cometadata/datacite-rtg-text-other-reclassification-records huggingface dataset:
Total synthesis of Sumalactone A
Creators: name: Reddy, G. Nagendra
name: Gudisela, Mura Reddy
name: Boddiboyena, Ramesh
name: Prasad, K. R. S.
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Microbiology
subject: FOS: Biological sciences
subject: Molecular Biology
subject: Physiology
subject: Biotechnology
subject: Evolutionary Biology
subject: 59999 Environmental Sciences not elsewhere classified
subject: FOS: Earth and related environmental sciences
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 80699 Information Systems not elsewhere classified
subject: FOS: Computer and information sciences

description: A simple and efficient stereoselective synthesis of 10-membered Benzannulated macrolactone, Sumalactone A has been accomplished from inexpensive and commercially available starting materials. This convergent synthesis utilizes Vilsmeier-Haack formylation, Jacobsen hydrolytic kinetic resolution, esterification under Yamaguchi conditions and ring-closing metathesis as key steps.
Life Beyond Kinases: Structure-Based Discovery of Sorafenib as Nanomolar Antagonist of 5-HT Receptors
Creators: name: Wang, Shaohui
name: Chen, Gang
name: Whaley, Ryan
name: Peng, Shiming
name: Wang, Simon X.
name: Zhang, Guoliang
name: Huang, Niu
name: Lin, Xingyu
name: Roth, Bryan L.
name: Huang, Xi-Ping
name: Wang, Yanli
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2012

description: Of great interest in recent years has been computationally predicting the novel polypharmacology of drug molecules. Here, we applied an “induced-fit” protocol to improve the homology models of 5-HT2A receptor, and we assessed the quality of these models in retrospective virtual screening. Subsequently, we computationally screened the FDA approved drug molecules against the best induced-fit 5-HT2A models, and chose six top scoring hits for experimental assays. Surprisingly, one well-known kinase inhibitor, sorafenib has shown unexpected promiscuous 5-HTRs binding affinities, Ki = 1959, 56 and 417 nM against 5-HT2A, 5-HT2B and 5-HT2C, respectively. Our preliminary SAR exploration supports the predicted binding mode, and further suggests sorafenib to be a novel lead compound for 5HTR ligand discovery. Although it has been well known that sorafenib produces anticancer effects through targeting multiple kinases, carefully designed experimental studies are desirable to fully understand whether its “off-target” 5-HTR binding activities contribute to its therapeutic efficacy or otherwise undesirable side effects.
Orally Active Adenosine A 1 Receptor Agonists with Antinociceptive Effects in Mice
Creators: name: Korboukh, Ilia
name: Setola, Vincent
name: Randhawa, Amarjit S.
name: Frye, Stephen V.
name: Jin, Jian
name: Coleman, Jennifer
name: Janzen, William P.
name: Fitzpatrick, Brendan J.
name: Rittiner, Joseph E.
name: Zylka, Mark J.
name: Hull-Ryde, Emily A.
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2012

description: Adenosine A1 receptor (A1AR) agonists have antinociceptive effects in multiple preclinical models of acute and chronic pain. Although numerous A1AR agonists have been developed, clinical applications of these agents have been hampered by their cardiovascular side effects. Herein we report a series of novel A1AR agonists, some of which are structurally related to adenosine 5′-monophosphate (5′-AMP), a naturally occurring nucleotide that itself activates A1AR. These novel compounds potently activate A1AR in several orthogonal in vitro assays and are subtype selective for A1AR over A2AAR, A2BAR, and A3AR. Among them, UNC32A (3a) is orally active and has dose-dependent antinociceptive effects in wild-type mice. The antinociceptive effects of 3a were completely abolished in A1AR knockout mice, revealing a strict dependence on A1AR for activity. The apparent lack of cardiovascular side effects when administered orally and high affinity (Ki of 36 nM for the human A1AR) make this compound potentially suitable as a therapeutic.
Table S1 and Figs S1-S4 from More than the sum of the parts: annual partitioning within spatial guilds underpins community regulation
Creators: name: A. E. Magurran
name: P. A. Henderson
Publisher: name: The Royal Society
Year: 2018
Subjects: subject: Environmental Science
subject: Ecology
subject: FOS: Biological sciences
subject: 60102 Bioinformatics
subject: FOS: Computer and information sciences
subject: 10202 Biological Mathematics
subject: FOS: Mathematics

description: Table of guild members and additional information on the randomisation tests undertaken
Bag-of-Vectors Autoencoders for Unsupervised Conditional Text Generation
Creators: name: Mai, Florian
name: Henderson, James
Publisher: name: arXiv
Year: 2021
Subjects: subject: Computation and Language (cs.CL)
subject: Artificial Intelligence (cs.AI)
subject: Machine Learning (cs.LG)
subject: FOS: Computer and information sciences

description: Text autoencoders are often used for unsupervised conditional text generation by applying mappings in the latent space to change attributes to the desired values. Recently, Mai et al. (2020) proposed Emb2Emb, a method to learn these mappings in the embedding space of an autoencoder. However, their method is restricted to autoencoders with a single-vector embedding, which limits how much information can be retained. We address this issue by extending their method to Bag-of-Vectors Autoencoders (BoV-AEs), which encode the text into a variable-size bag of vectors that grows with the size of the text, as in attention-based models. This allows to encode and reconstruct much longer texts than standard autoencoders. Analogous to conventional autoencoders, we propose regularization techniques that facilitate learning meaningful operations in the latent space. Finally, we adapt Emb2Emb for a training scheme that learns to map an input bag to an output bag, including a novel loss function and neural architecture. Our empirical evaluations on unsupervised sentiment transfer show that our method performs substantially better than a standard autoencoder.
description: Published at AACL 2022
Methods and results of an analysis of individual differences in comparative test batteries aiming at self-control (Amici et al., 2008; MacLean et al. 2014). from Comparative psychometrics: establishing what differs is central to understanding what evolves.
Creators: name: Völter, Christoph J.
name: Tinklenberg, Brandon
name: Call, Josep
name: Seed, Amanda
Publisher: name: The Royal Society
Year: 2018
Subjects: subject: Evolutionary Biology
subject: FOS: Biological sciences
subject: 170299 Cognitive Science not elsewhere classified
subject: FOS: Psychology
subject: 60801 Animal Behaviour

