gebhart/patrepeval huggingface dataset:
Distinct interaction profiles of the second generation Bcr-Abl inhibitors nilotinib and bosutinib with the ABCG2 multidrug transporter (2008)

LB-185 The human ABCG2 transporter provides tissue protection against numerous toxic compounds and accounts for a multidrug-resistant phenotype in cancer cells. It has been documented that ABCG2 displays a high affinity interaction with several small molecule tyrosine kinase inhibitors, including Imatinib (Glivec) that inhibits the Bcr-Abl fusion protein, the molecular marker of chronic myeloid leukemia (CML). In this study we investigated the interaction of ABCG2 with two second generation Bcr-Abl inhibitors already in clinical trials, Nilotinib and Bosutinib. We found that Nilotinib greatly stimulated the ATPase activity of the human wild-type ABCG2 (expressed in cholesterol-loaded Sf9 membranes), reaching a maximum stimulation at a Nilotinib concentration of 10 nM. This compound, in a similar concentration range (10-100 nM), also effectively inhibited Hoechst 33342 dye extrusion in Bcr-Abl+ K562 cells, overexpressing the ABCG2 protein (K562/ABCG2). These data suggest that ABCG2 interacts with Nilotinib with a high affinity, and this agent is a transported substrate for this multidrug transporter. In contrast, Bosutinib showed no stimulatory or inhibitory effect on the ABCG2-ATPase activity up to 1-2 uM concentrations, and in similar concentrations this compound did not inhibit the Hoechst 33342 dye extrusion in K562/ABCG2 cells either. The cytotoxic effects of Nilotinib and Bosutinib, as well as their modulatory potential on ABCG2 function were tested in K562 parental and K562/ABCG2 cells. In the parental K562 cells both of these compounds were cytotoxic at very low concentrations, the IC50 values being lower than 5 nM for Nilotinib, and about 10 nM for Bosutinib. In the K562/ABCG2 cells the IC50 vaules for Nilotinib increased by about one order of magnitude, up to 50 nM, while ABCG2 overexpression had no measurable effect on the cytotoxicity of Bosutinib. Based on these data we suggest that the novel Bcr-Abl inhibitors have major differences in their interaction profiles with ABCG2. While Nilotinib is a high affinity substrate and at higher concentrations is an effective inhibitor of the transporter, Bosutinib does not significantly interact with ABCG2 at therapeutically relevant concentrations. These findings may provide important information regarding the anticancer effects and ADME-Tox properties of these novel agents.
Effect of wind, current and non-linear second order drift forces on a moored multi-body system in an irregular sea (2002)

A study is made on the slowly varying oscillation of a moored multi-body system in wind, current and waves. Linear potential theory is used to describe the fluid motion and three dimensional source technique is applied to obtain the transfer function of drift forces in waves, which is used to obtain the slowly varying drift forces in horizontal plane for the multi-body floating system. Hydrodynamic forces are calculated including the interaction effect between the floating bodies. Davenport wind spectrum is adopted to calculate the fluctuating wind forces and OCIMF data are used for the estimation of wind and current forces. Interaction of currents between the vessels is not taken into account for the sake of simplicity. The non-linear time domain simulations are carried out in long crested irregular waves. Based on it, slowly varying motion responses is examined including the effects of the wind, current and non-linear second order drift forces. From the present study, it is found that the effect of second order drift forces is quite significant in comparison with effects of wind and current. The second order drift forces causes large slowly varying oscillation, and moored forces that relate for failure of the mooring system.
Noise Reduction using Wavelet Transform and Singular Vector Decomposition (2015)

Signals do not exist without noise. It must be removed from the data for further data analysis. The search for efficient noise reduction methods is still going on. Wavelet Transform (WT) is a powerful tool for removal of noise from various signals. Combining WT with other noise reducing techniques may result in further reduction of noise. Similar to WT, Singular Vector Decomposition (SVD) is also an effective noise reduction tool. In this experiment, wavelet transform is used along with Singular Vector Decomposition (SVD) for noise reduction. The results of noise reduction using Wavelet transform and combination of SVD with WT are compared. Error between coefficients of WT of original signal and coefficients of noise added signal SVD along with WT is found to be less as compare to WT operated alone on noisy signal.
Unified calibration technique and its applications in optical triangular profilometry (1999)

