gebhart/patrepeval huggingface dataset:
Identification of Cytochrome P450 Enzymes Involved in the Metabolism of FK228, a Potent Histone Deacetylase Inhibitor, in Human Liver Microsomes (2005)

FK228 (FR901228, depsipeptide) is a potent histone deacetylase inhibitor currently in phase II clinical trials for cancer treatment. In the present study, the cytochrome P450 (P450) enzymes responsible for FK228 metabolism in human liver microsomes were investigated. Incubation with human liver microsomes in the presence of an NADPH-generating system revealed that FK228 is metabolized to at least 10 different metabolites. Km and Vmax values for FK228 disappearance were 20.3 microM and 561.9 pmol/min/mg protein, respectively. Further studies were performed at a substrate concentration of 10 microM (half the Km value for FK228 disappearance). FK228 disappearance activities in human liver microsomes from 12 individuals strongly correlated (r2=0.957) with testosterone 6beta-hydroxylase activities, a marker enzyme activity of CYP3A4/5, but not with other P450 enzyme-specific activities (CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, and 4A). Among 14 recombinant heterologously expressed human P450s examined, CYP3A4 exhibited the highest activity of FK228 disappearance. CYP3A5, 1A1, 2B6, and 2C19 showed 16.8%, 5.2%, 1.6%, and 1.3% of the activity of CYP3A4, respectively. Other P450s showed no significant metabolic activity toward FK228. In addition, FK228 disappearance in human liver microsomes was markedly inhibited by ketoconazole, a potent CYP3A4 inhibitor, and an anti-CYP3A4 antibody. These results indicate that the metabolism of FK228 in human liver microsomes is catalyzed mainly by CYP3A enzymes, particularly CYP3A4.
ChemInform Abstract: TOTAL SYNTHESIS OF BETALAINES (1977)

Abstract Der Diester (I) reagiert mit dem modifizierten Horner‐Wittig‐Reagenz (II) zu den isomeren Dihydrobetalamsäurediester‐semicarbazonen (IIIa) und (IIIb).
Why Justify? Explaining Variation in Conflict Justification, 1980–2008 (2010)

This article is about state justifications for conflict initiation, an understudied yet nonetheless significant element of the foreign policy behavior of sovereign states. To what degree do such justifications vary among states? And what drives any variation that does exist? Regime type? Power status? Or, as implicitly assumed by some constructivist scholars, normative identification? Through an analysis of conflict justifications between 1980 and 2008, I find not only that states almost always publicly justify their actions and that conflict justifications always include at the very least an assertion of self-defense, but that there is also substantial variation regarding whether states make claims of humanitarianism and multilateralism and whether they utilize international law in their justificatory statements. The former is best explained through normative identification and the latter by the power status of the justifying state. Differences in regime type, however, do not play a significant role in conflict justification variation.
Effects of Trp- and Arg-Containing Antimicrobial-Peptide Structure on Inhibition of <i>Escherichia coli</i> Planktonic Growth and Biofilm Formation (2010)

Biofilms are sessile microbial communities that cause serious chronic infections with high morbidity and mortality. In order to develop more effective approaches for biofilm control, a series of linear cationic antimicrobial peptides (AMPs) with various arginine (Arg or R) and tryptophan (Trp or W) repeats [(RW)(n)-NH(2), where n = 2, 3, or 4] were rigorously compared to correlate their structures with antimicrobial activities affecting the planktonic growth and biofilm formation of Escherichia coli. The chain length of AMPs appears to be important for inhibition of bacterial planktonic growth, since the hexameric and octameric peptides significantly inhibited E. coli growth, while tetrameric peptide did not cause noticeable inhibition. In addition, all AMPs except the tetrameric peptide significantly reduced E. coli biofilm surface coverage and the viability of biofilm cells, when added at inoculation. In addition to inhibition of biofilm formation, significant killing of biofilm cells was observed after a 3-hour treatment of preformed biofilms with hexameric peptide. Interestingly, treatment with the octameric peptide caused significant biofilm dispersion without apparent killing of biofilm cells that remained on the surface; e.g., the surface coverage was reduced by 91.5 + or - 3.5% by 200 microM octameric peptide. The detached biofilm cells, however, were effectively killed by this peptide. Overall, these results suggest that hexameric and octameric peptides are potent inhibitors of both bacterial planktonic growth and biofilm formation, while the octameric peptide can also disperse existing biofilms and kill the detached cells. These results are helpful for designing novel biofilm inhibitors and developing more effective therapeutic methods.
Magnetic and Structural Properties of FePt–FeRh Exchange Spring Films for Thermally Assisted Magnetic Recording Media (2004)

