gebhart/patrepeval huggingface dataset:
Synthesis and evaluation of a new fluorine‐18 labeled rotenoid as a potential PET probe of mitochondrial complex I activity (1999)

Fluorine-18 labeled (6aS, 12aS, 5′R)-12-deoxo-6′,7′-dihydro-7′-fluororotenone (F-DDRT), a new potential PET probe of mitochondrial complex I activity, was synthesized. [18F]-DDRT was prepared with good specific activity by nucleophilic displacement with an overall radiochemical yield of 25% (EOB). The uptake of [18F]-DHRT in rat brain and heart was compared with the uptake of another fluorine-18 labeled rotenoid: [18F]-DHRT. In comparison to [18F]-DHRT, the brain and heart retention of [18F]-DDRT were both lower at any point of the study (respectively 0.49 and 2.82 dose/g vs 0.34 and 1.24% dose/g at 60 min post injection). Copyright © 1999 John Wiley & Sons, Ltd.
Tumor Targeting of Radiometal Labeled Anti-CEA Recombinant T84.66 Diabody and T84.66 Minibody:  Comparison to Radioiodinated Fragments (2001)

Recombinant antibody fragments offer potential advantages over intact monoclonal antibodies in the radioimmunoscintigraphy (RIS) of solid tumors. Due to their smaller molecular size, antibody fragments have shown rapid tumor targeting and blood clearance, a more uniform tumor distribution and a lower potential to elicit a human immune response. Previously, we have expressed two genetically engineered antibody fragments, the T84.66 diabody (scFv dimer) and the T84.66 minibody (scFv-CH3 dimer), specific to carcinoembryonic antigen (CEA). When radioiodinated, both antibody fragments exhibited rapid tumor targeting and rapid blood clearance in xenografted mice. To extend and optimize their future clinical RIS utility with radiometals, these antibody fragments were conjugated with the macrocycle 1,4,7,10-tetraazacyclododecane N,N',N' ',N' "-tetraacetic acid (DOTA) and labeled with 111In. Tumor targeting and biodistribution studies were carried out in athymic mice xenografted with a human colorectal tumor cell line, LS174T. The [111In]T84.66 diabody (55 kDa) exhibited very rapid tumor targeting with 12.5 +/- 0.4% injected dose per gram (% ID g(-1) +/- standard error) at 2 h and reached a maximum of 13.3 +/- 0.9% ID g(-1) at 6 h. However, kidney uptake was observed to reached a peak of 183.5 +/- 21.0% ID g(-1) at 6 h, a result similar to that reported by others for other low molecular weight fragments labeled with radiometals. Preadministration of an oral dose of D-lysine resulted in a 59% lowering of the renal accumulation at 6 h, but was accompanied by a 31% reduction of tumor uptake to 9.2 +/- 1.2% ID g(-1). The second recombinant antibody fragment, the [111In]T84.66 minibody (80 kDa), displayed rapid tumor targeting of 14.2 +/- 6.1% ID g(-1) at 2 h, and reached a maximum activity of 24.5 +/- 6.1% ID g(-1) by 12 h. Renal uptake achieved a plateau of 12-13% ID g(-1) which cleared to 7.2% ID g(-1) at 72 h. However, hepatic uptake was elevated and reached a maximum of 26.0 +/- 1.0% ID g(-1) at 12 h in these xenograft-bearing mice. Experiments in nontumor bearing mice showed a reduction of hepatic activity at 12 h to 16.6 +/- 1.5% ID g(-1), indicative of an intrinsic hepatic accumulation of the [111In]DOTA-T84.66 minibody or metabolites. While the anti-CEA [111In]DOTA-T84.66 diabody and T84.66 minibody retain the rapid tumor targeting properties of the radioiodinated form, the normal organ accumulation (kidneys and liver, respectively) of the [111In]DOTA forms appeared problematic for RIS and RIT applications. Development of alternative blocking strategies or new metabolizable chelates are under investigation to enhance the utility of the radiometal form of these and other promising recombinant antibody fragments.
Comparative Photophysics of [26]- and [28]Hexaphyrins(1.1.1.1.1.1):  Large Two-Photon Absorption Cross Section of Aromatic [26]Hexaphyrins(1.1.1.1.1.1) (2005)

