gebhart/patrepeval huggingface dataset:
Practical synthesis of cyclic peptides, with an example of dependence of cyclization yield upon linear sequence (1979)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPractical synthesis of cyclic peptides, with an example of dependence of cyclization yield upon linear sequenceStephen F. Brady, Sandor L. Varga, Roger M. Freidinger, Debra A. Schwenk, Michael Mendlowski, Frederick W. Holly, and Daniel F. VeberCite this: J. Org. Chem. 1979, 44, 18, 3101–3105Publication Date (Print):August 1, 1979Publication History Published online1 May 2002Published inissue 1 August 1979https://pubs.acs.org/doi/10.1021/jo01332a003https://doi.org/10.1021/jo01332a003research-articleACS PublicationsRequest reuse permissionsArticle Views965Altmetric-Citations132LEARN 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
Adenosine and adenosine receptors in the immunopathogenesis and treatment of cancer (2017)

Tumor cells overcome anti-tumor responses in part through immunosuppressive mechanisms. There are several immune modulatory mechanisms. Among them, adenosine is an important factor which is generated by both cancer and immune cells in tumor microenvironment to suppress anti-tumor responses. Two cell surface expressed molecules including CD73 and CD39 catalyze the generation of adenosine from adenosine triphosphate (ATP). The generation of adenosine can be enhanced under metabolic stress like tumor hypoxic conditions. Adenosine exerts its immune regulatory functions through four different adenosine receptors (ARs) including A1, A2A, A2B, and A3 which are expressed on various immune cells. Several studies have indicated the overexpression of adenosine generating enzymes and ARs in various cancers which was correlated with tumor progression. Since the signaling of ARs enhances tumor progression, their manipulation can be promising therapeutic approach in cancer therapy. Accordingly, several agonists and antagonists against ARs have been designed for cancer therapy. In this review, we will try to clarify the role of different ARs in the immunopathogenesis, as well as their role in the treatment of cancer.
INTRAVITREAL INJECTION OF LIPOSOME-ENCAPSULATED GANCICLOVIR IN A RABBIT MODEL (1987)

The authors determined the intravitreal clearance of liposome-encapsulated ganciclovir. Liposome-encapsulated ganciclovir (84.1 micrograms/0.1 ml) was injected into the vitreous cavity of New Zealand rabbits, which were killed at 24 hours and 7, 14, and 28 days after injection. Total ganciclovir concentrations in the vitreous, up to 28 days, were higher than ID50 (50% inhibitory dose) for different clinical and laboratory strains of viruses belonging to the herpes simplex family.
Mobile instant messaging through Hubbub (2002)

Associating online buddies with musical notes, Hubbub lets users (on both PCs and handhelds) interact by way of opportunistic impromptu exchanges, even as they move about.
Cloning and Molecular Characterization of an Immunogenic LigA Protein of Leptospira interrogans (2002)

A clone expressing a novel immunoreactive leptospiral immunoglobulin-like protein A of 130 kDa (LigA) from Leptospira interrogans serovar pomona type kennewicki was isolated by screening a genomic DNA library with serum from a mare that had recently aborted due to leptospiral infection. LigA is encoded by an open reading frame of 3,675 bp, and the deduced amino acid sequence consists of a series of 90-amino-acid tandem repeats. A search of the NCBI database found that homology of the LigA repeat region was limited to an immunoglobulin-like domain of the bacterial intimin binding protein of Escherichia coli, the cell adhesion domain of Clostridium acetobutylicum, and the invasin of Yersinia pestis. Secondary structure prediction analysis indicates that LigA consists mostly of beta sheets with a few alpha-helical regions. No LigA was detectable by immunoblot analysis of lysates of the leptospires grown in vitro at 30 degrees C or when cultures were shifted to 37 degrees C. Strikingly, immunohistochemistry on kidney from leptospira-infected hamsters demonstrated LigA expression. These findings suggest that LigA is specifically induced only in vivo. Sera from horses, which aborted as a result of natural Leptospira infection, strongly recognize LigA. LigA is the first leptospiral protein described to have 12 tandem repeats and is also the first to be expressed only during infection. Thus, LigA may have value in serodiagnosis or as a protective immunogen in novel vaccines.
[Microbiological studies of a nasal positive pressure respirator with and without a humidifier system]. (1996)