Recently a novel media structure for thermally assisted magnetic recording was proposed consisting of a layer of FePt exchange coupled to a FeRh layer. The FePt forms a high magnetocrystalline anisotropy, high coercivity ferromagnetic layer. The FeRh layer is antiferromagnetic at room temperature, but upon heating above a transition temperature becomes ferromagnetic with a large magnetic moment and low magnetocrystalline anisotropy. The coupled ferromagnetic FePt and FeRh layers form an exchange-spring system significantly lowering the coercive field of the composite system compared to a single layer of FePt. This feature opens intriguing possibilities for media applications for thermally assisted magnetic recording where the ferromagnetic phase of FeRh is exploited to help write the media while the low-temperature antiferromagnetic phase supports the long-term stability. Here temperature-dependent structural and magnetic measurements of undoped and doped FeRh single layer and FePt-FeRh bilayer films are presented and the promises and challenges of the exchange spring media structure are discussed.
<i>In vitro</i> viability, mitogenicity and clonogenic capacity of periodontal ligament cells after storage in four media at room temperature (2000)

The choice of storage medium for preserving traumatically avulsed teeth is important for the success of future replantation. The objective of this study was to compare the effectiveness of four recommended storage media (Hank's balanced salt solution [HBSS], culture medium, alpha minimal essential medium [alpha-MEM], and ViaSpan) to preserve cultured periodontal ligament fibroblasts (PDLF) at room temperature (22 degrees C). PDLF were obtained from explants of extracted healthy human teeth. Plates with confluent PDLF were soaked in the various media for 2, 8 and 24 h at room temperature. A control group was incubated with culture medium at 37 degrees C. After incubation, viability of the cells was determined by trypan blue exclusion test. Viable cells were then analyzed for mitogenic (with thymidine) and clonogenic capacity (by culturing one cell/well). Viability of PDLF stored up to 24 h was comparable in all tested media, and the differences were limited to 1%-3%. PDLF stored for up to 24 h in various media had statistically comparable mitogenicity to the control group. After 8 h of storage, the differences were limited to 2%-9%, except for the alpha-MEM group which had 23%-29% lower mitogenic capacity compared to the control group. Increasing the storage time up to 24 h further decreased the mitogenicity of the cells by 22%-47%. The highest mitogenicity after 24 h of storage was found in PDLF stored in culture medium or HBSS, and the lowest in alpha-MEM. PDLF stored for 2-8 h in various media had a comparable clonogenic capacity to the control group. However, after 24 h, the cells' clonogenic ability dropped by 14%-66%. A similar trend of reduction was noted in the mitogenic and clonogenic capacity, although it was statistically significant only in the clonogenic capacity. Culture medium and ViaSpan, followed by HBSS, were the most effective in preserving the clonogenic capacity of PDLF after 24 h of storage. The lowest clonogenic capacity after 24 h of storage was in the alpha-MEM group (66%, P < 0.0025). In conclusion, culture medium, followed by HBSS and ViaSpan, was the most effective media for preserving the viability, mitogenicity and clonogenic capacity of PDLF stored for up to 24 h at room temperature. The lowest functional abilities were found in PDLF stored in alpha-MEM.
Characterization of thiol‐conjugated metabolites of ginger components shogaols in mouse and human urine and modulation of the glutathione levels in cancer cells by [6]‐shogaol (2013)

