gebhart/patrepeval huggingface dataset:
Chiral Recognition:  Design and Preparation of Chiral Stationary Phases Using Selectors Derived from Ugi Multicomponent Condensation Reactions and a Combinatorial Approach (2003)

Combinatorial approaches together with high-throughput screening have been used to develop highly selective stationary phases for chiral recognition. Libraries of potential chiral selectors have been prepared by the Ugi multicomponent condensation reactions and screened for their enantioselectivity using the reciprocal approach involving a chiral stationary phase with immobilized model target compound N-(3,5-dinitrobenzoyl)-alpha-l-leucine. The best candidates were identified from the library of phenyl amides of 2-oxo-azetidineacetic acid derivatives. This screening also enabled specification of the functionalities of the selector desired to achieve the highest level of chiral recognition. The substituents of the phenyl ring adjacent to the chiral center of the selector candidates exhibited the most profound effect on the chiral recognition. The best candidate was then synthesized on a larger scale, resolved into single enantiomers using preparative enantioselective HPLC, and attached to porous poly(2-hydroxyethyl methacrylate-co-ethylene dimethacrylate) beads via an ester linkage to afford the desired stationary phase. Selectivities alpha as high as 3.2 were found for the separation of a variety of amino acid derivatives.
Synthesis and Evaluation of Trimetoquinol Derivatives:  Novel Thromboxane A2/Prostaglandin H2 Antagonists with Diminished β-Adrenergic Agonist Activity (1997)

Trimetoquinol (TMQ, 1) is a unique catecholamine with a strong stereodependence for agonism at beta-adrenergic (S > > R) and antagonism at thromboxane A2/prostaglandin H2 (TP; R > > S) receptors. Our laboratory has reported the effects of N-alkylation and modification of the trisubstituted benzyl group in these receptor systems. For iodinated derivative 5, maintaining potency in TP receptor systems (112%) was coupled with maintaining limited potency in beta-adrenergic receptor systems (34% for beta 1 and 47% for beta 2). In this study, several diverse TMQ derivatives were prepared to probe for binding interactions specific to a particular receptor system. Planar amidine 2, which was designed to explore the importance of TMQ's chiral center, showed a dramatic loss of potency (< 1%) in each receptor system. Likewise, the homologation of a previously described N-benzyl derivative (3) to the N-phenylethyl derivative 4 also showed reduced potency (< 3%) in both receptor systems. However, modification of the trimethoxybenzyl group of TMQ to a 4-hydroxy-3-nitrobenzyl group (7) provided a unique lead for TMQ derivatives with significant potency in TP receptor systems (91%) and reduced potency in beta-adrenergic receptor systems (4% for beta 1 and 19% for beta 2).
Repurposing Approach Identifies Auranofin with Broad Spectrum Antifungal Activity That Targets Mia40-Erv1 Pathway (2017)

Current antifungal therapies have limited effectiveness in treating invasive fungal infections. Furthermore, the development of new antifungal is currently unable to keep pace with the urgent demand for safe and effective new drugs. Auranofin, an FDA-approved drug for the treatment of rheumatoid arthritis, inhibits growth of a diverse array of clinical isolates of fungi and represents a new antifungal agent with a previously unexploited mechanism of action. In addition to auranofin's potent antifungal activity against planktonic fungi, this drug significantly reduces the metabolic activity of <i>Candida</i> cells encased in a biofilm. Unbiased chemogenomic profiling, using heterozygous <i>S. cerevisiae</i> deletion strains, combined with growth assays revealed three probable targets for auranofin's antifungal activity-<i>mia40, acn9</i>, and <i>coa4</i>. Mia40 is of particular interest given its essential role in oxidation of cysteine rich proteins imported into the mitochondria. Biochemical analysis confirmed auranofin targets the Mia40-Erv1 pathway as the drug inhibited Mia40 from interacting with its substrate, Cmc1, in a dose-dependent manner similar to the control, MB-7. Furthermore, yeast mitochondria overexpressing Erv1 were shown to exhibit resistance to auranofin as an increase in Cmc1 import was observed compared to wild-type yeast. Further <i>in vivo</i> antifungal activity of auranofin was examined in a <i>Caenorhabditis elegans</i> animal model of <i>Cryptococcus neoformans</i> infection. Auranofin significantly reduced the fungal load in infected <i>C. elegans</i>. Collectively, the present study provides valuable evidence that auranofin has significant promise to be repurposed as a novel antifungal agent and may offer a safe, effective, and quick supplement to current approaches for treating fungal infections.
Logical Analysis of the Talmudic Rules of General and Specific (Klalim-u-Pratim) (2011)

