gebhart/patrepeval huggingface dataset:
In vitro studies of 2,4-dihydroxyphenylalanine, a prodrug targeted against malignant melanoma cells. (1985)

We have evaluated the chemotherapeutic potential of 2,4-dihydroxyphenylalanine, a targeted prodrug that can be hydroxylated by tyrosinase (monophenol monooxygenase, EC 1.14.18.1) within melanoma cells to form the cellular toxin 2,4,5-trihydroxyphenylalanine (6-hydroxydopa). 2,4-Dihydroxyphenylalanine proved to be cytotoxic to both B-16 and Cloudman melanoma cells in vitro. The immediate effects of 2,4-dihydroxyphenylalanine included inhibition of DNA, RNA, and protein syntheses. In contrast, no decrease in macromolecular synthesis or viability was seen against cultures of MJY-alpha mammary tumor or L-1210 leukemia, two cell types that do not contain tyrosinase. Within the melanoma cultures, greater cytotoxicity was seen against melanotic (tyrosinase-containing) cells than against amelanotic (tyrosinase-lacking) cells. The cytotoxicity of 2,4-dihydroxyphenylalanine was blocked by 1-phenylthiourea, an inhibitor of tyrosinase. These results show that 2,4-dihydroxyphenylalanine is toxic to melanoma cells and that activation of 2,4-dihydroxyphenylalanine requires the presence of tyrosinase.
A Comparison of Chloroambucil- and Xylene-Containing Polyamines Leads to Improved Ligands for Accessing the Polyamine Transport System (2008)

Several disubstituted arylene- and chloroambucil-polyamine conjugates were synthesized and evaluated for their ability to target cells via their polyamine transport system (PAT). As compared to the monosubstituted analogues, the disubstituted arylene systems were superior PAT targeting agents. Using a Chinese hamster ovary (CHO) cell line (PAT active) and its CHO-MG mutant (PAT inactive), the series was screened for their PAT targeting ability. The data were expressed as a CHOMG/CHO IC 50 ratio. Indeed, the disubstituted systems gave high IC 50 ratios (e.g., ratio > 2000), which indicated high selectivity for the PAT. The chloroambucil adducts were less toxic than the corresponding arylmethyl compounds. In this regard, having the proper recognition element (i.e., homospermidine) and cytotoxic "cargo" were deemed paramount for successful drug delivery via the PAT.
Characterization of pH- and temperature-sensitive hydrogel nanoparticles for controlled drug release. (2007)

Monodispersed poly (N-isopropylacrylamide) (PNIPA) nanoparticles and their derivative poly (N-isopropylacrylamide-co-acrylic acid) (PNIPA-co-AA) nanoparticles were successfully synthesized. Regulation of the size and the lower critical solution temperature (LCST) of the hydrogel nanoparticles was intensively studied. The results showed that the diameters and LCST of the particles can be arbitrarily manipulated according to different application designs. The relationship between the size of the particles and the amount of surfactant were quantitatively disclosed. It was found that the LCST of PNIPA-co-AA nanoparticles ranging from 35-45 degrees C correlated with the molar fraction of acrylic acid which was copolymerized with NIPA. The pH sensitivity of PNIPA-co-AA nanoparticles was displayed by the transmittance transition of their aqueous solution in various pH conditions. Furthermore, the anti-cancer drug 5-fluorouracil (5-Fu) was first loaded into both PNIPA and PNIPA-co-AA hydrogel nanoparticles with an entrapment efficiency larger than 4%. In vitro release of 5-Fu from PNIPA-co-AA nanoparticle hydrogels was shown to be pH- and temperature-dependent, which demonstrated that the PNIPA-co-AA nanoparticles have great potential in the design of controlled drug delivery systems.
Novel rearrangement and cyclization processes resulting from bromination of 1,1-dibenzyltetralin derivatives (1992)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNovel rearrangement and cyclization processes resulting from bromination of 1,1-dibenzyltetralin derivativesBernard Miller and Xiaolian ShiCite this: J. Org. Chem. 1992, 57, 6, 1677–1681Publication Date (Print):March 1, 1992Publication History Published online1 May 2002Published inissue 1 March 1992https://pubs.acs.org/doi/10.1021/jo00032a015https://doi.org/10.1021/jo00032a015research-articleACS PublicationsRequest reuse permissionsArticle Views365Altmetric-Citations7LEARN 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
An embedded DRAM-FPGA chip with instantaneous logic reconfiguration (2002)