A unified calibration technique based on ray tracing for optical triangular profilometry is presented. The proposed technique based on the inherent geometric relation between depth and a distorted signal is capable of speedy and accurate measurement without the determination of geometric parameters. The technique can also reduce calibration error caused by the lens distortion of the projector and the camera owing to the reasonable assumption that mapping in a small local area is a linear transformation and the coefficients of the linear transformation may be varied in different local areas. Three classical systems of triangular profilometry, spot inspection, a single-line system, and a projection-grating system, are discussed and demonstrated by experiment.
Orexin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019)

Orexin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Orexin receptors [39]) are activated by the endogenous polypeptides orexin-A and orexin-B (also known as hypocretin-1 and -2; 33 and 28 aa) derived from a common precursor, preproorexin or orexin precursor, by proteolytic cleavage and some typical peptide modifications [102]. Currently the only orexin receptor ligand in clinical use is suvorexant, which is used as a hypnotic. Orexin receptor crystal structures have been solved [124, 123].
COMPACT PLANAR UWB ANTENNA WITH BAND NOTCH CHARACTERISTICS FOR WLAN AND DSRC (2013)

In this paper, a compact ultra-wideband microstrip-fed annular ring antenna with band notch characteristics for wireless local area network (WLAN) and dedicated short-range communication (DSRC) is proposed. The proposed antenna comprises an annular ring patch and a partial ground plane with a rectangular slot. The notched frequency band is achieved by etching a partial annular slot in the lower portion of the ring radiator. The centre frequency and bandwidth of the notched band can be controlled by adjusting the width and position of the annular slot. Measured results show that the proposed antenna achieved an impedance bandwidth of 3-10.6 GHz with a notched frequency band centred at 5.5 GHz. Compared to the recently reported band-notched UWB antennas, the proposed antenna has a simple configuration to realize the band notch characteristics to mitigate the possible interference between UWB and existing WLAN & DSRC systems. Furthermore, a symmetric radiation patterns, satisfactory gain and good time domain behaviour except at the notched frequency band makes the proposed antenna a suitable candidate for practical UWB applications.
The Metabolic and Hemodynamic Effects of Prolonged Bed Rest in Normal Subjects (1974)

The metabolic and hemodynamic effects of prolonged bed rest were studied in 6 normal subjects. Bed rest of 2-3 weeks duration produced exaggerated responses of heart rate, cardiac output, stroke volume, and peripheral vascular resistance to 70° tilt. Sympathetic nerve function and catecholamine metabolism were not impaired by bed rest. Pressor responses to infusions of norepinephrine and angiotensin and reflex vasoconstriction to a cool and warm environment were essentially unchanged during bed rest. Plasma catecholamines and urinary vanillylmandelic acid excretion were somewhat lower during bed rest than during ambulation, but the response of plasma catecholamines to 70° tilt was not diminished. The apparent turnover of norepinephrine in plasma was also similar in bed rest and control periods. Negative sodium and potassium balances and reductions in plasma volume were observed in all subjects, but plasma renin activity and aldosterone secretory rate showed no significant change. The major decreases in sodium balance and plasma volume occurred in the early bed rest period and did not correlate closely with the degree of orthostatic intolerance. The reductions in potassium balance appeared to be progressive throughout the study.
Application of Supercritical Fluid Extraction in Biotechnology (2005)

In the present paper recent investigations on the applications of supercritical fluid extraction (SCE) from post fermentation biomass or in situ extraction of inhibitory fermentation products as a promising method for increasing the yield of extraction have been reviewed. Although supercritical CO2 (SC-CO2) is unfriendly, or even toxic, for some living cells and precludes direct fermentation in dense CO2, it does not rule out other useful applications for in situ extraction of inhibitory fermentation products and fractional extraction of biomass constituents. This technique is a highly desirable method for fractional extraction of biomass constituents, and intracellular metabolites due to the potential of system modification by physical parameters and addition of co-solvents to selectively extract compounds of different polarity, volatility and hydrophilicity without any contamination.
Early miR-320b and miR-25-3p miRNA levels correlate with multiple sclerosis severity at 10 years: a cohort study (2023)