description: Detailed description of GLMM analysis of the dataset by MacLean et al. (2014) and correlation analyses of the dataset by Amici et al. (2008).
Synthesis and anticancer activity of oxazolo and oxazinoquinolinone derivatives
Creators: name: Talaat, Nancy
name: Abass, Mohamed
name: Hassanin, Hany Mohamed
name: Abdel-Kader, Dalia
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Molecular Biology
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: Immunology
subject: FOS: Clinical medicine
subject: 80699 Information Systems not elsewhere classified
subject: FOS: Computer and information sciences
subject: 110309 Infectious Diseases
subject: FOS: Health sciences
subject: 60506 Virology
subject: FOS: Biological sciences

description: A convenient and efficient reduction of 3-nitro-4-hydroxy-1-methylquinolin-2(1H)-one using tin and hydrochloric acid produced the novel 3-amino-4-hydroxyquinolinone derivative. The aminoquinoline was reacted with various electrophilic reagents such as acid anhydrides, acyl chlorides and esters to give a tricyclic system namely; oxazoloquinolinone and oxazinoquinolinone. Diazotization and alkylation of aminoquinoline were carried out affording the interesting N-alkylated quinoline and azodye derivatives. Selected products were screened for their anticancer activity against HepG-2 and MCF-7 cell lines. Among the various synthesized derivatives, the aminoquinoline compound is the strong antiproliferative agent and may consider a specific therapeutic index.
Methods and results of an analysis of individual differences in comparative test batteries aiming at self-control (Amici et al., 2008; MacLean et al. 2014). from Comparative psychometrics: establishing what differs is central to understanding what evolves
Creators: name: Völter, Christoph J.
name: Tinklenberg, Brandon
name: Call, Josep
name: Seed, Amanda
Publisher: name: The Royal Society
Year: 2018
Subjects: subject: Evolutionary Biology
subject: FOS: Biological sciences
subject: 170299 Cognitive Science not elsewhere classified
subject: FOS: Psychology
subject: 60801 Animal Behaviour

description: Detailed description of GLMM analysis of the dataset by MacLean et al. (2014) and correlation analyses of the dataset by Amici et al. (2008).
Improving Variational Autoencoders for New Physics Detection at the LHC with Normalizing Flows
Creators: name: Jawahar, Pratik
name: Aarrestad, Thea
name: Chernyavskaya, Nadezda
name: Pierini, Maurizio
name: Wozniak, Kinga A.
name: Ngadiuba, Jennifer
name: Duarte, Javier
name: Tsan, Steven
Publisher: name: arXiv
Year: 2021
Subjects: subject: High Energy Physics - Phenomenology (hep-ph)
subject: High Energy Physics - Experiment (hep-ex)
subject: Data Analysis, Statistics and Probability (physics.data-an)
subject: FOS: Physical sciences

description: We investigate how to improve new physics detection strategies exploiting variational autoencoders and normalizing flows for anomaly detection at the Large Hadron Collider. As a working example, we consider the DarkMachines challenge dataset. We show how different design choices (e.g., event representations, anomaly score definitions, network architectures) affect the result on specific benchmark new physics models. Once a baseline is established, we discuss how to improve the anomaly detection accuracy by exploiting normalizing flow layers in the latent space of the variational autoencoder.
description: 10 + 3 pages, 7 figures
Particle-vortex duality of 2d Dirac fermion from electric-magnetic duality of 3d topological insulators
Creators: name: Metlitski, Max A.
name: Vishwanath, Ashvin
Publisher: name: arXiv
Year: 2015
Subjects: subject: Strongly Correlated Electrons (cond-mat.str-el)
subject: Mesoscale and Nanoscale Physics (cond-mat.mes-hall)
subject: High Energy Physics - Theory (hep-th)
subject: FOS: Physical sciences

description: Particle-vortex duality is a powerful theoretical tool that has been used to study bosonic systems. Here we propose an analogous duality for Dirac fermions in 2+1 dimensions. The physics of a single Dirac cone is proposed to be described by a dual theory, QED3 with a dual Dirac fermion coupled to a gauge field. This duality is established by considering two alternate descriptions of the 3d topological insulator (TI) surface. The first description is the usual Dirac cone surface state. The second description is accessed via an electric-magnetic duality of the bulk TI coupled to a gauge field, which maps it to a gauged topological superconductor. This alternate description ultimately leads to a new surface theory - dual QED3. The dual theory provides an explicit derivation of the T-Pfaffian state, a proposed surface topological order of the TI, which is simply the paired superfluid state of the dual fermions. The roles of time reversal and particle-hole symmetry are exchanged by the duality, which connects some of our results to a recent conjecture by Son on particle-hole symmetric quantum Hall states.
description: 14 pages, 3 pages appendices, 1 figure
Structure-Based Discovery of Highly Selective Phosphodiesterase-9A Inhibitors and Implications for Inhibitor Design
Creators: name: Zhu, Xinhai
name: Ke, Hengming
name: Wan, Yiqian
name: Meng, Fei
name: Hou, Jing
name: Shao, Yong-Xian
name: Wu, Pei-Ying
name: Xu, Jie
name: Li, Zhe
name: Cai, Yonghong
name: Liu, Peiqing
name: Huang, Manna
name: Luo, Hai-Bin
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2012

