gebhart/patrepeval huggingface dataset:
Transfersomes, Liposomes and Other Lipid Suspensions on the Skin: Permeation Enhancement, Vesicle Penetration, and Transdermal Drug Delivery (1996)

Agents with MW < or = are being delivered transdermally with the aid of skin permeation enhancers that increase the agent's diffusivity and/or partitioning in the organ. Use of composite, lipidic agent-carriers (liposomes, niosomes) was not successful to date, due to the inability of such vehicles to pass through the narrow (< or = 30 nm) intercellular passages (virtual pores) in the outer skin layers. A solution to this problem are the orders of magnitude more deformable supramolecular aggregates, transfersomes. Such innovative drug-carriers are driven across the skin by the noturally occurring, concentration-insensitive, and probably hydration based, transepidermal gradient(s) and transport very efficient (> > 50%) and reproducibly various agents (200 < or = MW < or = 10(6); lipophilic/hydrophilic) into the body. Transfersomes were successfully used in animals and humans, also for the transcutaneous peptide and protein delivery. The theoretical rational for this is described together with the corresponding experimental models and practical examples.
Current Prodrug Strategies for the Delivery of Nucleotides into Cells (2005)

Nucleosides are currently used in the treatment of many infections caused by viruses and against various cancers. The principal historic limitations of the development of nucleoside drugs that either directly inhibit DNA or RNA polymerases or that inhibit RNA and DNA replication by virtue of their ability to act as alternative substrates for these polymerases, have been the requirements for cellular penetration of the uncharged nucleosides and their subsequent biological conversion to the pharmacologically active nucleoside triphosphate (NTP) species. Unfortunately, intracellular phosphorylation of nucleosides frequently results in toxic by-products, limiting the drug dose that can be administered. In the past few decades, intensive research has provided insights into the nature of chemical and biological requirements associated with the in vitro selective delivery of nucleotides into cells. As such, cleavable protecting groups represent a very powerful tool to increase not only drug delivery but also bioavailability. This review presents an update of prodrug strategies in which the most prominent masking groups currently in use for the treatment of cancer and viral diseases, their stability, toxicities and biological activities are discussed. In particular, the following prodrugs: S-acyl-2-thioethyl (SATE), pivaloyloxymethyl (POM), isopropyloxycarbonyloxymethyl (POC), amino acid esters, and polyethylene glycol drug conjugates will be addressed.
Off-Resonant Gold Superstructures as Ultrabright Minimally Invasive Surface-Enhanced Raman Scattering (SERS) Probes (2015)

Surface-enhanced Raman scattering (SERS) tags that serve as exogenous contrast agents for SERS-based bioimaging are comprised of size- and shape-controlled plasmonic nanostructures. For maximum SERS activity and image contrast, the localized surface plasmon resonance (LSPR) wavelength of SERS tags based on individual nanostructures must match with the excitation wavelength (typically in the near-infrared (NIR) therapeutic window, i.e., 650–900 nm). However, under the resonant excitation, these SERS tags typically exhibit very high photothermal conversion efficiency, resulting in excessive heat that can perturb or even damage the biological species being imaged. Here, we demonstrate bioenabled synthesis of a novel class of ultrabright SERS probes with built-in and accessible electromagnetic hotspots formed by densely packed satellite nanoparticles grown on a plasmonic core. Through the rational choice of the shape of the core, the LSPR wavelength of Au superstructures can be tuned to be either off- or on-resonant with the NIR excitation without sacrificing their high SERS activity. Consequently, the photothermal efficiency of these ultrabright SERS tags can be tuned to realize either contrast agents with minimal heating and perturbation or multifunctional theranostic agents that can image and photothermally kill the targeted cells.
Synthesis of Lithium and Manganese-Rich Cathode Materials via an Oxalate Co-Precipitation Method (2013)

