gebhart/patrepeval huggingface dataset:
Fucosyltransferase VII-Deficient Mice with Defective E-, P-, and L-Selectin Ligands Show Impaired CD4+ and CD8+ T Cell Migration into the Skin, but Normal Extravasation into Visceral Organs (2002)

The first step of leukocyte extravasation, leukocyte rolling, is mediated by E-, P-, and L-selectins. Mice deficient for alpha-1,3-fucosyltransferase VII (FucTVII)(-/-) are characterized by deficiency of E-, P-, and L-selectin ligand activity. This model system was used to evaluate the role of the interactions of selectins with their ligands in T and B cell responses. In the present study, FucTVII(-/-) mice showed reduced CD4+ T cell-mediated contact hypersensitivity reactions of the ears to FITC as well as reduced CD8+ T cell-mediated delayed-type hypersensitivity reactions of the footpads against lymphocytic choriomeningitis virus infection. As Langerhans cell migration to local lymph nodes as well as CD4+ and CD8+ T cell induction were found to be normal, the afferent arm of these reactions was not impaired. The reduced inflammatory reactions of the skin were due to inefficient lymphocyte extravasation into the skin. In contrast, extravasation of CD4+ and CD8+ T cells into visceral organs, such as the ovaries or the brain, was not impaired in FucTVII(-/-) mice. Elimination of vaccinia virus and of lymphocytic choriomeningitis virus from ovaries and brain, as well as elimination of tumor cells from several visceral organs was normal. Thus, interactions of selectins with their ligands are important for lymphocyte homing into the skin, but not for lymphocyte extravasation into visceral organs.
ChemInform Abstract: Dihydropyridines: A New Class of Angiotensin II Antagonists. (1994)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Macromelanosomes in X-linked ocular albinism (XLOA) (1985)

A case of X-linked ocular albinism is reported. Characteristic Masson-Fontana positive and Dopa positive giant melanin granules were found in keratinocytes, melanocytes and upper dermis. Ultrastructurally the macromelanosome was composed of a dense core and a less dense surrounding mantle.
Endothelin‐1 inhibits PAF‐induced paw oedema and pleurisy in the mouse (1992)

1. The current study analyses the effects of endothelin-1 (ET-1) on paw oedema and pleurisy induced by platelet activating factor (PAF) and other inflammatory agents in the mouse. 2. Combined subplantar injection of ET-1 (0.5 pmol/paw) did not modify oedema caused by histamine (1 to 100 mumol/paw), 5-hydroxytryptamine (1 to 100 mumol/paw) or bradykinin (1 to 100 nmol/paw) but markedly inhibited the response to PAF (0.95 to 3.8 nmol/paw). The selective action of ET-1 against PAF-induced (1.9 nmol/paw) oedema was dose-dependent, reaching a maximum at 0.5 pmol/paw and lasted up to 2 h. 3. ET-1 (0.5 pmol/paw) also inhibited paw oedema (3-4 h) caused by zymosan (500 micrograms/paw). In contrast, it did not modify either the early (1-4 h) or late (48-72 h) phases of the oedematogenic response to carrageenin (300 micrograms/paw), when given either together with or 24 h after the carrageenin. 4. Intrathoracic injection of PAF (1.9 nmol/cavity) induced pleurisy characterized by an increase in pleural exudate volume, and in accumulation of Evans Blue which was maximal at 30 min and lasted up to 4 h. When injected together with PAF, ET-1 (0.5 pmol/cavity) virtually abolished PAF-induced pleurisy. 5. It is concluded that ET-1 is a potent inhibitor of PAF-induced inflammation in the mouse. Its mechanism of anti-inflammatory action in this species, in contrast to what has been found in other species, does not appear to derive from its potent vasoconstrictor properties as ET-1, at the doses used, failed to affect oedematogenic responses to other inflammatory mediators.
Macrocycles. 17. The Role of Cyclization in Kinetically Controlled Polycondensations. 2. Polyamides (2001)

