gebhart/patrepeval huggingface dataset:
Chemistry and Structure of Mitomycin C1 (1965)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTChemistry and Structure of Mitomycin C1Calvin L. Stevens, K. Grant Taylor, Morton E. Munk, W. S. Marshall, Klaus Noll, G. D. Shah, L. G. Shah, and K. UzuCite this: J. Med. Chem. 1965, 8, 1, 1–10Publication Date (Print):January 1, 1965Publication History Published online1 May 2002Published inissue 1 January 1965https://pubs.acs.org/doi/10.1021/jm00325a001https://doi.org/10.1021/jm00325a001research-articleACS PublicationsRequest reuse permissionsArticle Views358Altmetric-Citations65LEARN 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
Susceptible MHC alleles, not background genes, select an autoimmune T cell reactivity (2003)

To detect and characterize autoreactive T cells in diabetes-prone NOD mice, we have developed a multimeric MHC reagent with high affinity for the BDC-2.5 T cell receptor, which is reactive against a pancreatic autoantigen. A distinct population of T cells is detected in NOD mice that recognizes the same MHC/peptide target. These T cells are positively selected in the thymus at a surprisingly high frequency and exported to the periphery. They are activated specifically in the pancreatic LNs, demonstrating an autoimmune specificity that recapitulates that of the BDC-2.5 cell. These phenomena are also observed in mouse lines that share with NOD the H-2g7 MHC haplotype but carry diabetes-resistance background genes. Thus, a susceptible haplotype at the MHC seems to be the only element required for the selection and emergence of autoreactive T cells, without requiring other diabetogenic loci from the NOD genome.
Cloning and expression of a cDNA encoding human endothelium-derived relaxing factor/nitric oxide synthase. (1992)

Nitric oxide, which accounts for the biological activity of endothelium-derived relaxing factor (EDRF), is synthesized in endothelial cells from L-arginine by nitric oxide synthase (NOS). We report here the cloning and functional expression of a cDNA encoding human endothelial NOS. Oligonucleotides corresponding to amino acid sequences shared by cytochrome P450 reductase and the recently identified brain NOS were synthesized to amplify a partial cDNA encoding a bovine endothelial cell NOS-related protein. This partial cDNA was used to isolate a cDNA encoding a human vascular endothelial NOS. The translated human protein is 1294 amino acids long and shares 52% of its amino acid sequence with brain NOS. Using RNA blot hybridization, abundant endothelial NOS mRNA was detected in unstimulated human umbilical vein endothelial cells. To determine the functional activity of the endothelial protein, we ligated the cDNA into an expression vector and transfected it into NIH3T3 cells. Cells expressing this cDNA contained abundant NADPH diaphorase activity, a histochemical marker for NOS. In co-culture assays, nitric oxide production by transfected cells increased guanylate cyclase activity in reporter rat fetal lung fibroblasts. In addition, NOS-catalyzed conversion of arginine to citrulline in transfected cells was significantly increased by A23187, a calcium ionophore. Isolation of a cDNA encoding a calcium-regulated, constitutively expressed human endothelial NOS, capable of producing EDRF in blood vessels, will accelerate the characterization of the role of this enzyme in normal and abnormal endothelial regulation of vascular tone.
Structure-activity relationship studies of CNS agents. Part 14: Structural requirements for the 5-HT1A and 5-HT2A receptor selectivity of simple 1-(2-pyrimidinyl)piperazine derivatives. (1994)

The 5-HT1A and 5-HT2A receptor affinity of model 1-(2-pyrimidinyl)-piperazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpiperazino)-4,6-di(2-thienyl)pyrimidine 26 is a new, highly active and selective 5-HT2A receptor ligand. The topography of a molecule and the stereoelectronic effects of the thiophene rings are the major factors responsible for the high affinity and selectivity of 26 towards 5-HT2A sites.
Insulin glargine: long-acting basal insulin analog for improved metabolic control (2003)

