gebhart/patrepeval huggingface dataset:
Design and development of curcumin bioconjugates as antiviral agents (2008)

A number of curcumin bioconjugates with fatty acid, dipeptide and folic acid, viz. di-O-decanoyl curcumin (2), di-O-tryptophanylphenylalanine curcumin (3), di-O-bis-(gamma, gamma)folyl curcumin (4), C(4)-ehyl-O-gamma-folyl curcumin (5) and 4-O-ethyl-O-gamma-folyl curcumin (6) have been synthesized. Conjugates 2-6 have shown good antiviral property with EC(50) ranging between 0.019-0.105 microM against a wide range of viruses, like HIV, HSV, VSV and many others.
[Prospects and current data in antiviral chemotherapy]. (1989)

The advances achieved in our knowledge on the virus multiplication cycle and the challenge created by the advent of AIDS have resulted in a rational development of new antiviral agents. However, antiviral chemotherapy is hindered by several obstacles: (1) most antiviral drugs are cytotoxic, with the exception of acyclovir which owes its remarkable safety to its activation by the thymidine kinase of the herpes simplex viruses and of the varicella-zoster virus; (2) the risk of selecting resistant strains by mutation of viral enzymes is the unavoidable price to pay for the specificity of new antiviral agents which interfere with these enzymes; so far, this risk seems to apply only to immunocompromised patients; (3) latent viral infection, defined as the lack of active multiplication of the virus, cannot be eradicated by the antiviral drugs available at present since these drugs are inhibitors of viral multiplication. However, anti-sens oligonucleotides could, at least in theory, be used to treat this type of infection which is not limited to the Retroviridae or Herpesviridae families. Finally, antiviral drugs active against life-threatening infections that are as common as rabies and the severe forms of measles or viral hepatitis remain to be discovered.
Expression and Purification of Human Interferon ω in yeast Pichia Pastoris (2006)

OBJECTIVE Cultivation conditions of the genetic engineering Pichia pastori(pPIC9K IFN-ω GS115)which expression recombinant human interferon-ω were optimized,and try for the most expression of interferon-ω.METHODS Orhogonal experiment design and visual analysis were employed to confirm the best conditions of fermentation.RESULTS use FBS culture medium,the best conditions of fermentation is: temperature 28℃,oxygen dissolution 50%,methanal concentration 1%,pH 7.0.CONCLUSION after the conditions of fermentation were optimized,the quantity of expressed interferon-ω has reached 90mg·L~(-1).
CMOS RF integrated circuits at 5 GHz and beyond (2000)

A strong demand for wireless products, an insatiable thirst for spectrum that pushes carrier frequencies ever upward, and the constant quest for higher performance at lower power and cost, have recently driven the development of radio frequency integrated circuit (RFIC) technology in unprecedented ways. These pressures are stimulating novel solutions that allow RFICs to enjoy more of the benefits of Moore's law than has been the case in the past. In addition to regular raw transistor speed increases, the growing number of interconnect layers allows the realization of improved inductors, capacitors, and transmission lines. A deeper understanding of noise at both the device and circuit level has improved the performance of low noise amplifiers (LNAs) and oscillators. Finally, an appropriate raiding of circuit ideas dating back to the vacuum tube era enables excellent performance, even when working close to the limits of a technology. This paper surveys some of these developments in the context of low-power RF CMOS technology, with a focus on an illustrative implementation of a low-power 5-GHz wireless LAN receiver in 0.25-/spl mu/m CMOS. Thanks to these recent advances in passive components and active circuits, the blocks comprising the receiver consume a total of approximately 37 mW. These blocks include an image-reject LNA, image-reject downconverter, and a complete frequency synthesizer. The overall noise figure is 5 dB, and the input-referred third-order intercept (IIP3) is -2 dBm. To underscore that 5 GHz does not represent an upper bound by any means, this paper concludes with a look at active circuits that function beyond 15-20 GHz, and a characterization of on-chip transmission lines up to 50 GHz, all in the context of how scaling is expected to shape future developments.
ChemInform Abstract: SYNTHESIS OF SOME 3‐ARYL‐5‐METHOXY‐7‐METHYLISOCOUMARINS (1979)