The synthesis of Li- and Mn- rich cathode materials with oxalate co-precipitation method was comprehensively investigated. Thermodynamic calculation and advanced characterizations were conducted to study the effects of reaction pH and precipitation agent on the morphology and composition of the precipitates. It was found that manganese oxalate has a higher solubility compared to nickel oxalate, especially at low reaction pH. In addition, the different capability of Ni2+ and Mn2+ to form transition metal ammonia complexes led to a composition discrepancy in the precipitation. The desired nickel manganese oxalate precursor composition could only be achieved when these factors were considered, and cathode materials synthesized based on this precursor exhibited satisfactory electrochemical performance (about 220 mAh·g−1 over 70 cycles under C/10 rate).
Inverse relationship between seizure expression and extrasynaptic NMDAR function following chronic NMDAR inhibition (2010)

We showed previously that electrographic seizures involving dentate granule cells in organotypic hippocampal slice cultures were dramatically reduced following chronic treatment with the NR2B-selective antagonist, Ro25,6981, but were increased following chronic treatment with the high-affinity competitive antagonist, D(-)-2-amino-5-phosphonopentanoic acid (D-APV). To begin to investigate the potential mechanisms underlying the differential effects of N-methyl-D-aspartate receptor (NMDAR) antagonists on seizures, electrophysiologic experiments were conducted in dentate granule cells in hippocampal slice cultures treated for the entire 17-21 day culture period with vehicle, Ro25,6981 or D-APV. Initial experiments revealed a lack of an association between miniature excitatory postsynaptic current (mEPSC) measures and seizures suggesting that shifts in mEPSC were unlikely to account for the differential effects of D-APV and Ro25,6981 on seizures. However, the amplitude of tonic NMDAR-mediated currents was reduced in cultures treated chronically with D-APV and dramatically enhanced in cultures treated chronically with Ro25,6981. Because tonic NMDAR currents are mediated primarily by extrasynaptic NMDAR, these data show an inverse relationship between changes in extrasynaptic NMDAR function and alterations in seizure expression.
Antineoplastic and Antiviral Activities of Some Cyclolignans (1993)

Nineteen cyclolignans of varied structures, most of them isolated from Juniperus sabina leaves, were evaluated for their antineoplastic and antiviral activities. They were subjected to screening against P-388 murine leukemia, A-549 human lung carcinoma, and HT-29 colon carcinoma, while the antiviral assays were performed on herpes simplex virus type 1 infecting fibroblasts of monkey kidney (HSV-1/CV-1) and on vesicular stomatitis virus infecting fibroblasts of hamster kidney (VSV/BHK). A number of substances were active in both types of assays at concentrations below 1 microgram/ml; deoxypodophyllotoxin and beta-peltatin A methyl ether being the most potent compounds in all cases, with IC50 values in the range 2.5-4 ng/ml for the three neoplastic systems.
Octreotide, a new somatostatin analogue. (1989)