The primary aim of insulin therapy is to replace endogenous insulin secretion in patients with type 1 or type 2 diabetes in a physiologically sound manner, mimicking normal secretion patterns to adequately regulate glucose metabolism. The currently available human insulins for basal therapy--neutral protamine Hagedorn (NPH), Lente and Ultralente--and analogs such as insulin glargine, differ in pharmacokinetic properties. Clinical trial data indicate that insulin glargine may satisfy basal insulin requirements, with an improved safety profile relative to other available insulins used for basal supplementation. This review describes the unique pharmacokinetic properties and clinical efficacy of insulin glargine.
Bead: explorations in information visualization (1992)

We describe work on the visualization of bibliographic data and, to aid in this task, the application of numerical techniques for multidimensional scaling.
Cochlear Pharmacokinetics with Local Inner Ear Drug Delivery Using a Three-Dimensional Finite-Element Computer Model (2006)

The 3D model clearly shows the presence of drug gradients across the basal scalae of guinea pigs, demonstrating the necessity of a 3D approach to predict drug movements across and between scalae with larger cross-sectional areas, such as the human, with accuracy. This is the first model to incorporate the volume of the spiral ligament and to calculate diffusion through this structure. Further development of the 3D model will have to incorporate a more accurate geometry of the entire inner ear and incorporate more of the specific processes that contribute to drug removal from the inner ear fluids. Appropriate computer models may assist in both drug and drug delivery system design and can thus accelerate the development of a rationale-based local drug delivery to the inner ear and its successful establishment in clinical practice.
The Fourth Surface-Exposed Region of the Outer Membrane Protein P5-Homologous Adhesin of Nontypable Haemophilus influenzae Is an Immunodominant But Nonprotective Decoying Epitope (2003)

Nontypable Haemophilus influenzae is a major cause of otitis media and other mucosal infections. After natural disease in children and experimental disease in chinchillas, we found a hierarchical pattern of immunodominance among the four surface-exposed regions of the P5-homologous adhesin, with the greatest response directed to region 4. However, Ab to region 4 is not protective. When this natural but biased response was refocused to region 3 by immunization, augmented bacterial clearance and protection from ascending otitis media was observed. Collectively, the data indicate that region 4 contains a highly immunodominant but nonprotective decoying epitope, the presence of which dampens the immune response to a subdominant but protective epitope in region 3.
An interdigitated printed antenna for PC card applications (1998)

A quarter-wavelength diversity patch configuration for the 2.4-GHz ISM band PC card application is reported. The structure is based on partly interdigitation of two quarter wavelength separated patches through a set of fingers for achieving the required space diversity on single side printed substrate with an easy matching on 50 /spl Omega/, high cross-polarization and within a given maximum space of 30 mm/spl times/50 mm. Measured antenna patterns for the developed structure are the same as for a classical patch and the bandwidth for a VSWR less than two is 2% with a maximum gain of 1.5 dB. This antenna has been incorporated in a high-speed wireless LAN PC card system.
Altered surfactant function and structure in SP-A gene targeted mice. (1996)

The surfactant protein A (SP-A) gene was disrupted by homologous recombination in embryonic stem cells that were used to generate homozygous SP-A-deficient mice. SP-A mRNA and protein were not detectable in the lungs of SP-A(-/-) mice, and perinatal survival of SP-A(-/-) mice was not altered compared with wild-type mice. Lung morphology, surfactant proteins B-D, lung tissue, alveolar phospholipid pool sizes and composition, and lung compliance in SP-A(-/-) mice were unaltered. At the highest concentration tested, surfactant from SP-A(-/-) mice produced the same surface tension as (+/+) mice. At lower concentrations, minimum surface tensions were higher for SP-A(-/-) mice. At the ultrastructural level, type II cell morphology was the same in SP-A(+/+) and (-/-) mice. While alveolar phospholipid pool sizes were unperturbed, tubular myelin figures were decreased in the lungs of SP-A(-/-) mice. A null mutation of the murine SP-A gene interferes with the formation of tubular myelin without detectably altering postnatal survival or pulmonary function.
Dimetalation of Furans and Thiophenes. One-Pot Procedures for Furan-2,5- and Thiophene-2,5-dicarboxaldehyde (1988)

