gebhart/patrepeval huggingface dataset:
Synthesis of high specific activity 6-[18F]fluorodopamine for positron emission tomography studies of sympathetic nervous tissue (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of high specific activity 6-[18F]fluorodopamine for positron emission tomography studies of sympathetic nervous tissueYu Shin Ding, Joanna S. Fowler, S. John Gatley, Stephen L. Dewey, Alfred P. Wolf, and David J. SchlyerCite this: J. Med. Chem. 1991, 34, 2, 861–863Publication Date (Print):February 1, 1991Publication History Published online1 May 2002Published inissue 1 February 1991https://pubs.acs.org/doi/10.1021/jm00106a055https://doi.org/10.1021/jm00106a055research-articleACS PublicationsRequest reuse permissionsArticle Views412Altmetric-Citations52LEARN 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
Binding of complement component C3b to glycoprotein C is modulated by sialic acid on herpes simplex virus type 1-infected cells (1985)

Neuraminidase treatment of cells infected with herpes simplex virus type 1 (HSV-1) markedly enhanced the binding of complement component C3b to HSV 1 glycoprotein C (gC). When HSV-1 was grown in BHK RicR14 cells in which glycoproteins had reduced amounts of N-linked complex oligosaccharides, including sialic acid, the binding of C3b to gC was markedly enhanced. We used neuraminidase treatment to demonstrate that cloning the gC gene from the HSV-1 F strain into an HSV-1 mutant which fails to express gC converted the mutant virus from C3b receptor negative to receptor positive. These results further support a role for gC as a C3b receptor and indicate that sialic acid modifies receptor activity.
Identification of an early activation antigen (Bac-1) on human B cells. (1986)

We have produced a monoclonal antibody, Bac-1, that appears to identify a novel antigen on activated human B cells. The Bac-1 antigen can be detected between 8 to 16 hr, as well as transferrin receptors (T9), after activation of small resting B cells with phorbol myristic acetate, anti-IgM antibody, Staphylococcus aureus Cowan I, or Epstein-Barr virus. The expression of the Bac-1 antigen precedes that of IL 2 receptors (Tac-1). Peak expression of the Bac-1 antigen was observed on day 3 after activation, and decreased thereafter. The Bac-1 antigen was present on a minor subpopulation of relatively large B cells isolated from blood samples, and on "preactivated" B cells of heterogeneous size isolated from spleens and tonsils. It was not detected on bone marrow pre-B cells, blood small B cells, or plasma cells, nor was it expressed by resting or activated T cells or nonlymphoid cells. Certain B cell neoplasms and B lymphoblastoid cell lines were Bac-1+, but neoplastic cells of non-B lineage were Bac-1-. With immunoperoxidase staining, Bac-1+ cells were detected predominantly in the germinal centers of tonsil sections. The Bac-1 antigen on activated B cells was destroyed by protease treatment and was enhanced by neuraminidase treatment, suggesting that the Bac-1 antibody detects a cell surface molecule via an antigenic determinant which is partially obscured by neighboring sialic acid residues. The reactivity pattern of Bac-1 differs from the patterns of cellular reactivity reported for other monoclonal antibodies with specificity for activated human B cells.
Video transcoding for fast forward/reverse video playback (2003)

Fast forward and fast reverse playbacks are two common video browsing functions provided in many analog and digital video players. They help users quickly find and access video segments of interest by scanning through the content of a video at a faster than normal playback speed. We propose a video transcoding approach to realizing fast forward and reverse video playbacks by generating a new compressed video from a pre-coded video. To reduce the computational requirements, we design and compare several fast algorithms for estimating the motion vectors required in transcoded video. To accommodate changes due to frame skipping for fast video playback, we also alter the group-of-pictures structure of transcoded video. In addition, subjective tests are conducted to assess the minimum video peak-signal-to-noise-ratio degradation that is perceptible to viewers at different fast playback speeds. To this end, we obtain an adaptive video transcoding method, which combines intra-coding and inter-coding with a fast motion vector reestimation method to strike a good balance between computational complexity and transcoded video quality. Experimental results are reported to show the efficacy of the proposed method.
A gene hypermethylation profile of human cancer. (2001)