13 patients with obstructive sleep apnea syndrome treated with CPAP-therapy and complicating affections of the nasal and pharyngeal mucosa were enrolled in a randomized cross-over study comparing therapy with a heated humidifier (HC 100, company Fisher & Paykel) and treatment with a heat and moisture exchanger (Typ I, company Dahlhausen). We assessed the bacterial and fungal colonisation of the nasal masks of all patients. Samples of mask rinses were taken after the two treatment periods (2 weeks each) and the period without humidification in between. All microbes were found to have pathological potency. There was no significant difference in the total concentration of the microbes in the different treatment modalities. In a few cases however, gram negative bacteria were detected on the masks during humidification with a heated humidifier, but not with heat and moisture exchangers. Legionella spec. were not detectable in any of the samples. Candida albicans was the only fungus detectable. No patient had any infection of the upper or lower respiratory system associated with humidification therapy.
Dose-Response Relationships in Mice Following Subchronic Exposure to 2,3,7,8-Tetrachlorodibenzo-p-dioxin: CYP1A1, CYP1A2, Estrogen Receptor, and Protein Tyrosine Phosphorylation (1994)

The dose-response relationships for different endpoints in different tissues were compared in response to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) treatment. TCDD was administered 5 days a week for 13 weeks at doses ranging from 1.5 to 150 ng/kg/day to female B6C3F1 mice. Ethoxyresorufin-O-deethylase (EROD) activity, a marker for CYP1A1, was increased in liver, lung, and skin at doses as low as 1.5 ng/kg/day. EROD activity did not attain maximal induction. Liver acetanilide-4-hydroxylase activity, a marker for CYP1A2, was significantly induced at 1.5 ng/kg/day and reached maximal induction at 45 ng/kg/day. TCDD treatment significantly increased the amount of phosphorylated forms of three phosphotyrosyl proteins (pp32, pp34, and pp38) in liver S-20 fractions. Changes in these phosphotyrosyl proteins occurred at 1.5 ng/kg/day and reached maximal induction at 4.5 ng/kg/day. No changes in phosphotyrosyl proteins were observed in skin. Hepatic and uterine estrogen receptor levels were not altered at any of the doses tested. These data indicate that induction of CYP1A1, CYP1A2, and the increases in phosphorylated forms of pp32, pp34, and pp38 are sensitive indicators of TCDD exposure. The dose-response curves for increases in CYP1A1, CYP1A2, and phosphorylated pp32, pp34, and pp38 in liver were different from each other. TCDD produces multiple effects with multiple dose-response curves suggesting that there are events in addition to receptor binding that are endpoint specific, leading to different dose-response relationships.
Rapid renaturation of complementary DNA strands mediated by cationic detergents: a role for high-probability binding domains in enhancing the kinetics of molecular assembly processes. (1991)

The rate of renaturation for complementary DNA strands can be enhanced greater than 10(4)-fold by the addition of simple cationic detergents, and the reaction is qualitatively and quantitatively very similar to that found with purified heterogeneous nuclear ribonucleoprotein A1 protein. Under optimal conditions, renaturation rates are greater than 2000-fold faster than reactions run in 1 M NaCl at 68 degrees C. The reaction is second-order with respect to DNA concentration, and reaction rates approach or equal the rate with which complementary strands are expected to encounter each other in solution. Renaturation can even be observed well above the expected melting temperature of the duplex DNA, demonstrating that some cationic detergents have DNA double-helix-stabilizing properties. The reaction is also extremely rapid in the presence of up to a 10(6)-fold excess of noncomplementary sequences, establishing that renaturation is specific and relatively independent of heterologous DNA. This finding also implies that up to several thousand potential target sequences can be sampled per strand per second. Such reagents may be useful for procedures that require rapid nucleic acid renaturation, and these results suggest ways to identify and design other compounds that increase the kinetics of association reactions. Moreover, this work provides further support for a model relating the existence of flexible, weakly interacting, repeating domains to their function in rapid molecular assembly processes in vitro and in vivo.
Dimerization and the effectiveness of ICAM-1 in mediating LFA-1-dependent adhesion (2001)