description: A new series of phosphodiesterase-9 (PDE9) inhibitors that contain a scaffold of 6-amino-pyrazolopyrimidinone have been discovered by a combination of structure-based design and computational docking. This procedure significantly saved load of chemical synthesis and is an effective method for the discovery of inhibitors. The best compound 28 has an IC50 of 21 nM and 3.3 µM respectively for PDE9 and PDE5, and about three orders of magnitude of selectivity against other PDE families. The crystal structure of the PDE9 catalytic domain in complex with 28 has been determined and shows a hydrogen bond between 28 and Tyr424. This hydrogen bond may account for the 860-fold selectivity of 28 against PDE1B, in comparison with about 30-fold selectivity of BAY73-6691. Thus, our studies suggest that Tyr424, a unique residue of PDE8 and PDE9, is a potential target for improvement of selectivity of PDE9 inhibitors.
A double white dwarf with a paradoxical origin?
Creators: name: Bours, M. C. P.
name: Marsh, T. R.
name: Gaensicke, B. T.
name: Tauris, T. M.
name: Istrate, A. G.
name: Badenes, C.
name: Dhillon, V. S.
name: Gal-Yam, A.
name: Hermes, J. J.
name: Kengkriangkrai, S.
name: Kilic, M.
name: Koester, D.
name: Mullally, F.
name: Prasert, N.
name: Steeghs, D.
name: Thompson, S. E.
name: Thorstensen, J. R.
Publisher: name: arXiv
Year: 2015
Subjects: subject: Solar and Stellar Astrophysics (astro-ph.SR)
subject: FOS: Physical sciences

description: We present Hubble Space Telescope UV spectra of the 4.6 h period double white dwarf SDSS J125733.63+542850.5. Combined with Sloan Digital Sky Survey optical data, these reveal that the massive white dwarf (secondary) has an effective temperature T2 = 13030 +/- 70 +/- 150 K and a surface gravity log g2 = 8.73 +/- 0.05 +/- 0.05 (statistical and systematic uncertainties respectively), leading to a mass of M2 = 1.06 Msun. The temperature of the extremely low-mass white dwarf (primary) is substantially lower at T1 = 6400 +/- 37 +/- 50 K, while its surface gravity is poorly constrained by the data. The relative flux contribution of the two white dwarfs across the spectrum provides a radius ratio of R1/R2 = 4.2, which, together with evolutionary models, allows us to calculate the cooling ages. The secondary massive white dwarf has a cooling age of about 1 Gyr, while that of the primary low-mass white dwarf is likely to be much longer, possibly larger than 5 Gyrs, depending on its mass and the strength of chemical diffusion. These results unexpectedly suggest that the low-mass white dwarf formed long before the massive white dwarf, a puzzling discovery which poses a paradox for binary evolution.
description: accepted for publication in MNRAS
title: Пути снижения анестезиолого-реаниматологических осложнений у беременных, рожениц и родильниц с ожирением
Creators: name: ELS IPR BOOKS
Publisher: name: Саратовский государственный медицинский университет им. В.И. Разумовского
Year: 2021

description: В монографии описаны возможные механизмы развития жизнеугрожающих осложнений у беременных, рожениц и родильниц с ожирением. Данные о динамике внутрибрюшного давления во время беременности и в перипартальный период позволяют уточнить и расширить научные представления о новых патогенетических механизмах осложненных исходов, позволяя составить более целостное понимание причин их появления и методов профилактики. Для специалистов в области анестезиологии и реаниматологии, акушерства и гинекологии.
PRESENTED IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE DEGREE OF EXECUTIVES MASTER OF BUSINESS ADMINISTRATION (EMBA)
Creators: name: SANNI JUHAR HALID
Publisher: name: Zenodo
Year: 2017

description: This study examined the benefits and challenges of adopting the International Public Sector

Accounting Standards (IPSAS) in the foreign charity organizations working in Ethiopia. The

objectives of the study was to provide an insight on the contribution of adopting IPSAS in

enhancing the level of accountability, transparency, strengthening the stakeholders perception

of the standards and taking educational and professional responsibilities. The population of

study was 353 foreign charity organizations and 2 government offices (CHSA and AABE). Using

purposive sampling,35 foreign charities organizations and 2 government offices were selected

for this study. 75 sample respondents, who were understanding IPSAS's objectives and were

responsible for the adoption process, were taken from the above institutions to fill the

questionnaire. Before processing the responses, the completed questionnaires were edited for

completeness and consistency.
(400478) Richard Ferrier
Creators: name: Professions, Victorian
Publisher: name: University of Oxford
Year: 2022
Subjects: subject: 220201 Business and Labour History
subject: FOS: Philosophy, ethics and religion
subject: History
subject: 140203 Economic History
subject: FOS: Economics and business

description: This three-year research project began in January 2014 and investigated whether, during the Victorian period, the professions formed a distinct self-sustaining social group with its own mores and values. The project looked at 16,000 individuals drawn from census data for Alnwick, Brighton, Bristol, Dundee, Greenock, Leeds, Merthyr Tydfil, Morpeth, and Winchester. The research project was funded by the UK Economic & Social Research Council and was based at the Universities of Oxford and Northumbria.
Structure–Functional Selectivity Relationship Studies of β-Arrestin-Biased Dopamine D 2 Receptor Agonists
Creators: name: Setola, Vincent
name: Wetsel, William C.
name: Jin, Jian
name: Frye, Stephen V.
name: Chen, Meng
name: Sassano, Maria F.
name: Bai, Xu
name: Chen, Xin
name: Roth, Bryan L.
name: Zheng, Lianyou
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2012