A new one-pot synthesis of furan-2,5-dicarboxaldehyde and thiophene-2, 5-dicarboxaldehyde in 80% and 75% yields, respectively, via dimetalation of furan and thiophene, is described. In addition, monoprotected furan-2,5-dicarboxaldehyde was prepared in 73% yield from furfural.
Vaults Are Up-regulated in Multidrug-resistant Cancer Cell Lines (1998)

Vaults are 13-MDa ribonucleoprotein particles composed largely of a 104-kDa protein, termed major vault protein or MVP, and a small vault RNA, vRNA. While MVP levels have been found to increase up to 15-fold in non-P-glycoprotein multidrug-resistant cell lines, the levels of vault particles have not been investigated. As both the function of vault particles and the mechanism of drug resistance in non-P-glycoprotein cells are unknown, we decided to determine whether vault synthesis was coupled to MDR. By cloning the human gene for vRNA and careful quantitation of the MVP and vRNA levels in MDR cells, we find that vRNA is in considerable excess to MVP. Sedimentation measurements of vault particles in multidrug resistance cells have indeed revealed up to a 15-fold increase in vault synthesis, coupled with a comparable shift of associated vRNA, demonstrating that vault formation is limited by expression of MVP or the minor vault proteins. The observation that vault synthesis is linked directly to multidrug resistance supports a direct role for vaults in drug resistance.
N-Heterocyclic carbenes as highly efficient ancillary ligands in homogeneous and immobilized metathesis ruthenium catalytic systems (2005)

This general overview focuses on novel N-heterocyclic carbene (NHC) Ru complexes, now at the forefront of research in metathesis chemistry, and on their derived multiple applications in targeted organic, polymeric and natural compound synthesis. This outstanding, large class of ruthenium precatalysts combines high activity and selectivity with increased stability and good tolerance towards organic functionalities, air and moisture. The NHC ancillary ligands allow manipulation of the catalytic performance through adjustment of electronic and steric parameters in the ruthenium coordination sphere, facilitate introduction of chiral motifs, and enable convenient immobilization of homogeneous initiators onto solid supports. A broad spectrum of practical applications is discussed.
A Receptor Protein-Based Bioassay for Quantitative Determination of Paclitaxel (1997)

A novel receptor-based bioassay for the quantitative measurement of Taxol was developed. The assay was based on the well-investigated and established finding that Taxol, its active analogs, and active metabolites bind reversibly to the receptor protein tubulin, a process similar to antibody and antigen interaction. The assay was performed in a competitive format by allowing a mixture of horseradish peroxidase-labeled Taxol and Taxol in the analyte sample to compete for the Taxol binding site of a polystyrene microtiter plate wall coated with purified tubulin and subsequently measuring the tubulin-Taxol complex by determining the activity of the horseradish peroxidase label. Using this method, Taxol was measured very sensitively, linear range of 0.0001-1 nM, and selectively, without interference from non-tumor-active compounds such as baccatin III, cephalomaninne, and 10-deacetyl taxol. The method was applied for the determination of picomolar concentrations of Taxol in human plasma.
Influence of interleukin-8 (IL-8) and IL-8 receptors on the migration of human keratinocytes, the role of PLC-γ and potential clinical implications (2011)

