gebhart/patrepeval huggingface dataset:
A Convergent Solution-Phase Synthesis of the Macrocycle Ac-Phe-[Orn-Pro-<scp>d</scp>-Cha-Trp-Arg], a Potent New Antiinflammatory Drug (2003)

Relatively few cyclic peptides have reached the pharmaceutical marketplace during the past decade, most produced through fermentation rather than made synthetically. Generally, this class of compounds is synthesized for research purposes on milligram scales by solid-phase methods, but if the potential of macrocyclic peptidomimetics is to be realized, low-cost larger scale solution-phase syntheses need to be devised and optimized to provide sufficient quantities for preclinical, clinical, and commercial uses. Here, we describe a cheap, medium-scale, solution-phase synthesis of the first reported highly potent, selective, and orally active antagonist of the human C5a receptor. This compound, Ac-Phe[Orn-Pro-d-Cha-Trp-Arg], known as 3D53, is a macrocyclic peptidomimetic of the human plasma protein C5a and displays excellent antiinflammatory activity in numerous animal models of human disease. In a convergent approach, two tripeptide fragments Ac-Phe-Orn(Boc)-Pro-OH and H-d-Cha-Trp(For)-Arg-OEt were first prepared by high-yielding solution-phase couplings using a mixed anhydride method before coupling them to give a linear hexapeptide which, after deprotection, was obtained in 38% overall yield from the commercially available amino acids. Cyclization in solution using BOP reagent gave the antagonist in 33% yield (13% overall) after HPLC purification. Significant features of the synthesis were that the Arg side chain was left unprotected throughout, the component Boc-d-Cha-OH was obtained very efficiently via hydrogenation of d-Phe with PtO(2) in TFA/water, the tripeptides were coupled at the Pro-Cha junction to minimize racemization via the oxazolone pathway, and the entire synthesis was carried out without purification of any intermediates. The target cyclic product was purified (>97%) by reversed-phase HPLC. This convergent synthesis with minimal use of protecting groups allowed batches of 50-100 g to be prepared efficiently in high yield using standard laboratory equipment. This type of procedure should be useful for making even larger quantities of this and other macrocyclic peptidomimetic drugs.
Application of a Fas Ligand Encoding a Recombinant Adenovirus Vector for Prolongation of Transgene Expression (1998)

An adenovirus vector encoding murine Fas ligand (mFasL) under an inducible control was derived. In vivo ectopic expression of mFasL in murine livers induced an inflammatory cellular infiltration. Furthermore, ectopic expression of mFasL by myocytes did not allow prolonged vector-mediated transgene expression. Thus, ectopic expression of functional mFasL in vector-transduced cells does not appear to confer, by itself, an immunoprivileged site sufficient to mitigate adenovirus vector immunogenicity.
Crustal evolution, intra-cratonic architecture and the metallogeny of an Archaean craton (2013)

Abstract The generation of the Earth's continental crust modified the composition of the mantle and provided a stable, buoyant reservoir capable of capturing mantle material and ultimately preserving ore deposits. Within the continental crust, lithospheric architecture and associated cratonic margins are a first-order control on camp-scale mineralization. Here we show that the evolving crustal architecture of the Archaean Yilgarn Craton, Western Australia, played a key role in controlling the localization of camp-scale gold, iron and nickel mineralized systems. The age and source characteristics of Archaean lithosphere are heterogeneous in both space and time and are recorded by the varying Nd isotopic signature of crustal rocks. Spatial and temporal variations in isotopic character document the evolution of an intra-cratonic architecture through time, and in doing so map transient lithospheric discontinuities where gold, nickel and iron mineral systems were concentrated. Komatiite-hosted nickel deposits cluster into camps localized within young, juvenile crust at the isotopic margin with older lithosphere; orogenic gold systems are typically localized along major structures within juvenile crust; and banded iron formation (BIF)-hosted iron deposits are localized at the edge of, and within, older lithospheric blocks. Furthermore, this work shows that crustal evolution plays an important role in the development and localization of favourable sources of nickel, gold and iron by controlling the occurrence of thick BIFs, ultramafic lavas and fertile (juvenile) crust, respectively. Fundamentally, this study demonstrates that the lithospheric architecture of a craton can be effectively imaged by isotopic techniques and used to identify regions prospective for camp-scale mineralization.
S0301-1-1 Effect of hydrogen on micromechanism of fatigue crack propagation (2009)