We have explored the electronic natures of representative expanded porphyrins, [26]- and [28]hexaphyrins, to investigate the interplay between the aromaticity and antiaromaticity that is brought by two electron oxidation/reduction processes. The excited singlet and triplet states of [26]hexaphyrin in solution exhibit lifetimes of 125 ps and 1.8 mus, respectively, as revealed by various time-resolved spectroscopic measurements. On the other hand, [28]hexaphyrin shows faster singlet and triplet lifetimes than those of [26]hexaphyrin, which is largely in accordance with the perturbation of aromaticity due to the pi electron formulation of [4n] in [28]hexaphyrins. The two-photon absorption cross-section values at 1200 nm for [26]hexaphyrins show ca. 9890 GM which is >10(2) larger than those of porphyrins. The reduced TPA values of 2600 and 810 GM of [28]hexaphyrin and perfluorinated [28]hexaphyrin, respectively, match well with their relatively short excited-state lifetimes. Overall, the enhanced excited-state lifetimes for various hexaphyrins go in line with the increased TPA cross-section values and the ring planarity.
An empirical correction for absorption anisotropy (1995)

A least-squares procedure is described for modeling an empirical transmission surface as sampled by multiple symmetry-equivalent and/or azimuth rotation-equivalent intensity measurements. The fitting functions are sums of real spherical harmonic functions of even order, ylm(-u0) + ylm(u1), 2 < or = l = 2n < or = 8. The arguments of the functions are the components of unit direction vectors, -u0 for the reverse incident beam and u1 for the scattered beam, referred to crystal-fixed Cartesian axes. The procedure has been checked by calculations against standard absorption test data.
Expression of a preproinsulin-beta-galactosidase gene fusion in mammalian cells. (1983)

As an approach to the study of mammalian gene expression, the promoters and translation initiation regions of the rat preproinsulin II and the simian virus 40 early genes were fused to the structural gene of Escherichia coli beta-galactosidase, a sensitive probe for gene expression. These fusions were introduced into COS-7 cells, a simian virus 40 large tumor-antigen-producing monkey kidney cell line, where they directed the synthesis of enzymatically active hybrid beta-galactosidase proteins. Conditions for transfection were varied to optimize the expression of beta-galactosidase activity in the transfected cells. The pH optimum of this activity was found to be 7.0, the same as that of native E. coli beta-galactosidase and distinct from the major lysosomal "acid" beta-galactosidase. The fused preproinsulin-beta-galactosidase was further characterized by gel electrophoresis of nondenatured cell extracts stained by a fluorogenic substrate and by immunoprecipitation and gel electrophoresis of 3H-labeled cell proteins. These results all indicate that fully active tetrameric beta-galactosidase hybrids can be produced in mammalian cells. The expression of preproinsulin-beta-galactosidase activity was measured in the presence of high glucose, insulin, dexamethasone, or epidermal growth factor but no regulatory changes were observed.
Taxol: A Unique Antineoplastic Agent with Significant Activity in Advanced Ovarian Epithelial Neoplasms (1989)

Study Objective: To assess the activity of taxol in patients with advanced, progressive, and drug-refractory ovarian cancer and to delineate more clearly the toxicity of taxol in this patient population. Design: Nonrandomized, prospective phase II trial. Patients: Forty-seven patients with drug-refractory epithelial ovarian cancer who had one or more lesions measurable in perpendicular diameters. Of these patients, 45 were evaluable for toxicity and 40 were evaluable for response. Interventions: Patients were treated every 22 days with varying doses of taxol (110 to 250 mg/m2 body surface) given as a 24-hour infusion with subsequent doses based on adverse effects. A premedication regimen was used to avoid acute hypersensitivity reactions. Measurements and Main Results: Twelve patients (30%; CI, 16% to 44%) responded to taxol for periods lasting from 3 to 15 months. The dose-limiting toxicity was myelosuppression with leukocytes affected more severely and commonly than thrombocytes or reticulocytes. Leukopenia was usually brief in duration but was associated with sepsis in 3 cases (2 fatal). Other adverse effects included myalgias, arthralgias, alopecia, diarrhea, nausea, vomiting, mucositis, and peripheral neuropathy. Rare cases of cardiac and central neurotoxicity were also noted. Conclusions: Taxol is an active agent in drug-refractory ovarian cancer and deserves further study in combination with other active drugs in previously untreated patients with advanced ovarian cancer.
Surface Properties of Heat‐Induced Soluble Soy Protein Aggregates of Different Molecular Masses (2015)