Interleukin (IL)-8 is a pro-inflammatory cytokine that has a direct effect on immune cells, including polymorphonuclear cells. Keratinocytes are a rich source of IL-8. However, there is little knowledge on the role of IL-8 in clinical wound healing and the direct biological effect of IL-8 on keratinocytes. In this study, the effect of recombinant human IL-8 (rhIL-8) on migration and adhesion was tested using HaCaT keratinocytes as a cell model. The cell functions were evaluated using impedance cell sensing. The expression of IL-8 receptor (IL-8R) transcripts in human skin and wounds (acute and chronic) was assessed using real-time transcript analysis. rhIL-8 significantly increased the migration of keratinocytes (3.5±0.3 for cells treated with IL-8 vs. 2.7±0.6 for controls; p=0.029). It is interesting to note that treatment of keratinocytes with IL-8 resulted in a marked shift in the responsive frequencies. IL-8 only resulted in a marginal increase in cell adhesion, which was particularly noticeable at high frequencies. The PLC-γ inhibitor completely eradicated the action of IL-8 on the migration of HaCaT cells. Using real time PCR, it was found that chronic wounds had significantly lower levels of the B form of the IL-8R (IL-8RB) (p=0.045) and marginally lower levels of the A form, IL-8RA, in comparison with acute wounds. Therefore, IL-8 has a direct and profound stimulatory effect on the migration of human keratinocytes, which is likely to occur via the PLC-γ pathway. Together with a reduced level of IL-8Rs in difficult-healing wounds, IL-8 has a clear prognostic and therapeutic value in wound healing.
High-speed phase imaging by parallel phase-shifting digital holography (2011)

Parallel phase-shifting digital holography can obtain three-dimensional information of a dynamically moving object with high accuracy by using space-division multiplexing of multiple holograms required for phase-shifting interferometry. We demonstrated high-speed parallel phase-shifting digital holography and obtained images of the phase variation of air caused by a compressed gas flow sprayed from a nozzle. In particular, we found the interesting phenomenon of periodic phase distributions. Reconstructed images were obtained at frame rates of 20,000 and 180,000 frames per second.
Identification, sequence, and expression of the gene encoding gamma-glutamyltranspeptidase in Bacillus subtilis (1996)

The Bacillus subtilis gene encoding gamma-glutamyltranspeptidase (GGT) activity encodes a protein of 587 amino acids having extensive homologies with other procaryotic GGTs. Inactivation of the gene abolished all measurable GGT activity, which in the wild type was found mainly to be excreted into the medium commencing at the end of vegetative growth.
Phase III interlaboratory study of FETAX part 3. FETAX validation using 12 compounds with and without an exogenous metabolic activation system (1999)

FETAX (Frog Embryo Teratogenesis Assay-Xenopus) is a 96-h whole-embryo developmental toxicity screening assay that can be used in ecotoxicology and in detecting mammalian developmental toxicants when an in vitro metabolic activation system is employed. A standardized American Society for Testing and Materials (ASTM) guide for the conduct of FETAX has been published, along with a companion atlas that helps in embryo staging and in identifying malformations. As part of the ASTM process, an interlaboratory validation study was undertaken to evaluate the repeatability and reliability of FETAX and to evaluate the potential teratogenic hazard of 12 compounds. Three different laboratories participated in the study. All three participating laboratories had extensive experience with the assay. FETAX intralaboratory and interlaboratory variability, as judged by coefficients of variation, were very low. Potential teratogenic hazard was evaluated using two major criteria from FETAX experiments employing metabolic activation systems (MAS). These were the teratogenic index TI (TI = 96-h lc(50)/96-h ec(50) (malformation)) and the minimum concentration that inhibits growth (MCIG). A compound was considered teratogenic by this criterion when the MCIG was significantly different from controls at concentrations below the 30% level of the MAS 96-h lc(50). Based on the results of this and other studies, a decision table was constructed in order to evaluate additional studies. Severity of malformations caused, especially near the MAS 96-h ec(50) (malformation), were also evaluated. Four compounds were non-teratogenic but two compounds were clearly teratogenic. The remaining six compounds were ranked as equivocal teratogens. The results were discussed in light of the difficulty of producing an adequate decision table. FETAX proved to yield repeatable and reliable data as long as care was taken during range-finding and technicians were adequately trained. The MAS was essential in using FETAX to predict developmental hazard in mammals, and still requires further development.
Switched parasitic feeds for parabolic antenna angle diversity (1999)

