gebhart/patrepeval huggingface dataset:
Sulfanilamide Derivatives. I (1939)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSulfanilamide Derivatives. IRoger. Adams, P. H. Long, and A. J. JohansonCite this: J. Am. Chem. Soc. 1939, 61, 9, 2342–2346Publication Date (Print):September 1, 1939Publication History Published online1 May 2002Published inissue 1 September 1939https://pubs.acs.org/doi/10.1021/ja01878a022https://doi.org/10.1021/ja01878a022research-articleACS PublicationsRequest reuse permissionsArticle Views428Altmetric-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
Intramitochondrial dyes allow selective in vitro photolysis of carcinoma cells. (1986)

Carcinoma cell mitochondria preferentially accumulate and retain certain cationic dyes to a much greater extent than most normal cells. Thus, they can potentially serve as targets for highly selective photochemotherapy. We evaluated 10 rhodamine and cyanine dyes as carcinoma-specific mitochondrial photosensitizers in vitro. The most effective, N,N'-bis(2-ethyl-1,3-dioxolane)kryptocyanine (EDKC), caused marked, light-dependent killing of human bladder, squamous, and colon carcinoma cell lines after 30-min incubations at 1-0.01 microM but was minimally toxic to human keratinocytes and to normal monkey kidney epithelial cells (CV-1). Carcinoma cell phototoxicity was proportional to the amount of dye incorporated by the different cell lines. Selective killing ratios were 70-1000 for 0.1 microM dye and light doses of 100-175 J/cm2 between 680 and 720 nm.
Human T cell activation. I. Monocyte-independent activation and proliferation induced by anti-T3 monoclonal antibodies in the presence of tumor promoter 12-o-tetradecanoyl phorbol-13 acetate. (1985)

Three monoclonal antibodies (mAb), of IgG1, IgG2a, and IgM isotypes, raised against the T3 complex, were used to probe the activation of human T cells. The IgM antibody 235 was not mitogenic for peripheral blood mononuclear cells (PMC). It efficiently blocked the proliferation of PMC induced by T cell mitogens, alloantigens, and soluble antigens. The other two antibodies were mitogenic, and behaved similarly to Leu 4 and OKT3, respectively. In T cell preparations with less than 0.1% monocytes (as assayed by nonspecific esterase staining), all three mAb were not mitogenic. They failed to induce either interleukin 2 (IL-2) receptor expression or IL-2 secretion. Addition of IL-1 failed to collaborate with anti-T3 mAb to induce these T cells to proliferate, but IL-2 enhanced T cell proliferation slightly. Monocyte-depleted T cells, however, proliferated in response to all three anti-T3 mAb, when TPA was added, in a dose-dependent manner. TPA induced a low level of IL-2 receptor expression in monocyte-depleted T cells, without inducing IL-2 secretion. Anti-T3 plus TPA induced a marked enhancement in both quantity and intensity of IL-2 receptor expression. IL-2 secretion was also detected. These results indicate that anti-T3 IgM can deliver an inductive signal despite its blockage of T cell proliferation, and that two signals are necessary and perhaps sufficient to induce human T cell activation and proliferation.
Decay of Endoplasmic Reticulum-Localized mRNAs During the Unfolded Protein Response (2006)

The unfolded protein response (UPR) allows the endoplasmic reticulum (ER) to recover from the accumulation of misfolded proteins, in part by increasing its folding capacity. Inositol-requiring enzyme-1 (IRE1) promotes this remodeling by detecting misfolded ER proteins and activating a transcription factor, X-box-binding protein 1, through endonucleolytic cleavage of its messenger RNA (mRNA). Here, we report that IRE1 independently mediates the rapid degradation of a specific subset of mRNAs, based both on their localization to the ER membrane and on the amino acid sequence they encode. This response is well suited to complement other UPR mechanisms because it could selectively halt production of proteins that challenge the ER and clear the translocation and folding machinery for the subsequent remodeling process.
Glanzmann thrombasthenia: deficient binding of von Willebrand factor to thrombin-stimulated platelets. (1982)