Reconfigurable computing is attracting wide attention as a novel general purpose computing paradigm for accelerating compute intensive and/or data-parallel applications, such as compression, encryption, searching, sorting, and image processing. A key enabling technology for a reconfigurable computer is in-system logic reconfiguration of SRAM-based FPGAs, through which its hardware architecture is dynamically customized for a specific task on demand. Quicker a reconfiguration is, more frequent the reconfigurations can become: i.e., a reconfigurable computer can adapt to applications which have more dynamic behavior. A whole-chip reconfiguration in conventional FPGAs, however, takes at least 100/spl mu/s. With this long latency, a reconfigurable computer is adaptable only to static applications, substantially losing the general-purposeness of the original concept. Integrating a DRAM with an FPGA can become an ideal solution to this problem. The on-chip DRAM can store hundreds of configuration programs, and the logic reconfiguration can get extremely faster by context-switching among the programs utilizing huge bandwidth internal to the DRAM core. Being driven by this observation, we have conducted prototype design of an embedded DRAM-FPGA chip.
Direct In Situ Measurement of Nitric Oxide in Mesenteric Resistance Arteries (1996)

The endothelium plays a critical role in maintaining vascular tone by releasing vasoconstrictor and vasodilator substances. Endothelium-derived nitric oxide is a vasodilator that can be rapidly inactivated by superoxide (reaction rate constant, K = 3.6 x 10(9) L/mol per second). The measurement of nitric oxide concentration in biological systems is a challenging analytic problem because nitric oxide is also rapidly inactivated by Fe(II), Fe(III), and O2, all of which are found in great abundance in biological systems. To date, no currently used instrumental technique has been suitable for direct in situ measurement of NO in isolated resistance arteries. We designed the present study to perform for the first time direct in situ measurements of NO in rat mesenteric resistance arteries and to delineate the effects of hypertension on the release of NO and/or its interaction with superoxide. We describe here an adaptation of the recently published design of a porphyrinic sensor for direct in vitro measurement of NO in a single cell. The most significant advantage of this modified porphyrinic microsensor is that its small size makes it ideal for NO measurement in resistance arteries with an internal diameter of 200 microns or less. Small segments of the third-order branch of the mesenteric artery were isolated from normotensive Wistar-Kyoto rats and stroke-prone spontaneously hypertensive rats and placed in an organ chamber filled with Hanks' balanced salt solution buffer (2 mL, 37 degrees C). The tip of the porphyrinic microsensor was inserted into the lumen of an isolated vascular ring, and NO release was monitored in situ after maximal stimulation of NO synthase with the receptor-independent agonist calcium ionophore A23187 (10 mumol/L). Maximal surface concentration of NO measured after A23187 administration was significantly smaller in 15-week-old hypertensive rats (0.28 +/- 0.03 mumol/L, n = 10) than in age-matched normotensive rats (0.38 +/- 0.03 mumol/L, n = 10, P < .03). However, in the presence of the superoxide scavenger superoxide dismutase (100 U/mL), the peak NO level from the hypertensive rats was 0.37 +/- 0.04 mumol/L (n = 10), which was comparable to that observed for the normotensive rats in the absence and presence of superoxide dismutase. In summary, our results demonstrate that in rat mesenteric resistance arteries hypertension is associated with increased NO decomposition by superoxide, whereas NO release remains unaffected. This may be important in the pathogenesis of hypertension and its cardiovascular complications.
Direct Reprogramming of Human Fibroblasts toward a Cardiomyocyte-like State (2013)