This article deals with a set-theoretic interpretation of the Talmudic rules of General and Specific, known as Klal and Prat (KP), Prat and Klal (PK), Klal and Prat and Klal (KPK) and Prat and Klal and Prat (PKP).
Increased Expression of Brain-Derived Neurotrophic Factor Preserves Retinal Function and Slows Cell Death from Rhodopsin Mutation or Oxidative Damage (2003)

There are no effective treatments for inherited retinal degenerations, which are prevalent causes of visual disability. Several proteins promote the survival of various types of neurons, and increasing expression of one or more of these survival factors is a promising strategy for a new treatment. Studies examining the effects of intravitreous injections of brain-derived neurotrophic factor (BDNF) in models of inherited retinal degenerations have suggested that BDNF has little survival-promoting activity for photoreceptors. In this study, we generated double transgenic mice with doxycycline-inducible expression of BDNF in the retina. In a model of primary rod photoreceptor degeneration, expression of BDNF resulted in significant delay in photoreceptor cell death and maintenance of retinal function assessed by electroretinogram recordings. Expression of BDNF also caused strong protection of photoreceptors from oxidative damage-induced cell death. These data suggest that continuous expression of BDNF, unlike intravitreous injections, results in morphologic and functional benefit in animal models of inherited retinal degeneration. Double transgenic mice with inducible expression of survival factors provide valuable tools for selection of survival factor candidates for gene therapy.
Adenovirus-Mediated Factor VIII Gene Expression Results in Attenuated Anti-Factor VIII-Specific Immunity in Hemophilia A Mice Compared with Factor VIII Protein Infusion (2001)

Hemophilia A patients are typically treated by factor VIII (FVIII) protein replacement, an expensive therapy that induces FVIII-specific inhibitors in approximately 30% of patients with severe hemophilia. FVIII gene therapy has the potential to improve the current treatment protocols. In this report, we used a hemophilia A mouse model to compare the humoral and cellular immune responses between an E1/E2a/E3-deficient adenovirus expressing human FVIII directed by a liver-specific albumin promoter and purified recombinant FVIII protein infusion. Adenovirus-mediated FVIII expression did not elicit detectable CD4+ or CD8+ T cell responses and induced a weak antibody immune response to FVIII. In contrast, FVIII protein administration resulted in a potent anti-FVIII antibody response and moderate CD4+ T cell response. Furthermore, hemophiliac mice preimmunized with FVIII protein infusion to induce anti-FVIII immunity, and subsequently treated by adenovirus-mediated FVIII gene therapy, expressed therapeutic levels of FVIII despite the presence of low levels of anti-FVIII antibodies. No FVIII was detected in the plasma of mice with intermediate or high antibody levels, although anti-FVIII antibody levels in some vector-treated animals declined. The data support the hypothesis that liver-specific gene therapy-mediated expression of FVIII may be less immunogenic than traditional protein replacement therapy.
Data from Phase I Dose-Escalation and -Expansion Study of Telisotuzumab (ABT-700), an Anti–c-Met Antibody, in Patients with Advanced Solid Tumors (2023)

&lt;div&gt;Abstract&lt;p&gt;This first-in-human phase I study evaluated the pharmacokinetics, safety, and preliminary efficacy of telisotuzumab, formerly called ABT-700, an antagonistic antibody directed against c-Met. For dose escalation (3+3 design), 3 to 6 patients with advanced solid tumors were enrolled into four dose cohorts (5–25 mg/kg). In the dose-expansion phase, a subset of patients was prospectively selected for &lt;i&gt;MET&lt;/i&gt; amplification (FISH screening). Patients received telisotuzumab intravenously on day 1 every 21 days. For dose expansion, 15 mg/kg was chosen as the dose on the basis of safety, pharmacokinetics, and other data from the escalation cohorts. Forty-five patients were enrolled and received at least one dose of telisotuzumab (dose escalation, &lt;i&gt;n&lt;/i&gt; = 15; dose expansion, &lt;i&gt;n&lt;/i&gt; = 30). Telisotuzumab showed a linear pharmacokinetics profile; peak plasma concentration was proportional to dose level. There were no acute infusion reactions and no dose-limiting toxicities were observed. The most common treatment-related adverse events included hypoalbuminemia (&lt;i&gt;n&lt;/i&gt; = 9, 20.0%) and fatigue (&lt;i&gt;n&lt;/i&gt; = 5, 11.1%). By Response Evaluation Criteria In Solid Tumors (RECIST), 4 of 10 (40.0%) patients with &lt;i&gt;MET&lt;/i&gt;-amplified tumors had confirmed partial response in target lesions (one ovarian, two gastric, and one esophageal), two (20.0%) had stable disease, three (30.0%) had progressive disease; one patient was unable to be evaluated. Among patients with nonamplified tumors (&lt;i&gt;n&lt;/i&gt; = 35), no objective responses were observed; however, 11 patients had stable disease per RECIST criteria. In conclusion, telisotuzumab has an acceptable safety profile with clinical activity observed in patients with &lt;i&gt;MET&lt;/i&gt;-amplified advanced solid tumors.&lt;/p&gt;&lt;/div&gt;
Characterization of Multi-Core Fiber Group Delay with Correlation OTDR and Modulation Phase Shift Methods (2020)