description: Functionally selective G protein-coupled receptor (GPCR) ligands, which differentially modulate canonical and non-canonical signaling, are extremely useful for elucidating key signal transduction pathways essential for both the therapeutic actions and side-effects of drugs. However, few such ligands have been created and very little purposeful attention has been devoted to studying what we term: ‘structure-functional selectivity relationships’ (SFSR). We recently disclosed the first β-arrestin-biased dopamine D2 receptor (D2R) agonists UNC9975 (44) and UNC9994 (36), which have robust in vivo antipsychotic drug-like activities. Here we report the first comprehensive SFSR studies focused on exploring four regions of the aripiprazole scaffold, which resulted in the discovery of these β-arrestin-biased D2R agonists. These studies provide a successful proof-of-concept for how functionally selective ligands can be discovered.
Supplementary Methods and Analyses from Risky business: linking Toxoplasma gondii infection and entrepreneurship behaviours across individuals and countries.
Creators: name: Johnson, Stefanie K.
name: Fitza, Markus A.
name: Lerner, Daniel A.
name: Calhoun, Dana M.
name: Beldon, Marissa
name: Chan, Elsa T.
name: Johnson, Pieter T. J.
Publisher: name: The Royal Society
Year: 2018
Subjects: subject: Environmental Science
subject: Health Care
subject: Diseases
subject: 111706 Epidemiology
subject: FOS: Health sciences
subject: 60801 Animal Behaviour
subject: FOS: Biological sciences

description: Disciplines such as business and economics often rely on the assumption of rationality when explaining complex human behaviours. However, growing evidence suggests that behaviour may concurrently be influenced by infectious microorganisms. The protozoan, Toxoplasma gondii, infects an estimated 2 billion people worldwide and has been linked to behavioural alterations in humans and other vertebrates. Here we integrate primary data from college students and business professionals with national-level information on cultural attitudes toward business to test the hypothesis that T. gondii infection influences individual as well as societal-scale entrepreneurship activities. Using a saliva-based assay, we found that students (n = 1495) who tested IgG positive for T. gondii exposure were 1.4× more likely to major in business and 1.70× more likely to have an emphasis in ‘management and entrepreneurship' over other business-related emphases. Among professionals attending entrepreneurship events, T. gondii-positive individuals were 1.8× more likely to have started their own business compared with other attendees (n = 197). Finally, after synthesizing and combining country-level databases on T. gondii infection from the past 25 years with the global entrepreneurship monitor of entrepreneurial activity, we found that infection prevalence was a consistent, positive predictor of entrepreneurial activity and intentions at the national scale, regardless of whether previously identified economic covariates were included. Nations with higher infection also had a lower fraction of respondents citing ‘fear of failure' in inhibiting initiating new business ventures. While correlational, these results highlight the linkage between parasitic infection and complex human behaviours, including those relevant to business, entrepreneurship, and economic productivity.
On the construction of gradient Ricci soliton warped product
Creators: name: Feitosa, F. E. S.
name: Filho, A. A. Freitas
name: Gomes, J. N. V.
Publisher: name: arXiv
Year: 2015
Subjects: subject: Differential Geometry (math.DG)
subject: FOS: Mathematics
subject: Primary 53C24, 53C25, Secondary 53C21

description: In this paper we show that an expanding or steady gradient Ricci soliton warped product $B^n\times_f F^m$, $m>1$, whose warping function $f$ reaches both maximum and minimum must be a Riemannian product. Moreover, we present a necessary and sufficient condition for constructing a gradient Ricci soliton warped product. As an application, we present a class of expanding Ricci soliton warped product having as a fiber an Einstein manifold with non-positive scalar curvature. We also discuss some obstructions to this construction, especially in the case when the base of the warped product is compact.
description: Final version. To appear in Journal of Nonlinear Analysis
ปัจจัยที่ส่งผลต่อการบริหารงานวิชาการของโรงเรียนมัธยมศึกษาในจังหวัดชัยนาท
Creators: name: ปรีชา ตุ้มโท
Publisher: name: มหาวิทยาลัยมหาจุฬาลงกรณราชวิทยาลัย วิทยาเขตนครสวรรค์
Year: 2022
Subjects: ปัจจัยที่ส่งผล
การบริหารงานวิชาการ
โรงเรียนมัธยมศึกษา

description: The Journal of Research and Academics, 5, 5, 303-316
(Biphenyl-4-yl)methylammonium Chlorides: Potent Anticonvulsants That Modulate Na + Currents
Creators: name: Park, Ki Duk
name: Wilson, Sarah M.
name: Lee, Hyosung
name: Dustrude, Erik T.
name: Khanna, Rajesh
name: Yang, Xiao-Fang
name: Kohn, Harold
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: We have reported that compounds containing a bi-aryl linked unit (Ar-X-Ar′) modulated Na+ currents by promoting slow inactivation and fast inactivation processes and by inducing frequency (use)-dependent inhibition of Na+ currents. These electrophysiological properties have been associated with the mode of action of several antiepileptic drugs. In this study, we demonstrate that the readily accessible (biphenyl-4-yl)methylammonium chlorides (compound class B) exhibited a broad range of anticonvulsant activities in animal models and in the maximal electroshock seizure test the activity of (3′-trifluoromethoxybiphenyl-4-yl)methylammonium chloride (8) exceeded that of phenobarbital and phenytoin upon oral administration to rats. Electrophysiological studies of 8 using mouse catecholamine A– differentiated cells and rat embryonic cortical neurons confirmed that 8 promoted slow and fast inactivation in both cell types but did not affect the frequency (use)-dependent block of Na+ currents.
title: Руководство по грудному вскармливанию
Creators: name: ELS IPR BOOKS
Publisher: name: Саратовский государственный медицинский университет им. В.И. Разумовского
Year: 2021