Dimeric intercellular adhesion molecule-1 (ICAM-1) binds more efficiently to lymphocyte function-associated antigen-1 (LFA-1) than monomeric ICAM-1. However, it is unknown whether dimerization enhances binding simply by providing two ligand-binding sites and thereby increasing avidity, or whether it serves to generate a single "fully competent" LFA-1-binding surface. Domain 1 of ICAM-1 contains both the binding site for LFA-1, centered on residue E34, and a homodimerization interface. Whether the LFA-1-binding site extends across the homodimerization interface has not been tested. To address this question, we constructed four different heterodimeric soluble forms of ICAM-1 joined at the C terminus via an alpha-helical coiled coil (ACID-BASE). These heterodimeric ICAM-1 constructs include, (i) E34/E34 (two intact LFA-1-binding sites), (ii) E34/K34 (one disrupted LFA-1-binding site), (iii) E34/DeltaD1-2 (one deleted LFA-1-binding site), and (iv) K34/K34 (two disrupted LFA-1-binding sites). Cells bearing activated LFA-1 bound similarly to surfaces coated with either E34/K34 or E34/DeltaD1-2 and with an approximately 2-fold reduction in efficiency compared with E34/E34, suggesting that D1 dimerization, which is precluded in E34/DeltaD1-D2, is not necessary for optimal LFA-1 binding. Furthermore, BIAcore (BIAcore, Piscataway, NJ) affinity measurements revealed that soluble open LFA-1 I domain bound to immobilized soluble ICAM-1, E34/E34, E34/K34, and E34/DeltaD1-D2 with nearly identical affinities. These studies demonstrate that a single ICAM-1 monomer, not dimeric ICAM-1, represents the complete, "fully competent" LFA-1-binding surface.
Disrupting the biofilm matrix improves wound healing outcomes (2015)

By directly targeting the wound biofilm matrix, wound healing outcomes are improved.
Alpha 1(XVIII), a collagen chain with frequent interruptions in the collagenous sequence, a distinct tissue distribution, and homology with type XV collagen. (1994)

We report on the isolation of mouse cDNA clones which encode a collagenous sequence designated here as the alpha 1 chain of type XVIII collagen. The overlapping clones cover 2.8 kilobases and encode an open reading frame of 928 amino acid residues comprising a putative signal peptide of 25 residues, an amino-terminal noncollagenous domain of 301 residues, and a primarily collagenous stretch of 602 residues. The clones do not cover the carboxyl-terminal end of the polypeptide, since the translation stop codon is absent. Characteristic of the deduced polypeptide is the possession of eight noncollagenous interruptions varying in length from 10 to 24 residues in the collagenous amino acid sequence. Other features include the presence of several putative sites for both N-linked glycosylation and O-linked glycosaminoglycan attachment and homology of the amino-terminal noncollagenous domain with thrombospondin. It is of particular interest that five of the eight collagenous sequences of type XVIII show homology to the previously reported type XV collagen, suggesting that the two form a distinct subgroup among the diverse family of collagens. Northern blot hybridization analysis revealed a striking tissue distribution for type XVIII collagen mRNAs, as the clones hybridized strongly with mRNAs of 4.3 and 5.3 kilobases that were present only in lung and liver of the eight mouse tissues studied.
New small-molecule tubulin inhibitors (2001)