Using a Correlation-OTDR and a modulation phase shift method we characterized four multi-core fibers. The results show that the differential delay depends on the position of the core in the fiber and varies with temperature.
ChemInform Abstract: EMD 95885, a New Eliprodil Analogue with Higher Affinity for the N‐ Methyl‐D‐aspartate (NMDA) Receptor. (1997)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ChemInform Abstract: Chiral Synthesis via Organoboranes. Part 5. Asymmetric Allylboration via Chiral Allyldialkylboranes. Synthesis of Homoallylic Alcohols with Exceptionally High Enantiomeric Excess (1986)

Abstract Das aus (+)‐a‐Pinen (I) zugängliche optisch aktive Allylbomn (IV) reagiert mit Aldehyden (V) mit hoher Enantioselcktivität zu den Homoallylalkoholen (VI).
Low vision system for rapid near- and far-field magnification switching (2015)

People suffering from low vision, a condition caused by a variety of eye-related diseases and/or disorders, find their ability to read greatly improved when text is magnified between 2 and 6 times. Assistive devices currently on the market are either geared towards reading text far away (~20 ft.) or very near (~2 ft.). This is a problem especially for students suffering from low vision, as they struggle to flip their focus between the chalkboard (far-field) and their notes (near- field). A solution to this problem is of high interest to eye care facilities in the developing world - no devices currently exist that have the aforementioned capabilities at an accessible price point. Through consultation with specialists at L.V. Prasad Eye Institute in India, the authors propose, design and demonstrate a device that fills this need, directed primarily at the Indian market. The device utilizes available hardware technologies to electronically capture video ahead of the user and zoom and display the image in real-time on LCD screens mounted in front of the user's eyes. This design is integrated as a wearable system in a glasses form-factor.
Trading off the costs of inference vs. probing in diagnosis (1995)

This paper proposes a new algorithm which when provided the relative costs of computation vs. probing minimizes the total cost of diagnosis. During the diagnosis process the decision of whether to probe or to compute is dependent on the expected costs and benefits of each alternative. It is unlikely that we will be able to find general analytic and simple-to-compute models for the costs and benefits. Therefore, we base our algorithm on simple empirically derived models of costs and benefits. With these models, our algorithm operates by continuously choosing the optimum action to make next. This algorithm will not blow up on the rare pathological cases and will always (on average) find diagnoses at equal to or better cost than a conventional GDE/Sherlock. When the cost of probing is high, then our algorithm behaves exactly the same as GDE/Sherlock. When the cost of computation is high, the algorithm performs the diagnosis at far lower cost than GDE/Sherlock.
Pharmacokinetics of ADS-5102 (Amantadine) Extended Release Capsules Administered Once Daily at Bedtime for the Treatment of Dyskinesia (2018)

ADS-5102 can be administered once-daily qhs to achieve high amantadine plasma concentrations in the morning and throughout the day, when symptoms of dyskinesia occur.
The BOOMERANG North America Instrument: A Balloon‐borne Bolometric Radiometer Optimized for Measurements of Cosmic Background Radiation Anisotropies from 0.3 to 4o (2002)

We describe the BOOMERANG North America instrument, a balloon-borne bolometric radiometer designed to map the cosmic microwave background (CMB) radiation with 0.3degrees resolution over a significant portion of the sky. This receiver employs new technologies in bolometers, readout electronics, millimeter-wave optics and filters, cryogenics, scan, and attitude reconstruction. All these subsystems are described in detail in this paper. The system has been fully calibrated in flight using a variety of techniques, which are described and compared. Using this system, we have obtained a measurement of the first peak in the CMB angular power spectrum in a single, few hour long balloon flight. The instrument described here was a prototype of the BOOMERANG Long Duration Balloon experiment.
Modeling of surface roughness in deeply etched photonic MEMS mirrors and filters (2022)