Glanzmann thrombasthenia is an inherited bleeding disorder characterized by the failure of platelets to aggregate in response to almost all stimuli. However, thrombasthenic platelets will aggregate with bovine and porcine von Willebrand factor (vWF) and will show normal ristocetin-induced binding and aggregation in the presence of human vWF. In contrast, we now report that the specific binding of vWF to the thrombin-stimulated platelets was less than 20% of normal in three patients with Glanzmann thrombasthenia. Analysis of binding isotherms was based on the assumption of one class of binding sites for vWF on the platelet membrane. Double-reciprocal plots were used to calculate maximal binding at saturation and apparent dissociation constant (Kd). In nine normals, 2.82 +/- 0.64 micrograms (+/- SD) of vWF bound to 10(8) platelets at saturation, with Kd (+/- SD) = 3.65 +/- 1.23 micrograms/ml. In two patients with thrombasthenia binding was markedly decreased and did not approach saturation. In the third patient, binding at saturation corresponded to 0.21 micrograms per 10(8) platelets, with Kd = 3.93 micrograms/ml. These findings suggest that mechanisms underlying the vWF-platelet interaction are incompletely reflected in ristocetin-dependent assay systems. Moreover, these results, in addition to those previously reported for fibronectin, suggest that the platelet defect in Glanzmann thrombasthenia is not limited to decreased binding of fibrinogen but involves several glycoproteins that are known to interact with platelets.
Minnesota Agricultural Economist no. 676 (1994)

Farm Spending and Local Selling: How Do They Match Up?; Changing Fiscal Patterns for Minnesota County Governments
Multiple myeloma and bone marrow mesenchymal stem cells’ crosstalk: Effect on translation initiation (2015)

Multiple myeloma (MM) malignant plasma cells reside in the bone marrow (BM) and convert it into a specialized pre-neoplastic niche that promotes the proliferation and survival of the cancer cells. BM resident mesenchymal stem cells (BM-MSCs) are altered in MM and in vitro studies indicate their transformation by MM proximity is within hours. The response time frame suggested that protein translation may be implicated. Thus, we assembled a co-culture model of MM cell lines with MSCs from normal donors (ND) and MM patients to test our hypothesis. The cell lines (U266, ARP-1) and BM-MSCs (ND, MM) were harvested separately after 72 h of co-culture and assayed for proliferation, death, levels of major translation initiation factors (eIF4E, eIF4GI), their targets, and regulators. Significant changes were observed: BM-MSCs (ND and MM) co-cultured with MM cell lines displayed elevated proliferation and death as well as increased expression/activity of eIF4E/eIF4GI; MM cell lines co-cultured with MM-MSCs also displayed higher proliferation and death rates coupled with augmented translation initiation factors; in contrast, MM cell lines co-cultured with ND-MSCs did not display elevated proliferation only death and had no changes in eIF4GI levels/activity. eIF4E expression was increased in one of the cell lines. Our study demonstrates that there is direct dialogue between the MM and BM-MSCs populations that includes translation initiation manipulation and critically affects cell fate. Future research should be aimed at identifying therapeutic targets that may be used to minimize the collateral damage to the cancer microenvironment and limit its recruitment into the malignant process. © 2015 Wiley Periodicals, Inc.
[Sulfur-containing nitrosoureas]. (1986)

N′-[N-(2-chloroethyl)-N-nitroso] carbamoyl cysteamine (CNC-cysteamine) and several related compounds as well as 2,2-disubstituted CNC-thiazolidines, the condensation products with ketones, have been synthesized and tested against L 1210 leukemia in mice.
Reaction of CNC-azide with cysteamine yielded CNC-cysteamine and bis (CNC) cystamine. Reaction of CNC-azide with cystamine in the presence of triethylamine gave bis-(CNC) cystamine, unexpectedly, formation of CNC-cystamine carboxylazide as a minor reaction product was also observed. Because the presence of triethylamine was necessary, an intermediate azidocarboxyl triethylammonium cation was supposed as the azidocarboxylating agent.
N-(2-Chloroethyl) carbamoyl cysteamine 2-chloroethylcarbamate was formed when 2-chloroethyl isocyanate was reacted with cysteamine. Nitrosation of this cysteamine N,S-dicarbamoyl derivative or of CNC-cysteamine 2-chloroethylcarbamate, formed by reaction of CNC-cysteamine with 2-cyloroethyl isocyanate, led to formation of a mixture of two dinitroso isomers.
The 2,2-disubstituted 3-CNC-thiazolidine derivatives were synthesized by nitrosation of corresponding 2,2-disubstituted 3-[N-(2-chlorpethyl) carbamoyl] thiazolidines, which could be obtained by carbamoylating of thiazolidine derivatives with 2-chloroethyl isocyanate. The 2-monosubstituted 3-[N-(2-chloroethyl) carbamoyl] thiazolidines decomposed by nitrosation under ring cleavage.
Preliminary test of the newly synthesized CNC-derivatives in L_(1210) leukemia in mice revealed that the CNC-cysteamnie and its disulfide, as well as the CNC-cystamine carboxylazide are highly active against L_(1210) laukemia in mice, whereas the 2-chloroethylearbamate and the thiazolidine derivatives are ineffective except one compound, namely the (±) 2-methyl-2-ethoxycarbonylmethyl-3-CNC-thiazolidine, the high activity excited great attention.
Molecular population genetics of the alcohol dehydrogenase locus in the Hawaiian drosophilid D. mimica (1996)

