cometadata/datacite-rtg-text-other-reclassification-records huggingface dataset:
Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Creators: name: Röhrig, Ute F.
name: Majjigapu, Somi Reddy
name: Vogel, Pierre
name: Reynaud, Aline
name: Pojer, Florence
name: Dilek, Nahzli
name: Reichenbach, Patrick
name: Ascenção, Kelly
name: Irving, Melita
name: Coukos, George
name: Michielin, Olivier
name: Zoete, Vincent
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Immunology
subject: FOS: Clinical medicine
subject: Biological Sciences not elsewhere classified
subject: Information Systems not elsewhere classified

description: The haem enzyme indoleamine 2,3-dioxygenase 1 (IDO1) catalyses the rate-limiting step in the kynurenine pathway of tryptophan metabolism and plays an essential role in immunity, neuronal function, and ageing. Expression of IDO1 in cancer cells results in the suppression of an immune response, and therefore IDO1 inhibitors have been developed for use in anti-cancer immunotherapy. Here, we report an extension of our previously described highly efficient haem-binding 1,2,3-triazole and 1,2,4-triazole inhibitor series, the best compound having both enzymatic and cellular IC50 values of 34 nM. We provide enzymatic inhibition data for almost 100 new compounds and X-ray diffraction data for one compound in complex with IDO1. Structural and computational studies explain the dramatic drop in activity upon extension to pocket B, which has been observed in diverse haem-binding inhibitor scaffolds. Our data provides important insights for future IDO1 inhibitor design.
title: Interdisziplinäre Prospektion im Ampurdán : Vorbericht der Kampagne September 1996
title: Interdisziplinäre Prospektion im Ampurdán : Vorbericht der Kampagne September 1996
titleType: Subtitle
Creators: name: Blech, Michael
name: Marzoli, Dirce
name: Burjachs Casas, Françesc
Publisher: name: Deutsches Archäologisches Institut
Year: 2020

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Deutsche Zusammenfassung folgt.
Developing optimal methods for theta burst prefrontal brain stimulation
Creators: name: SUNG WOOK CHUNG
Publisher: name: Monash University
Year: 2019
Subjects: Neuroscience

description: Theta burst stimulation (TBS) is a non-invasive brain stimulation technique which has the ability to alter brain activity in humans. Due to its rapid administration duration, TBS has gained popularity both in research and clinical trials. Despite its benefits, wide adoption of this technique in the treatment of psychiatric disorders has been limited due to the lack of understanding of its effects when it is applied to the prefrontal. In addition, little is known about the effect of different stimulation parameters. The aim of this thesis was to develop the optimal method of TBS application in the prefrontal cortex.
Automated assessment of non-native learner essays: Investigating the role of linguistic features
Creators: name: Vajjala, Sowmya
Publisher: name: arXiv
Year: 2016
Subjects: subject: Computation and Language (cs.CL)
subject: FOS: Computer and information sciences

description: Automatic essay scoring (AES) refers to the process of scoring free text responses to given prompts, considering human grader scores as the gold standard. Writing such essays is an essential component of many language and aptitude exams. Hence, AES became an active and established area of research, and there are many proprietary systems used in real life applications today. However, not much is known about which specific linguistic features are useful for prediction and how much of this is consistent across datasets. This article addresses that by exploring the role of various linguistic features in automatic essay scoring using two publicly available datasets of non-native English essays written in test taking scenarios. The linguistic properties are modeled by encoding lexical, syntactic, discourse and error types of learner language in the feature set. Predictive models are then developed using these features on both datasets and the most predictive features are compared. While the results show that the feature set used results in good predictive models with both datasets, the question "what are the most predictive features?" has a different answer for each dataset.
description: Article accepted for publication at: International Journal of Artificial Intelligence in Education (IJAIED). To appear in early 2017 (journal url: http://www.springer.com/computer/ai/journal/40593)
title: El lecho funerario de época orientalizante de "El Torrejón de Abajo" (Cáceres)
title: El lecho funerario de época orientalizante de "El Torrejón de Abajo" (Cáceres)
titleType: Subtitle
Creators: name: Jiménez Ávila, Javier
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: El Torrejón de Abajo (Cáceres)
subject: El Torrejón de Abajo (Cáceres)

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Folgt.
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Creators: name: Abdallah, Abdallah E.
name: Mabrouk, Reda R.
name: Al Ward, Maged Mohammed Saleh
name: Eissa, Sally I.
name: Elkaeed, Eslam B.
name: Mehany, Ahmed B. M.
name: Abo-Saif, Mariam A.
name: El-Feky, Ola A.
name: Alesawy, Mohamed S.
name: El-Zahabi, Mohamed Ayman
Publisher: name: Taylor & Francis
Year: 2022
Subjects: Biochemistry
Cell Biology
Molecular Biology
Pharmacology
Biotechnology
Chemical Sciences not elsewhere classified
Biological Sciences not elsewhere classified
Information Systems not elsewhere classified
Cancer

description: Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 µM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 µM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.
title: El cilindro-sello de Vélez-Málaga
title: El cilindro-sello de Vélez-Málaga
titleType: Subtitle
Creators: name: García Alfonso, Eduardo
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Vélez-Málaga (Málaga)
subject: Vélez-Málaga (Málaga)