Two series of kinetically controlled polycondensations were conducted yielding polyamides of aliphatic dicarboxylic acids. First, the bis(trimethylsilyl) derivatives of 1,3-diaminobenzene, 4,4‘-diaminodiphenylmethane, 1,12-diamino-4,9-dioxadodecane, and 1,12-diaminododecane were polycondensed with dicarboxylic acid dichlorides in N-methylpyrrodidone below 0 °C. After optimization of the reaction conditions mainly cyclic polyamides were detectable in the MALDI−TOF mass spectra (up to 13 000 Da) of the semiaromatic polyamides in contrast to the Carothers−Flory theory. In the case of silylated aliphatic diamines, side reactions of the acid chlorides prevented a complete conversion of the amino groups, so that the reaction products mainly consisted of cycles and linear chains having two amino end groups. Second, normal interfacial polycondensations were performed either with 1,6-diaminohexane and adipoyl chloride or with 1,12-diaminododecane and decane-1,10-dicarbonyl chloride. When the loss of acid chloride groups by hydrolysis was compensated by an excess of dicarboxylic acid dichlorides cyclic polyamides were again the main reaction products up to masses of 4000−5000 Da. A new version of the “Carothers equation” taking into account the role of cyclization in kinetically controlled step-growth polymerizations is discussed.
Toll-like Receptor 4 Ligands Down-regulate Fcγ Receptor IIb (FcγRIIb) via MARCH3 Protein-mediated Ubiquitination (2015)

Monocytes and macrophages are critical for the effectiveness of monoclonal antibody therapy. Responses to antibody-coated tumor cells are largely mediated by Fcγ receptors (FcγRs), which become activated upon binding to immune complexes. FcγRIIb is an inhibitory FcγR that negatively regulates these responses, and it is expressed on monocytes and macrophages. Therefore, deletion or down-regulation of this receptor may substantially enhance therapeutic outcomes. Here we screened a panel of Toll-like receptor (TLR) agonists and found that those selective for TLR4 and TLR8 could significantly down-regulate the expression of FcγRIIb. Upon further examination, we found that treatment of monocytes with TLR4 agonists could lead to the ubiquitination of FcγRIIb protein. A search of our earlier microarray database of monocytes activated with the TLR7/8 agonist R-848 (in which FcγRIIb was down-regulated) revealed an up-regulation of membrane-associated ring finger (C3HC4) 3 (MARCH3), an E3 ubiquitin ligase. Therefore, we tested whether LPS treatment could up-regulate MARCH3 in monocytes and whether this E3 ligase was involved with LPS-mediated FcγRIIb down-regulation. The results showed that LPS activation of TLR4 significantly increased MARCH3 expression and that siRNA against MARCH3 prevented the decrease in FcγRIIb following LPS treatment. These data suggest that activation of TLR4 on monocytes can induce a rapid down-regulation of FcγRIIb protein and that this involves ubiquitination.
Konkave Makroheterocyclen (1993)

Concave Macroheterocycles Macrocyclic compounds of the general type 2 having a spherical shape and a molecular cavity have been synthesized. A „fold and paste”︁‐type cyclization step generates the macroheterocycles 4, 10, 11, 14 , and 21 . Since this approach is difficult to apply for O ‐substituted derivatives, the „spheriphane”︁ 24 was synthesized by intermolecular cyclizaiton. The X‐ray structure analysis of 11 shows intermolecular interactions („dimer formation”︁) in the crystal.
A novel certificateless deniable authentication protocol. (2013)

Abstract: Deniable authenticated protocol is a new and attractive protocol compared to the traditional authentication protocol. It allows the appointed receiver to identify the source of a given message, but not to prove the identity of the sender to a third party even if the appointed receiver is willing to reveal its private key. In this paper, we first define a security model for certificateless deniable authentication protocols. Then we propose a non-interactive certificateless deniable authentication protocol, by combining deniable authentication protocol with certificateless cryptography. In addition, we prove its security in the random oracle model.
Partial Muscle Carnitine Palmitoyltransferase-A Deficiency (1987)

After initiation of ibuprofen therapy, a 45-year-old woman developed muscle weakness and tenderness with rhabdomyolysis, culminating in respiratory failure. A muscle biopsy specimen showed a vacuolar myopathy, and markedly decreased muscle carnitine content and carnitine palmitoyltransferase activity. Following recovery, muscle carnitine content was normal but carnitine palmitoyltransferase activity was still abnormally low. The ratio of palmitoyl— coenzyme A plus carnitine to palmitoylcarnitine oxidation by muscle mitochondria isolated from the patient was markedly decreased. We conclude that transiently decreased muscle carnitine content interacted with partial deficiency of carnitine palmitoyltransferase-A to produce rhabdomyolysis and respiratory failure and that ibuprofen may have precipitated the clinical event. (<i>JAMA</i>1987:257:62-65)
Pre-mRNA Splicing-Modulatory Pharmacophores: The Total Synthesis of Herboxidiene, a Pladienolide–Herboxidiene Hybrid Analog and Related Derivatives (2013)