Abstract Die Homophthalsäure (I) kondensiert mit den phenolischen Verbindungen (II) zu den Isocumarinen (III), die mit flüssigem NH 3 zu den Isochinolonen (IV) reagieren.
Calcitonin Gene–Related Peptide Receptor Antagonist BIBN 4096 BS for the Acute Treatment of Migraine (2004)

The CGRP antagonist BIBN 4096 BS was effective in treating acute attacks of migraine.
Down-regulation of Cdc6, a Cell Cycle Regulatory Gene, in Prostate Cancer (2002)

CDC6 plays a critical role in regulation of the onset of DNA replication in eukaryotic cells. We have found that Cdc6 expression is down-regulated in prostate cancer as detected by semiquantitative reverse transcriptase-PCR of prostate cell lines and laser-captured microdissected prostate tissues. This result was substantiated by immunohistochemical analysis of paraffin-embedded tissue sections and immunoblot analysis of benign (BPH-1) and adenocarcinomatous prostatic cells. Furthermore, a 100-fold reduction in the transcription efficiency of the Cdc6 promoter-luciferase construct was noted in the metastatic PC3 cells compared with that in BPH-1 cells. Concentration of the E2F and Oct1 transcription factors that have putative binding sites in the Cdc6 promoter was substantially low in PC3 cells compared with BPH cells. Mutagenesis of the two E2F binding sites on the Cdc6 promoter resulted in increased promoter activity in PC3 cells owing to elimination of the negative regulation by pRb.E2F complex but not to the level of that obtained in BPH cells. We conclude that an altered interaction of transcription factors may be responsible for the down-regulation of Cdc6 transcription in PC3 cells. Our study suggests a potential use of the lack of CDC6 expression as an index of prostate cancer development.
Cytotoxicity of oxidized low‐density lipoprotein to mouse peritoneal macrophages: An ultrastructural study (1993)

Mouse peritoneal macrophages (MPM) were incubated in culture medium containing low-density lipoprotein (LDL), oxidized LDL (oxLDL), or as controls, for 24 h. Scanning electron microscopy of MPM exposed to oxLDL showed loss of membrane ruffles and extensive plasmalemmal 'blebbing'. Transmission electron microscopy showed changes in up to 50 per cent of the cells, including vacuolation of the rough endoplasmic reticulum and reorganization of heterochromatin in the nuclei, characteristic of apoptosis. These changes were not seen in controls, nor in macrophages exposed to native LDL. Electron-dense crystals were found in the cytoplasm of 1 in 50 of cells exposed to oxLDL. These were found to have a high content of calcium and phosphorus. It is proposed that oxLDL is capable of inducing apoptosis, which might explain the origin of the necrotic base of advanced atherosclerotic plaques.
Extensive proliferative capacity of single isolated CD34 human cord blood cells in suspension culture. (1994)

Nonadherent, low-density T-lymphocyte-depleted (NALT-) CD34 cells from normal human cord blood were assessed in suspension culture for the effects of recombinant cytokines on their proliferation, differentiation, and generation of myeloid progenitor cells. In this cell population, 82% of cells expressed c-kit protein as assessed by in situ hybridization, and their cloning efficiency was 85% when cells were plated at low cell numbers with combinations of growth factors. CD34 cells were sorted as 1, 5, or 10 cell(s) per well and also at 5000 cells per dish to initiate stromal-free suspension cultures in the presence of steel factor (SLF), interleukin (IL)-1 alpha, and IL-3. Forty-eight percent of the wells started with a single CD34 cell were positive for growth after 14 days, and the wells contained greater than 5 x 10(3) cells by 21-28 days. Progenitors were assayed weekly with cultures initiated with 1 or 5000 cells. While the fold expansion of nucleated cells was greater in cultures initiated with one cell per well (> 5000 compared to 791-fold expansion for 5000 cells), the fold expansion of progenitors was greater than 5000 cells were used to initiate cultures. Under optimal conditions, there was, respectively, a 160-, 164-, and 57-fold output of high proliferative potential colony-forming cells, granulocyte-macrophage colony-forming units, and erythroid burst-forming units/granulocyte erythroid macrophage megakaryocyte colony-forming units within 1-3 weeks for cultures initiated with 5000 CD34 cells compared with respective fold increases of 29, 16, and 1, for single-initiated cultures. These results demonstrate the expansion capacity of single CD34 cord blood cells and demonstrate that factors in addition to SLF, IL-1 alpha, and IL-3 are necessary for optimal expansion of progenitors from single isolated CD34 cells.
Multimedia information broadcasting using digital TV channels (1997)