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Folgt.
Additional file 2 of EZH2 mitigates the cardioprotective effects of mesenchymal stem cell-secreted exosomes against infarction via HMGA2-mediated PI3K/AKT signaling
Creators: name: Jiao, Wei
name: Hao, Jie
name: Xie, Yanan
name: Meng, Mingjie
name: Gao, Weinian
Publisher: name: figshare
Year: 2022
Subjects: subject: Biochemistry
subject: Medicine
subject: Cell Biology
subject: Physiology
subject: FOS: Biological sciences
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Developmental Biology
subject: Cancer
subject: Infectious Diseases
subject: FOS: Health sciences
subject: Virology

description: Additional file 2: Original, full-length gel and lot images of Fig 3F.
Elicitação gramatical sobre Juma com anotações de campo / Grammatical elicitation on Juma with fieldwork notes
Creators: name: Juma, Mandei
name: Dos Santos, Wesley
Publisher: name: California Language Archive, University of California, Berkeley
Year: 2025
Subjects: subject: jua

description: Este conjunto de arquivos contém gravações de áudio da variedade Juma (ISO jua) da língua Kawahiva e provêm de sessões de elicitação gramatical com a consultora Mandei Juma (identificado pelas iniciais mju) com o linguista Wesley Nascimento dos Santos (identificada pelas iniciais wns) em janeiro de 2022, em Porto Velho, Rondônia.

Essas gravações somam o total de 24 arquivos .wav. A estrutura do rótulo do arquivo está assim definida:

jua_data_abreviação.do.nome.da.consultora_abreviação.do.nome.do.linguista._número.da.sessão_elicit.wav

As anotações realizadas durante essas seções de elicitação estão no documento PDF.

= = = = = = = = = = = = = = = = = = = =

This file bundle contains audio recordings of the Juma variety (ISO jua) of the Kawahíva language and comes from grammatical elicitation sessions with the consultant Mandei Juma (identified with the initials mju) with the linguist Wesley Nascimento dos Santos (identified with the initials wns) in January 2022 in Porto Velho, state of Rondônia, Brazil.

These recordings total 24 files in .wav format. The structure of the file name is as follows:

language.ISO.code_date_consultant.abbreviation_collector.abbreviation_number_elicit.wav

The field notes taken during the sessions are in the pdf document.
Nodeless superconductivity and the peak effect in the quasi-skutterudites $\mathrm{Lu}_3\mathrm{Os}_4\mathrm{Ge}_{13}$ and $\mathrm{Y}_3\mathrm{Ru}_4\mathrm{Ge}_{13}$
Creators: name: Weng, Z. F.
name: Smidman, M.
name: Pang, G. M.
name: Prakash, O.
name: Chen, Y.
name: Zhang, Y. J.
name: Ramakrishnan, S.
name: Yuan, H. Q.
Publisher: name: arXiv
Year: 2017
Subjects: subject: Superconductivity (cond-mat.supr-con)
subject: FOS: Physical sciences

description: We report an investigation of the superconducting states of $\mathrm{Lu}_3\mathrm{Os}_4\mathrm{Ge}_{13}$ and $\mathrm{Y}_3\mathrm{Ru}_4\mathrm{Ge}_{13}$ single crystals by measurements of the electrical resistivity, ac susceptibility and London penetration depth. The analysis of the penetration depth and the derived superfluid density indicates the presence of nodeless superconductivity and suggest that there are multiple superconducting gaps in both materials. Furthermore, ac susceptibility measurements of both compounds display the peak effect in the low temperature region of the $H-T$ phase diagram. This anomalous increase of the critical current with field gives an indication of a change of the arrangement of flux lines in the mixed state, as found in some of the isostructural stannide materials.
description: 7 pages, 8 figures
Additional file 4 of EZH2 mitigates the cardioprotective effects of mesenchymal stem cell-secreted exosomes against infarction via HMGA2-mediated PI3K/AKT signaling
Creators: name: Jiao, Wei
name: Hao, Jie
name: Xie, Yanan
name: Meng, Mingjie
name: Gao, Weinian
Publisher: name: figshare
Year: 2022
Subjects: subject: Biochemistry
subject: Medicine
subject: Cell Biology
subject: Physiology
subject: FOS: Biological sciences
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Developmental Biology
subject: Cancer
subject: Infectious Diseases
subject: FOS: Health sciences
subject: Virology

description: Additional file 4: Original, full-length gel and lot images of Fig 5D.
Equivalent Markov processes under gauge group
Creators: name: Caruso, M.
name: Jarne, C.
Publisher: name: arXiv
Year: 2017
Subjects: subject: Statistical Mechanics (cond-mat.stat-mech)
subject: FOS: Physical sciences

description: We have studied Markov processes on denumerable state space and continuous time. We found that all these processes are connected via gauge transformations. We have used this result before as a method for resolution of equations, included the case where the sample space is time dependent in a previous work \textit{Phys. Rev. E} \textbf{90}, 022125 (2014). We found a general solution through a dilation of the state space, although the prior probability distribution of the states defined in this new space takes smaller values with respect to the one in the initial problem. The gauge (local) group of dilations modifies the distribution on the dilated space to restore the original process. In this work we show how Markov process in general could be linked via gauge (local) transformations and we present some illustrative examples for this results.
title: Pflanzenreste aus der Probegrabung 1991 im bronzezeitlichen Siedlungsplatz El Argar, prov. Almería, Südostspanien
title: Pflanzenreste aus der Probegrabung 1991 im bronzezeitlichen Siedlungsplatz El Argar, prov. Almería, Südostspanien
titleType: Subtitle
Creators: name: Stika, Hans-Peter
name: Jurich, Bettina
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: El Argar (Cuevas del Almanzora, Almería)
subject: El Argar (Cuevas del Almanzora, Almería)