The authors have previously observed a marked effect of hydrogen on cyclic slip behavior around a {110} fatigue crack tip in Fe-3.2wt.%Si alloy (Scripta Mater, 61(2009),145). In this study, a sustained load test is conducted to confirm the possible effect of hydrogen-assisted cracking (HAC). The result shows that no HAC exists along the {110} plane, demonstrating that the observed effect of hydrogen is limited solely to the cyclic slip mechanism. Crack growth process is then further discussed.
Optical WDM node for highly-reliable AGC/ALC of EDFAs by employing power-managed control channel (2000)

We propose an optical node configuration that controls the gain and level of an erbium-doped fiber amplifier by employing control channel. Experimental results show that the power excursion of less than ±1 dB is achieved.
An inactivated mycoplasma pneumoniae vaccine (1965)

An experimental vaccine was prepared with<i>Mycoplasma pneumonia</i>, the agent of primary atypical pneumonia. Its injection elicited antibody in rabbits and monkeys and induced resistance to multiplication of myoplasma in lungs of vaccinated hamsters. The vaccine was well tolerated in preliminary studies with 36 human subjects, and encouraging evidence of antigenicity was obtained when 25 of 30 developed significant rises in mycoplasma growth-inhibiting antibody titers. The response was best (17 of 19) in men in whom prevaccination antibody was absent or low. The vaccine was prepared with a new culture medium in which chloroform extract of egg yolk and a chemically defined salt-amino acid-vitamin solution was substituted for the allergenic horse serum and beef infusion components of standard medium.
Millimeter-wave Fresnel-zone plate lens and antenna (1995)

A new variety of millimeter-wave Fresnel-zone plate lens with enhanced focusing quality is described. Each full-wave zone of the lens is divided into four quarter-wave subzones, which are covered by dielectric rings having equal thickness but different permittivities. More practical equations are derived for the radii of the zones, and for the thickness of the lens by taking into account the angle of incidence of the electromagnetic wave. A Fresnel-zone plate antenna (FZPA) consisting of a quarterwave lens and a scalar feed is developed and analysed theoretically. Equations for the aperture field and far field are derived using multiple ray tracing through dielectric plates and vectorial Kirchhoff diffraction theory, respectively. It is demonstrated that the proposed transmissive-type FZPA has an aperture efficiency of more than 50% in the 60 GHz frequency band. This computed efficiency agree with the measured overall efficiency reported by other researchers for an X-band quarter-wave reflector-type FZPA.
Searching for pharmacophoric patterns in databases of three‐dimensional chemical structures (1995)

This paper provides an overview of the research that has been carried out in Sheffield over the last decade into searching techniques for databases of three-dimensional (3D) chemical structures. A 3D structure or query pattern is represented by a labelled graph, in which the nodes and the edges of the graph are used to represent atoms and the associated inter-atomic distances, respectively. The presence of a pharmacophore in each of the structures in a database can then be tested by means of a subgraph isomorphism algorithm, the computational requirements of which are minimized by the use of an initial screening procedure that eliminates the majority of the structures from the subgraph-isomorphism search. Analogous graph-based representation and searching methods can also be used with flexible 3D structures: in this case, the edges of the graphs represent inter-atomic distance ranges and a final conformational search needs to be carried out for those molecules that match the query pharmacophore in the subgraph-isomorphism search. The paper also reviews related work on the automatic identification of pharmacophoric patterns and on 3D similarity searching.
Information Technology: New Opportunities--New Problems. (1988)