We study the impact of the surface roughness on the response of deeply etched silicon Bragg mirrors and resonators. The transfer matrix method is extended to account for the roughness in multilayered systems. The model is first verified numerically using the finite difference time domain (FDTD) method for surface roughness values up to 80 nm at a wavelength of 1550 nm. The response of the mirrors and filters having an RMS roughness of 30 nm is calculated by the developed model and compared with the numerical results of the FDTD results, and it shows a good agreement. Then the model results are compared with the experimental data of a Bragg mirror and filter, fabricated by the deep reactive ion etching Bosch process of silicon on an insulator wafer; they show a very good agreement in the insertion loss and 3-dB bandwidth due to the roughness model. Finally, the transmission, 3-dB bandwidth and quality factor of the optical filters based on single, double, and triple silicon layer mirrors are examined using the model and accounting for Gaussian beam excitation. The presented model can be used to guide the requirements on the fabrication quality of optical surfaces and the choice of the optimum number of layers.
93 Sacituzumab govitecan in uterine and ovarian carcinosarcomas (2019)

<h3>Objectives</h3> Carcinosarcomas (CS) are highly aggressive gynecologic malignancies containing both carcinomatous and sarcomatous elements. Sacituzumab govitecan (SG) is a novel antibody-drug conjugate (ADC) targeting trophoblast antigen 2 (Trop-2), a cell surface glycoprotein highly expressed in many epithelial tumors, to deliver SN-38, the active metabolite of irinotecan. This study aimed to evaluate the efficacy of SG in primary CS cell lines and xenografts. <h3>Methods</h3> Trop-2 expression in primary tumor cell lines and cell viability after exposure to SG, non-targeting control ADC (h679-CL2A-SN-38), and naked parental antibody hRS7 IgG were evaluated using flow-cytometry-based-assays. Antibody-dependent-cell-cytotoxicity (ADCC) against Trop-2+ and Trop-2- CS cell lines was evaluated <i>in vitro</i> using 4-h Chromium-release-assays. <i>In vivo</i> activity of SG was tested against Trop-2+ CS xenografts. <h3>Results</h3> High expression of Trop-2 was detected in 55,5% (5 of 9) of primary CS cell lines. Primary tumors overexpressing Trop-2 were significantly more sensitive to SG when compared to control ADC (p&lt;0.05). Both SG and parental hRS7 mediated high level of ADCC against Trop2+ CS cell lines while no cytotoxicity was detected against Trop-2 negative tumors. Importantly, SG also induced bystander killing of Trop-2 negative tumors. <i>In vivo</i> experiments with SG demonstrated significantly greater antitumor effects and increased survival compared to control ADC (p&lt;0.05). SG therapy was well tolerated by the animals. <h3>Conclusions</h3> SG demonstrated remarkable antitumor activity against biologically aggressive CS overexpressing Trop-2 and due to its hydrolizable linker may cause a significant bystander killing effect in CS with heterogenous TROP-2 expression. Clinical trials are warranted.
Supplementary Figure 2 from α<sub>v</sub>β<sub>3</sub>/α<sub>v</sub>β<sub>5</sub> Integrins-FAK-RhoB: A Novel Pathway for Hypoxia Regulation in Glioblastoma (2023)

Supplementary Figure 2 from α&lt;sub&gt;v&lt;/sub&gt;β&lt;sub&gt;3&lt;/sub&gt;/α&lt;sub&gt;v&lt;/sub&gt;β&lt;sub&gt;5&lt;/sub&gt; Integrins-FAK-RhoB: A Novel Pathway for Hypoxia Regulation in Glioblastoma
Valorization of coffee bean waste: a coffee bean waste derived multifunctional catalyst for photocatalytic hydrogen production and electrocatalytic oxygen reduction reactions (2016)

The valorization of coffee bean waste (CBW) by producing nitrogen doped porous carbon with photocatalytic and electrocatalytic properties using a silica templating method.
2-Substituted-2,4-endo-dimethyl-8-oxabicyclo[3.2.1]octan-3-ones as catalysts for the asymmetric epoxidation of some alkenes with Oxone® (2002)

A range of 2-substituted-2,4-dimethyl-8-oxabicyclo[3.2.1]octan-3-ones 13–18 are available in four steps and in states of high optical purity. The fluoroketone 18 was shown to be a catalyst for the asymmetric epoxidation of stilbene, (E)-methylstilbene, phenylstilbene and chalcone (59–68% ee at 24–67% conversion) using Oxone® as the primary oxidant.
Adhesive and Composite Properties of a New Phenylethynyl Terminated Imide (2002)