description: Руководство содержит основные сведения о физиологии лактации, составе и свойствах грудного молока, режимах и технике грудного вскармливания младенцев, парафизиологических и патологических состояниях, ассоциированных с грудным вскармливанием и методах коррекции. Отражает последние требования к организации работы медицинских работников по поддержанию практики грудного вскармливания детей первого года жизни; составлено в соответствии с программой общего усовершенствования врачей по специальности «педиатрия». Адресовано слушателям кафедры педиатрии, врачам-педиатрам, неонатологам, врачам общей практики, клиническим ординаторам и аспирантам.
4β-Methyl-5-(3-hydroxyphenyl)morphan Opioid Agonist and Partial Agonist Derived from a 4β-Methyl-5-(3-hydroxyphenyl)morphan Pure Antagonist
Creators: name: Carroll, F. Ivy
name: Navarro, Hernán A.
name: Mascarella, S. Wayne
name: Roth, Bryan L.
name: Gichinga, Moses G.
name: Thomas, James B.
name: Vardy, Eyal
name: Williams, John D.
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: In previous studies we reported that addition of 7α-acylamino groups to N-phenylpropyl-4β-methyl-5-(3-hydroxyphenyl)morphan (4) led to compounds that were pure opioid receptor antagonists. In contrast to these findings we report in this study that addition of a 7α-amino (5a), 7α-alkylamino (5b–e), or 7α-dialkylamino (5f–h) group to 4 leads to opioid receptor ligands with varying degrees of agonist/antagonist activity. The 7α-amino and 7α-methylamino analogues were full agonists at the μ and δ receptors and antagonists at the κ receptor. The 7α-cyclopropylmethylamino analogue 5h was a full agonist at the μ receptor with weaker agonist activity at the δ and κ receptors. Whereas the addition of a 7α-acylamino group to the pure non-selective opioid receptor antagonist N-phenylpropyl-4β-methyl-5-(3-hydroxyphenyl)morphan (4) led to κ selective pure opioid receptor antagonist, the addition of a 7α-amino, 7α-alkylamino or 7α-dialkylamino group to 4 leads to opioid ligands that are largely μ or δ agonist with mixed agonist/antagonist properties.
Colloidal Aggregation Causes Inhibition of G Protein-Coupled Receptors
Creators: name: Shoichet, Brian K.
name: Roth, Bryan L.
name: Doak, Allison K.
name: Sassano, Maria F.
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: Colloidal aggregation is the dominant mechanism for artifactual inhibition of soluble proteins, and controls against it are now widely deployed. Conversely, investigating this mechanism for membrane-bound receptors has proven difficult. Here we investigate the activity of four well-characterized aggregators against three G protein-coupled receptors (GPCRs) recognizing peptide and protein ligands. Each of the aggregators was active at micromolar concentrations against the three GPCRs in cell-based assays. This activity could be attenuated by either centrifugation of the inhibitor stock solution or by addition of Tween-80 detergent. In the absence of agonist, the aggregators acted as inverse agonists, consistent with a direct receptor interaction. Meanwhile, several literature GPCR ligands that resemble aggregators themselves formed colloids, by both physical and enzymological tests. These observations suggest that some GPCRs may be artifactually antagonized by colloidal aggregates, an effect that merits the attention of investigators in this field.
(400475) Margaret Gall
Creators: name: Professions, Victorian
Publisher: name: University of Oxford
Year: 2022
Subjects: subject: 220201 Business and Labour History
subject: FOS: Philosophy, ethics and religion
subject: History
subject: 140203 Economic History
subject: FOS: Economics and business

description: This three-year research project began in January 2014 and investigated whether, during the Victorian period, the professions formed a distinct self-sustaining social group with its own mores and values. The project looked at 16,000 individuals drawn from census data for Alnwick, Brighton, Bristol, Dundee, Greenock, Leeds, Merthyr Tydfil, Morpeth, and Winchester. The research project was funded by the UK Economic & Social Research Council and was based at the Universities of Oxford and Northumbria.
(400476) David Ferrier
Creators: name: Professions, Victorian
Publisher: name: University of Oxford
Year: 2022
Subjects: subject: 220201 Business and Labour History
subject: FOS: Philosophy, ethics and religion
subject: History
subject: 140203 Economic History
subject: FOS: Economics and business

description: This three-year research project began in January 2014 and investigated whether, during the Victorian period, the professions formed a distinct self-sustaining social group with its own mores and values. The project looked at 16,000 individuals drawn from census data for Alnwick, Brighton, Bristol, Dundee, Greenock, Leeds, Merthyr Tydfil, Morpeth, and Winchester. The research project was funded by the UK Economic & Social Research Council and was based at the Universities of Oxford and Northumbria.
(400477) William Ferrier
Creators: name: Professions, Victorian
Publisher: name: University of Oxford
Year: 2022
Subjects: subject: 220201 Business and Labour History
subject: FOS: Philosophy, ethics and religion
subject: History
subject: 140203 Economic History
subject: FOS: Economics and business