Our results show that miR-320b and miR-25-3p expression are early biomarkers associated with MS severity and brain atrophy. This study provides class III evidence of that miR-320b and miR-25-3p are associated with long-term MS disability which may be a potential tool to risk-stratify patients with MS for early treatment decisions.
Building bridges between Europe and China to strengthen social work field education: preliminary findings from Guangdong Province (2021)

Jie Leia, Wei Lub*, Staffan Höjerc, Agnieszka Repod, Zhenhao Sua, Mengyu Oua, Heng Yange, Ling Yuf & Boya Fengga School of Sociology and Anthropology, Sun Yat-sen University, Guangzhou, Chinab Department of Social Work, Xiamen University, Xiamen, Chinac Department of Social Work, University of Gothenburg, Gothenburg, Swedend Department of Social Science, University of Eastern Finland, Joensuu and Kuopio, Finlande School of Humanities, Zhuhai City Polytechnic, Zhuhai, Chinaf Shenzhen Social Work College, Shenzhen, Chinag Department of Social Work, Guangdong University of Technology, Guangzhou, China
Cutaneous effects associated with fluconazole in patients treated for coccidioidomycosis (2018)

For the treatment of coccidioidomycosis, patients receiving fluconazole reported significantly more severe cutaneous effects, including dry lips, dry skin, and alopecia, than untreated patients. Our findings identify an association but do not prove causality.
A passive wingtip load alleviation system (1974)

A passive wingtip load alleviation system was devised, tested, and analyzed for its effect on the reduction of structural deformations and the extension of flutter speed. The sensors responded to changes in angle of attack and vertical movement of the wingtip and were used to deflect a trailing edge flap to alleviate the induced loads.
Quantitative Measurement of Nanoparticle Halo Formation around Colloidal Microspheres in Binary Mixtures (2008)

A new colloidal stabilization mechanism, known as nanoparticle "haloing" (Tohver, V.; Smay, J. E.; Braem, A.; Braun, P. V.; Lewis, J. A. Proc. Natl. Acad. Sci. U.S.A. 2001, 98, (16), 8950-8954), has been predicted theoretically and inferred experimentally in microsphere-nanoparticle mixtures that possess high charge and size asymmetry. The term "halo" implies the existence of a nonzero separation distance between the highly charged nanoparticles and the negligibly charged microspheres that they surround. By means of ultrasmall-angle X-ray scattering, we have quantified the microsphere-nanoparticle separation distance as well as the number of nanoparticles and their lateral separation distance within the self-organized halos that form in these binary mixtures.
The treatment of high strength wastewater containing high concentrations of ammonium in a staged anaerobic and aerobic membrane bioreactor (2002)

In this paper, a staged anaerobic and aerobic membrane bioreactor was constructed and used to study the treatment of high strength wastewater containing high concentrations of ammonium. The membrane module was submerged in the aerobic zone (upper part) of the bioreactor and was operated under an alternating suction mode and air backwash mode. Air backwash and aeration around the membrane module served as the cleaning mechanism for the membrane; this resulted in the steady operation of the reactor at the flux of 514 L m 2 h 1 for 120200 h without any additional cleaning. The efficiencies of the chemical oxygen demand (COD) removal were &gt;99% for up to 10.08 g COD L 1 d 1 of the volumetric loading rate. Between 60 and 80% of COD was anaerobically biodegraded in the anaerobic zone (lower part) of the reactor and converted to methane that could serve as a carbon source for the denitrification in the upper part of the reactor. The intermittent aeration resulted in simultaneous nitrification and denitrification in the aerobic zone of the reactor. The capacity of the ammonium removal reached 0.5 g NH 4 + -N L 1 d 1 . Between 84 and 94% of the total oxidized nitrogen converted from the oxidization of ammonium was denitrified. Key words: air backwash membrane bioreactor (MBR), high strength wastewater, anaerobic and aerobic treatment, ammonium removal, methanotrophic denitrification.
A Physics-Based Reduced-Order Model for the Dynamic and Post-Buckling Behavior of Tensegrity Structures and Metamaterials (2017)