Sequence variation among 10 alleles of the alcohol dehydrogenase (Adh) gene of the Hawaiian drosophilid D. mimica was analyzed with reference to the evolutionary history of the Hawaiian subgroup as well as to levels and patterns of polymorphism of the Adh gene in continental drosophilid species. The Adh gene of D. mimica is less polymorphic than that of other drosophilid species, and no replacement substitutions were found. Statistical analyses of the Adh alleles suggested the action of balancing selection and revealed significant linkage disequilibrium among three of the variable sites. The effective population size was estimated to be only slightly smaller than that of continental species and, surprisingly, on the same order of magnitude as the actual size.
Safety and efficacy of alirocumab 150 mg every 2 weeks, a fully human proprotein convertase subtilisin/kexin type 9 monoclonal antibody: A Phase II pooled analysis (2015)

At the highest Q2W dose under development (150 mg), alirocumab appears well tolerated and produces robust LDL-C reductions. These data suggest that alirocumab 150 mg Q2W is an appropriate dose for further evaluation in Phase III trials.
DNA Enrichment by Allele-Specific Hybridization (DEASH): A Novel Method for Haplotyping and for Detecting Low-Frequency Base Substitutional Variants and Recombinant DNA Molecules (2003)

Detecting rare sequence variants in genomic DNA is central to the analysis of de novo mutation and recombination events and the detection of rare pathological mutations in mixed cell populations. Current PCR techniques suffer from noise that limits detection to variants present at a frequency of at least 10(-4)-10(-5) per cell. We now describe an alternative approach that recovers genomic DNA molecules containing a known single-nucleotide variant by hybridization selection using a biotinylated allele-specific oligonucleotide, followed by hybrid capture on streptavidin-coated paramagnetic beads and subsequent analysis by PCR. This technique of DNA enrichment by allele-specific hybridization (DEASH) is fast, effective for all tested single-nucleotide polymorphisms (SNPs), and can recover large (>10 kb) single-stranded molecules. A single round of DEASH is effective in separating haplotypes from genomic DNA and can not only readily detect and validate DNA molecules containing a single base change at a frequency of 10(-5) per cell, but can also place these changes within the context of an extended haplotype. This technique offers a new approach to the analysis of mutation and recombination, and has the potential to detect very rare de novo base substitutions.
Enforcing Periodic Secondary Structures in Hybrid Peptides:  A Novel Hybrid Foldamer Containing Periodic γ-Turn Motifs (2006)

This note describes the design, synthesis, and conformational studies of a novel hybrid foldamer that adopts a definite compact, three-dimensional structure determined by a combined effect of the special conformational properties of the foldamer constituents. The striking feature of this de novo designed foldamer is its ability to display periodic gamma-turn conformations stabilized by intramolecular hydrogen bonds. Conformational investigations by single-crystal X-ray studies, solution-state NMR, and ab initio MO theory at the HF/6-31G* level strongly support the prevalence of gamma-turn motifs in both the di- and tetrapeptide foldamers, which are presumably stabilized by bifurcated hydrogen bonds in the solid and solution states. The strategy disclosed herein for the construction of hybrid foldamers with periodic gamma-turn motifs has the potential to significantly augment the conformational space available for foldamer design with diverse backbone structures and conformations.
Design and Implementation of the communication protocol for efficient CBC mode processing in IPSec (2006)