Herboxidiene is a natural product that has previously been shown to exhibit antitumor activity by targeting the spliceosome. This activity makes herboxidiene a valuable starting point for the development of anticancer drugs. Here, we report an improved enantioselective synthesis of herboxidiene and the first report of its biologically active totally synthetic analog: 6-norherboxidiene. The synthesis of the tetrahydropyran moiety utilizes the novel application of inverse electron-demand Diels-Alder chemistry and the Ferrier-type rearrangement as key steps. We report, for the first time, cytotoxicity IC50s for synthetic herboxidiene and analogs in human tumor cell lines. We have also demonstrated that synthetic herboxidiene and its analogs can potently modulate the alternate splicing of MDM-2 pre-mRNA.
Adhesion enhancement of Cr/polyimide interfaces using RF pre-sputtering of polyimide surfaces (1990)

The effects of Ar ion RF pre-sputtering of polyimide surfaces on the adhesion of Cr/polyimide interfaces have been examined by TEM, XPS, and peel test. With Ar pre-sputtering, the peel strength of Cu/Cr to polyimide increases remarkably from 1 g/mm to 130 g/mm and 90 g/mm on PMDA-ODA spun on Si and silica substrates, respectively. The negligible change in the polyimide surface morphology by RF sputtering and the little change in the adhesion strength by a long exposure to the air after the sputtering prior to metal deposition eliminate contributions of mechanical interlocking and surface cleaning effects to this adhesion enhancement. Thus, adhesion enhancement by RF pre-sputtering is mainly attributed to chemical changes of the polyimide surface facilitating bonding with the deposited Cr. Such a surface treatment with RF sputtering was also found to be effective for the retardation of the moisture-induced failure of Cr/polyimide interfaces. It has been observed that cracks develop in both Cr and polyimide, and that the size of the cracks varies depending on the RF power density and on the stress state of the polyimide. The cracks at the interface are suggested to be the main path of moisture penetration for the degradation of adhesion strength.
Youth, Popular Culture, and Identity (2002)

Beginning in the early twentieth century and continuing through today, American culture in general, and more specifically African-American culture and identity, has played a significant role in the construction of identity, popular culture, and the struggle for equality in southern Africa. Of particular interest is how American culture (particularly the African-American component), mediated through South Africa, has impacted the political and cultural identity of Basotho youth in the 1990s. Basotho and South African youth identify with aspects of American culture that provide them with new meanings, which help negotiate their landscape. As an enclave in South Africa, Lesotho not only illustrates the impact of aspects of American culture on South Africa, but in this case has also contributed to a decreasing national identity that is being replaced by an increased identification with South Africa.
Use of plastic membrane ion-selective electrodes for the analysis of drug substances (1995)

An overview is given on plastic membrane ion-selective electrodes of the conventional and/or coated-wire type constructed for 23 drug compounds. These are based on incorporation of ion-pairs or ion-associates in poly(vinyl chloride) network in the presence of dioctyl phthalate as a plasticizer. The electrodes are very selective to their respective drugs; a comparative study proved that stereospecifity is a major factor affecting their selectivity. They have a relatively large working pH-ranges (more than 4 pH units for most cases). The isothermal temperature coefficients. (dE°/dT) of the electrodes range from 2.5×10-5 to 32.0×10-4 V/°C over a wide temperature limits. The electrodes can be employed successfully for assaying the investigated drugs in many of their pharmaceutical preparations.
Guidelines on the management of valvular heart disease: The Task Force on the Management of Valvular Heart Disease of the European Society of Cardiology (2006)

of the individual patients, in consultation with that patient, and where appropriate and necessary the patient's guardian or carer. It is also the health professional's responsibility to verify the rules and regulations applicable to drugs and devices at the time of prescription.
Induction of NAD(P)H:quinone Reductase by Probucol: A Possible Mechanism for Protection against Chemical Carcinogenesis and Toxicity (2003)