Abstract The variety of biological agents directed toward the tubulin system exceeds those acting on DNA, making it an important target for cancer chemotherapy. However, the complicated chemical structures and restricted access to the natural resources, in combination with the development of drug resistance, limit the first generation of natural products. Considerable efforts in the search and synthesis of new synthetic compounds, such as small molecular tubulin inhibitors, gave access to novel potential/promising drugs. Among these substances, two series of novel, easily accessible indole classes were identified as tubulin-destabilizing agents. Owing to the synthetic nature, potent in vitro and in vivo antitumoral activity, and efficacy against multidrug-resistant (MDR) tumors, D-24851 and D-64131 have significant potential in cancer treatment.
Some aspects of proximity searching in text retrieval systems (1992)

Describes and evaluates the proximity search facili ties in external online systems and in-house retrieval software Discusses and illustrates capabilities, syntax and circum stances ot use. Presents measurements of the overheads re quired by proximity for storage, record import time and search time The search strategy narrowing effect of proximity is illustrated by Recall and Precision test results. Usage and problems lead to a number ot design ideas for better imple mentation. some based on existing Boolean strategies. one on the use of weighted proximity to automatically produce ranked output A comparison of Boolean, quorum and proximate term pairs distance is included
The MLL recombinome of acute leukemias in 2013 (2013)

Chromosomal rearrangements of the human MLL (mixed lineage leukemia) gene are associated with high-risk infant, pediatric, adult and therapy-induced acute leukemias. We used long-distance inverse-polymerase chain reaction to characterize the chromosomal rearrangement of individual acute leukemia patients. We present data of the molecular characterization of 1590 MLL-rearranged biopsy samples obtained from acute leukemia patients. The precise localization of genomic breakpoints within the MLL gene and the involved translocation partner genes (TPGs) were determined and novel TPGs identified. All patients were classified according to their gender (852 females and 745 males), age at diagnosis (558 infant, 416 pediatric and 616 adult leukemia patients) and other clinical criteria. Combined data of our study and recently published data revealed a total of 121 different MLL rearrangements, of which 79 TPGs are now characterized at the molecular level. However, only seven rearrangements seem to be predominantly associated with illegitimate recombinations of the MLL gene (≈ 90%): AFF1/AF4, MLLT3/AF9, MLLT1/ENL, MLLT10/AF10, ELL, partial tandem duplications (MLL PTDs) and MLLT4/AF6, respectively. The MLL breakpoint distributions for all clinical relevant subtypes (gender, disease type, age at diagnosis, reciprocal, complex and therapy-induced translocations) are presented. Finally, we present the extending network of reciprocal MLL fusions deriving from complex rearrangements.
A cellular binding site for the Mr 55,000 form of the human plasminogen activator, urokinase. (1985)

The secretion of plasminogen activators has been implicated in the controlled extracellular proteolysis that accompanies cell migration and tissue remodeling. We found that the human plasminogen activator urokinase (Uk) (Mr 55,000 form) binds rapidly, specifically, and with high affinity to fresh human blood monocytes and to cells of the monocyte line U937. Upon binding Mr 55,000 Uk was observed to confer high plasminogen activator activity to the cells. Binding of the enzyme did not require a functional catalytic site (located on the B chain of the protein) but did require the noncatalytic A chain of Mr 55,000 Uk, since Mr 33,000 Uk did not bind. These results demonstrate the presence of a membrane receptor for Uk on monocytes and show a hitherto unknown function for the A chain of Uk: binding of secreted enzyme to its receptor results in Uk acting as a membrane protease. This localizes plasminogen activation near the cell surface, an optimal site to facilitate cell migration.
Preparation and Evaluation of Ibuprofen Solid Dispersion Systems with Kollidon Particles Using a Pulse Combustion Dryer System (2007)