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Deutsche Zusammenfassung folgt.
A Pilot Case Study on Innovative Behaviour: Lessons Learned and Directions for Future Work
Creators: name: Monteiro, Cleviton
name: da Silva, Fabio Queda Bueno
name: Capretz, Luiz Fernando
Publisher: name: arXiv
Year: 2016
Subjects: subject: Computers and Society (cs.CY)
subject: FOS: Computer and information sciences

description: Context: A case study is a powerful research strategy for investigating complex social-technical and managerial phenomena in real life settings. However, when the phenomenon has not been fully discovered or understood, pilot case studies are important to refine the research problem, the research variables, and the case study design before launching a full-scale investigation. The role of pilot case studies has not been fully addressed in empirical software engineering research literature. Objective: To explore the use of pilot case studies in the design of full-scale case studies, and to report the main lessons learned from an industrial pilot study. Method: We designed and conducted an exploratory case study to identify new relevant research variables that influence the innovative behaviour of software engineers in the industrial setting and to refine the full-scale case study design for the next phase of our research. Results: The use of a pilot case study identified several important research variables that were missing in the initial framework. The pilot study also supported a more sophisticated case study design, which was used to guide a full-scale study. Conclusions: When a research topic has not been fully discovered or understood, it is difficult to create a case study design that covers the relevant research variables and their potential relationships. Conducting a full-scale case study using an untested case design can lead to waste of resources and time if the design has to be reworked during the study. In these situations, the use of pilot case studies can significantly improve the case study design.
description: 6 pages in 10th International Symposium on Empirical Software Engineering and Measurement (ESEM), Ciudad Real, Spain, September 2016
Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
Creators: name: Walczak, Juliusz Maksymilian
name: Iwaszkiewicz-Grześ, Dorota
name: Ziomkowska, Michalina
name: Śliwka-Kaszyńska, Magdalena
name: Daśko, Mateusz
name: Trzonkowski, Piotr
name: Cholewiński, Grzegorz
Publisher: name: Taylor & Francis
Year: 2022
Subjects: Biochemistry
Medicine
Cell Biology
Biotechnology
Chemical Sciences not elsewhere classified

description: The group of 18 new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5′-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis of 14 of them employed uronium-type activating system (TBTU/HOBt/DIPEA) while 4 of them concerned phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without the need of phenolic group protection. Most of optimised protocols did not require complicated reaction work-ups, including chromatographic, solvent-consuming methods. The biological activity assay was performed on the T-Jurkat cell line and peripheral mononuclear blood cells (PBMCs) which are both dedicated for antiproliferative activity determination. Each of designed derivatives was characterised by reduced cytotoxicity and benzoxazole analogue (A2) revealed the most promising activity. Subsequently, an observed structure-activity relationship was discussed.
title: Fuente Alamo : Vorbericht über die Grabung 1996 in der bronzezeitlichen Höhensiedlung
title: Fuente Alamo : Vorbericht über die Grabung 1996 in der bronzezeitlichen Höhensiedlung
titleType: Subtitle
Creators: name: Pingel, Volker
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Fuente Álamo (Cuevas del Almanzora, Almería)
subject: Fuente Álamo (Cuevas del Almanzora, Almería)

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Folgt.
title: El Neolítico en Galicia : nuevas evidencias y nuevas perspectivas
title: El Neolítico en Galicia : nuevas evidencias y nuevas perspectivas
titleType: Subtitle
Creators: name: Suárez Otero, José
name: Carballo Arceo, Luis Xulio
name: Amil Baltasar, Juan Carlos
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Galicia (s. auch/ v. también Gallaecia)
subject: Galicia (s. auch/ v. también Gallaecia)

description: Madrider Mitteilungen, Vol. 39 (1998)
description: Folgt.
Additional file 1 of EZH2 mitigates the cardioprotective effects of mesenchymal stem cell-secreted exosomes against infarction via HMGA2-mediated PI3K/AKT signaling
Creators: name: Jiao, Wei
name: Hao, Jie
name: Xie, Yanan
name: Meng, Mingjie
name: Gao, Weinian
Publisher: name: figshare
Year: 2022
Subjects: subject: Biochemistry
subject: Medicine
subject: Cell Biology
subject: Physiology
subject: FOS: Biological sciences
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Developmental Biology
subject: Cancer
subject: Infectious Diseases
subject: FOS: Health sciences
subject: Virology