Traditional approaches for modeling the behavior of tensegrity structures have their origin either on form-finding applications or on the desire to capture their quasi-static behavior. As such, they generally assume that (i) bars are perfectly rigid, (ii) cables are linear elastic, and (iii) bars experience pure compression and strings pure tension. In addition, a common design constraint is to assume that the structure would fail whenever any of its bars reaches the corresponding Euler buckling load. In reality, these assumptions tend to break down in the presence of dynamic events. In this work, we develop a physics-based reduced-order model to study aspects related to the dynamic and nonlinear response of tensegrity-based structures. With very few degrees of freedom, our model captures their buckling and post-buckling behavior as well as their dynamic response. We then adopt our model to show how, under dynamic events, buckling of individual members of a tensegrity structure does not necessarily imply structural failure. Finally, we show how through successive reflection operations it is possible to architecture a 3D tensegrity metamaterial, and analyze its response to impacts. Our research suggests that efficient structural design of impact-tolerant tensegrity structures and metamaterials could be achieved by exploiting rather than avoiding the buckling behavior of its compression members.
Nonreciprocal devices in integrated optics (1989)

Abstract This article reviews the solutions that have been studied for the implementation of nonreciprocal devices in integrated optics. These components, either isolators or circulators, use the nonreciprocal interaction between light and a magnetic medium. The only two isolators that have been experimented on to date are described in detail with their advantages and drawbacks, and some solutions are proposed to overcome the difficulties encountered.
Lightning location system increases personnel safety in Swedish power transmission network (2003)

Vattenfall (formerly the Swedish State Power Board) is utilizing data from a nationwide lightning location system in an effort to prevent or minimize lightning damage on personnel and power systems. Real-time lightning data are presented on color graphic displays at regional power network control centers for optimal and safe operation of the transmission network during thunderstorms, warning to maintenance and service crews at power lines and substations to terminate operations hazardous in the case of lightning, and rapid positioning of emergency crews to locate network damage in areas of detected lightning.
Turbo decoding with erasures for high-speed transmission in the presence of impulse noise (2003)

If impulse noise is not taken into account, turbo codes are highly attractive for transmissions over asymmetric digital subscriber lines. We show that impulse noise could devastate turbo coding performance if appropriate precautions are not taken. A possible solution of using an outer Reed-Solomon code to combat impulse noise results in very large delays. We propose erasure turbo decoding to improve the turbo trellis coded modulation performance against impulse noise. We also show that when a concatenated coding structure is employed, in addition to improving the bit error rate performance, erasure turbo decoding can also significantly reduce the delay of the outer Reed-Solomon code.
Bifurcation in parallel-connected boost DC/DC converters (2002)

This paper describes the bifurcation phenomena of a system of parallel-connected boost dc/dc converters. The results provide useful information for the design of stable current sharing in a master-slave configuration. Computer simulations are performed to capture the effects of variation of some chosen parameters on the qualitative behaviour of the system. It is found that variation of some parameters leads to Neimark-Sacker bifurcation. Analysis is presented to establish the possibility of the bifurcation phenomena.
Integrated Wireless Neural Recording and Electrode Positioning System (2012)

In neurophysiological research, the recording of brain activity in animals is fundamental. Conventional wire-based technologies allow such recordings only in movement-restraint animals. Head-mounted wireless recording technologies allow investigating a broader spectrum of behaviors and have the potential to improve animal welfare and mark an important step towards implantable neuroprosthetic devices. We developed a lightweight, head-mountable neural recording system, which allows bidirectional communication for remote signal acquisition on the one hand and remote pre-amp gain adjustments and microelectrode position adjustments, on the other hand.
A Restoration Aid Expert System for Distribution Substations (1996)