description: This three-year research project began in January 2014 and investigated whether, during the Victorian period, the professions formed a distinct self-sustaining social group with its own mores and values. The project looked at 16,000 individuals drawn from census data for Alnwick, Brighton, Bristol, Dundee, Greenock, Leeds, Merthyr Tydfil, Morpeth, and Winchester. The research project was funded by the UK Economic & Social Research Council and was based at the Universities of Oxford and Northumbria.
Discovery of Novel Trypanosoma brucei Phosphodiesterase B1 Inhibitors by Virtual Screening against the Unliganded TbrPDEB1 Crystal Structure
Creators: name: Orrling, Kristina M.
name: Ke, Hengming
name: Wang, Huanchen
name: Jansen, Chimed
name: Seebeck, Thomas
name: de Esch, Iwan J. P.
name: Kooistra, Albert J.
name: Tenor, Hermann
name: de Graaf, Chris
name: Bailey, David
name: Leurs, Rob
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: Trypanosoma brucei cyclic nucleotide phosphodiesterase B1 (TbrPDEB1) and TbrPDEB2 have recently been validated as new therapeutic targets for human African Trypanosomiasis by both genetic and pharmacological means. In this study we report the crystal structure of the catalytic domain of the unliganded TbrPDEB1 and its use for the in silico screening for new TbrPDEB1 inhibitors with novel scaffolds. The TbrPDEB1 crystal structure shows the characteristic folds of human PDE enzymes, but also contains the parasite-specific P-pocket found in the structures of Leishmania major PDEB1 and Trypanosoma cruzi PDEC. The unliganded TbrPDEB1 X-ray structure was subjected to a structure-based in silico screening approach that combines molecular docking simulations with a protein-ligand interaction fingerprint (IFP) scoring method. This approach identified, six novel TbrPDEB1 inhibitors with IC50 values of 10–80 μM, which may be further optimized as potential selective TbrPDEB inhibitors.
ALMA maps the Star-Forming Regions in a Dense Gas Disk at z~3
Creators: name: Swinbank, Mark
name: Dye, Simon
name: Nightgale, James
name: Furlanetto, Christina
name: Smail, Ian
name: Cooray, Asantha
name: Dannerbauer, Helmut
name: Dunne, Loretta
name: Eales, Steve
name: Gavazzi, Raphael
name: Hunter, Todd
name: Ivison, Rob
name: Negrello, Mattia
name: Oteo, Ivan
name: Smit, Renske
name: van der Werf, Paul
name: Vlahakis, Catherine
Publisher: name: arXiv
Year: 2015
Subjects: subject: Astrophysics of Galaxies (astro-ph.GA)
subject: Cosmology and Nongalactic Astrophysics (astro-ph.CO)
subject: FOS: Physical sciences

description: We exploit long-baseline ALMA sub-mm observations of the lensed star-forming galaxy SDP 81 at z=3.042 to investigate the properties of inter-stellar medium on scales of 50-100pc. The kinematics of the CO gas within this system are well described by a rotationally-supported disk with an inclination-corrected rotation speed, v=320+/-20km/s and a dynamical mass of M=(3.5+/-1.0)x10^10Mo within a radius of 1.5 kpc. The disk is gas rich and unstable, with a Toomre parameter, Q=0.30+/-0.10 and so should collapse in to star-forming regions with Jeans length L_J~130pc. We identify five star-forming regions within the ISM on these scales and show that their scaling relations between luminosity, line-widths and sizes are significantly offset from those typical of molecular clouds in local Galaxies (Larson's relations). These offsets are likely to be caused by the high external hydrostatic pressure for the interstellar medium (ISM), P/kB=(40+/-20)x10^7K/cm3, which is ~10,000x higher than the typical ISM pressure in the Milky Way. The physical conditions of the star-forming ISM and giant molecular clouds appears to be similar to the those found in the densest environments in the local Universe, such as those in the Galactic center.
description: 6 pages, 2 figures. ApJL in press
Dual-Functional abeo -Taxane Derivatives Destabilizing Microtubule Equilibrium and Inhibiting NF-κB Activation
Creators: name: Goto, Masuo
name: Su, Jia
name: Zhao, Yu
name: Zhao, Qin-Shi
name: Yao, Zhu-Jun
name: Morris-Natschke, Susan L.
name: Lee, Kuo-Hsiung
name: Li, Yan
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: Taxchinin A, with a 11(15→1)-abeo-taxane skeleton, is a major, but inactive taxoid contained in leaves of Taxus chinensis. In our design of dual-functional antitumor abeo-taxane derivatives, two fragments from antitumor agents with different molecular targets (the N-acyl-3′-phenylisoserine side chain from the antimitotic agent paclitaxel and an α,β-unsaturated carbonyl system from NF-κB inhibitors) were incorporated into the scaffold of taxchinin A. The resulting compounds displayed broad inhibitory effects against proliferation of tumor cell lines, with notable selectivity towards colon cancer, melanoma and renal cancer, when evaluated in the NCI-60 human tumor cell line screening panel. Based on the NCI-60 assay data, structure-activity relationship (SAR) correlations were elucidated. Mechanistic studies indicated that this new compound type can both destabilize microtubules and inhibit NF-κB activation, thereby inducing tumor cell apoptosis. This first report of the dual-functional taxoid-core compounds thus provides new opportunities for future drug development based on natural taxoid scaffolds.
Feedback-Induced Flutter Instability of a Flexible Beam in Fluid Flow
Creators: name: Aspelund, Sanders
name: Mukherjee, Ranjan
name: Hellum, Aren
Publisher: name: arXiv
Year: 2021
Subjects: subject: Fluid Dynamics (physics.flu-dyn)
subject: Systems and Control (eess.SY)
subject: FOS: Physical sciences
subject: FOS: Electrical engineering, electronic engineering, information engineering