We are in an era where the potential exists for deriving comprehensive profiles of DNA alterations characterizing each form of human cancer. Such profiles would provide invaluable insight into mechanisms underlying the evolution of each tumor type and will provide molecular markers, which could radically improve cancer detection. To date, no one type of DNA change has been defined which accomplishes this purpose. Herein, by using a candidate gene approach, we show that one category of DNA alteration, aberrant methylation of gene promoter regions, can enormously contribute to the above goals. We have now analyzed a series of promoter hypermethylation changes in 12 genes (p16(INK4a), p15(INK4b), p14(ARF), p73, APC,(5) BRCA1, hMLH1, GSTP1, MGMT, CDH1, TIMP3, and DAPK), each rigorously characterized for association with abnormal gene silencing in cancer, in DNA from over 600 primary tumor samples representing 15 major tumor types. The genes play known important roles in processes encompassing tumor suppression, cell cycle regulation, apoptosis, DNA repair, and metastastic potential. A unique profile of promoter hypermethylation exists for each human cancer in which some gene changes are shared and others are cancer-type specific. The hypermethylation of the genes occurs independently to the extent that a panel of three to four markers defines an abnormality in 70-90% of each cancer type. Our results provide an unusual view of the pervasiveness of DNA alterations, in this case an epigenetic change, in human cancer and a powerful set of markers to outline the disruption of critical pathways in tumorigenesis and for derivation of sensitive molecular detection strategies for virtually every human tumor type.
Bispecific Antibody Derivatives Based on Full-Length IgG Formats (2012)

Monoclonal antibodies have emerged as an effective therapeutic modality, and numerous antibodies have been approved for the treatment of several severe diseases or are currently in clinical development. To improve their therapeutic potential, monoclonal antibodies are constantly evolved by protein engineering. Particularly, the generation of bispecific antibodies raised special interest because of their ability to bind two different antigens at the same time, and the efficiency of these formats has been demonstrated in several clinical and preclinical studies. Up to now, the major drawbacks in using bispecific antibodies as a therapeutic agent have been difficult design and low-yield expression of homogeneous antibody populations. However, major technological improvements were made in protein engineering during the last years. This allows the design of several new IgG-based bispecific antibody formats that can be prepared in high yields and high homogeneity using conventional expression and purification techniques. Especially, recent development of IgG-fusions with disulfide-stabilized Fv fragments and of CrossMab-technologies facilitates the generation of bispecific antibodies with IgG-like architectures. Here we describe design principles and methods to express and purify different bispecific antibody formats derived from full-length IgGs.
Potential Impact of Conjugate Pneumococcal Vaccines on Pediatric Pneumococcal Diseases (2004)

Children younger than age 2 years have the highest rates of invasive pneumococcal disease and play an important role in its transmission. In the United States, seven pneumococcal serotypes cause approximately 80% of invasive disease and represent approximately 60% of middle-ear isolates in children younger than age 2 years; the majority of penicillin-resistant strains are confined to these same few serogroups. Although unconjugated polysaccharide pneumococcal vaccines have demonstrated effectiveness in preventing invasive disease in adults, these vaccines fail to protect against otitis media or nasopharyngeal carriage and are poorly immunogenic in children younger than age 2 years. A new generation of pneumococcal vaccines has been developed, linking the capsular polysaccharide of seven to 11 serotypes to a protein carrier. The only pneumococcal vaccine approved to date for children younger than age 2 years is a seven-valent conjugate vaccine (PnCRM-7) (Prevnar; Wyeth Vaccines, Pearl River, New York), which contains serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F. PnCRM-7 is more immunogenic than the polysaccharide pneumococcal vaccines and is 80-100% effective against vaccine-type invasive disease and 50-60% effective against vaccine-type pneumococcal otitis media. Routine immunization with pneumococcal conjugate vaccines should substantially reduce the morbidity, mortality, and costs associated with pneumococcal disease in children.
Mutation detection by fluorescent chemical cleavage: application to hemophilia B. (1994)