Suspensions (2% and 5%, w/v) of soy protein isolate (SPI) were heated at 80, 90, or 100 °C for different time periods to produce soluble aggregates of different molecular sizes to investigate the relationship between particle size and surface properties (emulsions and foams). Soluble aggregates generated in these model systems were characterized by gel permeation chromatography and sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Heat treatment increased surface hydrophobicity, induced SPI aggregation via hydrophobic interaction and disulfide bonds, and formed soluble aggregates of different sizes. Heating of 5% SPI always promoted large-size aggregate (LA; >1000 kDa) formation irrespective of temperature, whereas the aggregate size distribution in 2% SPI was temperature dependent: the LA fraction progressively rose with temperature (80→90→100 °C), corresponding to the attenuation of medium-size aggregates (MA; 670 to 1000 kDa) initially abundant at 80 °C. Heated SPI with abundant LA (>50%) promoted foam stability. LA also exhibited excellent emulsifying activity and stabilized emulsions by promoting the formation of small oil droplets covered with a thick interfacial protein layer. However, despite a similar influence on emulsion stability, MA enhanced foaming capacity but were less capable of stabilizing emulsions than LA. The functionality variation between heated SPI samples is clearly related to the distribution of aggregates that differ in molecular size and surface activity. The findings may encourage further research to develop functional SPI aggregates for various commercial applications.
Molecular Identification and Characterization of a Family of Kinases with Homology to Ca2+/Calmodulin-dependent Protein Kinases I/IV (2006)

Despite the critical importance of Ca(2+)/calmodulin (CaM)-dependent protein kinase (CaMK) II signaling in neuroplasticity, only a limited amount of work has so far been available regarding the presence and significance of another predominant CaMK subfamily, the CaMKI/CaMKIV family, in the central nervous system. We here searched for kinases with a core catalytic structure similar to CaMKI and CaMKIV. We isolated full-length cDNAs encoding three mouse CaMKI/CaMKIV-related kinases, CLICK-I (CL1)/doublecortin and CaM kinase-Like (DCAMKL)1, CLICK-II (CL2)/DCAMKL2, and CLICK-I,II-related (CLr)/DCAMKL3, the kinase domains of which had an intermediate homology not only to CaMKI/CaMKIV but also to CaMKII. Furthermore, CL1, CL2, and CLr were highly expressed in the central nervous system, in a neuron-specific fashion. CL1alpha and CL1beta were shorter isoforms of DCAMKL1, which lacked the doublecortin-like domain (Dx). In contrast, CL2alpha and CL2beta contained a full N-terminal Dx, whereas CLr only possessed a partial and dysfunctional Dx. Interestingly, despite a large similarity in the kinase domain, CL1/CL2/CLr had an impact on CRE-dependent gene expression distinct from that of the related CaMKI/CaMKIV and CaMKII. Although these were previously shown to activate Ca(2+)/cAMP-response element-binding protein (CREB)-dependent transcription, we here show that CL1 and CL2 were unable to significantly phosphorylate CREB Ser-133 and rather inhibited CRE-dependent gene expression by a dominant mechanism that bypassed CREB and was mediated by phosphorylated TORC2.
Oligonucleotides Complementary to the Oxytricha nova Telomerase RNA Delineate the Template Domain and Uncover a Novel Mode of Primer Utilization (1994)