Vis-a-vis des nouvelles techniques informatiques, en particulier les banques et base de donnees et les reseaux permettant d'y acceder, les bibliotheques peuvent jouer le role de conseiller technique, de formateur ou de fournisseur d'information aux utilisateurs defavorises. Ces attitudes impliquent de mettre l'accent sur l'acces et non plus seulement sur l'acquisition. Les bibliotheques sont preparees a ce changement car leur personnel a acquis les competences necessaires. De nouvelles questions se posent neanmoins: l'interdisciplinarite et l'aspect commercial de la connaissance, le cout, le droit d'auteur et la passation en d'autres mains du pouvoir de decision
Alopecia areata: a new treatment plan (2011)

Many therapeutic modalities have been used to treat alopecia areata, with variable efficacy and safety profiles. Unfortunately, none of these agents is curative or preventive. Also, many of these therapeutic agents have not been subjected to randomized, controlled trials, and, except for topical immunotherapy, there are few published studies on long-term outcomes. The treatment plan is designed according to the patient's age and extent of disease. In this paper, the therapeutic agents are organized according to their efficacy and safety profiles into first-line, second-line, and third-line options.
Prox-RBAC (2011)

As mobile computing devices are becoming increasingly dominant in enterprise and government organizations, the need for fine-grained access control in these environments continues to grow. Specifically, advanced forms of access control can be deployed to ensure authorized users can access sensitive resources only when in trusted locations. One technique that has been proposed is to augment role-based access control (RBAC) with spatial constraints. In such a system, an authorized user must be in a designated location in order to exercise the privileges associated with a role. In this work, we extend spatially aware RBAC systems by defining the notion of proximity-based RBAC. In our approach, access control decisions are not based solely on the requesting user's location. Instead, we also consider the location of other users in the system. For instance, a policy in a government application could prevent access to a sensitive document if any civilians are present. We introduce our spatial model and the notion of proximity constraints. We define the syntax and semantics for the Prox-RBAC language, which can be used to specify these policy constraints. We introduce our enforcement architecture, including the protocols and algorithms for enforcing Prox-RBAC policies, and give a proof of functional correctness. Finally, we describe our work toward a Prox-RBAC prototype and present an informal security analysis.
Evaluation of changes in epicardial blood flow in experimental animals by cardiothermography (1982)

Journal Article Evaluation of changes in epicardial blood flow in experimental animals by cardiothermography Get access D. TZIVONI, D. TZIVONI Department of Cardiology, Cedars-Sinai Medical CenterLos Angeles, California, U.S.A. Search for other works by this author on: Oxford Academic PubMed Google Scholar A. CRIBIER, A. CRIBIER Department of Cardiology, Cedars-Sinai Medical CenterLos Angeles, California, U.S.A. Search for other works by this author on: Oxford Academic PubMed Google Scholar K. KANMATSUSE, K. KANMATSUSE Department of Cardiology, Cedars-Sinai Medical CenterLos Angeles, California, U.S.A. Search for other works by this author on: Oxford Academic PubMed Google Scholar C. CHEW, C. CHEW Department of Cardiology, Cedars-Sinai Medical CenterLos Angeles, California, U.S.A. Search for other works by this author on: Oxford Academic PubMed Google Scholar W. GANZ W. GANZ Department of Cardiology, Cedars-Sinai Medical CenterLos Angeles, California, U.S.A. Search for other works by this author on: Oxford Academic PubMed Google Scholar European Heart Journal, Volume 3, Issue 4, August 1982, Pages 382–388, https://doi.org/10.1093/oxfordjournals.eurheartj.a061321 Published: 01 August 1982 Article history Received: 17 June 1981 Revision received: 05 November 1981 Published: 01 August 1982
Effects of switching from dopamine agonists to zonisamide on psychiatric and motor symptoms in patients with Parkinson’s disease (2021)