description: A pinned-free beam in axial fluid flow, subjected to feedback-based actuation at the pinned end, is investigated. The actuation may be a moment or a prescribed angle and it is proportional to the state (curvature, slope, or displacement) of the beam at some point along its length. All equations and boundary condition terms are non-dimensionalized and the stability of the system is studied over a range of external flow velocity and sensing location. For each combination of flow velocity and sensing location, the critical gain (positive or negative) for the onset of flutter is determined. This process, which is repeated for each combination of actuation and sensing modes, reveals that the closed-loop system exhibits a rich set of stability transitions, each associated with a traveling waveform in the flexible beam at the onset of flutter. With the intent of exploring the use of flexible fluttering beams for underwater propulsion, the efficiency of these waveforms is computed using slender-body theory. Additional insights into the efficiency of the waveforms are obtained through considerations of the smoothness of the traveling waveforms.
title: Хирургия с учетом коэффициентов натяжения тканей у человека
Creators: name: ELS IPR BOOKS
Publisher: name: Саратовский государственный медицинский университет им. В.И. Разумовского
Year: 2020

description: Монография посвящена вопросам хирургии сосудов с учетом коэффициентов натяжения тканей внутри организма человека. Показаны статистически достоверные различия коэффициентов натяжения сосудов отдельных локализаций, их взаимосвязь, динамика с возрастом и при атеросклерозе. Обоснована прикладная роль фактора натяжения тканей в хирургии, в частности при операциях на сосудах, других органах, в микрохирургии. Для ангиологов, ангиохирургов, хирургов, терапевтов, анатомов, физиологов, патофизиологов, биологов.
title: Анестезиологическое пособие при операциях высокого риска массивной акушерской кровопотери
Creators: name: ELS IPR BOOKS
Publisher: name: Саратовский государственный медицинский университет им. В.И. Разумовского
Year: 2021

description: Руководство для врачей основано на методологии анестезиологического пособия при операциях высокого риска массивного акушерского кровотечения. Систематизированы сведения об основных направлениях интенсивной терапии массивного акушерского кровотечения, бóльшая часть из которых отводится анестезиологическому пособию, осуществляемому в условиях трансфузиологической поддержки. Авторами анализируется комплексное применение методов анестезиологических пособий и интенсивной терапии в различных вариантах у пациенток с массивными акушерскими кровотечениями. Предназначено для подготовки кадров в рамках повышения квалификации по специальностям «анестезиология и реаниматология» и «акушерство и гинекология».
Isospin and momentum polarized orders in bilayer graphene
Creators: name: Dong, Zhiyu
name: Davydova, Margarita
name: Ogunnaike, Olumakinde
name: Levitov, Leonid
Publisher: name: arXiv
Year: 2021
Subjects: subject: Mesoscale and Nanoscale Physics (cond-mat.mes-hall)
subject: FOS: Physical sciences

description: Electron bands in the untwisted bilayer graphene flatten out in a transverse electric field, offering a promising platform for correlated electron physics. We predict that the spin/valley isospin magnetism, resembling that seen in moiré bands, coexists with momentum-polarized phases occurring via a ``flocking transition'' in momentum space. This transition results in the electron momentum distribution being spontaneously displaced relative to the $K$ and $K'$ valley centers. These phases feature unusual observables such as persistent currents in the ground state. Momentum-polarized carriers ``sample'' the Berry curvature of the conduction band, resulting in a unique behavior of the anomalous Hall conductivity and other effects that do not occur in previously studied systems.
description: 10pgs, 2fgs
Cramér type large deviations for trimmed L-statistics
Creators: name: Gribkova, Nadezhda
Publisher: name: arXiv
Year: 2015
Subjects: subject: Probability (math.PR)
subject: FOS: Mathematics
subject: 60F10, 62G30, 60F05, 62E20

description: In this paper, we propose a new approach to the investigation of asymptotic properties of trimmed $L$-statistics and we apply it to the Cramér type large deviation problem. Our results can be compared with ones in Callaert et al.(1982) -- the first and, as far as we know, the single article, where some results on probabilities of large deviations for the trimmed $L$-statistics were obtained, but under some strict and unnatural conditions. Our approach is to approximate the trimmed $L$-statistic by a non-trimmed $L$-statistic (with smooth weight function) based on Winsorized random variables. Using this method, we establish the Cramér type large deviation results for the trimmed $L$-statistics under quite mild and natural conditions.
description: 17 pages
New Betulinic Acid Derivatives for Bevirimat-Resistant Human Immunodeficiency Virus Type-1
Creators: name: Lee, Kuo-Hsiung
name: Qian, Keduo
name: Chen, Chin-Ho
name: Zhu, Lei
name: Dang, Zhao
name: Huang, Li
name: Ho, Phong
Publisher: name: The University of North Carolina at Chapel Hill University Libraries
Year: 2013

description: Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. However, clinical trials of 1 have revealed a high baseline drug resistance that is attributed to naturally-occurring polymorphisms in HIV-1 Gag. To overcome the drug resistance, 28 new derivatives of 1 were synthesized and tested against compound 1-resistant (BVM-R) HIV-1 variants. Among them, compound 6 exhibited much improved activity against several HIV-1 strains carrying BVM-R polymorphisms. Compound 6 was at least 20-fold more potent than 1 against the replication of NL4-3/V370A, which carries the most prevalent clinical BVM-R polymorphism in HIV-1 Gag-SP1. Thus, compound 6 merits further development as a potential anti-AIDS clinical trial candidate.
The SCUBA-2 Cosmology Legacy Survey: ALMA resolves the bright-end of the sub-millimeter number counts
Creators: name: Simpson, James
name: Smail, Ian
name: Swinbank, Mark
name: Chapman, Scott
name: Geach, James
name: Ivison, Rob
name: Thomson, Alasdair
name: Aretxaga, Itziar
name: Blain, Andrew
name: Cowley, Will
name: Chen, Chian-Chou
name: Coppin, Kristen
name: Dunlop, Jim
name: Edge, Alastair
name: Farrah, Duncan
name: Ibar, Edo
name: Karim, Alex
name: Knudsen, Kirsten
name: Meijerink, Rowin
name: Michalowski, Michal
name: Scott, Douglas
name: Spanns, Marco
name: van der Werf, Paul
Publisher: name: arXiv
Year: 2015
Subjects: subject: Astrophysics of Galaxies (astro-ph.GA)
subject: Cosmology and Nongalactic Astrophysics (astro-ph.CO)
subject: FOS: Physical sciences

description: We present high-resolution 870-um ALMA continuum maps of 30 bright sub-millimeter sources in the UKIDSS UDS field. These sources are selected from deep, 1-square degrees 850-um maps from the SCUBA--2 Cosmology Legacy Survey, and are representative of the brightest sources in the field (median SCUBA2 flux S_850=8.7+/-0.4 mJy). We detect 52 sub-millimeter galaxies (SMGs) at >4-sigma significance in our 30 ALMA maps. In 61+/-17% of the ALMA maps the single-dish source comprises a blend of >=2 SMGs, where the secondary SMGs are Ultra--Luminous Infrared Galaxies (ULIRGs) with L_IR>10^12 Lo. The brightest SMG contributes on average 80+/-4% of the single-dish flux density, and in the ALMA maps containing >=2 SMGs the secondary SMG contributes 25+/-3% of the integrated ALMA flux. We construct source counts and show that multiplicity boosts the apparent single-dish cumulative counts by 20% at S_870>7.5mJy, and by 60% at S_870>12mJy. We combine our sample with previous ALMA studies of fainter SMGs and show that the counts are well-described by a double power-law with a break at 8.5+/-0.6mJy. The break corresponds to a luminosity of ~6x10^12Lsol or a star-formation rate of ~1000Mo/yr. For the typical sizes of these SMGs, which are resolved in our ALMA data with r=1.2+/-0.1kpc, this yields a limiting SFR density of ~100Msol/yr/kpc2. Finally, the number density of S_870>2mJy SMGs is 80+/-30 times higher than that derived from blank-field counts. An over-abundance of faint SMGs is inconsistent with line-of-sight projections dominating multiplicity in the brightest SMGs, and indicates that a significant proportion of these high-redshift ULIRGs must be physically associated.
description: 14 pages, 6 figures. ApJ in press
Supplementary Methods and Analyses from Risky business: linking Toxoplasma gondii infection and entrepreneurship behaviours across individuals and countries
Creators: name: Johnson, Stefanie K.
name: Fitza, Markus A.
name: Lerner, Daniel A.
name: Calhoun, Dana M.
name: Beldon, Marissa
name: Chan, Elsa T.
name: Johnson, Pieter T. J.
Publisher: name: The Royal Society
Year: 2018
Subjects: subject: Environmental Science
subject: Health Care
subject: Diseases
subject: 111706 Epidemiology
subject: FOS: Health sciences
subject: 60801 Animal Behaviour
subject: FOS: Biological sciences

description: Disciplines such as business and economics often rely on the assumption of rationality when explaining complex human behaviours. However, growing evidence suggests that behaviour may concurrently be influenced by infectious microorganisms. The protozoan, Toxoplasma gondii, infects an estimated 2 billion people worldwide and has been linked to behavioural alterations in humans and other vertebrates. Here we integrate primary data from college students and business professionals with national-level information on cultural attitudes toward business to test the hypothesis that T. gondii infection influences individual as well as societal-scale entrepreneurship activities. Using a saliva-based assay, we found that students (n = 1495) who tested IgG positive for T. gondii exposure were 1.4× more likely to major in business and 1.70× more likely to have an emphasis in ‘management and entrepreneurship' over other business-related emphases. Among professionals attending entrepreneurship events, T. gondii-positive individuals were 1.8× more likely to have started their own business compared with other attendees (n = 197). Finally, after synthesizing and combining country-level databases on T. gondii infection from the past 25 years with the global entrepreneurship monitor of entrepreneurial activity, we found that infection prevalence was a consistent, positive predictor of entrepreneurial activity and intentions at the national scale, regardless of whether previously identified economic covariates were included. Nations with higher infection also had a lower fraction of respondents citing ‘fear of failure' in inhibiting initiating new business ventures. While correlational, these results highlight the linkage between parasitic infection and complex human behaviours, including those relevant to business, entrepreneurship, and economic productivity.
The Spin $L$-function on $\mathrm{GSp}_6$ for Siegel modular forms
Creators: name: Pollack, Aaron
Publisher: name: arXiv
Year: 2015
Subjects: subject: Number Theory (math.NT)
subject: Representation Theory (math.RT)
subject: FOS: Mathematics

description: We give a Rankin-Selberg integral representation for the Spin (degree eight) $L$-function on $\mathrm{PGSp}_6$. The integral applies to the cuspidal automorphic representations associated to Siegel modular forms. If $π$ corresponds to a level one Siegel modular form $f$ of even weight, and if $f$ has a non-vanishing maximal Fourier coefficient (defined below), then we deduce the functional equation and finiteness of poles of the completed Spin $L$-function $Λ(π,Spin,s)$ of $π$.
description: differs slightly from published counterpart
(400474) Barbara Gall
Creators: name: Professions, Victorian
Publisher: name: University of Oxford
Year: 2022
Subjects: subject: 220201 Business and Labour History
subject: FOS: Philosophy, ethics and religion
subject: History
subject: 140203 Economic History
subject: FOS: Economics and business

description: This three-year research project began in January 2014 and investigated whether, during the Victorian period, the professions formed a distinct self-sustaining social group with its own mores and values. The project looked at 16,000 individuals drawn from census data for Alnwick, Brighton, Bristol, Dundee, Greenock, Leeds, Merthyr Tydfil, Morpeth, and Winchester. The research project was funded by the UK Economic & Social Research Council and was based at the Universities of Oxford and Northumbria.