The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects and drug interactions, dosage, availability and cost, and indications for use of octreotide, a new synthetic analogue of the peptide hormone somatostatin (SS), are reviewed. Like SS, octreotide suppresses secretion of pituitary growth hormone (GH) and thyrotropin and decreases release of a variety of pancreatic islet cell hormones including insulin, glucagon, and vasoactive intestinal peptide (VIP). Octreotide also reduces splanchnic blood flow, gastric acid secretion, GI motility, and pancreatic exocrine function and alters the absorption of water, electrolytes, and nutrients from the GI tract. The elimination half-life of i.v. octreotide is 72-98 minutes, compared with 2-3 minutes for i.v. SS. Usual administration of octreotide is by the i.v. or s.c. route. Octreotide has been studied in the treatment of hormone-secreting pituitary tumors and pancreatic islet cell tumors. Octreotide therapy lowers GH secretion and improves clinical symptoms in patients with acromegaly and may suppress clinical symptoms to a greater degree than bromocriptine. Patients with carcinoid syndrome and VIP-secreting tumors (vipomas) have had substantial improvement in clinical symptoms with administration of octreotide. This agent does not appear to be effective in the treatment of nonvariceal upper GI bleeding and acute pancreatitis; its relative usefulness in the treatment of variceal bleeding is not established. Adverse effects associated with octreotide therapy generally have been mild, including pain or burning at the injection site, abdominal pain, and diarrhea. Octreotide has been shown to interfere with absorption of oral cyclosporine. Standard initial therapy is octreotide acetate 50-100 micrograms s.c. every 8-12 hours, with titration based on clinical and biochemical effects. Up to 3000 micrograms/day of octreotide acetate has been administered to patients with acromegaly without serious adverse effect. Octreotide is marketed under the brand name Sandostatin and is available in 1-mL ampuls containing 50, 100, and 500 micrograms of octreotide acetate. Because the conditions for which octreotide appears to be most effective are uncommon, the drug should be considered for addition to the formulary in tertiary-care institutions only; addition of octreotide to the formulary of a community hospital is probably unnecessary. The synthetic analogue octreotide is longer acting and more specific in pharmacologic action than SS.(ABSTRACT TRUNCATED AT 400 WORDS)
An indexing model for structured documents to support queries on content, structure and attributes (2002)

The complex internal structure of documents can be described and captured by documentation representation standards such as SGML and SGML related standards like HTML and XML. The hierarchical structure of documents and the attributes of documents as well as attributes of document components at all levels of the document hierarchy can be encoded with markup tags. In traditional text database systems, only queries on content are supported. The rich structural information contained in documents and the attributes of document components are not captured in these systems, and queries on structure and attributes are not supported. We propose a text model, a query language and an indexing scheme which can support queries on content, structure, and attributes of documents as well as attributes of text elements within documents. This model is schema-independent, and query evaluation time is at worst linear. We show that our indexing scheme can efficiently support a wide range of queries in a database for highly heterogeneous collections of structured documents. We provide query examples to show how all the information encoded in documents marked up according to the TEI Guidelines, an encoding standard adopted by the humanities disciplines, can be indexed and queried in our indexing model.
Efficient Synthesis of a Sialyl T-antigen-linked Glycopeptide by the Chemoenzymatic Method (2000)

A sialyl T-antigen-linked tetrapeptide was prepared by the combined method of chemical synthesis and enzymatic synthesis. The GalNAc-linked peptide was first obtained by using a commercial peptide synthesizer, and then a galactose residue was attached with beta-(1-->3)-linkage by transglycosylating with a recombinant beta-galactosidase from Bacillus circulans. The sialic acid residue was then combined by alpha-(2-->3)-linkage with sialytransferase from rat liver.
Soluble derivatives of feather keratin. 2. Molecular weight and conformation (1964)

It has been shown (Fraser & MacRae, 1963) that solutions of unfractionated feather-keratin deriva- tives can be dried down into films that give well- oriented X-ray-diffraction patterns containing many of the features associated with the microfibrillar structure of the native material.It was found that similar films could be obtained from the fractions described by Harrap & Woods (1964).In most cases spontaneous birefringence developed around the edge of the film during drying.The X-ray-diffraction patterns yielded by these films when the X-ray beam passed parallel to the surface were similar to those of the unfractionated derivatives at low angles of diffraction, with a prominent meridional reflexion at 23A and equatorial reflexion at 33A.At wider angles the fractionated materials show strong layer lines at 4*8 and 2-4k and a series of equatorials which index as orders of a 33i spacing.The electron micrographs shown in Plate 1 were obtained by spraying a 1:1 (v/v) mixture of 0 05 % protein solution and 1 % phosphotungstate, pH 5 6, on to grids covered with a carbon-collodion fihm and using the negative-staining method of Brenner & Horne (1959).It is apparent from Plate 1 that, on drying, the fractionated derivatives spon- taneously polymerize to form fibrils.The apparent thickness of the fibrils varies from 40 to 60 A at their narrowest part (arrow in Plate 1 b) to approx.130A at their widest part, suggesting that they are helical with a pitch of approx.1500 k.At first sight the fibrils appear to consist of two filaments coiled around each other to give a two-strand rope, but a ribbon containing three strands cannot be excluded at present.A feature is the tendency of the fibrils to aggregate laterally in precise register.At the present time it is not clear whether the individual filaments about 40A in diameter in the fractionated proteins are structurally similar to the microfibrils in the native feather material (Rogers & Filshie, 1962; Filshie & Rogers, 1962; Fraser & MacRae, 1963), although the similarity between the low-angle X-ray patterns supports this view.
In vivo protection against endotoxin by plasma high density lipoprotein. (1993)

