gebhart/patrepeval huggingface dataset:
Syntheses and conformational analyses of some 3‐amino‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1<i>H</i>‐1‐benzazepine derivatives: X‐ray crystal structure of 35–3‐[[(1,1‐dimethylethoxy)carbonyl]amino]‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1<i>H</i>‐1‐benzazepine (1990)

Abstract The constrained dipeptide mimic 1 was synthesized from 2 in three steps with 65% overall yield. Analyses of the 1 H nmr data of a number of 3‐amino‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1 H ‐1‐benzazepine derivatives led to the conclusion that these compounds adopt a similar conformation and that this ring system is rigid. X‐ray crystallography was used to define the structure of 3 , and computer‐aided energy minimization of 6 gave a preferred conformation similar to that observed in the crystal of 3 .
Effects of clozapine on the δ‐ and κ‐opioid receptors and the G‐protein‐activated K<sup>+</sup> (GIRK) channel expressed in <i>Xenopus</i> oocytes (1998)

1. To investigate the effects of clozapine, an atypical antipsychotic, on the cloned mu-, delta- and kappa-opioid receptors and G-protein-activated inwardly rectifying K+ (GIRK) channel, we performed the Xenopus oocyte functional assay with each of the three opioid receptor mRNAs and/or the GIRK1 mRNA. 2. In the oocytes co-injected with either the delta- or kappa-opioid receptor mRNA and the GIRK1 mRNA, application of clozapine induced inward currents which were attenuated by naloxone, an opioid-receptor antagonist, and blocked by Ba2+, which blocks the GIRK channel. Since the opioid receptors functionally couple to the GIRK channel, these results indicate that clozapine activates the delta- and kappa-opioid receptors and that the inward-current responses are mediated by the GIRK channel. The action of clozapine at the delta-opioid receptor was more potent and efficacious than that at the kappa-opioid receptor. In the oocytes co-injected with the mu-opioid receptor and GIRK1 mRNAs, application of clozapine (100 microM) did not induce an inward current, suggesting that clozapine could not activate the mu-opioid receptor. 3. Application of clozapine caused a reduction of the basal inward current in the oocytes injected with the GIRK1 mRNA alone, but caused no current response in the uninjected oocytes. These results indicate that clozapine blocks the GIRK channel. 4. To test the antagonism of clozapine for the mu- and kappa-opioid receptors, we applied clozapine together with each selective opioid agonist to the oocytes co-injected with either the mu- or kappa-opioid receptor mRNA and the GIRK1 mRNA. Each of the peak currents induced by each selective opioid agonist together with clozapine was almost equal to the responses to a selective opioid agonist alone. These results indicate that clozapine has no significant antagonist effect on the mu- and kappa-opioid receptors. 5. We conclude that clozapine acts as a delta- and kappa-agonist and as a GIRK channel blocker. Our results suggest that the efficacy and side effects of clozapine under clinical conditions may be partly due to activation of the delta-opioid receptor and blockade of the GIRK channel.
Crystal Structure of the Kelch Domain of Human Keap1 (2004)

Keap1 is a substrate adaptor protein for an ubiquitin ligase complex that targets the Nrf2 transcription factor for degradation. Keap1 binds Nrf2 through its C-terminal Kelch domain, which contains six copies of the evolutionarily conserved kelch repeat sequence motif. The structure of the Kelch domain from human Keap1 has been determined by x-ray crystallography to a resolution of 1.85 A. The Kelch domain forms a 6-bladed beta-propeller structure, with residues at the C terminus forming the first strand in the first blade. Key structural roles have been identified for the highly conserved glycine, tyrosine, and tryptophan residues that define the kelch repeat sequence motif. In addition, we show that substitution of a single amino acid located within a loop that extends out from the bottom of the beta-propeller structure abolishes binding of Nrf2. The structure of the Kelch domain of Keap1 represents a high quality model for the superfamily of eukaryotic kelch repeat proteins and provides insight into how disease-causing mutations perturb the structural integrity of the Kelch domain.
Einführung (1997)