Direct reprogramming of adult somatic cells into alternative cell types has been shown for several lineages. We previously showed that GATA4, MEF2C, and TBX5 (GMT) directly reprogrammed nonmyocyte mouse heart cells into induced cardiomyocyte-like cells (iCMs) in vitro and in vivo. However, GMT alone appears insufficient in human fibroblasts, at least in vitro. Here, we show that GMT plus ESRRG and MESP1 induced global cardiac gene-expression and phenotypic shifts in human fibroblasts derived from embryonic stem cells, fetal heart, and neonatal skin. Adding Myocardin and ZFPM2 enhanced reprogramming, including sarcomere formation, calcium transients, and action potentials, although the efficiency remained low. Human iCM reprogramming was epigenetically stable. Furthermore, we found that transforming growth factor β signaling was important for, and improved the efficiency of, human iCM reprogramming. These findings demonstrate that human fibroblasts can be directly reprogrammed toward the cardiac lineage, and lay the foundation for future refinements in vitro and in vivo.
Control-free calling of copy number alterations in deep-sequencing data using GC-content normalization (2010)

Source code and sample data are available at http://bioinfo-out.curie.fr/projects/freec/.
Characterization of the CCL21-mediated melanoma-specific immune responses and in situ melanoma eradication (2007)

Previous studies have shown that secondary lymphoid chemokine, CCL21, can be used for modulation of tumor-specific immune responses. Here, using B16F0 melanoma cells stably expressing CCL21 under the control of cytomegalovirus and ubiquitin promoters, we showed that CCL21-activated immune responses depend on the amount of melanoma-derived chemokine, which, in turn, depends on the strength of the promoter. We showed that ubiquitin promoter-driven expression of CCL21 enabled massive infiltration of tumors with CD4(+)CD25(-), CD8(+) T lymphocytes, and CD11c(+) dendritic cells, and consequent activation of cellular and humoral immune responses sufficient for complete rejection of CCL21-positive melanomas within 3 weeks in all tumor-inoculated mice. Mice that rejected CCL21-positive tumors acquired protective immunity against melanoma, which was transferable to naive mice via splenocytes and central memory T cells. Moreover, melanoma-derived CCL21 facilitated immune-mediated remission of preestablished, distant wild-type melanomas. Overall, these results suggest that elevated levels of tumor-derived CCL21 are required for the activation of strong melanoma-specific immune responses and generation of protective immunologic memory. They also open new perspectives for the development of novel vaccination strategies against melanoma, which use intratumoral delivery of the optimized CCL21-encoding vectors in conjunction with DNA-based vaccines.
What If Cars Could Drive Themselves (2000)

V E N W H E N cars were still young, futurists began thinking about vehicles that could drive themselves, without human help.Perhaps the best known of these conjectures was the General Motors Futurama, the hit of the 1939 New York Wo r l d ' s Fa i r.During the following decades interest in automated vehicles rose and fell several times.N o w, at the start of the new century, it's worth taking a fresh look at this concept and asking how automation might change transportation and the quality of our lives.
Guest Editorial: Drug Delivery for Treatment of Inner Ear Disease: Current State of Knowledge (2010)

Department of Otolaryngology; Washington University School of Medicine in St. Louis; St. Louis, Missouri Dr. Salt is a member of the Scientific Advisory Board of Otonomy, Inc., and may receive income based on equity holdings.
The role of interleukin-1 in allergy-related disorders (2012)

The recent findings support a crucial role for IL-1β and inflammasome components in a variety of allergy-related disorders.
Purification, characterization and cDNA cloning of human lung surfactant protein D (1992)