The IV (initial vector) used in CBC mode must be varied per message, must not be used arbitrarily by attackers, and must be created randomly. To meet these requirements, IV encrypted before a message is sent. Note, however, that this method requires additional steps for IV encryption before sending a message and decryption by the receiver. This paper proposed the method that does not require IV encryption/decryption and developed the lightweight protocol and security API specification based on the proposed method. As a result of the experiment, system performance improvement can be achieved. In an environment with small-sized packet data, in particular, greater system performance improvement can be achieved. Moreover, since small-sized random numbers are sent without the entire IV, sending overhead can be reduced considerably compared to the existing methods
Role of nitric oxide in implantation and menstruation (2000)

Nitric oxide (NO) is a major paracrine mediator of various biological processes, including vascular functions and inflammation. In blood vessels, NO is produced by the low-input constitutive endothelial NO synthase (eNOS) and is a potent vasodilator and platelet aggregation inhibitor. The inducible NOS isoform (iNOS) is capable of producing NO at high concentrations which have pro-inflammatory properties. Immunohistochemical and molecular studies of endometrial NOS expression, as well as animal experiments with NOS inhibitors, indicate that NO plays an important role in endometrial functions such as endometrial receptivity, implantation and menstruation. In rodents, both iNOS and eNOS are highly up-regulated in the implantation sites, and NOS inhibitors show synergistic effects with antiprogestins in inhibiting the establishment of pregnancy. In the human endometrium, eNOS have been localized in the glandular epithelium and in endometrial microvascular endothelium, primarily during the luteal phase. iNOS has been found in the endometrial epithelium during menstruation, in immunocompetent endometrial cells, and in decidualized stromal cells. In primates, NO may be involved in the initiation and maintenance of menstrual bleeding by inducing tissue breakdown and vascular relaxation as well as by inhibiting platelet aggregation. Endometrium-derived NO may also play a role in myometrial relaxation during menstruation. These studies open up new applications for NO-donating and -inhibiting agents in uterine disorders. NO donors may be useful in the treatment of dysmenorrhoea and for promoting fertility. Antiprogestins, progesterone receptor modulators and iNOS inhibitors may find applications in the treatment and prevention of abnormal uterine bleeding.
THE CHEMOTACTIC EFFECT OF MIXTURES OF ANTIBODY AND ANTIGEN ON POLYMORPHONUCLEAR LEUCOCYTES (1962)

An in vitro technique is described for assessing the chemotactic activity of soluble substances on motile cells. Antibody-antigen mixtures when incubated (37 degrees C) in medium containing fresh (i.e. non-inactivated) normal rabbit serum exert a strong chemotactic effect on rabbit polymorphonuclear leucocytes. Results are described which indicate that, when antibody-antigen complexes are incubated (37 degrees C) in fresh serum, a heat-stable (56 degrees C) substance (or substances) is produced which acts directly as a chemotactic stimulus on the polymorphs. This heat-stable chemotactic substance is not produced when antibody-antigen complexes are incubated in serum which has been heated at 56 degrees C for 30 minutes.
Dysbiosis of fecal microbiota in Crohnʼs disease patients as revealed by a custom phylogenetic microarray (2010)

The microarray detected differences in abundance of bacterial populations within the phylum Firmicutes that had been reported previously for the same samples based on phylogenetic analysis of metagenomic clone libraries. In addition, the microarray showed that Enterococcus sp. was in higher abundance in the CD patients. This microarray should be another useful tool to examine the diversity and abundance of human intestinal microbiota.
Improving Therapeutic Efficacy of a Complement Receptor by Structure-based Affinity Maturation (2009)