“Zuchthaus, Gefängnis und Haft, als Verbrechens-, Vergehens-, Übertretungsstrafe gedacht, unterscheiden sich voneinander nur nach der Quantität der Strafdauer und des Strafleidens, während die durch die Person der Straffälligen bedingten qualitativen Verschiedenheiten der Freiheitsstrafe lediglich die Bedeutung von Vollzugsunterschieden innerhalb dieser Strafarten haben sollen.” (RADBRUCH 1911, S. 186). Das für den Nicht-Experten sicherlich etwas exotische und sehr schwer zugängliche Feld des Strafvollzugs, welches nur selten in den Medien anzutreffen ist, blieb bisher, pädagogischen und psychologischen Interventionen zum Trotze, in Bezug zu den “richtigen Maßnahmen” für die Insassen ein weitgehend unerschlossenes Feld.
Hypnotherapy in Palliative Care (1996)

Complementary therapies have found increasing vogue in the management of patients with cancer, although little formal evaluation has been undertaken. We report on our experience of offering hynotherapy to palliative care outpatients in a hospice day care setting. During 2 1/2 years, 256 patients had hypnotherapy, all singly; two-thirds (n = 104) were women. Only 13% (n = 21) had four or more treatment sessions. At the time of survey, the 52 patients still alive were mailed an evaluation sheet, of whom 41 responded. 61% reported improved coping with their illness. 7% (n = 3) reported harmful or negative effects from hypnotherapy. Amongst those whose coping was unchanged, many found the therapy a pleasant experience. 35 respondents (85%) appended positive comments to their questionnaire returns. Despite the limitations of a retrospective questionnaire, our findings suggest that hypnotherapy, used within strict guidelines in patients with advanced cancer, is a safe complementary therapy to enhance coping.
Characterization of the methotrexate transport pathway in murine L1210 leukemia cells: involvement of a membrane receptor and a cytosolic protein (1988)

A radioiodinated photoaffinity analogue of methotrexate, N alpha-(4-amino-4-deoxy-10-methyl-pteroyl)-N epsilon-(4-azidosalicylyl)-L- lysine (APA-ASA-Lys), was recently used to identify the plasma membrane derived binding protein involved in the transport of this folate antagonist into murine L1210 cells [Price, E. M., & Freisheim, J. H. (1987) Biochemistry 26, 4757-4763]. The labeled protein has an apparent molecular weight of 46K-48K when analyzed by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, but no such labeling occurs in a methotrexate transport-defective cell line (L1210/R81). Labeling of the total cytosolic protein from disrupted cells, followed by electrophoresis and autoradiography, showed, among other proteins, a 21K band, corresponding to dihydrofolate reductase (DHFR), in both the parent and R81 cells and a 38K band only in the parent cells. However, when whole cells were UV irradiated at various times at 37 degrees C following addition of radiolabeled APA-ASA-Lys, the 38K protein and DHFR were the only cytosolic proteins labeled in the parent cells, while the intact R81 cells showed no labeled cytosolic protein, since the photoprobe is not transported. Further, when the parent cells were treated with a pulse of radiolabeled photoprobe, followed by UV irradiation at different times at 37 degrees C, the probe appeared sequentially on the 48K membrane protein and both the 38K cytosolic protein and dihydrofolate reductase.(ABSTRACT TRUNCATED AT 250 WORDS)
Challenge of the Copolymerization of Olefins with N-Containing Polar Monomers. Systematic Screening of Nickel(II) and Palladium(II) Catalysts with Brookhart and Grubbs Ligands. 2. Chain-Propagation Barriers, Intrinsic Regioselectivity, and Curtin-Hammett Reactivity (2002)

The second level of a computational screening of late-transition-metal catalysts and nitrogen-containing polar monomers toward an incorporation of amines and nitriles in the polymer chain of polyolefins is reported. The structures and energies of the transition states for the insertion of the CC bond of ethylene, propylene, acrylonitrile, and vinylamine into the metal−carbon bond of generic models for Ni(II) and Pd(II) complexes with diimine (Brookhart) and salicylaldiminato (Grubbs) ligands have been calculated using density functional theory. The calculations reveal the general trend that the activation energies for the ethylene, propylene, and acrylonitrile insertion in the Brookhart systems are similar, whereas the activation energies for the vinylamine insertion are much higher. The nickel systems show lower insertion barriers than do their palladium counterparts. For the chain propagation with the Grubbs catalysts, a Curtin−Hammett-type energy profile involving cis−trans isomerization and subsequent C−C insertion is predicted. The regioselectivity of the propylene, acrylonitrile, and vinylamine insertion is rationalized by the analysis of the frontier orbitals of the free monomers.
Effect of NH4+ ions on phi 29 DNA-protein p3 replication: formation of a complex between the terminal protein and the DNA polymerase (1987)