description: Additional file 1: Original, full-length gel and lot images of Fig 2G.
title: In memoriam Wilhelm Schüle
title: In memoriam Wilhelm Schüle
titleType: Subtitle
Creators: name: Brandherm, Dirk
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Wilhelm Schüle (1928-1997)
subject: Wilhelm Schüle (1928-1997)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: In memoriam Wilhelm Schüle (1928-1997).
Fracture imaging within a granitic rock aquifer using multiple-offset single-hole and cross-hole GPR reflection data
Creators: name: Dorn, C.
name: Linde, N.
name: Doetsch, J.
name: Borgne, T. Le
name: Bour, O.
Publisher: name: arXiv
Year: 2017
Subjects: subject: Geophysics (physics.geo-ph)
subject: FOS: Physical sciences

description: The sparsely spaced highly permeable fractures of the granitic rock aquifer at Stang-er-Brune (Brittany, France) form a well-connected fracture network of high permeability but unknown geometry. Previous work based on optical and acoustic logging together with single-hole and cross-hole flowmeter data acquired in 3 neighboring boreholes (70-100 m deep) have identified the most important permeable fractures crossing the boreholes and their hydraulic connections. To constrain possible flow paths by estimating the geometries of known and previously unknown fractures, we have acquired, processed and interpreted multifold, single- and cross-hole GPR data using 100 and 250 MHz antennas. The GPR data processing scheme consisting of time-zero corrections, scaling, bandpass filtering and F-X deconvolution, eigenvector filtering, muting, pre-stack Kirchhoff depth migration and stacking was used to differentiate fluid-filled fracture reflections from source-generated noise. The final stacked and pre-stack depth-migrated GPR sections provide high-resolution images of individual fractures (dipping 30-90°) in the surroundings (2-20 m for the 100 MHz antennas; 2-12 m for the 250 MHz antennas) of each borehole in a 2D plane projection that are of superior quality to those obtained from single-offset sections. Most fractures previously identified from hydraulic testing can be correlated to reflections in the single-hole data. Several previously unknown major near vertical fractures have also been identified away from the boreholes.
title: Zu zwei geometrischen Kuppelornamenten der Alhambra in Granada
title: Zu zwei geometrischen Kuppelornamenten der Alhambra in Granada
titleType: Subtitle
Creators: name: Schneider, Gerhard
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Alhambra (Granada)
subject: Alhambra (Granada)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.
HFC-32 and HFC-125 adsorption in the zeolite silicalite
Creators: name: Maginn, Ed
name: Yancey-Jardon, Andrew David
name: Shiflett, Mark B.
name: Marin-Rimoldi, Eliseo
Publisher: name: OSF
Year: 2023
Subjects: adsorption
climate change
global warming
grand canonical monte carlo
hydrofluorocarbon
molecular dynamics simulation
molecular simulations
monte carlo
r125
r32
silicalite
thermodynamics

description: This project contains the raw data obtained from experiments and grand canonical Monte Carlo simulations of adsorption of HFC-32 and HFC-125 in the zeolite silicalite.
A SICA compartmental model in epidemiology with application to HIV/AIDS in Cape Verde
Creators: name: Silva, Cristiana J.
name: Torres, Delfim F. M.
Publisher: name: arXiv
Year: 2016
Subjects: subject: Populations and Evolution (q-bio.PE)
subject: Dynamical Systems (math.DS)
subject: FOS: Biological sciences
subject: FOS: Mathematics
subject: 34C60, 34D23, 92D30

description: We propose a new mathematical model for the transmission dynamics of the human immunodeficiency virus (HIV). Global stability of the unique endemic equilibrium is proved. Then, based on data provided by the "Progress Report on the AIDS response in Cape Verde 2015", we calibrate our model to the cumulative cases of infection by HIV and AIDS from 1987 to 2014 and we show that our model predicts well such reality. Finally, a sensitivity analysis is done for the case study in Cape Verde. We conclude that the goal of the United Nations to end the AIDS epidemic by 2030 is a nontrivial task.
description: This is a preprint of a paper whose final and definite form is with 'Ecological Complexity', ISSN 1476-945X, available at [http://dx.doi.org/10.1016/j.ecocom.2016.12.001]. Submitted 29/April/2016; Revised 21/Oct/2016; Accepted 02/Dec/2016
Searching for drug leads targeted to the hydrophobic cleft of dengue virus capsid protein
Creators: name: Ortlieb, Liliane O.
name: Caruso, Ícaro P.
name: Mebus-Antunes, Nathane C.
name: Da Poian, Andrea T.
name: da C. Petronilho, Elaine
name: Figueroa-Villar, José Daniel
name: Nascimento, Claudia J.
name: Almeida, Fabio C. L.
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biophysics
subject: Biochemistry
subject: Pharmacology
subject: Biotechnology
subject: Chemical Sciences not elsewhere classified
subject: Cancer
subject: Mental Health
subject: Infectious Diseases
subject: FOS: Health sciences
subject: Virology

description: We synthesised and screened 18 aromatic derivatives of guanylhydrazones and oximes aromatic for their capacity to bind to dengue virus capsid protein (DENVC). The intended therapeutic target was the hydrophobic cleft of DENVC, which is a region responsible for its anchoring in lipid droplets in the infected cells. The inhibition of this process completely suppresses virus infectivity. Using NMR, we describe five compounds able to bind to the α1-α2 interface in the hydrophobic cleft. Saturation transfer difference experiments showed that the aromatic protons of the ligands are important for the interaction with DENVC. Fluorescence binding isotherms indicated that the selected compounds bind at micromolar affinities, possibly leading to binding-induced conformational changes. NMR-derived docking calculations of ligands showed that they position similarly in the hydrophobic cleft. Cytotoxicity experiments and calculations of in silico drug properties suggest that these compounds may be promising candidates in the search for antivirals targeting DENVC.
title: Topografía funeraria rural entre el Miño y el Duero durante la antigüedad tardía, siglos V - VII. Aproximación a un marco cronológico y tipológico
title: Topografía funeraria rural entre el Miño y el Duero durante la antigüedad tardía, siglos V - VII. Aproximación a un marco cronológico y tipológico
titleType: Subtitle
Creators: name: Quiroga, Jorge López
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Minho
subject: Minho