In 11 patients with Parkinson's disease (PD) who were using levodopa and had hallucinations and/or delusions considered to be attributed to use of dopamine agonists (DAs), we reduced or discontinued DAs and added zonisamide, and we then evaluated the effects of this treatment on psychiatric and motor symptoms. As a result, changes in the Movement Disorder Society-sponsored revision of the Unified Parkinson's Disease Rating Scale Part 1.2 (Hallucinations and Psychosis) and Part 3 (Motor Examination) scores 12 weeks from baseline were -2.4 ± 0.2 and -5.1 ± 0.9 (least-squares mean ± standard error), respectively, with the score reductions being statistically significant. These results indicated that zonisamide switching therapy is a useful strategy for managing psychiatric and motor symptoms in patients with PD when DAs are reduced or discontinued to avoid the onset or exacerbation of hallucinations and delusions.
Nano‐Composites for Water Remediation: A Review (2014)

As global populations continue to increase, the pressure on water supplies will inevitably intensify. Consequently the international need for more efficient and cost effective water remediation technologies will also rise. The introduction of nano-technology into the industry may represent a significant advancement and zero-valent iron nano-particles (INPs) have been thoroughly studied for potential remediation applications. However, the application of water dispersed INP suspensions is limited and somewhat contentious on the grounds of safety, whilst INP reaction mechanisms, transport properties and ecotoxicity are areas still under investigation. Theoretically, the development of nano-composites containing INPs to overcome these issues provides the logical next step for developing nano-materials that are better suited to wide application across the water industry. This review provides an overview of the range of static, bulk nano-composites containing INPs being developed, whilst highlighting the limitations of individual solutions, overall classes of technology, and lack of comparative testing for nano-composites. The review discusses what further developments are needed to optimize nano-composite water remediation systems to subsequently achieve commercial maturity.
Production of prostaglandin D synthase as a keratan sulfate proteoglycan by cultured bovine keratocytes. (2001)

These results indicate that bovine keratocytes, when cultured under serum-free conditions, produce the four known leucine-rich proteoglycans decorin, keratocan, lumican, and osteoglycin/mimecan and maintain a phenotype that is comparable to that of in situ keratocytes. Additionally, these cells produce PGDS, a known retinoid transporter, as a KSPG.
Fabrication of 100nm metal lines on flexible plastic substrate using ultraviolet curing nanoimprint lithography (2006)

Since polymer is flexible, lightweight, reliable and transparent and its material properties can easily be modified, it is a suitable substrate material for organic electronic devices, biomedical devices, and especially for flexible displays. To build a nano-device on a polymer substrate, nano to microsized patterning must be done. However, conventional photolithography cannot be used to fabricate patterns on flexible polymer substrate, due to the focusing and substrate handling issue associated with flexibility of polymer substrate and potential interaction between polymer and developer or other organic solvents used in photolithography. Degradation of polymer substrate during resist baking process over 120°C can be another problem. In this study, 100nm sized resist patterns were made on flexible polyethylene-terephthalate (PET) film using newly developed monomer based UV curing imprinting lithography. Compared to conventional imprint lithography, UV curing imprint lithography uses monomer based liquid phase resin and thus patterns can be fabricated without residual layer at room temperature and at much lower pressure (&lt;3–5atm) with UV illumination. No degradation of PET film was observed due to the imprint process and, as a result, 100nm sized Ti–Au metal patterns were successfully formed on PET film using UV curing imprint lithography and lift-off process.
ChemInform Abstract: Synthesis and Antitumor Activity of Novel C‐7 Paclitaxel Ethers (I): Discovery of BMS‐184476 (Ia). (2002)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Uniformly dispersed submicrometric BaTiO<inf>3</inf> particles in HDPE based composites morphology, structure and dielectric properties (2013)