The structure of a new system used to broadcast multimedia information within a digital TV channel is outlined. The proposed scheme is based on the the Digital Storage Media Command and Control (DSM-CC) functions, and uses a newly developed protocol that allows to efficiently convey multimedia information. Such information has the same characteristics of HTML files used in WWW environments, as it may contain text, images, sounds and animation organized as an hypertext. The transport structure used is the MPEG-2 Transport Stream, which is the most standardized platform for the development of new digital TV services. A prototype software was developed to encode the file system by means of DSM-CC operations and include it in a MPEG-2 compatible Transport Stream.
Physical processes of phase noise in differential LC oscillators (2002)

There is an unprecedented interest among circuit designers today to obtain insight into the mechanisms of phase noise in LC oscillators. For only with this insight is it possible to optimize oscillator circuits using low-quality integrated resonators to comply with the exacting phase noise specifications of modern wireless systems. In this paper we concentrate on an understanding of the popular differential LC oscillator. We introduce simple models to capture the nonlinear processes that convert voltage or current thermal noise in resistors or transistors into phase noise in the oscillator. The analysis does not require hypothetical elements, such as limiters or amplitude control loops, to fully explain phase noise. A simple expression at the end accurately specifies thermally induced phase noise, and lends substance to Leeson's original hypothesis. Next, the upconversion of flicker noise into phase noise is traced to mechanisms first identified in the 1930's, but apparently since forgotten. Unlike thermally induced phase noise, which appears as phase modulation sidebands, flicker noise is shown to upconvert by bias-dependent frequency modulation. The results are validated against SpectreRF simulations and measurements on two differential CMOS oscillators tuned by resonators with very different Q's.
CD22: an inhibitory enigma (2008)

CD22 is an inhibitory coreceptor of the B-cell receptor (BCR), and plays a critical role in establishing signalling thresholds for B-cell activation. Like other coreceptors, the ability of CD22 to modulate B-cell signalling is critically dependent upon its proximity to the BCR, and this in turn is governed by the binding of its extracellular domain to alpha2,6-linked sialic acid ligands. Manipulation of CD22 ligand binding in various experimental settings has profound effects on B-cell signalling, but as yet there is no complete model for how ligand binding in vivo controls normal CD22 function. Several elegant studies have recently shed light on this issue, although the results appear to suggest two mutually exclusive models for the role of ligand binding; in either promoting or inhibiting, CD22 function. We shall therefore discuss these results in detail, and suggest possible approaches by which these conflicting experimental findings might be reconciled. We shall also consider a second important issue in CD22 biology, which relates to the role that defects in this receptor might play in mediating autoimmune disease. We review the current evidence for this, and discuss the importance of genetic background in modifying CD22 function and predisposition to autoimmunity.
Effect of recombinant human insulin-like growth factor-1 on the inflammatory response to acute renal injury. (1996)

Renal ischemic injury evokes an inflammatory response with increased cytokine and major histocompatibility complex (MHC) expression and a mild interstitial infiltrate. This "injury response" could contribute to the tendency of ischemically injured renal transplants to reject. The studies presented here evaluated the ability of recombinant human insulin-like growth factor-1 (rhlGF-1) given after renal injury to prevent renal inflammation. The left renal pedicle of CBA and BALB/c mice was clamped for 60 min, and rhlGF-1 (25, 50, 100 micrograms) was administered sc at 2, 24, 48, 72, and 96 h after reflow. Cytokine and MHC expression was monitored in the injured kidney, compared with the contralateral kidney. In untreated mice, a single episode of injury induced the expression of MHC mRNA and products and tumor necrosis factor-alpha (TNF-alpha) mRNA, and depressed preproepidermal growth factor (ppEGF) mRNA, for up to 5 wk. With immunohistology, epithelial Class I and II MHC expression was shown to be increased for 2 wk, and Class II positive interstitial cells were shown to be increased for up to 5 wk. The ischemically injured kidneys from mice treated with rhlGF-1 and examined at 5 days showed a dose-dependent normalization of all of the changes of the injury response. This included prevention of the increased expression of MHC and cytokines and the Class II positive interstitial cells, and restoration of ppEGF mRNA. Thus the complex and long-lasting increase in proinflammatory cytokines and MHC expression that follow renal ischemia can be interrupted by treatment with rhlGF-1 beginning 2 h after the injury. This therapy may have applications to the injury response in renal transplants.
Neutralization-sensitive epitopes are exposed on the surface of infectious Cryptosporidium Parvum sporozoites (1989)