Shogaols are metabolized extensively in mouse and human to form thiol-conjugated metabolites and GSH might play an important role in the cancer-preventive activity of ginger.
Change of residual strains in arteries due to hypertrophy caused by aortic constriction. (1989)

The stress and strain that remain in an organ when the external load is removed are called residual stress and strain. They can be revealed by cutting up the organ in such a way as to reveal the zero-stress configuration. The function of the organ depends on the residual strain. For a blood vessel, the zero-stress configuration is very different from that of the no-load condition, and it changes over time when the physical stress acting on the vessel is changed. Data on rat aorta are presented. Physical changes were obtained by constricting the aorta at the celiac trunk level with a band of metal. Banding causes an increase of blood pressure and hypertrophy of the vessel in the upper body and a transient decrease of blood pressure in the lower body. If the aorta is cut transversely into rings and each ring is cut radially, it will open up into a noncircular arc, which may be characterized by its opening angle. It is shown that the opening angle varies systematically along the aorta and that it changes significantly together with changes of blood pressure and hypertrophy. In the ascending aorta, the opening angle increased from 171 degrees and to 214 degrees in 4 days after banding, then decreased gradually to an asymptotic value of 126 degrees in 40 days. At other sections, the swing of opening angle is smaller. The implications are discussed.
The Group of the Quadratic Residue Tournament (1970)

A tournament T n is a set of n nodes a 1 a 2 , …, a n such that every pair ( a i , a j ) of distinct nodes is joined by exactly one of the oriented edges or . If is in T n , then we say that a i dominates a j and write a i → a j . The (automorphism) group G ( T n ) of a tournament T n is the group of all permutations ϕ of the nodes of T n such that ϕ(a)→ϕ(b) if and only if a → b. It is known [9] that there exist tournaments whose group is abstractly isomorphic to a given group H if and only if H has odd order; thus all tournament groups are solvable, by the Feit-Thompson Theorem [7].
Optical design and evaluation of a 4 mm cost-effective ultra-high-definition arthroscope (2014)

High definition and magnification rigid endoscope plays an important role in modern minimally invasive medical surgery and diagnosis. In this paper, we present the design and evaluation methods of a high definition rigid endoscope, specifically an arthroscope, with a large depth of field (DOF). The incident heights and exit angles of the sampled rays on the relay lens are controlled during the optimization process to ensure an effective field view (70°) and a normal ray path within the limited lens diameter of 2.7 mm. The lens is set up as a multi-configuration system with two extreme and one middle object distances to cover a large DOF. As a result, an entrance pupil of 0.3 mm is achieved for the first time, to bring the theoretical resolution to 23.1 lps/mm in the object space at a working distance of 20 mm, with the wavelength of 0.532 um. The modulation transfer function (MTF) curves approach diffraction limit, and the values are all higher than 0.3 at 160 line pairs/mm (lps/mm) in the image space. Meanwhile, stray light caused by total internal reflection on the inner wall of the rod lenses and the objective lens is eliminated. The measured resolution in the object space at a 20 mm working distance is 22.3 lps/mm, and test results show that other performance characteristics also fulfill design requirements. The relay lenses are designed with only one type of the spacer and two types of lenses to greatly reduce the fabrication and assembly cost. The design method has important research and application values for lens systems used in modern minimally invasive medical surgery and industrial non-destructive testing area.
Optimizing Soft Vector Processing in FPGA-Based Embedded Systems (2016)