The use of nanofillers to induce certain changes in electrical properties of polymeric materials, show great interest for electronic and electrical engineering applications. In this paper, composites of HDPE filled with submicrometric particles of tetragonal BaTiO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> have been prepared. An extraordinary uniform dispersion of the particles was achieved from a first process of mixing by high energy ball milling and subsequent hot pressing. Some electric measurements such as dielectric strength and resistivity were carried out to evaluate the final electrical properties as a function of the processing and the amount of BaTiO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> particles. It was observed how the resistivity decreases when the amount of BaTiO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> increases. Besides, the dielectric strength decreases as the amount of BaTiO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> particles increases. Finally it was observed that as the BaTiO <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> content increases the cylindrical-like “conducting channel”, in which the dielectric failure happens, disappears, occurring a dielectric breakdown with a less regular shape.
Human Breast Cancer Cells Selected for Resistance to Trastuzumab <i>In vivo</i> Overexpress Epidermal Growth Factor Receptor and ErbB Ligands and Remain Dependent on the ErbB Receptor Network (2007)

These results are consistent with the inability of trastuzumab to block the heterodimerization of HER2 and suggest that amplification of ligand-induced activation of ErbB receptors is a plausible mechanism of acquired resistance to trastuzumab that should be investigated in primary mammary cancers.
Data Hiding in H. 264 Encoded Video Sequences (2007)

A new method for high capacity data hiding in H.264 streams is presented. The proposed method takes advantage of the different block sizes used by the H.264 encoder during the inter prediction stage in order to hide the desirable data. It is a blind data hiding scheme, i.e. the message can be extracted directly from the encoded stream without the need of the original host video. This fragile data hiding approach can be mainly used for content-based authentication and covert communication.
Syntheses and characterizations of thiolato-functionalized N-heterocyclic carbene Pd(ii) complexes with normal and mesoionic binding modes (2011)

The thiolato-bridged dimeric Pd(II) NHC complex 1 has been synthesized from the reaction of thioester-functionalized imidazolium salt B and Pd(OAc)(2). The isolation of its interesting constitutional isomer 2 bearing both classical C(2)-bound and mesoionic C(4)-bound ligands coordinating to two different metal centers in the same complex allowed for a direct comparison of these isomeric carbenes. Reactivity studies of 1 with NaSCH(CH(3))(2) and NaBF(4) afforded the tetranuclear compound 3 with a [Pd(4)S(4)] macrocycle. All complexes have been fully characterized by multinuclei NMR spectroscopies, ESI mass spectrometry and X-ray diffraction analysis.
GSM/DCS air interface enhancements for high speed data applications (2002)

There has been a significant increase in demand for high speed data services over cellular networks, particularly by PCS in North America. The paper presents a proposal for enhancement of the GSM air interface to achieve the data rate expansion. The new proposal modifies the GSM air interface to allow multiple time-slot access of the TDMA frame by a single MS. Such a solution provides the platform for GSM to support a mixture of wide ranges of services with only moderate modifications of the air interface involved where the GSM modulation and basic TDMA frame structures are retained.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Amino Silica Gels Acting as a Carbon Dioxide Absorbent (1992)

Abstract Amino silica gels, silica gels bound with amines through covalent bond, were prepared by hydrolysis-condensation polymerization using three aminoalkyltrimethoxysilanes. The 2-[4-(2-aminoethylaminomethyl)phenyl]ethyl group absorbed CO2 with equal efficiency both in the silica gel and in the aminoalkyltrimethoxysilane. Suspension of amino silica gels in DMF and in water absorbed CO2 effectively and reversibly.
Theoretical Studies on cis-Amide Preference in N-Methylanilides (1995)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTheoretical Studies on cis-Amide Preference in N-MethylanilidesShoichi Saito, Yoshiharu Toriumi, Nobuo Tomioka, and Akiko ItaiCite this: J. Org. Chem. 1995, 60, 15, 4715–4720Publication Date (Print):July 1, 1995Publication History Published online1 May 2002Published inissue 1 July 1995https://pubs.acs.org/doi/10.1021/jo00120a011https://doi.org/10.1021/jo00120a011research-articleACS PublicationsRequest reuse permissionsArticle Views704Altmetric-Citations108LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts