12.7)% and (20.0 12.3)% of the JEFF3.1 emission probabilities of the most intense -ray of respectively 171 Er, 181 Hf and 243 Pu. In the near future, this technique will be applied to 238 Np and 244 Am.
Circumscribed palmo‐plantar hypokeratosis: a disease of desquamation? Immunohistological study of five cases and literature review (2010)

The immunohistopathologic features of CPH suggest that an altered (accelerated) corneocyte desquamation process could be the main pathological mechanism underlying the development of lesions.
The pea chloroplast membrane‐associated protein, IEP96, is a subunit of acetyl‐CoA carboxylase (1996)

Two forms of acetyl-CoA carboxylase (ACCase) have been characterized in pea (Pisum sativum L.) leaves; a heteromeric chloroplast enzyme and a homomeric, presumably cytosolic enzyme. The biotin carboxylase (BC), biotin carboxyl carrier protein (BCCP), and beta-carboxyltransferase (CT) subunits of the plastidial-ACCase have recently been characterized and cloned. To further characterize the carboxyltransferase, an improved assay for CT was developed and used to follow its partial purification. CT activity co-purifies with ACCase activity during gel permeation chromatography. However, upon anion-exchange chromatography or native PAGE, CT separates from the BC and BCCP subunits of plastidial-ACCase and ACCase activity is lost. In addition, it is demonstrated that a previously sequenced pea chloroplast cDNA of unknown function (IEP96) with a predicted molecular weight of 91 kDa encodes the alpha-CT subunit of the MS-ACCase. Antibodies raised against the first 404 amino acids of IEP96 protein detected a polypeptide with molecular weight of 91 kDa that co-eluted during gel permeation chromatography with plastidial CT and ACCase activities. These antibodies also immunoprecipitated the activities of both ACCase and CT with the concomitant precipitation of the beta-CT subunit. Furthermore, antibodies against beta-CT immunoprecipitated the IEP96 protein. Two-dimensional PAGE and DEAE purification of ACCase protein demonstrated that the beta-CT forms a tight association with the IEP96 protein. Pea leaf was fractionated into soluble and membrane fractions and the alpha-CT subunit was primarily associated with the membrane fraction. Together, these data demonstrate that IEP96 is the alpha-CT subunit of pea chloroplast ACCase.
Reevaluation of absolute luminescence quantum yields of standard solutions using a spectrometer with an integrating sphere and a back-thinned CCD detector (2009)

We reevaluate the absolute fluorescence and phosphorescence quantum yields of standard solutions by using a novel instrument developed for measuring the absolute emission quantum yields of solutions. The instrument consists of an integrating sphere equipped with a monochromatized Xe arc lamp as the light source and a multichannel spectrometer. By using a back-thinned CCD (BT-CCD) as the detector, the sensitivity for spectral detection in both the short and long wavelength regions is greatly improved compared with that of an optical detection system that uses a conventional photodetector. Using this instrument, we reevaluate the absolute fluorescence quantum yields (Phi(f)) of some commonly used fluorescence standard solutions by taking into account the effect of reabsorption/reemission. The value of Phi(f) for 5 x 10(-3) M quinine bisulfate in 1 N H(2)SO(4) is measured to be 0.52, which is in good agreement with the value (0.508) obtained by Melhuish by using a modified Vavilov method. In contrast, the value of Phi(f) for 1.0 x 10(-5) M quinine bisulfate in 1 N H(2)SO(4), which is one of the most commonly used standards in quantum yield measurements based on the relative method, is measured to be 0.60. This value is significantly larger than Melhuish's value (0.546), which was estimated by extrapolating the value of Phi(f) for 5 x 10(-3) M quinine bisulfate solution to infinite dilution using the self-quenching constant. The fluorescence quantum yield of 9,10-diphenylanthracene in cyclohexane is measured to be 0.97. This system can also be used to determine the phosphorescence quantum yields (Phi(p)) of metal complexes that emit phosphorescence in the near-infrared region: the values of Phi(p) for [Ru(bpy)(3)](2+) (bpy = 2,2'-bipyridine) are estimated to be 0.063 in water and 0.095 in acetonitrile under deaerated conditions at 298 K, while that in aerated water, which is frequently used as a luminescent reference in biological studies, is reevaluated to be 0.040.
<title>Optical advantages in retinal scanning displays</title> (2000)

Virtual Retinal Display<SUP>TM</SUP> technology is a retinal scanning display (RSD) technology being developed at Microvision, Inc., for a variety of applications including microdisplays. An RSD scans a modulated light beam onto a viewer's retina to produce a perceived image. Red, green and blue light sources, such as lasers, laser diodes or LEDs combine with Microvision's proprietary miniaturized scanner designs to make the RSD very well suited for head-worn and helmet-mounted displays (HMD). This paper compares the features of RSD technology to other display technologies such as the cathode ray tubes or matrix-based displays for HMD and other wearable display applications, and notes important performance advantages due to the number of pixel- generating elements. Also discussed are some fundamental optical limitations for virtual displays used in the HMD applications.
A Novel Approach to Arterial Thrombolysis (1999)