Cryptosporidiosis is a diarrheal disease of humans, calves, and other mammals caused by the coccidian parasite Cryptosporidium parvum. Immune bovine serum and two surface-reactive antisporozoite mAb with neutralizing activity were used to identify sporozoite surface Ag by radioimmunoprecipitation/SDS-PAGE and immunoblotting. When isolated sporozoites were incubated with mAb 18.44, 12 to 25 times the ID50 for mice was completely neutralized. This mAb binds diffusely to the sporozoite surface and recognizes a sporozoite surface Ag that eluted in the void volume of a Bio Gel A column with an exclusion limit of 500,000 daltons. The Ag recognized by mAb 18.44 was not radiolabeled with 125I or [35S] methionine, migrated with the dye front in SDS-PAGE, and was insensitive to proteinase K digestion, suggesting a non-protein composition. mAb 17.41 significantly neutralized 25 times the ID50 of sporozoites for mice. This mAb binds multifocally to the sporozoite surface and recognizes [35S] methionine-labeled sporozoite surface Ag of 28,000 m.w., 55,000 m.w., and 98,000 m.w. Immune bovine serum immunoprecipitated [35S] methionine- or 125I-labeled sporozoite Ag ranging from less than 14,300 m.w. to greater than 200,000 m.w., including surface Ag of 28,000 m.w. and 55,000 m.w. The results indicate that two different molecules capable of inducing neutralizing antibody are exposed on the surface of C. parvum sporozoites.
Phase I/II open-label study of the biologic effects of the interleukin-2 immunocytokine EMD 273063 (hu14.18-IL2) in patients with metastatic malignant melanoma (2009)

EMD 273063 demonstrated biologic activity with increased immune-related cytokines and intratumoral changes in some patients consistent with the suspected mechanism of action of this immunocytokine.
19.1 Receiver with >20MHz bandwidth self-interference cancellation suitable for FDD, co-existence and full-duplex applications (2015)

In this paper, a 0.8-to-1.4GHz receiver with a tunable, reconfigurable RF SI canceller at the RX input is presented that supports >20MHz cancellation BW across a variety of antenna interfaces (nearly 10× improvement over a conventional canceller). This is accomplished by (i) a bank of tunable, reconfigurable 2nd-order high-Q RF bandpass filters in the canceller to emulate the antenna interface isolation (essentially RF frequency-domain equalization), and (ii) a linear N-path Gm-C filter implementation with embedded variable attenuation and phase shifting. For FDD, SIC enhances effective OOB IIP3 and IIP2 to +25-27d Bm and +90d Bm respectively. For SC-FD, SIC eliminates RX gain compression for as high as -8 dBm of peak in-band SI, and enhances effective in-band IIP3 and IIP2 by 22dB and 58 dB.
The CCN family of genes: a perspective on CCN biology and therapeutic potential (2007)

The CCN family of genes currently comprises six secreted proteins (designated CCN1-6 after Cyr61/CCN1; ctgf/CCN2; Nov/CCN3; WISP1/CCN4; WISP2/CCN5, WISP3/CCN6) with a similar mosaic primary structure. It is now well accepted that CCN proteins are not growth factors but matricellular proteins that modify signaling of other molecules, in particular those associated with the extracellular matrix. CCN proteins are involved in mitosis, adhesion, apoptosis, extracellular matrix production, growth arrest and migration of multiple cell types. Since their first identification as matricellular factors, the CCN proteins now figure prominently in a variety of major diseases and are now considered valid candidates for therapeutic targeting. Dissection of the molecular mechanisms governing the biological properties of these proteins is being actively pursued by an expanding network of scientists around the globe who will meet this year at the 5th International Workshop on the CCN family of Genes, organized by the International CCN Society ( http://ccnsociety.com ), home for an international cadre of collaborators working in the CCN field.
The N‐terminal Region of α‐Dystroglycan is an Autonomous Globular Domain (1997)