Dietary antioxidants protect laboratory animals against induction of tumours by a variety of chemical carcinogens. Among possible mechanism, protection against chemical carcinogenesis could be mediated via antioxidant-dependent induction of detoxifying enzymes, including quinone reductase and glutathione S-transferase (GSH transferase). Probucol is used cholesterol-lowering drug used in the clinic, with pronounced antioxidant effect that protect against chemical carcinogenesis and toxicity. In the present study we therefore examined the ability of probucol to induce activities of quinone reductase in the cytosolic fractions of various tissues of mice. Quinone reductase activity was increased significantly in 6 of 8 tissues examined from probucol-fed mice. The greatest proportionate increase, to 1.8 times control levels, was observed in liver. Probucol also increased quinone reductase activities of forestomach, heart, kidney, lungs and spleen. Quinone reductase is a major enzyme of xenobiotic metabolism that carries out obligatory two-electron reductions and thereby protects cells against toxicity of quinones. It is induced in many tissues coordinately with other enzymes that protect against electrophilic toxicity. The protective effects of probucol appear to be due, at least in part, to the ability of this antioxidant to increase the activities in rodent tissues of several enzymes involved in the non-oxidative metabolism of a wide variety of xenobiotics. The induction of such enzyme, quinone reductase by probucol suggests the potential value of this compound as a protective agent against chemical carcinogenesis and other forms of electrophilic toxicity. The significance of these results can be implicated in relation to cancer chemopreventive effects of probucol in various target organs.
Extraction fractionation of polyvinyl acetate and of polyvinyl alcohol (1959)

Abstract Methods for rapid fractionation of polyvinyl acetate and of polyvinyl alcohol are described. By a slightly modified Fuchs' extraction technique, polyvinyl acetate can be fractionated into relatively homogeneous fractions. The ratio of osmotically determined M̄ n of the nonfractionated sample to that calculated from fractionation data is 1.19. Extraction fractionation of polyvinyl alcohol is complicated by the crystallinity of this polymer. The molecular weight distribution of polyvinyl alcohol can be determined, however, in relatively short time, by first reacetylating the polymer and then fractionating the obtained polyvinyl acetate.
Telomere erosion is independent of microsatellite instability but related to loss of heterozygosity in gastric cancer (2001)

The development of gastric cancer can arise through two different genetic pathways. In high MSI gastric cancers, defective mismatch repair allows mutations to accumulate and generate the high MSI phenotype. In gastric cancers showing either low MSI or MSS, multiple deletions may represent the LOH pathway. Telomere erosion is independent of high MSI phenotype but related to the LOH pathway in gastric cancer.
Abstract 353: High Density Lipoprotein Regulates Tumor Necrosis Factor Alpha and Jun Kinase Signaling Pathway in Adipocytes (2020)

Background: High-density lipoproteins (HDL) is presumed to exhibit cardiovascular protection, since HDL mediate the reverse transport of cholesterol and exhibit strong anti-inflammatory potential. Previous studies have found that HDL can reduce the level of IL-8 secreted by the inflammatory adipocytes, as well as affect the expression of adiponectin and tumor necrosis factor-alpha (TNF-α) under the inflammatory condition in adipocytes. These studies indicate that HDL is closely related to the inflammatory response of adipose tissue, yet its mechanism has not been fully understood. Secretory leucocyte protease inhibitor (SLPI), a nonglycosylated single-chain polypeptide protein, may play an important role in diet-induced obesity and adipocyte inflammation. Purpose: To study the role of SLPI in HDL anti-inflammatory action in the adipocytes, and explore the mechanism of the action. Methods: 3T3-L1 Adipocytes were induced to differentiation and maturation by culturing. Acute inflammation in adipocytes was induced by LPS (100 ng/ml, 6h), and then the adipocytes were pretreated with HDL and/or SLPI-siRNA. The protein and mRNA levels of SLPI, TNF-α and JNK were examined by Western blotting and qRT-PCR assay, respectively. In addition, the levels of inflammatory factors were measured by ELISA. Results: HDL up-regulated SLPI expression, down-regulated TNF-α expression, and inhibited the secretion of inflammatory factors such as IL-1, IL-6, IL-8 and MCP-1 in 3T3-L1 Adipocytes pre-treated by LPS. Silencing of SLPI by its siRNA effectively abolished the anti-inflammatory effect of HDL. JNK inhibitor (SP600125) partially restored the anti-inflammatory effects of HDL decreased by SLPI knockdown and decreased the secretion of inflammatory factors. Conclusions: These data suggest that HDL up-regulate the expression of SLPI and inhibit the inflammation in 3T3-L1 Adipocytes pre-treated by LPS. The anti-inflammatory effect of HDL, including inhibition of the secretion of inflammatory factors via TNF-α/JNK signaling pathway, probably viat up-regulating the SLPI expression. Key words: high-density lipoprotein, Inflammation, Adipocytes
The N-Terminal Region of Arabidopsis Cystathionine γ-Synthase Plays an Important Regulatory Role in Methionine Metabolism (2002)