Human pulmonary surfactant protein D (SP-D) was identified in lung lavage by its similarity to rat SP-D in both its molecular mass and its Ca(2+)-dependent-binding affinity for maltose [Persson, Chang & Crouch (1990) J. Biol. Chem. 265, 5755-5760]. For structural studies, human SP-D was isolated from amniotic fluid by affinity chromatography on maltose-Sepharose followed by f.p.l.c. on Superose 6, which showed it to have a molecular mass of approx. 620 kDa in non-dissociating conditions. On SDS/PAGE the human SP-D behaved as a single band of 150 kDa or 43 kDa in non-reducing or reducing conditions respectively. The presence of a high concentration of glycine (22%), hydroxyproline and hydroxylysine in the amino acid composition of human SP-D indicated that it contained collagen-like structure. Collagenase digestion yielded a 20 kDa collagenase-resistant globular fragment which retained affinity for maltose. Use of maltosyl-BSA as a neoglycoprotein ligand in a solid-phase binding assay showed that human SP-D has a similar carbohydrate-binding specificity to rat SP-D, but a clearly distinct specificity from that of other lectins, such as conglutinin, for a range of simple saccharides. Amino acid sequence analysis established the presence of collagen-like Gly-Xaa-Yaa triplets in human SP-D and also provided sequence data from the globular region of the molecule which was used in the synthesis of oligonucleotide probes. Screening of a human lung cDNA library with the oligonucleotide probes, and also with rabbit anti-(human SP-D), allowed the isolation of two cDNA clones which overlap to give the full coding sequence of human SP-D. The derived amino acid sequence indicates that the mature human SP-D polypeptide chain is 355 residues long, having a short non-collagen-like N-terminal section of 25 residues, followed by a collagen-like region of 177 residues and a C-terminal C-type lectin domain of 153 residues. Comparison of the human SP-D and bovine serum conglutinin amino acid sequences indicated that they showed 66% identity despite their marked differences in carbohydrate specificity.
Research Guides: Asian Studies Research Guide: South and Southeast Asian Studies (2007)

Resources for students and faculty in the Asian Studies programs: East Asian Studies; South and Southeast Asian Studies; Central and Southwest Asian Studies.
Difluorodioxirane (1993)

At 22 °C, difluorodioxirane 1 is stable in the gas phase. Thus, theoretical predictions were confirmed with compound l, which was prepared in pure form for the first time [Eq. (a)]. This reaction was carried out over pelletized CsF in a flow system and gave 1 in 20–50% yield. X2 = ClF, Cl2, F2.
PROLACTIN CONCENTRATION IN VAGINAL FLUID: A NEW METHOD FOR DIAGNOSING RUPTURED MEMBRANES (1981)

Prolactin concentrations were assayed in vaginal fluid, urine and plasma in 20 women between 38 and 41 weeks gestation. Plasma concentrations of 12.3 (7.3-20.8) mU/ml (n = 40) were found whereas urine concentrations were low or undetectable. Vaginal fluid concentrations were generally lower than 0.25 mU/ml but occasionally elevated up to 3 mU/ml in women with unruptured membranes. Half an hour after artificial rupture of the membranes, vaginal fluid prolactin concentrations were always higher than paired maternal plasma concentrations (p less than 0.001). In women suspected of premature rupture of the membranes, prolactin concentrations in vaginal fluid were always higher than the plasma concentrations except in those in whom the clinical outcome showed that the membranes had not ruptured. A rapid prolactin radioimmunoassay is therefore recommended as a new clinical tool for the diagnosis or exclusion of prematurely ruptured membranes.
Oncotic pressure in solid tumors is elevated. (2000)

Oncotic and hydrostatic pressure differences control the movement of fluid and large molecules across the microvascular wall of normal and tumor tissues. Recent studies have shown that the interstitial fluid pressure in tumors is elevated and is approximately equal to the microvascular pressure. Whereas oncotic pressure in blood plasma of various species is known, no data are available on the oncotic pressure in the interstitial space of tumors. We hypothesize that because of the leaky nature of tumor vessels, oncotic pressure in tumor interstitium should be close to that in plasma. To this end, we first developed a chronic wick method for the direct measurement of oncotic pressures in the interstitial fluid of tumors grown in mice. We found interstitial oncotic pressures in four human tumor xenografts to be higher than in s.c. tissue and comparable to that in plasma [rhabdomyosarcoma (RD), 24.2+/-4.7; squamous cell carcinoma (FaDu), 19.9+/-1.9; small cell lung carcinoma (54A), 21.1+/-2.8; colon adenocarcinoma (LIS174T), 16.7+/-3.0 mm Hg; s.c. tissue, 8.2+/-2.3; plasma, 20.0+/-1.6 mm Hg]. These results support our hypothesis that the oncotic pressure difference across the tumor microvascular wall is low. The high oncotic pressure in tumors is consistent with the elevated interstitial fluid pressure, and it contributes to the suboptimal delivery of large therapeutic agents to neoplastic cells.
Clinical predictive value of the in vitro cell line, human xenograft, and mouse allograft preclinical cancer models. (2003)