The structure of the N-terminal region of mouse alpha-dystroglycan (DGN) was investigated by expression of two protein fragments (residues 30-180 and 30-438) in Escherichia coli cells. Trypsin susceptibility experiments show the presence of a stable alpha-dystroglycan N-terminal region (approximately from residue 30 to 315). In addition, guanidinium hydrochloride (Gdn/HCl) denaturation of DGN-(30-438)-peptide, monitored by means of tryptophan fluorescence, produces a cooperative transition typical of folded protein structures. These results strongly suggest that the alpha-dystroglycan N-terminal is an autonomous folding unit preluding a flexible mucin-like region and that its folding is not influenced by the absence of glycosylation. In order to obtain more information on the structural features of the N-terminal domain we have also used circular dichroism, analytical sedimentation and electron microscopy analysis. Circular dichroic spectra show the absence of typical secondary structure (e.g. alpha-helix or beta-sheet) and closely resemble those recorded for loop-containing proteins. This is consistent with a sequence similarity of the alpha-dystroglycan domain with the loop-containing protein elastase. Analytical ultracentrifugation and electron microscopy analysis reveal that the N-terminal domain has a globular structure. DGN-(30-438)-peptide does not bind in the nanomolar range to an iodinated agrin fragment which binds with high affinity to tissue purified alpha-dystroglycan. No binding was detected also to laminin. This result suggests that the alpha-dystroglycan N-terminal domain does not contain the binding site to its extracellular matrix binding partners. It is less likely than the lack of glycosylation reduces its binding affinity, because the N-terminal globular domain only contains two glycosylation sites.
Degenerate PCR-Based Cloning Method for Eph Receptors and Analysis of Their Expression in the Developing Murine Central Nervous System and Vasculature (2001)

Eph receptors and their membrane-associated ephrin ligands regulate cell-cell interactions during development. The biochemical and biologic functions of this receptor tyrosine kinase family are still being elucidated but include roles in nervous system segmentation, axon pathfinding, and angiogenesis. To isolate murine orthologs of three zebrafish Eph family members (zek1, zek2, and zek3), we have used a degenerate RT-PCR-based cloning method specific for members of the Eph family. Although this method was effective for isolation of Eph receptor cDNAs, including members of both the A and B subfamilies, our results suggested that zek1 may not have a murine ortholog. The isolated cDNAs were also used to generate RNA in situ hybridization probes to examine the expression patterns of murine EphA2, A3, A4, A7, B1, B2, and B4 in 9.5-dpc mouse embryos. In addition to the expected abundant expression of these Eph receptors in the developing CNS and the presence of EphB receptors in vascular tissues, several of the EphA receptors were expressed in discrete regions of the developing vasculature. These results suggest a role for both EphA and EphB receptors in vascular development.
Functional Structure of Adipocytes Differentiated from Human Umbilical Cord Stroma-Derived Stem Cells (2008)

It has been previously demonstrated that human umbilical cord stroma-derived stem cells (HUCSCs) are competent to differentiate into adipocytes. However, controversies have arisen as to whether HUCSCs can become mature adipocytes or not, and to what extent these cells can be induced in adipogenic pathway. Here, we extensively analyzed their adipogenic potency with a structural and functional approach by determining lipid formation dynamics in concordance to adipocyte-specific markers. During a 35-day period, HUCSCs respond to adipogenic induction, at which point 88% of cells exhibited multilocular lipid granules (LGs) having a mean diameter of 3 mum in round-shaped, F-actin-poor cells. Although the 1st week of induction did not generally display typical lipidogenic phenotypes, the degree of adipogenesis was dissected and confirmed by mRNA expressions of peroxisome proliferator-activated receptor gamma, C/EBP-beta, sterol regulatory element-binding transcription factor 1, adipophilin, stearoyl-CoA desaturase, glycerol 3-phosphate dehydrogenase 1, LIPE, adiponectin, and leptin. All markers tested were found elevated in various amounts (3-70-fold) around day 7 and reached a plateau after day 14 or 21 (5-335-fold). Perilipin as a surface protein around the LGs was confined exclusively to the enlarging LGs. Conclusively, we propose that after the termination of proliferation, HUCSCs possess the biochemical and cellular machinery to successfully differentiate into maturing adipocytes under adipogenic conditions, and this feature will ultimately allow these fetus-derived stem cells to be used for various therapeutic or esthetic purposes.