Achieving early, complete, and sustained reperfusion after acute myocardial infarction does not occur in approximately 50% of patients, even with the most potent established thrombolytic therapy. Bleeding is observed with increased concentrations of thrombolytics as well as with adjunctive antithrombotic and antiplatelet agents. A novel approach to enhance thrombolytic therapy is to inhibit the activated form of thrombin-activatable fibrinolysis inhibitor (TAFI), which attenuates fibrinolysis in clots formed from human plasma. Identification of TAFI in rabbit plasma facilitated the development of a rabbit arterial thrombolysis model to compare the thrombolytic efficacy of tissue-plasminogen activator (tPA) alone or with an inhibitor, isolated from the potato tuber (PTI), of activated TAFI (TAFIa). Efficacy was assessed by determining the time to patency, the time the vessel remained patent, the maximal blood flow achieved during therapy, the percentage of the original thrombus, which lysed, the percentage change in clot weight, the net clot accreted, and the release of radioactive fibrin degradation products into the circulation. The results indicate that coadministration of PTI and tPA significantly improved tPA-induced thrombolysis without adversely affecting blood pressure, activated partial thromboplastin time, thrombin clotting time, fibrinogen, or alpha-2-antiplasmin concentrations. The data indicate that inhibitors of TAFIa may comprise novel and very effective adjuncts to tPA and improve thrombolytic therapy to achieve both clot lysis and vessel patency.
Inhibition of <i>Pneumocystis carinii</i>, <i>Toxoplasma </i><i>gondii</i>, and <i>Mycobacterium avium</i> Dihydrofolate Reductases by 2,4-Diamino-5-[2-methoxy-5-(ω-carboxyalkyloxy)benzyl]pyrimidines:  Marked Improvement in Potency Relative to Trimethoprim and Species Selectivity Relative to Piritrexim (2001)

A series of previously undescribed 2,4-diamino-5-[2-methoxy-5-alkoxybenzyl]pyrimidines (3a-e) and 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines (3f-k) with up to eight CH2 groups in the alkoxy or omega-carboxyalkyloxy side chain were synthesized and tested for the ability to inhibit partially purified dihydrofolate reductase (DHFR) from Pneumocystis carinii (Pc), Toxoplasma gondii (Tg), Mycobacterium avium (Ma), and rat liver in comparison with two standard inhibitors, trimethoprim (1) and piritrexim (2). The latter drug is known to be extremely potent but shows a marked preference for binding to mammalian DHFR, whereas the former is very selective for the parasite enzymes but is a much weaker inhibitor. The underlying strategy for the synthesis of compounds 3a-k was that a hybrid structure embodying some features of both 1 and 2 might possess a more favorable combination of potency and selectivity than either parent drug. The choice of analogues 3f-k was based on the idea that the acidic omega-carboxyl group might interact preferentially with a basic center in the active site of DHFR from any of the parasite species relative to the active site of mammalian DHFR. In addition, the omega-carboxyl group was expected to improve water solubility relative to 1 or 2. In standardized spectrophotometric assays with dihydrofolate as the substrate and NADPH as the cofactor, 2,4-diamino-5-[(2-methoxy-4-carboxybutyloxy)benzyl]pyrimidine (3g) inhibited Pc DHFR with an IC(50) of 0.049 microM and rat DHFR with IC(50) of 3.9 microM. Its potency against Pc DHFR was 140-fold greater than that of 1 and close to that of 2, and its selectivity index, defined as the ratio IC(50)(rat liver)/IC(50)(P. carinii), was 8-fold higher than that of 1 and >10(4)-fold higher than that of 2. Although it was less potent and less selective against Tg than Pc DHFR, it was very potent as well as highly selective against Ma DHFR, with an IC(50) of 0.0058 microM and an IC(50)(rat liver)/IC(50)(M. avium) ratio of >600. Because of this favorable combination of potency and selectivity relative to 1 and 2, compound 3g may be viewed as a promising lead in the search for new antifolates with potential clinical activity against P. carinii and other opportunistic pathogens in patients with AIDS.
Validation and Calibration of Physical Activity Monitors in Children (2002)

The validation of the CSA and MM monitors against AEE and their calibration for sedentary, light, moderate, and vigorous thresholds certify these monitors as valid, useful devices for the assessment of physical activity in children.
The Impact of a BI-Supported Performance Measurement System on a Public Police Force (2014)

Performance measurement, as an effective tool for implementing organizational strategy and assisting ongoing control and surveillance, is broadly adopted today. The performance measurement system (PMS) explored in this case study was implemented, using business intelligence (BI) technologies, for a public police force. The system lets police commanders view and analyze the performance scores of their own units and get feedback on the success of their activities. The study examines the system's impact, through analysis of the metric results over a time period of five years. The results show that the vast majority of the metrics examined indeed improved. Further, the results underscore the moderation effect of relative metrics weights, as well as the different behavior of metrics that reflect activity versus those that reflect outcomes. The study underscores both the positive and the negative aspects of those results, and discusses their implications for future PMS implementation with BI technologies.
Iminoboronate-based dual-responsive micelles via subcomponent self-assembly for hydrophilic 1,2-diol-containing drug delivery (2017)

Iminoboronate-based dual-responsive micelles were fabricated <italic>via</italic> simple subcomponent self-assembly for delivery of hydrophilic 1,2-diol-containing drugs.