Overwhelming bacterial infection is accompanied by fever, hypotension, disseminated intravascular coagulation, and multiple organ failure leading to death in 30-80% of cases. These classical symptoms of septic shock are caused by potent cytokines that are produced in response to endotoxin released from Gram-negative bacteria. Treatments with antibodies and receptor antagonists to block endotoxin or cytokine mediators have given mixed results in clinical trials. High density lipoprotein (HDL) is a natural component of plasma that is known to neutralize endotoxin in vitro. We report here that raising the plasma HDL concentration protects mice against endotoxin in vivo. Transgenic mice with 2-fold-elevated plasma HDL levels had more endotoxin bound to HDL, lower plasma cytokine levels, and improved survival rates compared with low-HDL mice. Intravenous infusion of HDL also protected mice, but only when given as reconstituted HDL prepared from phospholipid and either HDL apoprotein or an 18-amino acid peptide synthesized to mimic the structure of apolipoprotein A-I of HDL. Intact plasma HDL was mildly toxic, and HDL apoprotein was ineffective. The effectiveness of the reconstituted peptide renders very unlikely any significant contribution to protection by trace proteins in apo-HDL. These data suggest a simple leaflet insertion model for binding and neutralization of lipopolysaccharide by phospholipid on the surface of HDL. Plasma HDL may normally act to protect against endotoxin; this protection may be augmented by administration of reconstituted HDL or reconstituted peptides.
The Role of B7-1 and B7-2 Costimulation for the Generation of CTL Responses In Vivo (1998)

The role of B7-1 and B7-2 costimulatory molecules in the generation of Ag-specific CD8+ CTLs is not well understood. In this paper, we analyze the role of both B7-1 and B7-2 in the generation of CTLs to nonliving, exogenous Ag and to live virus. To analyze the role of B7 costimulation in the induction of CTLs, we blocked B7-1 and/or B7-2 in vivo by injecting C57BL/6 mice with anti-B7-1 and/or anti-B7-2 mAbs; the mice were subsequently immunized with either chicken OVA that had been cross-linked to beads as a model of exogenous Ags or with wild-type and recombinant vaccinia virus expressing different forms of chicken OVA as models of viral Ags. Our results indicate that B7 costimulation is necessary in the generation of CTLs for all of these Ags. Since the B7 molecules could be costimulating CD8+ and/or CD4+ T cells in wild-type animals, we also examined the role of costimulation in the generation of CTLs to exogenous and viral Ag in MHC class II-deficient mice lacking most CD4+ T cells. In these animals, a combination of both mAbs also blocked all CTL responses, indicating that the Th cell-independent activation of CTLs is dependent upon the B7-costimulatory signals supplied to the CD8+ cell. These findings contribute to the understanding of the role of costimulation for the generation of CTLs. We also discuss the implications of these findings on the role of professional APCs in the initiation of CTL responses.
ProPred1: prediction of promiscuous MHC Class-I bindingsites (2003)