The telomerase reverse transcriptase uses an essential RNA subunit as a template to direct telomeric DNA synthesis. The 190-nucleotide Oxytricha nova telomerase RNA was identified by using an oligonucleotide probe complementary to the predicted CCCCAAAA template. This RNA displays extensive sequence similarity to the Euplotes crassus telomerase RNA and carries the same 5' CAAAACCCCAAAACC 3' telomeric domain. Antisense oligonucleotides were used to map the boundaries of the functional template and to investigate the mechanism of primer recognition and elongation. On the basis of their ability to inhibit or to prime telomerase, oligonucleotides were classified into three categories. Category 1 oligonucleotides, which extended 5' of residue 42 in the RNA, abolished elongation of (T4G4)3 and (G4T4)3 primers in vitro. In contrast, oligonucleotides terminating between residues 42 and 50 (categories 2 and 3), served as efficient telomerase primers. We conclude that the O. nova template comprises residues 42 to 50 in the 190-nucleotide RNA, a different set of nucleotides than are used by the E. crassus enzyme. Category 2 primer reactions amassed short products, and their abundance could be decreased by altering the 5' sequence of the primer, consistent with the two-primer-binding-site model for telomerase. Category 3 primers generated a bimodal distribution of short and long products, each having a unique elongation profile. The long-product profile is inconsistent with sequence-specific primer alignment. Rather, each primer was extended by the same register of TTTTGGGG repeats, suggesting shuttling to a default position within the template. The parallels between telomerase and RNA polymerase elongation mechanisms are discussed.
Lithiation of cyclopropylcarbinols (1979)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTLithiation of cyclopropylcarbinolsG. W. Klumpp, M. Kool, M. Schakel, R. F. Schmitz, and C. BoutkanCite this: J. Am. Chem. Soc. 1979, 101, 23, 7065–7066Publication Date (Print):November 1, 1979Publication History Published online1 May 2002Published inissue 1 November 1979https://pubs.acs.org/doi/10.1021/ja00517a048https://doi.org/10.1021/ja00517a048research-articleACS PublicationsRequest reuse permissionsArticle Views130Altmetric-Citations26LEARN 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
BENEFIT-COST ASSESSMENT OF THE UTILITY OF ROAD WEATHER INFORMATION SYSTEMS FOR SNOW AND ICE CONTROL (1992)

In 1988, the Strategic Highway Research Program initiated a project to look at the potential effectiveness of road weather information system technologies for improving and reducing costs of highway snow and ice control. These technologies include pavement and meteorological sensors, pavement and weather condition forecasts, roadway thermography, and the communications, both human and electronic, required for effective dissemination of the information. The investigation required the performance of a benefit-cost analysis of road technologies. The benefit-cost assessment is complex because it has to take into account variations in the distribution of weather events and road conditions, as well as snow and ice control practices, in different regions of the country. Described in this paper is the statistical model used to perform the benefit-cost assessment, to include the one-, two-, and three-dimensional matrices that form the basis for computing costs. Benefits are the reductions in snow and ice control costs resulting from the use of the weather information technologies. Finally, presented in the paper are the results obtained from running the model. Model results show that the use of weather technologies can be cost-effective when decisions become proactive with the use of weather information. The model shows that detailed forecasts of road conditions provide the greatest benefit-cost ratio; however, the combination of forecasts, sensors, and road thermography synergistically provides improved level of service for snow and ice control, a significant reduction in decision errors, as well as a benefit-cost ratio greater than one.
Purification and Lipid Dependence of the Recombinant Hyaluronan Synthases from Streptococcus pyogenes andStreptococcus equisimilis (1999)

The two hyaluronan synthases (HASs) from Streptococcus pyogenes (spHAS) and Streptococcus equisimilis (seHAS) were expressed in Escherichia coli as recombinant proteins containing His6 tails. Both enzymes were expressed as major membrane proteins, accounting for approximately 5-8% of the total membrane protein. Using nickel chelate affinity chromatography, the HASs were purified to homogeneity from n-dodecyl beta-D-maltoside extracts. High levels of HAS activity could be achieved only if the purified enzymes were supplemented with either bovine or E. coli cardiolipin (CL), although bovine CL gave consistently greater activity. Mass spectroscopic analysis revealed that the fatty acid compositions of these two CL preparations did not overlap. The two HAS enzymes showed similar but distinct activation profiles with the 10 other lipids tested. For example, phosphatidic acid and phosphatidylethanolamine stimulated seHAS, but not spHAS. Phosphatidylserine stimulated both enzymes. spHAS appears to be more CL-specific than seHAS, although both purified enzymes still contain endogenous CL that can not easily be removed. Both seHAS and spHAS were inhibited by phosphatidylcholine, sphingomyelin, and sulfatides and were not substantially stimulated by cerebrosides, phosphatidylglycerol, or phosphatidylinositol. With both HASs, CL increased the Km for UDP-GlcUA, but decreased the Km for UDP-GlcNAc and gave an overall stimulation of Vmax. A kinetic characterization of the two membrane-bound and purified HASs is presented in the accompanying paper (Tlapak-Simmons, V. L., Baggenstoss, B. A., Kumari, K., Heldermon, C., and Weigel, P. H. (1999) J. Biol. Chem. 274, 4246-4253). Both purified HASs became inactive after storage for approximately 5 days at 4 degreesC. Both purified enzymes also lost activity over 4-5 days when stored at -80 degreesC in the presence of CL, but reached a level of activity that then slowly decreased over a period of months. Although the purified enzymes stored in the absence of CL at -80 degreesC were much less active, the enzymes retained this same low level of activity for at least 5 weeks. When both spHAS and seHAS were stored without CL at -80 degreesC, even after 2 months, they could be stimulated by the addition of bovine CL to approximately 60% of the initial activity of the freshly purified enzyme.
Synthesis and anti-tumour activity of topologically-related analogues of flavoneacetic acid. (1989)