Soft vector processors can augment and extend the capability of FPGA-based embedded systems-on-chip such as the Xilinx Zynq. However, configuring and optimizing the soft processor for best performance is hard. We must consider architectural parameters such as precision, vector lane count, vector length, chunk size, and DMA scheduling to ensure efficient execution of code on the soft vector processing platform. To simplify the design process, we develop a compiler framework and an autotuning runtime that splits the optimization into a combination of static and dynamic passes that map data-parallel computations to the soft processor. We compare and contrast implementations running on the scalar ARM processor, the embedded NEON hard vector engine, and low-level streaming Verilog designs with the VectorBlox MXP soft vector processor. Across a range of data-parallel benchmarks, we show that the MXP soft vector processor can outperform other organizations by up to 4 × while saving ≈ 10% dynamic power. Our compilation and runtime framework is also able to outperform the gcc NEON vectorizer under certain conditions by explicit generation of NEON intrinsics and performance tuning of the autogenerated data-parallel code. When constrained by IO bandwidth, soft vector processors are even competitive with spatial Verilog implementations of computation.
A Possible Explanation for a Neurotoxic Effect of the Anticancer Agent Oxaliplatin on Neuronal Voltage-Gated Sodium Channels (2001)

Oxaliplatin, a new widely used anticancer drug, displays frequent, sometimes severe, acute sensory neurotoxicity accompanied by neuromuscular signs that look like the symptoms observed in tetany and myotonia. The whole cell patch-clamp technique was employed to investigate the oxaliplatin effects on the electrophysiological properties of short-term cultured dorsal unpaired median (DUM) neurons isolated from the CNS of the cockroach Periplaneta americana. Within the clinical concentration range, oxaliplatin (40-500 microM), applied intracellularly, decreased the amplitude of the voltage-gated sodium current resulting in a reduction of half the amplitude of the action potential. For comparison, two other platinum derivatives, cisplatin and carboplatin, were found to be ineffective at reducing the sodium current amplitude. In addition, we compared the oxaliplatin action to those of its metabolites dichloro-diaminocyclohexane platinum (dach-Cl(2)-platin) and oxalate. Oxalate (500 microM) was found to be effective, like oxaliplatin, at reducing the inward sodium current amplitude, whereas dach-Cl(2)-platin (500 microM) failed to change the current amplitude. Interestingly, the effect of oxalate or oxaliplatin could be mimicked by using intracellularly applied 10 mM bis-(o-aminophenoxy)-N,N,N',N'-tetraacetic acid (BAPTA), known as chelator of calcium ions. We concluded that oxaliplatin was capable of altering the voltage-gated sodium channels through a pathway involving calcium ions probably immobilized by its metabolite oxalate. The medical interest of preventing acute neurotoxic side effects of oxaliplatin by infusing Ca(2+) and Mg(2+) is discussed.
Antibody Engineering Using Phage Display with a Coiled-Coil Heterodimeric Fv Antibody Fragment (2011)

A Fab-like antibody binding unit, ccFv, in which a pair of heterodimeric coiled-coil domains was fused to V(H) and V(L) for Fv stabilization, was constructed for an anti-VEGF antibody. The anti-VEGF ccFv showed the same binding affinity as scFv but significantly improved stability and phage display level. Furthermore, phage display libraries in the ccFv format were constructed for humanization and affinity maturation of the anti-VEGF antibody. A panel of V(H) frameworks and V(H)-CDR3 variants, with a significant improvement in affinity and expressibility in both E. coli and yeast systems, was isolated from the ccFv phage libraries. These results demonstrate the potential application of the ccFv antibody format in antibody engineering.
Review of breast cancer screening guidelines (1992)

In this article, the author provides a historical description of the initiation of the Breast Cancer Detection Demonstration Project (BCDDP) and the subsequent development of screening guidelines for breast cancer by the American Cancer Society and other organizations.
Voltage sag ride-through for adjustable speed drives with active rectifiers (2002)

Adjustable speed drives (ASDs) trip due to voltage sags, interfering with production and incurring financial losses. In this paper, a methodology for incorporating voltage sag ride-through in the design of ASDs with active rectifiers is presented. The magnitude of the voltage sag for which ride-through can be provided is determined by the current rating of the active rectifier and load condition of the ASD but a sag of any duration can be compensated for.
An introduction to optical burst switching (2003)