The radiation direction from a parabolic dish antenna can be electronically controlled through the use of a switched parasitic element closely coupled to a dipole feed. Through the application of a dc voltage, the half-wavelength-long parasitic element is switched between open and short circuit using a p-i-n diode at its center. With a parasitic element vertically offset from the horizontal dipole, the performance of the antenna in both switch positions has been optimized. At 1.5 GHz, using a 2.4 m diameter reflector, beam skewing on the order of 1.5° at the −6 dB point can be achieved for a feed element spacing of 0.6 wavelengths. At a parasitic element spacing of 0.5 wavelengths, the main lobe is better than 15 dB above the unshifted null. The analysis of such a structure requires the calculation of the current in both the driven element and the parasitic element and the summation of their fields on the surface of the reflector independently. ©1999 John Wiley & Sons, Inc. Microwave Opt Technol Lett 23: 200–203, 1999.
The detection of large deletions or duplications in genomic DNA (2002)

While methods for the detection of point mutations and small insertions or deletions in genomic DNA are well established, the detection of larger (>100 bp) genomic duplications or deletions can be more difficult. Most mutation scanning methods use PCR as a first step, but the subsequent analyses are usually qualitative rather than quantitative. Gene dosage methods based on PCR need to be quantitative (i.e., they should report molar quantities of starting material) or semi-quantitative (i.e., they should report gene dosage relative to an internal standard). Without some sort of quantitation, heterozygous deletions and duplications may be overlooked and therefore be under-ascertained. Gene dosage methods provide the additional benefit of reporting allele drop-out in the PCR. This could impact on SNP surveys, where large-scale genotyping may miss null alleles. Here we review recent developments in techniques for the detection of this type of mutation and compare their relative strengths and weaknesses. We emphasize that comprehensive mutation analysis should include scanning for large insertions and deletions and duplications.
Oxide Nanoparticle Uptake in Human Lung Fibroblasts:  Effects of Particle Size, Agglomeration, and Diffusion at Low Concentrations (2005)

Quantitative studies on the uptake of nanoparticles into biological systems should consider simultaneous agglomeration, sedimentation, and diffusion at physiologically relevant concentrations to assess the corresponding risks of nanomaterials to human health. In this paper, the transport and uptake of industrially important cerium oxide nanoparticles, into human lung fibroblasts is measured in vitro after exposing thoroughly characterized particle suspensions to a fibroblast cell culture for particles of four separate size fractions and concentrations ranging from 100 ng g(-1) to 100 microg g(-1) of fluid (100 ppb to 100 ppm). The unexpected findings at such low but physiologically relevant concentrations reveal a strong dependence of the amount of incorporated ceria on particle size, while nanoparticle number density or total particle surface area are of minor importance. These findings can be explained on the basis of a purely physical model. The rapid formation of agglomerates in the liquid is strongly favored for small particles due to a high number density while larger ones stay mainly unagglomerated. Diffusion (size fraction 25-50 nm) or sedimentation (size fraction 250-500 nm) limits the transport of nanoparticles to the fibroblast cells. The biological uptake processes on the surface of the cell are faster than the physical transport to the cell at such low concentrations. Comparison of the colloid stability of a series of oxide nanoparticles reveals that untreated oxide suspensions rapidly agglomerate in biological fluids and allows the conclusion thatthe presented transport and uptake kinetics at low concentrations may be extended to other industrially relevant materials.
Proteoglycans as organizers of the intercellular matrix (1983)

Conference Article| December 01 1983 Proteoglycans as organizers of the intercellular matrix HELEN MUIR HELEN MUIR 1The Mathilda and Terence Kennedy Institute of Rheumatology, 6 Bute Gardens, Hammersmith, London W6 7DW, U.K. Search for other works by this author on: This Site PubMed Google Scholar Biochem Soc Trans (1983) 11 (6): 613–622. https://doi.org/10.1042/bst0110613 Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Facebook Twitter LinkedIn MailTo Cite Icon Cite Get Permissions Citation HELEN MUIR; Proteoglycans as organizers of the intercellular matrix. Biochem Soc Trans 1 December 1983; 11 (6): 613–622. doi: https://doi.org/10.1042/bst0110613 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAll JournalsBiochemical Society Transactions Search Advanced Search This content is only available as a PDF. © 1983 Biochemical Society1983 Article PDF first page preview Close Modal You do not currently have access to this content.