Ammonium ions stimulated the formation of the phi diameter 29 protein p3-dAMP initiation complex by decreasing the Km value for dATP in a purified system containing the viral terminal protein p3, the viral DNA polymerase p2, and the phi 29 DNA-protein p3 complex as a template. In addition, NH4+ ions stimulated the amount of p3-dAMP complex elongation and increased by about twofold the rate of elongation. The stimulatory effect of NH4+ ions on in vitro phi 29 DNA replication is probably related to the formation of a stable complex between the terminal protein and the DNA polymerase, which was detected only in the presence of NH4+ ions.
Methylene Blue Is Neuroprotective against Mild Traumatic Brain Injury (2014)

Traumatic brain injury (TBI) is a leading cause of death and disability worldwide. Methylene blue (MB) has known energy-enhancing and antioxidant properties. This study tested the hypothesis that MB treatment reduces lesion volume and behavioral deficits in a rat model of mild TBI. In a randomized double-blinded design, animals received either MB (n=5) or vehicle (n=6) after TBI. Studies were performed on 0, 1, 2, 7, and 14 days following an impact to the primary forelimb somatosensory cortex. MRI lesion was not apparent 1 h after TBI, became apparent 3 h after TBI, and peaked at 2 days for both groups. The MB-treated animals showed significantly smaller MRI lesion volume than the vehicle-treated animals at all time points studied. The MB-treated animals exhibited significantly improved scores on forelimb placement asymmetry and foot fault tests than did the vehicle-treated animals at all time points studied. Smaller numbers of dark-stained Nissl cells and Fluoro-Jade(®) positive cells were observed in the MB-treated group than in vehicle-treated animals 14 days post-TBI. In conclusion, MB treatment minimized lesion volume, behavioral deficits, and neuronal degeneration following mild TBI. MB is already approved by the United States Food and Drug Administration (FDA) to treat a number of indications, likely expediting future clinical trials in TBI.
Analysis of discrete implementation of generalized cross correlator (1981)

A common discrete implementation of the cross correlator uses a parabolic fit to the peak when the delay is not an integral multiple of the sampling period. This correspondence analyzes and assesses the pitfalls of this approach. It is shown that this yields a biased estimate of the time delay, with both the bias and variance of the estimate dependent on the location of the delay between samples, SNR, signal and noise bandwidths, and the prefilter or window used in the generalized correlator.
Unsupervised color image segmentation for content based application (2002)

We present an efficient unsupervised color image segmentation algorithm by combining the local and global color information. By first processing a color image via the proposed color sigma filter, pixels within the same semantic region become more concentrated around their centroid in the perceptual color coordinate system. A k-mean algorithm is then designed to automatically distinguish the image into non-overlapping semantic regions, of which centroids with similar color features are merged automatically. Because of the periodicity in the hue component, we apply two manifolds to completely cover the hue vector, and fuse distinguished regions from both manifolds to obtain the final image segmentation. The computational complexity of our algorithm is O(N), where N is the total number of pixels, and no priori information is assumed. We download sample images from the Internet randomly and apply the proposed algorithm to illustrate the performance of our procedure.
GLUCOCORTICOID ACTIVITY OF VARIOUS PROGESTERONE ANALOGS: CORRELATION BETWEEN SPECIFIC BINDING IN THYMUS AND LIVER AND BIOLOGIC ACTIVITY<sup>*</sup> (1977)

When tested in an in vitro assay system, progesterone and various analogs of this steroid were shown to compete with [3H] triamcinolone acetonide (TA) for specific glucocorticoid receptors in both rat liver and thymus. Of these analogs, the following derivatives of progesterone were potent competitors of TA binding and, when injected into adrenalectomized rats, induced regression of the thymus and marked increases in hepatic tyrosine aminotransferase activity: 11 beta-hydroxyl, 6 alpha-methyl, 6 alpha, 16 alpha-dimethyl, and 6 alpha-methyl-17 alpha-hydroxyl. In contrast, progesterone, 16 alpha-methyl, and 17 alpha-hydroxy progesterone competed with TA in vitro but failed to elicit either gluco- or antiglucocorticoid activity in vivo. Also, we observed that the oral contraceptive 6 alpha-methyl-17-(1-propynyl)testosterone competes very effectively with TA in a cell-free preparation of rat liver and induces an increase in hepatic tyrosine aminotransferase activity. The 11 beta-hydroxyl group has previously been thought to be essential for glucocorticoid activity. Our studies indicate that substitution of progesterone or testosterone with a 6 alpha-methyl group negates the need for an 11 beta-hydroxyl substitutuent as a prerequisite for glucocorticoid activity.
Bathless Dissolution: Validation of System Performance (1998)