A relatively new phenylethynyl terminated imide oligomer (PETI) from the reaction of 2,3,3&amp;apos;,4&amp;apos;- biphenyltetracarboxylic dianhydride, 4,4&amp;apos;-oxydianiline and endcapped with 4phenylethynylphthalic anhydride at a calculated number average molecular weight of 5000 g/mole was evaluated as an adhesive and composite matrix. The asymmetric dianhydride imparts a low melt viscosity to the oligomer and a high glass transition temperature to the cured resin. Preliminary adhesive work with titanium (6A1-4V) adherend gave good room temperature (RT) tensile shear strengths and excellent retention of RT strength at 260C. Preliminary composite work using unsized IM7 carbon fiber provided moderate to high mechanical properties. The chemistry, mechanical, and physical properties of the new PETI in neat resin, adhesive and composite form are presented.
Optical Crossbar Switch with Semiconductor Optical Amplifiers (1993)

Semiconductor optical amplifiers (SOAs) have a number of attractive properties for use in photonic switches. SOAs offer nanosecond switching times, extinction ratios in excess of 40 dB, and small signal gains of approximately 15 dB. In addition they can be monolithically integrated, and thus can potentially be fabricated in volume and used in large switch matrices. Here we report on our recent demonstration of an 8×8 optical crossbar switch based upon discrete SOAs. Other authors [1-3] have reported on SOA-based optical switches at the device level. Our work focuses on the demonstration of the technology at the system level. This demonstration is a significant step towards the widespread use of SOA-based optical switches because it provides a testbed for exploring and identifying the relationships between device parameters and system performance requirements. A block diagram of the optical crossbar switch is shown in Figure 1. The switch is constructed in a modular fashion and consists of optical, digital, analog, and computer modules. Figure 2 shows two photographs of the completed optical crossbar switch.
Episodes from the Continuous Search for Solutions against Downy Mildew Diseases (2019)

DOAJ is a unique and extensive index of diverse open access journals from around the world, driven by a growing community, committed to ensuring quality content is freely available online for everyone.
Suppressing molecular motions for enhanced room-temperature phosphorescence of metal-free organic materials (2015)

Metal-free organic phosphorescent materials are attractive alternatives to the predominantly used organometallic phosphors but are generally dimmer and are relatively rare, as, without heavy-metal atoms, spin-orbit coupling is less efficient and phosphorescence usually cannot compete with radiationless relaxation processes. Here we present a general design rule and a method to effectively reduce radiationless transitions and hence greatly enhance phosphorescence efficiency of metal-free organic materials in a variety of amorphous polymer matrices, based on the restriction of molecular motions in the proximity of embedded phosphors. Covalent cross-linking between phosphors and polymer matrices via Diels-Alder click chemistry is devised as a method. A sharp increase in phosphorescence quantum efficiency is observed in a variety of polymer matrices with this method, which is ca. two to five times higher than that of phosphor-doped polymer systems having no such covalent linkage.
Analysis of trimethylgallium decomposition by high-resolution mass spectrometry (2020)

Abstract The decomposition of trimethylgallium (Ga(CH 3 ) 3 ) was examined under H 2 and N 2 atmospheres using a high-resolution (about 0.002 u) time-of-flight mass spectrometry system, which enabled the separation of N 2 and ethene (C 2 H 4 ) signals. Under H 2 atmosphere, the main decomposition product was methane (CH 4 ) formed by the hydrogenolysis of Ga(CH 3 ) 3 . However, under N 2 atmosphere, the main product is ethane (C 2 H 6 ) at temperature lower than 660 °C. Above 660 °C, the C 2 H 6 further decomposes into CH 4 , acetylene (C 2 H 2 ) and C 2 H 4 , and the main components in the gas phase are C 2 H 2 and C 2 H 4 above 1000 °C. Since these are effective carbon dopants, the molar ratio of H 2 to the Ga(CH 3 ) 3 raw material in the carrier gas should be maintained above 300 to inhibit the formation of hydrocarbons in N 2 .
Investigation of founder effects for the Thr377Met Myocilin mutation in glaucoma families from differing ethnic backgrounds. (2007)

The Thr377Met myocilin mutation has arisen at least three separate times. Evidence for genetic founder effects in this prevalent age-related, yet heterogeneous, disease has important implications for future gene identification strategies.