Server is available at http://www.imtech.res.in/raghava/propred1/. Mirror site of this server is available at http://bioinformatics.uams.edu/mirror/propred1/ SUPPLEMENTARY INFORMATION: Matrices and document on server are available at http://www.imtech.res.in/raghava/propred1/page2.html
Analytical model of deeply-scaled thyristors for memory applications (2012)

In this paper we propose an analytical model for the static operation of thyristor, aiming at clarifying the basic physics involved in the switching from the low-conductance to the high-conductance state of the device. Modeling results are compared to TCAD numerical simulations, showing that the analytical calculations can nicely reproduce the main features of the current-voltage device characteristics.
Synthesis of 2- and 4-fluoroestradiol (1968)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of 2- and 4-fluoroestradiolTorleif Utne, Ronald B. Jobson, and Robert D. BabsonCite this: J. Org. Chem. 1968, 33, 6, 2469–2473Publication Date (Print):June 1, 1968Publication History Published online1 May 2002Published inissue 1 June 1968https://pubs.acs.org/doi/10.1021/jo01270a065https://doi.org/10.1021/jo01270a065research-articleACS PublicationsRequest reuse permissionsArticle Views141Altmetric-Citations18LEARN 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
A Carbon Fiber Implant to Aid Interbody Lumbar Fusion (1993)

The success of posterior lumbar interbody fusion (PLIF) has been limited by mechanical and biologic deficiencies of the donor bone. The authors have designed a carbon fiber-reinforced polymer implant that separates the mechanical and biologic functions of PLIF. The cagelike implant provides an actual device designed to meet the mechanical requirements of PLIF and replaces the donor bone with autologous bone, the best possible bone for healing. The authors report 2-year follow-up results for their first 26 consecutive patients, 18 of whom were postsurgical failed backs with a total of 37 previous surgeries. At 2 years, 28 of 28 PLIF cage fusion levels and 6 of 11 (54.5%) allograft levels exhibited radiographic fusion, a statistically significant difference at P = 0.0002. Clinical results were excellent in 11/26, good in 10/26, fair in 3/26, and poor in 2/26. Fair and poor results were attributable to objective identifiable problems unrelated to the carbon cage. The carbon implant achieved successful fusion in 6/6 (100%) of followed patients treated for a failed ETO allograft interbody fusion. A prospective controlled multi-centered study is being initiated.
Comparison of Emasculation and Nonemasculation for Hybridization of Soybeans1 (1979)

Emasculation and nonemasculation of the soybean [ Glycine max (L.) Merr.] flower for hybridization were compared for percentage of pollinations that produced a pod (percent success), number of seeds per pod, number of selfed seed, percentage of hybrid seed based on total pollinations, and time required for hybridization. Two persons made pollinations with three sets of parents in each of three Iowa and two Puerto Rico environments. The gene controlling flower and hypocotyl color was used to differentiate hybrid and selfed seed. Average percentage of successful pollinations across environments was significantly greater for nonemasculation (44%) than for emasculation (36%). Average number seeds per pod was similar for the two procedures. The average number of selfed seed was not significantly different for nonemasculation and emasculation. The percentage of hybrid seed based on total pollinations averaged across environments was significantly greater for nonemasculation (94%) than for emasculation (73%). Time saved by not emasculating the female parent permitted at least 10% more flowers to be pollinated per hour than when emasculation was used. Emasculation of soybean flowers prior to pollination is not justified on the basis of these results.
Statistics on concurrent fault and design error simulation (2002)

Basic data of the nature presented here on fault and design error simulation processes have not been previously reported. Experiments are performed on c-sim, a gate level concurrent simulator developed at the University of Texas at Austin. Three types of statistics are considered: event based statistics, gate evaluation statistics and memory requirements. These statistics are important for design verification researchers and engineers for numerous reasons. For example, they help simulator developers tune up or optimize their concurrent simulators. They also fulfill the increasing need for experimental data concerning design error simulation. Most importantly, these statistics provide guidance to hardware accelerator designers in evaluating and comparing various design options.