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
title: A Comparative Study on the Spatial Capacity of University Campuses in Guangdong Province
Creators: name: Guo, Weihong
name: Ding, Yaqian
name: Yang, Guang
name: Liu, Xiao
Publisher: name: Conference Proceedings XXIX International Seminar on Urban Form ISUF 2022 Urban Redevelopment and Revitalisation A Multidisciplinary Perspective/ Lodz University of Technology Press
Year: 2023
Subjects: Comparative Study, Chinese University Campuses, Guangdong Province, Renewal, Spatial Capacity

description: In an era of stock development, the objective is to propose strategies to adapt to the future spatial renewal and transformation of university campuses in urban areas of Guangdong to resolve the contradiction between the limited campus capacity and the annually increasing number of students. In this paper, eight universities in Guangdong are selected, and their spatial patterns and capacities are compared and analysed in terms of the theoretical concepts of urban morphology, extracting the planar layout, floor area, street space, and number of students and teachers of the eight universities, and comparing them with those of some other universities in China and with the index requirements in the relevant Chinese standards and regulations. The analysis indicates that the campuses in Guangdong have reached their maximum student and instructor population, construction density, and spatial capacity. The ensuing spatial expansion of the campus should prioritize stock development and internal spatial adjustment and optimization, with the teaching function taking precedence and a broader public service area supporting the talent cultivation program. In this manner, the concept of Guangdong-specific spatial rejuvenation of university campuses is discussed.
title: Zum 1. Bildnistypus der Faustina Minor
title: Zum 1. Bildnistypus der Faustina Minor
titleType: Subtitle
Creators: name: Trunk, Markus
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Sevilla, Casa de Pilatos
subject: Sevilla, Casa de Pilatos

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.
title: Die Dorfkirche von Sant'Ana do Campo : Beobachtungen an einem ungewöhnlichen römischen Tempel
title: Die Dorfkirche von Sant'Ana do Campo : Beobachtungen an einem ungewöhnlichen römischen Tempel
titleType: Subtitle
Creators: name: Schattner, Thomas G.
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Sant'Ana do Campo (Arraiolos, Évora, Port.)
subject: Sant'Ana do Campo (Arraiolos, Évora, Port.)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Die Beobachtungen an dem seit langem bekannten römischen Tempel, der Teil der Dorfkirche von Sant’Ana ist, führen zu einer Rekonstruktion der gesamten Anlage, die demnach aus einem Hof von gestaucht breitrechteckiger bzw. annähernd quadratischer Form besteht, an den der Tempel (mit vergleichbarem Grundriß) angefügt ist. Die herausgearbeiteten Merkmale sind kennzeichnend für die Zuweisung zu einer Gruppe von römischen Tempelanlagen, die vor allem in Nordafrika verbreitet sind. Der Carneus-Tempel stellt erst das zweite Beispiel in Europa dar. Es wird häufig vermutet, daß diese Anlagen ältere punische Kultplätze als Vorgängerheiligtümer besitzen. Zur Überprüfung dieser Annahme in Sant’Ana und ihrer Weiterungen wäre eine Grabung erforderlich.
title: La pintura romana en Hispania de Augusto a Nerón
title: La pintura romana en Hispania de Augusto a Nerón
titleType: Subtitle
Creators: name:  Mostalac Carrillo,  Antonio
Publisher: name: Deutsches Archäologisches Institut
Year: 2020

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
title: Resulta factible identificar la región minera de Três Minas, norte de Portugal, con el Metallum Albucrarense de Plinio?
title: Resulta factible identificar la región minera de Três Minas, norte de Portugal, con el Metallum Albucrarense de Plinio?
titleType: Subtitle
Creators: name:  Rodríguez Colmenero, Antonio
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Três Minas (Vila Pouca de Aguiar, Vila Real, Port.)
subject: Três Minas (Vila Pouca de Aguiar, Vila Real, Port.)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
title: La necrópolis de época tardo-púnica de los Campos Elíseos (Gibralfaro, Málaga)
title: La necrópolis de época tardo-púnica de los Campos Elíseos (Gibralfaro, Málaga)
titleType: Subtitle
Creators: name: Martín Ruiz, Juan Antonio
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Málaga
subject: Málaga

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
title: Zur Wiederaufnahme archäologischer Forschungen in den römischen Lagern bei Renieblas (prov. Soria)
title: Zur Wiederaufnahme archäologischer Forschungen in den römischen Lagern bei Renieblas (prov. Soria)
titleType: Subtitle
Creators: name: Breuer, Peter
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Renieblas (Numancia, Soria)
subject: Renieblas (Numancia, Soria)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.
title: El santuario heroico de "El Pajarillo" de Huelma (Jaén)
title: El santuario heroico de "El Pajarillo" de Huelma (Jaén)
titleType: Subtitle
Creators: name: Molinos Molinos, Manuel
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: El Pajarillo (Huelma, Jaén)
subject: El Pajarillo (Huelma, Jaén)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
Using Big Data to Enhance the Bosch Production Line Performance: A Kaggle Challenge
Creators: name: Mangal, Ankita
name: Kumar, Nishant
Publisher: name: arXiv
Year: 2017
Subjects: subject: Machine Learning (cs.LG)
subject: FOS: Computer and information sciences

description: This paper describes our approach to the Bosch production line performance challenge run by Kaggle.com. Maximizing the production yield is at the heart of the manufacturing industry. At the Bosch assembly line, data is recorded for products as they progress through each stage. Data science methods are applied to this huge data repository consisting records of tests and measurements made for each component along the assembly line to predict internal failures. We found that it is possible to train a model that predicts which parts are most likely to fail. Thus a smarter failure detection system can be built and the parts tagged likely to fail can be salvaged to decrease operating costs and increase the profit margins.
description: IEEE Big Data 2016 Conference
Additional file 3 of EZH2 mitigates the cardioprotective effects of mesenchymal stem cell-secreted exosomes against infarction via HMGA2-mediated PI3K/AKT signaling
Creators: name: Jiao, Wei
name: Hao, Jie
name: Xie, Yanan
name: Meng, Mingjie
name: Gao, Weinian
Publisher: name: figshare
Year: 2022
Subjects: subject: Biochemistry
subject: Medicine
subject: Cell Biology
subject: Physiology
subject: FOS: Biological sciences
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Developmental Biology
subject: Cancer
subject: Infectious Diseases
subject: FOS: Health sciences
subject: Virology

description: Additional file 3: Original, full-length gel and lot images of Fig 5A.
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Creators: name: Abdallah, Abdallah E.
name: Mabrouk, Reda R.
name: Ward, Maged Mohammed Saleh Al
name: Eissa, Sally I.
name: Elkaeed, Eslam B.
name: Mehany, Ahmed B. M.
name: Abo-Saif, Mariam A.
name: El-Feky, Ola A.
name: Alesawy, Mohamed S.
name: El-Zahabi, Mohamed Ayman
Publisher: name: Taylor & Francis
Year: 2022
Subjects: Biochemistry
Cell Biology
Molecular Biology
Pharmacology
Biotechnology
Chemical Sciences not elsewhere classified
Biological Sciences not elsewhere classified
Information Systems not elsewhere classified
Cancer

description: Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 µM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 µM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.
TiO2 nanotube immobilised 5-lipoxygenase-mediated screening and isolation of anti-inflammatory active compounds from the leaves of lonicera japonica thunb
Creators: name: Zhu, Jinhua
name: Zhou, Danyang
name: Wu, Dandan
name: Liu, Wei
name: Liu, Xiuhua
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Genetics
subject: FOS: Biological sciences
subject: Neuroscience
subject: Pharmacology
subject: Biotechnology
subject: Environmental Sciences not elsewhere classified
subject: Chemical Sciences not elsewhere classified
subject: Ecology
subject: Immunology
subject: FOS: Clinical medicine
subject: Biological Sciences not elsewhere classified

description: In this work, a highly effective separation approach mediated by 5-Lipoxygenase (5-LOX) was established for screening and isolation of anti-inflammatory ingredients from leaves of Lonicera japonica Thunb. (LLJT). Using 5-LOX immobilised on TiO2 nanotubes as a microreactor, the targeted screening was exploited by combining with HPLC-MS system. Four compounds confirmed as luteolin, luteoside, lonicerin, and isochlorogenic acid C and a fraction (M1) were screened out to be potent inhibitors of 5-LOX. Their anti-inflammatory activities were further investigated and confirmed by RAW 264.7 cells inflammation model and rat foot swelling model. Furthermore, M1 was prepared by MCI GEL CHP20P column chromatography, and further separated by Pre-HPLC. One new compound confirmed to be 5,7,3′,4′-tetrahydroxyflavone-7-O-sambubioside was first isolated from LLJT. The results provide a new method for the effective separation of active components derived from natural products.HighlightsA 5-LOX mediated separation method was established for isolation of anti-inflammatory compounds.An anti-inflammatory ingredient was separated by MCI GEL CHP20P column chromatography.One new compound was first isolated from leaves of Lonicera japonica Thunb.5-LOX was immobilised on TiO2 nanotubes and exploited by combining with HPLC-MS system.The anti-inflammatory activity of screened components was evaluated. A 5-LOX mediated separation method was established for isolation of anti-inflammatory compounds. An anti-inflammatory ingredient was separated by MCI GEL CHP20P column chromatography. One new compound was first isolated from leaves of Lonicera japonica Thunb. 5-LOX was immobilised on TiO2 nanotubes and exploited by combining with HPLC-MS system. The anti-inflammatory activity of screened components was evaluated.
Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold with apoptotic activity
Creators: name: Mandour, Asmaa A.
name: Nassar, Ibrahim F.
name: Aal, Mohammed T. Abdel
name: Shahin, Mahmoud A. E.
name: El-Sayed, Wael A.
name: Hegazy, Maghawry
name: Yehia, Amr Mohamed
name: Ismail, Ahmed
name: Hagras, Mohamed
name: Elkaeed, Eslam B.
name: Refaat, Hanan M.
name: Ismail, Nasser S. M.
Publisher: name: Taylor & Francis
Year: 2022
Subjects: Biochemistry
Cell Biology
Pharmacology
Biotechnology
Chemical Sciences not elsewhere classified
Biological Sciences not elsewhere classified
Information Systems not elsewhere classified
Cancer
Hematology

description: Cyclin-dependent kinase inhibition is considered a promising target for cancer treatment for its crucial role in cell cycle regulation. Pyrazolo pyrimidine derivatives were well established for their antitumor activity via CDK2 inhibition. In this research, new series of pyrazolopyrimidine derivatives (4–15) was designed and synthesised as novel CDK2 inhibitors. The anti-proliferative activities against MCF-7, HCT-116, and HepG-2 were used to evaluate their anticancer activity as novel CDK2 inhibitors. Most of the compounds showed superior cytotoxic activity against MCF-7 and HCT-116 compared to Sorafenib. Only compounds 8, 14, and 15 showed potent activity against HepG-2. The CDK2/cyclin A2 enzyme inhibitory activity was tested for all synthesised compounds. Compound 15 showed the most significant inhibitory activity with IC50 0.061 ± 0.003 µM. It exerted remarkable alteration in Pre G1 and S phase cell cycle progression and caused apoptosis in HCT cells. In addition, the normal cell line cytotoxicity for compound 15 was assigned revealing low cytotoxic results in normal cells rather than cancer cells. Molecular docking was achieved on the designed compounds and confirmed the two essential hydrogen binding with Leu83 in CDK2 active site. In silico ADMET studies and drug-likeness showed proper pharmacokinetic properties which helped in structure requirements prediction for the observed antitumor activity.
title: La necrópolis tartésica de la Cruz del Negro (Carmona, Sevilla), ayer y hoy
title: La necrópolis tartésica de la Cruz del Negro (Carmona, Sevilla), ayer y hoy
titleType: Subtitle
Creators: name: Maier, Jorge
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Cruz del Negro, La (Carmona, Sevilla)
subject: Cruz del Negro, La (Carmona, Sevilla)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Folgt.
Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors
Creators: name: Yang, Man
name: Li, Chenyao
name: Li, Yajing
name: Cheng, Chen
name: Shi, Meiyun
name: Yin, Lei
name: Xue, Hongyu
name: Liu, Yajun
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biophysics
subject: Biochemistry
subject: Medicine
subject: Microbiology
subject: FOS: Biological sciences
subject: Cell Biology
subject: Genetics
subject: Molecular Biology
subject: Pharmacology
subject: Biotechnology
subject: Environmental Sciences not elsewhere classified
subject: Chemical Sciences not elsewhere classified
subject: Biological Sciences not elsewhere classified
subject: Developmental Biology

description: The molecular chaperone HSP90 plays an essential role in cancer occurrence and development. Therefore, it is an important target for the development of anticancer drugs. 1,3-Dibenzyl-2-aryl imidazolidine (8) is a previously reported inhibitor of HSP90; however, its anticancer activity is poor. In this work, chemical modification of 8 led to the discovery of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as two types of novel HSP90 N-terminal inhibitors. 16l and 22k exhibited antiproliferative activity against multiple breast cancer cell lines with IC50 values at the low micromolar level. 16l and 22k induced significant degradation of the client proteins AKT and ERK and a lower level of the heat shock response in comparison with tanespimycin (17-AAG). 22k exhibited a strong affinity for the HSP90α N-terminus with an IC50 value of 0.21 μM. A molecular docking study revealed that 16l and 22k successfully bind to the geldanamycin binding site at the N-terminus of HSP90α.
Trends in Students Media Usage
Creators: name: Gidion, Gerd
name: Capretz, Luiz Fernando
name: Grosch, Michael
name: Meadows, Ke
Publisher: name: arXiv
Year: 2016
Subjects: subject: Computers and Society (cs.CY)
subject: FOS: Computer and information sciences

description: Trends in media usage by students can affect the way they learn. Students demand the use of technology, thus institutions and instructors should meet students requests. This paper describes the results of a survey where drivers in the use of media show continuously increasing or decreasing values from the first to the fourth year of study experience at the Western University, Canada, highlighting trends in the usage of new and traditional media in higher education by students. The survey was used to gather data on students media usage habits and user satisfaction from first to fourth year of study and found that media usage increases over the years from first to fourth. The presentation of data using bar charts reveals a slight increase over the years in students owning notebooks or laptops off-campus and a significant increase from first to fourth year of students accessing online academic periodicals and journals. Another noteworthy finding relates to fourth year students being more conscious of the quality of information that they read on the Internet in comparison to students in first year, even though this is a slight year on year increase.
description: arXiv admin note: text overlap with arXiv:1507.06857
Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer
Creators: name: Abdelsalam, Esraa A.
name: El-Hafeez, Amer Ali Abd
name: Eldehna, Wagdy M.
name: Hassab, Mahmoud A. El
name: Marzouk, Hala Mohamed M.
name: Elaasser, Mahmoud M.
name: Taleb, Nageh A. Abou
name: Amin, Kamilia M.
name: Abdel-Aziz, Hatem A.
name: Ghosh, Pradipta
name: Hammad, Sherif F.
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Cell Biology
subject: Molecular Biology
subject: Pharmacology
subject: Biotechnology
subject: Chemical Sciences not elsewhere classified
subject: Biological Sciences not elsewhere classified
subject: Developmental Biology
subject: Cancer
subject: Hematology
subject: Infectious Diseases
subject: FOS: Health sciences

description: New series of thiazolyl-pyrazoline derivatives (7a–7d, 10a–10d and 13a–13f) have been synthesised and assessed for their potential EGFR and VEGFR-2 inhibitory activities. Compounds 10b and 10d exerted potent and selective inhibitory activity towards the two receptor tyrosine kinases; EGFR (IC50 = 40.7 ± 1.0 and 32.5 ± 2.2 nM, respectively) and VEGFR-2 (IC50 = 78.4 ± 1.5 and 43.0 ± 2.4 nM, respectively). The best anti-proliferative activity for the examined thiazolyl-pyrazolines was observed against the non-small lung cancer cells (NSCLC). Compounds 10b and 10d displayed pronounced efficacy against A549 (IC50 = 4.2 and 2.9 µM, respectively) and H441 cell lines (IC50 = 4.8 and 3.8 µM, respectively). Moreover, our results indicated that 10b and 10d were much more effective towards EGFR-mutated NSCLC cell lines (NCI-H1650 and NCI-H1975 cells) than gefitinib. Finally, compounds 10b and 10d induce G2/M cell cycle arrest and apoptosis and inhibit migration in A549 cancerous cells.
title: Castelo Velho de Freixo de Numäo (Vila Nova de Foz Cöa, Portugal). Geschichte der Interpretationsversuche
title: Castelo Velho de Freixo de Numäo (Vila Nova de Foz Cöa, Portugal). Geschichte der Interpretationsversuche
titleType: Subtitle
Creators: name: Oliveira Jorge, Susana
Publisher: name: Deutsches Archäologisches Institut
Year: 2020

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.
Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors
Creators: name: González-Naranjo, Pedro
name: Pérez, Concepción
name: González-Sánchez, Marina
name: Gironda-Martínez, Adrián
name: Ulzurrun, Eugenia
name: Bartolomé, Fernando
name: Rubio-Fernández, Marcos
name: Martin-Requero, Angeles
name: Campillo, Nuria E.
name: Páez, Juan A.
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Neuroscience
subject: Pharmacology
subject: Biotechnology
subject: Chemical Sciences not elsewhere classified
subject: Immunology
subject: FOS: Clinical medicine
subject: Biological Sciences not elsewhere classified
subject: Cancer

description: Multitarget drugs are a promising therapeutic approach against Alzheimer’s disease. In this work, a new family of 5-substituted indazole derivatives with a multitarget profile including cholinesterase and BACE1 inhibition is described. Thus, the synthesis and evaluation of a new class of 5-substituted indazoles has been performed. Pharmacological evaluation includes in vitro inhibitory assays on AChE/BuChE and BACE1 enzymes. Also, the corresponding competition studies on BuChE were carried out. Additionally, antioxidant properties have been calculated from ORAC assays. Furthermore, studies of anti-inflammatory properties on Raw 264.7 cells and neuroprotective effects in human neuroblastoma SH-SY5Y cells have been performed. The results of pharmacological tests have shown that some of these 5-substituted indazole derivatives 1–4 and 6 behave as AChE/BuChE and BACE1 inhibitors, simultaneously. In addition, some indazole derivatives showed anti-inflammatory (3, 6) and neuroprotective (1–4 and 6) effects against Aβ-induced cell death in human neuroblastoma SH-SY5Y cells with antioxidant properties.
title: Kupferzeitliche Pflanzenreste aus Almizaraque und Las Pilas (prov. Almería, Südostspanien)
title: Kupferzeitliche Pflanzenreste aus Almizaraque und Las Pilas (prov. Almería, Südostspanien)
titleType: Subtitle
Creators: name: Stika, Hans-Peter
name: Jurich, Bettina
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Las Pilas (Mojácar, Almería)
subject: Almizaraque (Almería)
subject: Las Pilas (Mojácar, Almería)
subject: Almizaraque (Almería)
subject: Las Pilas (Mojácar, Almería)
subject: Almizaraque (Almería)

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.
title: Vorbericht über die Tierknochenfunde aus Ambrona (prov. Soria)
title: Vorbericht über die Tierknochenfunde aus Ambrona (prov. Soria)
titleType: Subtitle
Creators: name: Liesau, Corina
Publisher: name: Deutsches Archäologisches Institut
Year: 2020
Subjects: subject: Ambrona (Miño de Medinaceli, Soria)
subject: Domestikation
subject: Tierknochenfunde
subject: Transhumanz
subject: Ambrona (Miño de Medinaceli, Soria)
subject: domestication
subject: animal bone finds
subject: transhumance
subject: Ambrona (Miño de Medinaceli, Soria)
subject: domesticación
subject: huesos de animales
subject: transhumancia

description: Madrider Mitteilungen, Vol. 40 (1999)
description: Deutsche Zusammenfassung folgt.