Chemical mismatch detection when combined with PCR or RT-PCR amplification represents one of the most efficient mutation screening methods. This procedure has been used for the analysis of both large populations of mutants and large and complex genes because it detects and locates virtually all sequence variations in segments of DNA of up to 1.7 kb cleaving at, and/or adjacent to, mismatches in heteroduplexes formed by target and probe DNA. By using fluorescent tags and an automatic gel scanning system, the efficiency of the method has been increased fourfold with gains also in the safety and quality control of probes and in the flexibility of the procedure. Using 12 hemophilia B patients, 8 with known mutations and 4 chosen at random, we show how the chemical mismatch cleavage of up to four DNA segments can be multiplexed and examined in a single gel lane and how the increase in efficiency thus obtained can be used either totally to maximize the DNA screened per lane or partly to locate the mutation unequivocally so that only one sequencing reaction is needed to characterize it fully.
Periodic ethylene-vinyl alcohol copolymers via ADMET polymerization: Synthesis, characterization, and thermal property (2013)

Periodic copolymers of ethylene and vinyl alcohol (EVA) were synthesized via acyclic diene metathesis (ADMET) polymerization of a series of structurally symmetric α,ω-diene monomers that containing two vinyl acetate (VAc) units, followed by exhaustive hydrogenation and subsequent hydrolysis. This synthetic methodology provided a new type of EVA copolymer with defined sequence and ever highest VA content via ADMET. These polymer samples were characterized by gel permeation chromatography (GPC), NMR, and matrix-assisted laser desorption/ionization time-of-fight mass spectroscopy (MALDI-TOF-MS). Thermal properties of EVAc and EVA copolymers were investigated by thermal gravimetric analysis (TGA) and differential scanning calorimetry (DSC). EVAc copolymers exhibited two-stage decompositions on TGA traces and displayed a glass transition on DSC thermograms. Meanwhile, the EVA copolymers showed glass transition stages and sharp melting peaks on DSC thermograms, with the Tm values being comparable to that of high density polyethylene (HDPE).
Noninvasive Glucose Monitoring of the Aqueous Humor of the Eye: Part II. Animal Studies and the Scleral Lens (1982)

We have discussed the nature of a scleral lens that will allow us to follow changes in aqueous humor glucose levels in animals by a method based on optical rotation and a technique described in an earlier paper. We have shown how this lens can be micro-miniaturized and can be used in humans as a non-invasive glucose monitor. We have described preliminary experiments designed to show the correlation between the blood glucose assay (BGA) and the aqueous humor glucose concentration as determined by chemical assay (AGA) and by optical rotation determination (ARD). The last mentioned has been obtained by paracentesis directly into a microcell used in conjunction with instrumentation capable of measuring optical rotations as low as 0.0013 degrees (4.5") corresponding to 20 mg/dl glucose with a sensitivity of 0.0001 degrees (0.36"). The variability among normal rabbits as a function of individuality and diurnal changes is described, and the correlation between AGA and ARD shown to be essentially 1.0. Such rabbits are examined when undergoing very rapid decreases in BGA (insulin treatment) or very rapid increases in BGA (bolus of glucose). The AGA and ARD are shown to lag behind the BGA, and this is discussed in terms of the rate of change of BGA with respect to time and its concomitant change in AGA/ARD as well as a simple procedure that would materially reduce this lag.
Antibiotic Prescribing for Children With Nasopharyngitis (Common Colds), Upper Respiratory Infections, and Bronchitis Who Have Health-Professional Parents (2005)