These results suggest that under the right framework and when panels are used, the in vitro cell line and human xenograft models may be useful in predicting the Phase II clinical trial performance of cancer drugs. Murine allograft models, as used in this analysis, appear of limited utility.
Sphenopalatine Blocks in the Treatment of Pain in Fibromyalgia and Myofascial Pain Syndrome (1997)

Sphenopalatine blocks have been used to treat pain for more than 80 years. Anecdotal support for sphenopalatine ganglion blocks has been very strong in those who believe in the technique, but the research results have been inconclusive. Therefore, a double blind, placebo-controlled study was performed on 61 patients, 42 with fibromyalgia and 19 with myofascial pain syndrome. Pain was measured using visual analogue scales prior to treatment, during treatment, and 28 days after the treatment. Headaches were evaluated in frequency and location prior to and after treatment. Sphenopalatine ganglion blocks were performed under direct vision using 4% lidocaine and sterile water as a placebo. Analysis of the results showed no statistical differences between the lidocaine and the placebo groups.
Human anti-murine immunoglobulin responses in patients receiving monoclonal antibody therapy. (1985)

Human anti-murine immunoglobulin responses were assessed in serum from three groups of patients receiving murine monoclonal antibody therapy. Each of the three patient groups responded differently. Chronic lymphocytic leukemia patients demonstrated little or no preexisting murine immunoglobulin G-reactive antiglobulin prior to treatment, while the cutaneous T-cell lymphoma and melanoma patients demonstrated preexisting antiglobulin levels in the same range as those demonstrated in healthy controls. None of 11 chronic lymphocytic leukemia patients receiving the T101 monoclonal antibody demonstrated an antiglobulin response, whereas all four of the cutaneous T-cell lymphoma patients receiving the same antibody developed increased levels of antiglobulins. Three of nine malignant melanoma patients receiving the 9.2.27 monoclonal antibody showed an increase in antiglobulin titers. In patients developing antiglobulin responses, the response was rapid, typically being detectable within 2 weeks. The antiglobulins were primarily immunoglobulin G and, with the exception of a single melanoma patient in whom the response appeared to have a substantial 9.2.27-specific component (i.e., antiidiotype), were cross-reactive with most murine immunoglobulin G preparations tested. This pattern of results suggested that the antiglobulin was a secondary immune reaction with elevation of the levels of preexisting antiglobulin which was cross-reactive with the mouse antibody administered. While the presence of serum antiglobulin would be expected to present major complications to monoclonal antibody therapy, no clinical toxicity related to antiglobulin responses was observed in these patients, and no inhibition of antibody localization on tumor cells was seen.
Molecular Mechanisms of Myocardial Remodeling (1999)

"Remodeling" implies changes that result in rearrangement of normally existing structures. This review focuses only on permanent modifications in relation to clinical dysfunction in cardiac remodeling (CR) secondary to myocardial infarction (MI) and/or arterial hypertension and includes a special section on the senescent heart, since CR is mainly a disease of the elderly. From a biological point of view, CR is determined by 1 ) the general process of adaptation which allows both the myocyte and the collagen network to adapt to new working conditions; 2) ventricular fibrosis, i.e., increased collagen concentration, which is multifactorial and caused by senescence, ischemia, various hormones, and/or inflammatory processes; 3) cell death, a parameter linked to fibrosis, which is usually due to necrosis and apoptosis and occurs in nearly all models of CR. The process of adaptation is associated with various changes in genetic expression, including a general activation that causes hypertrophy, isogenic shifts which result in the appearance of a slow isomyosin, and a new Na+-K+-ATPase with a low affinity for sodium, reactivation of genes encoding for atrial natriuretic factor and the renin-angiotensin system, and a diminished concentration of sarcoplasmic reticulum Ca2+-ATPase, beta-adrenergic receptors, and the potassium channel responsible for transient outward current. From a clinical point of view, fibrosis is for the moment a major marker for cardiac failure and a crucial determinant of myocardial heterogeneity, increasing diastolic stiffness, and the propensity for reentry arrhythmias. In addition, systolic dysfunction is facilitated by slowing of the calcium transient and the downregulation of the entire adrenergic system. Modifications of intracellular calcium movements are the main determinants of the triggered activity and automaticity that cause arrhythmias and alterations in relaxation.