CRIg is a recently discovered complement C3 receptor expressed on a subpopulation of tissue-resident macrophages. The extracellular IgV domain of CRIg (CRIg-ECD) holds considerable promise as a potential therapeutic because it selectively inhibits the alternative pathway of complement by binding to C3b and inhibiting proteolytic activation of C3 and C5. However, CRIg binds weakly to the convertase subunit C3b (K(D) = 1.1 microm), and thus a relatively high concentration of protein is required to reach nearly complete complement inhibition. To improve therapeutic efficacy while minimizing risk of immunogenicity, we devised a phage display strategy to evolve a high affinity CRIg-ECD variant with a minimal number of mutations. Using the crystal structure of CRIg in complex with C3b as a guide for library design, we isolated a CRIg-ECD double mutant (Q64R/M86Y, CRIg-v27) that showed increased binding affinity and improved complement inhibitory activity relative to CRIg-ECD. In a mouse model of arthritis, treatment with a Fc fusion of CRIg-v27 resulted in a significant reduction in clinical scores compared with treatment with an Fc fusion of CRIg-ECD. This study clearly illustrates how phage display technology and structural information can be combined to generate proteins with nearly natural sequences that act as potent complement inhibitors with greatly improved therapeutic efficacy.
Spectroscopic, Electrochemical, and Kinetic Characterization of New Ruthenium(II) Tris‐chelates Containing Five‐Membered Heterocyclic Moieties (1987)

Abstract Synthesis, redox, photophysical, and photochemical properties of Ru(NN) complexes NN = 2‐((2′‐pyridyl)thiazole (pyth), 2‐(2′‐pyrazyl)thiazole (pzth), 2,2′‐bithiazole (bth), 5‐(2′‐pyridyl)‐1,2,4‐thiadiazole (pytda), 2‐(2′‐pyridyl)imidazole (pyim), 1‐methyl‐2‐(2′‐pyridyl)imidazole (Mepyim), and 2‐(2′‐pyridyl)oxazole (pyox)) are described. Oxidation potentials for the Ru 3+/2+ couples in MeCN varied from about 0.80 V to 1.60 V vs. NHE. Three reduction waves were observed in all the cases except for Ru(pyim) and Ru(Mepyim) complexes and asigned to the one‐electron reduction of each bidentate ligand. Absorption spectra contained bands in the UV (280–325 nm) and VIS (437–481 nm) regions which have been assigned to ligand‐centered π‐π* and metal‐to‐ligand charge‐transfer dπ‐π* transitions, respectively. Emission spectra at 77 K were determined for all the complexes presenting maxima in the 580–650‐nm region, with vibrational progression in some of them. Only pyth, pzth, bth, and pytda tris‐chelates showed luminescence at room temperature in aqueous solution, with quantum yields ranging from 0.0013 to 0.0095 and excited‐state lifetimes from 55 to 390 ns, as determined from pulsed laser techniques. Their E 0–0 spetroscopic energies have been estimated from emission wavelength maxima at 77 K which, in turn, have allowed calculation of excited‐state redox potentials. A plot of E 0–0 vs. Δ E 1/2 , where Δ E 1/2 = E 1/2 (3+/2+) − E 1/2 (2+/+), was linear with a slope of ca. 1.1 and a correlation coefficient of 0.999, demonstrating an identical nature of the orbital involved in spectroscopic and electrochemical processes. Photochemical properties of Ru(NN) complexes have been tested using methyl viologen (MV 2+ ) in Ar‐purged aqueous solution at pH 5. Stern‐Volmer treatment has led to the determination of bimolecular quenching constants (0.5 to 2 × 10 9 m −1 ·s −1 ) which parallel electron‐transfer free‐energy changes. Homogeneous back‐reaction of primarily produced MV +· and Ru(NN) has been measured resulting to be slightly higher than diffusion control and independent of ligand nature. Rate constants for the scavenging of Ru(NN) by added edta have been also determined (1.7 to 8.2 × 10 8 M −1 · S −1 ). Under such conditions, net production of MV +· is attained with quantum yields varying from 0.003 to 0.038 (single‐shot laser results).
A system architecture for subject-centric data sharing (2018)

With the rapid growth of online social networks, the mindset of the people about sharing of their personal information has changed significantly. Individuals (data subjects) are more willing to share their personal information with others. However, contemporary data sharing mechanisms often do not capture the individual's fine-grained data sharing requirements. Furthermore, data subjects have to use diverse access control mechanisms available for each different data custodian to control its dissemination, which often lead to data and privacy leakage. To overcome these limitations, we present a novel system architecture puts the data subject in charge of selectively assigning access rights to resources using a centralized authorization manager. We have also implemented a prototype to show how the proposed subject-centric and privacy-preserving data sharing framework works.