This finding supports our hypothesis that better parental education does help to reduce the frequency of injudicious antibiotic prescribing. Medical knowledge alone, however, may not fully reduce the overuse of antibiotics. Physician-parents, the expected medically savvy parents, can serve as a benchmark for the improvement potentially achievable in Taiwan through a combination of educational, regulatory, communication, and policy efforts targeted at more appropriate antibiotic prescribing in ambulatory settings.
Molecular Determinants of Cardiac Ca2+ Channel Pharmacology (1995)

Cardiac L-type Ca2+ channels are multisubunit complexes composed of alpha 1C, alpha 2 delta, and beta 2 subunits. We tested the roles of these subunits in forming a functional complex by characterizing the effects of subunit composition on dihydropyridine binding, its allosteric regulation, and the ability of dihydropyridines to inhibit channel activity. Transfection of COS.M6 cells with cardiac alpha 1C-a (alpha 1) led to the appearance of dihydropyridine ([3H]PN200-110) binding which was increased by coexpression of cardiac beta 2a (beta), alpha 2 delta a (alpha 2), and the skeletal muscle gamma. Maximum binding was achieved when cells expressed alpha 1, beta, and alpha 2. Cells transfected with alpha 1 and beta had a binding affinity that was 5-10-fold lower than that observed in cardiac membranes. Coexpression of alpha 2 normalized this affinity. (-)-D600 and diltiazem both partially inhibited PN200-100 binding to cardiac microsomes, but stimulated binding in cells transfected with alpha 1 and beta. Again, coexpression of alpha 2 normalized this allosteric regulation. Therefore coexpression of alpha 1 beta and alpha 2 completely reconstituted high affinity dihydropyridine binding and its allosteric regulation as observed in cardiac membranes. Skeletal muscle gamma was not required for this reconstitution. Expression in Xenopus oocytes demonstrated that coexpression of alpha 2 with alpha 1 beta increased the potency and maximum extent of block of Ca2+ channel currents by nisoldipine, a dihydropyridine Ca2+ channel antagonist. Our results demonstrate that alpha 2 subunits are essential components of the cardiac L-type Ca2+ channel and predict a minimum subunit composition of alpha 1C beta 2 alpha 2 delta for this channel.
Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3 (2004)

Present studies show that LBH589, a novel cinnamic hydroxamic acid analog histone deacetylase inhibitor, induces acetylation of histone H3 and H4 and of heat shock protein 90 (hsp90), increases p21 levels, as well as induces cell-cycle G(1) phase accumulation and apoptosis of the human chronic myeloid leukemia blast crisis (CML-BC) K562 cells and acute leukemia MV4-11 cells with the activating length mutation of FLT-3. In MV4-11 cells, this was associated with marked attenuation of the protein levels of p-FLT-3, FLT-3, p-AKT, and p-ERK1/2. In K562 cells, exposure to LBH589 attenuated Bcr-Abl, p-AKT, and p-ERK1/2. Treatment with LBH589 inhibited the DNA binding activity of signal transducers and activators of transcription 5 (STAT5) in both K562 and MV4-11 cells. The hsp90 inhibitor 17-allyl-amino-demethoxy geldanamycin (17-AAG) also induced polyubiquitylation and proteasomal degradation of FLT-3 and Bcr-Abl by reducing their chaperone association with hsp90. Cotreatment with LBH589 and 17-AAG exerted synergistic apoptosis of MV4-11 and K562 cells. In the imatinib mesylate (IM)-refractory leukemia cells expressing Bcr-Abl with the T315I mutation, treatment with the combination attenuated the levels of the mutant Bcr-Abl and induced apoptosis. Finally, cotreatment with LBH589 and 17-AAG also induced more apoptosis of IM-resistant primary CML-BC and acute myeloid leukemia (AML) cells (with activating mutation of FLT-3) than treatment with either agent alone.
DNA SENSORS (2002)