A number of structural analogues of the solid tumour active drug flavoneacetic acid have been prepared and evaluated for in vivo activity against colon 38 adenocarcinoma, in order to extend the limited structure-activity relationships available for compounds with this type of activity. Apart from the fused ring analogue xanthenone-4-acetic acid, structural and electronic modifications of the nucleus led to inactive compounds, suggesting the existence of quite narrow structure-activity relationships.
High-Efficiency Transduction and Long-Term Gene Expression with a Murine Stem Cell Retroviral Vector Encoding the Green Fluorescent Protein in Human Marrow Stromal Cells (1999)

Bone marrow stromal cells (MSCs) are unique mesenchymal cells that have been utilized as vehicles for the delivery of therapeutic proteins in gene therapy protocols. However, there are several unresolved issues regarding their potential therapeutic applications. These include low transduction efficiency, attenuation of transgene expression, and the technical problems associated with drug-based selection markers. To address these issues, we have developed a transduction protocol that yields high-level gene transfer into human MSCs, employing a murine stem cell virus-based bicistronic vector containing the green fluorescent protein (GFP) gene as a selectable marker. Transduction of MSCs plated at low density for 6 hr per day for 3 days with high-titer viral supernatant resulted in a gene transfer efficiency of 80+/-6% (n = 10) as measured by GFP fluorescence. Neither centrifugation nor phosphate depletion increased transduction efficiency. Assessment of amphotropic receptor (Pit-2) expression by RT-PCR demonstrated that all MSCs expressing the receptor were successfully transduced. Cell cycle distribution profiles measured by propidium iodide staining showed no correlation with the susceptibility of MSCs to transduction by the retroviral vector. Human MSCs sequentially transduced with an adenoviral vector encoding the ecotropic receptor and ecotropic retroviral vector encoding GFP demonstrated that all MSCs are susceptible to retroviral transduction. We further showed that both genes of bicistronic vector are expressed for at least 6 months in vitro and that transgene expression did not affect the growth or osteogenic differentiation potential of MSCs. Future studies will be directed toward the development of gene therapy protocols employing this strategy.
A data-driven reflectance model (2003)

We present a generative model for isotropic bidirectional reflectance distribution functions (BRDFs) based on acquired reflectance data. Instead of using analytical reflectance models, we represent each BRDF as a dense set of measurements. This allows us to interpolate and extrapolate in the space of acquired BRDFs to create new BRDFs. We treat each acquired BRDF as a single high-dimensional vector taken from a space of all possible BRDFs. We apply both linear (subspace) and non-linear (manifold) dimensionality reduction tools in an effort to discover a lower-dimensional representation that characterizes our measurements. We let users define perceptually meaningful parametrization directions to navigate in the reduced-dimension BRDF space. On the low-dimensional manifold, movement along these directions produces novel but valid BRDFs.
Angular distribution of sputtered atoms from polycrystalline metal targets (1981)

Angular distribution of sputtered atoms from polycrystalline metal targets with crystallographic-preferred orientation was measured for 0.5- and 1.0-keV Ar+ ions at incidence angles of 0° and 45°. The distribution was compared with that for a Si (100) single-crystal target. Atoms sputtered from Au, Pt, Al, and NiFe targets are ejected preferentially in the directions of their close packing in the lattice. For the Si target, the distribution is under cosine. These results are explained in terms of the target-surface crystal structure during and after ion bombardment. The surface structure for the metal targets remains essentially unchanged, but not for the Si target. Sputtered-atom ejection along the target normally increases with increasing incident-ion energy. Even at oblique incidence, heavy-target atoms such as Au, appear to have preferentially ejected atoms in the close-packed directions.