cncomp.lss in g the system in stal ­ lation, operati o n, and, in some cases, performa nce qu alifi ca­ t io n . iVr os t ve ndo rs, und e r ­ sta nd ing that FDA ho lds th e end lIscr res po nsibl e fo r on-site val ­ i(b r io11 , have t e nde d to limi t th eir suppo rt to providing g uid­ ance v~llid . Hion protocols as a lin t: ite m o pti o n avail abl e to the use r. T ypi c<lll y, vendo rs will al so charge fo r additio nal suppo rt in deve loping t he end user's vt1l i­ datio n protocol. In some cases, wh e n t he user has purc hased direct ve ndo r va lida t ion s up­ po rt, ve ndo rs have provid ed t heir pe rsonnel to perfo rm the uscr's approved va lid ation pro­ tocol, with th e user 's quali ty uni t acting as t he review a nd :1 pprova l agen t. metbud bn:; proved to be n robust test for delenllillil1g tbe dissolution 1fIfeS of solid dosllge }orllls. 77,is flrtide f(){:lIses all vnlidlltillg fbi' pe'forlllllllce
A PDA-based high-level human-robot interaction (2005)

This paper describes an innovative architecture for a high-level interaction between a human and a robot via a personal digital assistant (PDA). A PDA is a design to provide small and lightweight mobile interaction devices. This interface architecture differs from previous PDA human-robot interfaces in that it uses high-level task decomposition, and an adaptive user interface (UI) rather than teleoperation interfaces. An adaptive user interface typically refers to a flexible interaction strategy between a human and a computer to contribute what is best-suited at the most appropriate time. We extended this concept to human-robot interaction (HRI) and employed the architecture into mobile devices (i.e. PDA and PocketPC). Such devices could provide mobility and durability for robot operations. This work implemented an agent-based high-level human-robot interface on a PDA to provide interactions with robots. Four PDA user interfaces were developed: a map-based robot control screen, a laser range finder screen, a sonar sensor screen, and a camera view with an object selection screen. The proposed framework has been implemented to develop a prototypical PDA-based human-robot interaction system. The initial results are encouraging and demonstrate the capabilities of such a human-robot framework.
Integration of embryonic nephrogenic cells carrying a reporter gene into functioning nephrons (1991)

We developed a procedure to introduce and stably express foreign genes into the kidney. The Lac Z reporter gene encoding the bacterial protein beta-galactosidase was introduced by retrovirus-mediated gene transfer into rat nephrogenic mesenchymal cells, which were induced for 24 h with embryonic spinal cord in vitro. The Lac Z-tagged mesenchymal cells were subsequently transplanted underneath the capsule of the neonatal kidney. Two weeks after transplantation, the Lac Z-tagged cells derived from transplants were identified by their beta-galactosidase expression. Well-differentiated Lac Z positive cells were observed in glomerulus and proximal and distal nephron segments. To determine if the tagged mesenchymal cells developed into functional nephrons, fluorescein isothiocyanate-labeled dextran was infused into transplanted animals before death. We observed that fluorescent apical vesicles were colocalized to beta-galactosidase positive proximal tubular cells, indicating that the transplanted mesenchymal cells were integrated into reabsorbing nephrons. These results show the feasibility of introducing foreign genes into epithelia of functioning nephron segments.
The Nonantibiotic Anti-Inflammatory Effect of Antimicrobial Growth Promoters, the Real Mode of Action? A Hypothesis (2007)