Cystathionine gamma-synthase (CGS) is a key enzyme of Met biosynthesis in bacteria and plants. Aligning the amino acid sequences revealed that the plant enzyme has an extended N-terminal region that is not found in the bacterial enzyme. However, this region is not essential for the catalytic activity of this enzyme, as deduced from the complementation test of an Escherichia coli CGS mutant. To determine the function of this N-terminal region, we overexpressed full-length Arabidopsis CGS and its truncated version that lacks the N-terminal region in transgenic tobacco (Nicotiana tabacum) plants. Transgenic plants expressing both types of CGS had a significant higher level of Met, S-methyl-Met, and Met content in their proteins. However, although plants expressing full-length CGS showed the same phenotype and developmental pattern as wild-type plants, those expressing the truncated CGS showed a severely abnormal phenotype. These abnormal plants also emitted high levels of Met catabolic products, dimethyl sulfide and carbon disulfide. The level of ethylene, the Met-derived hormone, was 40 times higher than in wild-type plants. Since the alien CGS was expressed at comparable levels in both types of transgenic plants, we further suggest that post-translational modification(s) occurs in this N-terminal region, which regulate CGS and/or Met metabolism. More specifically, since the absence of the N-terminal region leads to an impaired Met metabolism, the results further suggest that this region plays a role in protecting plants from a high level of Met catabolic products such as ethylene.
The Next Generation of Artificial Pancreas Control Algorithms (2008)

Creating a wearable artificial pancreas (AP) by closing the loop between a glucose sensor and an insulin infusion pump has the potential to significantly impact the complications associated with and improve the quality of life of diabetic individuals. Despite recent progress on glucose sensor and insulin infusion technologies, control algorithms built on the simple glucose value efferent and insulin dose afferent model are not efficient and reliable. Based on glucose regulatory mechanisms known to date, their impairment in the diabetic state, and fundamental principles of control theory, some corrections to the present course of research are proposed to facilitate the removal of this barrier. A greater emphasis on model predictive controllers or controllers that exploit a mathematical representation, or model, of the patient's own physiology is proposed. Whole-body physiologically based pharmacokinetics-pharmacodynamics-type models hold the best odds for enabling a successful closed-loop AP. However, two major improvements to the diabetes modeling state of the art are required to make them practical for daily care: integrating hypothalamus-pituitary-adrenal axis and gastrointestinal tract submodels. Although there are simple representations of these in current existence, large concerted efforts between experimentalists and modelers will be required to enhance their accuracy. Finally, changes in hardware that complements controller performance are suggested. For instance, the development of dual control inputs of insulin and glucagon could relax tolerances on controller accuracy.
Visible Light‐Induced Methoxycarbonyldifluoromethylation of Trimethylsilyl Enol Ethers and Allyltrimethylsilanes with FSO<sub>2</sub>CF<sub>2</sub>CO<sub>2</sub>Me (2018)

Abstract A photocatalytic methoxycarbonyldifluoromethylation of trimethylsilyl enol ethers with FSO 2 CF 2 CO 2 Me in the presence of fac ‐Ir(ppy) 3 was developed. This reaction provided a practical strategy for the construction of various α‐CF 2 CO 2 R aromatic ketones, which are difficult to access by other methods. Furthermore, a series of methoxycarbonyldifluoromethylated allylic compounds could also be obtained from allyltrimethylsilanes using the same strategy. The resulting CF 2 CO 2 R‐containing products are useful building blocks and potentially valuable in medicinal chemistry and material sciences.