This paper presents a practical restoration aid expert system for 154 kV distribution substations. The proposed expert system has a topology-based simple structure and utilizes basic rules suggested by the Korean electric power company including heuristic rules, topology identification rules and search rules to generate switching sequences for feasible restoration processes. In this paper, the general system structure as well as rules and data representations are discussed. The expert system is realized using an HP9000 workstation. X-window and Motif shells are used for the user-friendly GUI. The system has been tested in a practical sub-control center as a part of an intelligent fault diagnosis and restoration aid system to assist the decision making of SCADA operators.
Cyclopropylamines as suicide substrates for cytochromes P-450 (1979)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTCyclopropylamines as suicide substrates for cytochromes P-450Robert P. Hanzlik, Vimal Kishore, and Robert TullmanCite this: J. Med. Chem. 1979, 22, 7, 759–761Publication Date (Print):July 1, 1979Publication History Published online1 May 2002Published inissue 1 July 1979https://pubs.acs.org/doi/10.1021/jm00193a002https://doi.org/10.1021/jm00193a002research-articleACS PublicationsRequest reuse permissionsArticle Views158Altmetric-Citations43LEARN 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
Proliferation-associated nuclear antigen Ki-S1 is identical with topoisomerase II alpha. Delineation of a carboxy-terminal epitope with peptide antibodies. (1995)

Proliferation-linked expression of the nuclear Ki-S1 antigen is a significant prognostic indicator in mammary carcinomas. Here, we show staining of a protein of 170 kd by Ki-S1 antibody in immunoblots of Saccharomyces cerevisiae expressing human topoisomerase II alpha but not in the parental strain. In HL-60 cells containing both isoforms of human topoisomerase II, Ki-S1 antibody binds selectively to the 170-kd isoenzyme in a similar fashion as peptide-antibodies directed against amino acid residues 1 to 15 or 1512 to 1530 of human topoisomerase II alpha. Conversely, antibodies directed against carboxyl-terminal sequences of human topoisomerase II beta selectively stain a 180-kd protein. The immunoreactive pattern of V8 endoproteinase restriction digests of human topoisomerase II alpha was identical for Ki-S1-antibody and peptide-antibodies directed against residues 1512 to 1530 but different for peptide-antibodies directed against residues 1 to 15. The Rf values of the smallest fragment commonly recognized by Ki-S1 antibody and the carboxy terminus-specific peptide-antibody place the Ki-S1 epitope within the last 495 carboxyl-terminal amino acid residues of topoisomerase II alpha.
Biosynthesis of rare hexoses using microorganisms and related enzymes (2013)

Rare sugars, referred to as monosaccharides and their derivatives that rarely exist in nature, can be applied in many areas ranging from foodstuffs to pharmaceutical and nutrition industry, or as starting materials for various natural products and drug candidates. Unfortunately, an important factor restricting the utilization of rare sugars is their limited availability, resulting from limited synthetic methods. Nowadays, microbial and enzymatic transformations have become a very powerful tool in this field. This article reviews the biosynthesis and enzymatic production of rare ketohexoses, aldohexoses and sugar alcohols (hexitols), including D-tagatose, D-psicose, D-sorbose, L-tagatose, L-fructose, 1-deoxy-L-fructose, D-allose, L-glucose, L-talose, D-gulose, L-galactose, L-fucose, allitol, D-talitol, and L-sorbitol. New systems and robust catalysts resulting from advancements in genomics and bioengineering are also discussed.
Bloody Diarrhea—A Possible Complication of Sulfasalazine Transferred Through Human Breast Milk (1986)

Summary: Sulfasalazine very rarely causes bloody diarrhea. A 3-month-old infant had bloody diarrhea that could be related to sulfasalazine that had been taken by his mother and was transferred through his mother's breast milk. The patient was exclusively breast fed, and no other known etiological factors could be detected for the infant's bloody diarrhea.