Optical burst switching is a promising solution for all-optical WDM networks. It combines the benefits of optical packet switching and wavelength routing while taking into account the limitations of the current all-optical technology. In OBS, the user data is collected at the edge of the network, sorted based on a destination address, and grouped into variable sized bursts. Prior to transmitting a burst, a control packet is created and immediately sent toward the destination in order to set up a bufferless optical path for its corresponding burst. After an offset delay time, the data burst itself is transmitted without waiting for a positive acknowledgment from the destination node. The OBS framework has been widely studied in the past few years because it achieves high traffic throughput and high resource utilization. However, despite the OBS trademarks such as dynamic connection setup or strong separation between data and control, there are many differences in the published OBS architectures. In this article we summarize in a systematic way the main OBS design parameters and the solutions that have been proposed in the open literature.
Improved method for the synthesis of poly(organophosphazenes) and hindered cyclophosphazenes (1983)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTImproved method for the synthesis of poly(organophosphazenes) and hindered cyclophosphazenesPaul E. Austin, Geoffrey H. Riding, and Harry R. AllcockCite this: Macromolecules 1983, 16, 5, 719–722Publication Date (Print):May 1, 1983Publication History Published online1 May 2002Published inissue 1 May 1983https://pubs.acs.org/doi/10.1021/ma00239a002https://doi.org/10.1021/ma00239a002research-articleACS PublicationsRequest reuse permissionsArticle Views346Altmetric-Citations48LEARN 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
The Analysis of Two Different Types of Tapers on Exercise Performance (2010)

Athletes depend on tapers to allow repair and rest for the individual prior to competition. Many variables affect the performance of a taper. These variables include volume, intensity, duration, frequency, and the type of taper. The type of taper may include a step taper, progressive taper, or exponential decay taper. Manipulation of these variables may be the best accommodation for the athlete. The purpose of this study is to compare the differences in a step taper and an exponential decay taper across time. The variables that are statistically studied are heart rate, rate of perceived exertion, and VO2 max at the pre-test and post-test periods. Method: Nineteen subjects volunteered and participated in the study (age 24 11.04 years). The subjects were divided into two groups; the step taper group (n=8) and the exponential decay taper group (n=11). The participant's baseline tested, trained for a middle-distance run for 4 weeks, and pre-tested. The participants were then randomly assigned to one of the groups and performed the one week designated taper. Following the taper was a post-test period. Findings: There was a significant difference in stage 4 (Brue Protocol Test) in the pre-test and stage2 in the post-test periods for RPE comparisons(p &#8804; .05). There was also a significant difference in stages 1 and 2 of the pre-test in regards to submax HR values. VO&#8322; max values did not show any statistical significance across time. According to this study, the statistics show there is no significant benefit to either taper. Conclusion: In previous research, there has been evidence that an exponential decay taper is more beneficial to a step taper. More research should be analyzed to compare the variables. It is recommended that the study be conducted over a longer period with multiple trials. The study should be conducted in a real setting rather than a clinical one. The taper should also compare more than one endurance event such as swimming, running , and cycling. An increase in participant numbers would produce a better reliability of the athletic population.
Color regulation in the archaebacterial phototaxis receptor phoborhodopsin (sensory rhodopsin II) (1990)

Phoborhodopsin, a repellent phototaxis receptor in Halobacterium halobium, exhibits vibrational fine structure, a feature that has not been identified for any other rhodopsin pigment at physiological temperatures. This conclusion follows form analysis of the absorption properties of the pigment in H. halobium membranes containing native retinal and an array of retinal analogues. The absorption spectrum of the native pigment has a maximum at 487 nm with a pronounced shoulder at 460 nm; however, the bandwidth is that expected for a single retinylidene species. Gaussian band-shape simulation with a spacing corresponding to the vibrational frequencies of polyene stretching modes reproduces the structured absorption spectra of native pigment as well as of analogue phoborhodopsin. Absorption shifts produced by a series of dihydroretinal and other retinal analogues strongly indicate that the dominant factor regulating the color of the pigment is planarization of the retinal ring with respect to the polyene chain.