Societal concern and government regulations increasingly press for restricting the use of antibiotics as antimicrobial growth promoters (AGP). The search for alternatives is on, hampered by a lack of knowledge about the exact mechanism of AGP. Feed additives, such as AGP and alternatives, interact with the intestine. In the intestine, feed components, microbiota, and the mucosa interact in a very complex and dynamic way. Various mechanisms for AGP have been proposed, invariably based on the direct antibiotic influence on the microbial composition of the intestines. In the literature on antibiotics, however, the direct effects of antibiotics on host cells, in particular inflammatory cells, have been described. It is curious that this has never been considered in the literature on AGP. Presently, a case is being made that AGP most likely work as growth permitters by inhibiting the production and excretion of catabolic mediators by intestinal inflammatory cells. Concomitant or subsequent changes in microflora are most likely the consequence of an altered condition of the intestinal wall. This common, basic mechanism potentially offers an excellent explanation for the highly reproducible effects of AGP, as opposed to those obtained by alternatives aimed at microflora management. Therefore, the search for alternatives could be aimed at nonantibiotic compounds with an effect on the inflammatory system similar to that of AGP.
Fattening Up Allograft Rejection (2016)

In Brief This commentary on immunological consequences of obesity highlights that transplant outcomes may be affected by the NF-KB2 pathway and that TNF-production by M1 macrophages is increased in mouse obesity models. Further studies will need to define the mechanisms by which obesity affects APCs and increases alloreactivity.
Man's Most Dangerous Myth: The Fallacy of Race. By M. F. Ashley Montagu. New York: Columbia University Press, 1942 and Race, Reason & Rubbish: A Primer of Race Biology. By Gunnar Dahlberg. Translated from the Swedish by Lancelot Hogben. New York: Columbia University Press, 1942 (1943)

Journal Article Man's Most Dangerous Myth: The Fallacy of Race. By M. F. Ashley Montagu. New York: Columbia University Press, 1942 and Race, Reason & Rubbish: A Primer of Race Biology. By Gunnar Dahlberg. Translated from the Swedish by Lancelot Hogben. New York: Columbia University Press, 1942 Get access Guy B. Johnson Guy B. Johnson University of North Carolina Search for other works by this author on: Oxford Academic Google Scholar Social Forces, Volume 21, Issue 4, May 1943, Pages 493–494, https://doi.org/10.2307/2571199 Published: 01 May 1943
Measures for Corpus Similarity and Homogeneity (1998)

How similar are two corpora? A measure of corpus similarity would be very useful for NLP for many purposes, such as estimating the work involved in porting a system from one domain to another. First, we discuss difficulties in identifying what we mean by &apos;corpus similariti: human similarity judgements are not finegrained enough, corpus similarity is inherently multidimensional, and similarity can only be interpreted in the light of corpus homogeneity. We then present an operational definition of corpus similarity \\vhich addresses or circumvents the problems, using purpose-built sets of aknown-similarity corpora&quot;. These KSC sets can be used to evaluate the measures. We evaluate the measures described in the literature, including three variants of the information theoretic measure &apos;perplexity&apos;. A x 2-based measure, using word frequencies, is shnwn to be the best of those tested. The Problem How similar arc two corpora? The question arises on many occasions. In NLP, many useful results can be generated from corpora, but when can the results developed using one corpus be applied to another? How much will it cost to port an NLP application from one domain, with one corpus, to another, with another? For linguistics, does it matter whether language researchers use this corpora or that, or are they similar enough for it to mal&lt;e no difference? There are also questions of more general interest. Looking at British national newspapers: is the Independent more like the Guardian or the Telegraph?&apos; What are the constraints on a measure for corpus similarity? The first is simply that its findings correspond to unequivocal human judgements. It must
A reconfigurable 0-L<inf>1</inf>-L<inf>2</inf> S-MASH<sup>2</sup> modulator with high-level sizing and power estimation (2014)

This paper presents a cascade sigma-delta modulator that uses concepts of 0-L MASH and Sturdy MASH sigma-delta modulator architectures to implement the higher-order multi-loop 0-L <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> -L <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> S-MASH <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> architecture. The combination of the above two architectures results in achieving larger input-signal levels and eliminates the use of digital-filters, thus removing high gain amplifiers. The presented architecture is made reconfigurable with variable loop-filter order, number of quantizer bits, OSR and inter-stage gains to demonstrate its usage in different standards like GSM, UMTS, WiMAX and WLAN for next generation software defined radios. A high level power estimation is carried out for the presented reconfigurable sigma-delta modulator. Time-domain behavioral simulations are shown to validate the benefits of the proposed modulator design.