ABSTRACT A review of DNA sensors is presented. Firstly, the history and the applications of DNA sensors are explained. Next, the different probes and immobilisation are reviewed, and their advantages and disadvantages are contrasted. Different methods for the immobilisation characterisation and the hybridisation detection are presented. Finally, sample and signal amplification strategies are mentioned.
The Factor IXa Heparin-Binding Exosite Is a Cofactor Interactive Site:  Mechanism for Antithrombin-Independent Inhibition of Intrinsic Tenase by Heparin (2005)

Therapeutic heparin concentrations selectively inhibit the intrinsic tenase complex in an antithrombin-independent manner. To define the molecular target and mechanism for this inhibition, recombinant human factor IXa with alanine substituted for solvent-exposed basic residues (H92, R170, R233, K241) in the protease domain was characterized with regard to enzymatic activity, heparin affinity, and inhibition by low molecular weight heparin (LMWH). These mutations only had modest effects on chromogenic substrate hydrolysis and the kinetics of factor X activation by factor IXa. Likewise, factor IXa H92A and K241A showed factor IXa-factor VIIIa affinity similar to factor IXa wild type (WT). In contrast, factor IXa R170A demonstrated a 4-fold increase in apparent factor IXa-factor VIIIa affinity and dramatically increased coagulant activity relative to factor IXa WT. Factor IXa R233A demonstrated a 2.5-fold decrease in cofactor affinity and reduced ability to stabilize cofactor half-life relative to wild type, suggesting that interaction with the factor VIIIa A2 domain was disrupted. Markedly (R233A) or moderately (H92A, R170A, K241A) reduced binding to immobilized LMWH was observed for the mutant proteases. Solution competition demonstrated that the EC(50) for LMWH was increased less than 2-fold for factor IXa H92A and K241A but over 3.5-fold for factor IXa R170A, indicating that relative heparin affinity was WT > H92A/K241A > R170A >> R233A. Kinetic analysis of intrinsic tenase inhibition demonstrated that relative affinity for LMWH was WT > K241A > H92A > R170A >> R233A, correlating with heparin affinity. Thus, LMWH inhibits intrinsic tenase by interacting with the heparin-binding exosite in the factor IXa protease domain, which disrupts interaction with the factor VIIIa A2 domain.
Reversion of the P-glycoprotein-mediated multidrug resistance of cancer cells by FK-506 derivatives (1993)

FK-506 is a resistance-modulating agent (RMA) for tumor cells whose multidrug resistance (MDR) involves a P-glycoprotein (Pgp)-mediated anti-cancer drug efflux. The family of FK-506 relatives and derivatives includes analogs which display a whole range of chemosensitizing strengths, from no detectable RMA activity to a complete reversion of the MDR phenotype. Similarly, FK-506 analogs display a whole range of immunosuppressive activities, including inactive ones. FK-506 was compared for RMA activity with 11 FK-506 analogs which were at least 20-fold less active than FK-506 for the inhibition of the bi-directional mixed lymphocyte reaction displayed the whole range of RMA activity. One such strong RMA derivative of FK-506 (SDZ 280-629) was further shown able to restore completely daunomycin retention by highly resistant MDR P388 tumor cells.
Preparation of hydroxyalkyl-substituted nicotinoids (1986)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPreparation of hydroxyalkyl-substituted nicotinoidsJeffrey I. Seeman, Charles G. Chavdarian, Henry V. Secor, and T. S. OsdeneCite this: J. Org. Chem. 1986, 51, 9, 1548–1551Publication Date (Print):May 1, 1986Publication History Published online1 May 2002Published inissue 1 May 1986https://pubs.acs.org/doi/10.1021/jo00359a032https://doi.org/10.1021/jo00359a032research-articleACS PublicationsRequest reuse permissionsArticle Views254Altmetric-Citations9LEARN 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