Solid dispersions (SDs) of ibuprofen (IBU) were prepared with four carriers: Kollidon 25, Kollidon 30, Kollidon VA64, and Kollidon CL, using a newly developed pulse combustion dryer system, HYPULCON. Physicochemical properties of the SDs obtained were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscope (SEM), and Fourier transformation IR spectroscopy (FT-IR). Powder X-ray diffraction (PXRD) showed that the crystal diffraction peaks of IBU in SDs disappeared completely, and in differential scanning calorimetry (DSC) curves, the endothermic peaks of IBU in SDs were not observed. Fourier transformation IR spectroscopy (FT-IR) proved that interactions between the drug and carrier existed. These findings demonstrated that IBU changed to an amorphous form in the SDs with the four carriers using the pulse combustion dryer system. The dissolution property of IBU in the SDs was markedly enhanced. The dissolution test showed that after 5 min of dissolution, the concentrations of IBU in the SDs with Kollidon CL as the carrier was 43.81 mug/ml, corresponding to 13.0 times that of pure IBU. So, it is demonstrated that the pulse combustion dryer system is very useful for preparing SDs of IBU with Kollidon of different grades as carriers.
The Plasma Lipoproteins: Structure and Metabolism (1978)

The Hippo pathway was initially discovered in Drosophila melanogaster as a key regulator of tissue growth. It is an evolutionarily conserved signaling cascade regulating numerous biological processes, including cell growth and fate decision, organ size ...Read More
Retinal Disease Expression in Bardet-Biedl Syndrome-1 (BBS1) Is a Spectrum from Maculopathy to Retina-Wide Degeneration (2006)

The cardinal feature of retinal degeneration in BBS1 can show a wide spectrum of disease expression.
E3, a hematopoietic-specific transcript directly regulated by the retinoic acid receptor alpha (1996)

Retinoic acid (RA)-induced maturation mediated by the retinoic acid receptor alpha (RAR alpha) has been implicated in myeloid development. We have used differential hybridization analysis of a cDNA library constructed from the murine RA-inducible MPRO promyelocyte cell line to identify immediate-early genes induced by RA during granulocytic differentiation. E3, one of nine sequences identified, was upregulated in an immediate-early manner, with transcript levels peaking after 60 minutes exposure to RA. E3 transcripts were RA-inducible in HL60 cells, but not in an RA-resistant subclone, HL60R, that harbors a mutated RAR alpha gene. However, when HL60R cells were transduced with a functional copy of the RAR alpha gene, RA induced a 10-fold increase in E3 mRNA levels. E3 transcripts are present in the myeloid, B-lymphoid, and erythroid lineages, absent in nonhematopoietic cells, and encode a highly hydrophobic, potentially phosphorylated polypeptide of unknown function with significant homology to a putative protein expressed in myeloid cells. The murine E3 promoter harbors a single bipartite retinoic acid response element which in transient transfection assays conferred RA sensitivity. These results indicate that E3 is a hematopoietic-specific gene that is an immediate target for the activated RAR alpha during myelopoiesis.
Studies of the release and turnover of a human neutrophil lipocalin (1995)

A 24-kDa protein was purified from human neutrophil extracts and shown to be the newly discovered neutrophil gelatinase-associated lipocalin (NGAL), based on structural and immunochemical data. A specific enzyme-linked immunosorbent assay (ELISA) was developed for the determination of NGAL in human plasma and tissue fluids. Normal human plasma contains 72 micrograms l-1 of NGAL (range 40-109 micrograms l-1) in two main forms, monomer and dimer. 35S-methionine metabolic studies of human neutrophils showed that granulocyte macrophagecolony-stimulating factor (GMCSF) stimulated significant synthesis and secretion of NGAL in a dose- and time-dependent fashion. NGAL was rapidly released as monomer and dimer on incubation of heparinized whole blood with opsonized yeast, reaching a plateau corresponding to about 35% of total cell content after 30 min. Following intravenous injection of 125-iodine labelled NGAL there was a more rapid initial clearance of the monomeric than of the dimeric form; t1/2 10 min vs. 20 min. During the second phase the two forms cleared at similar rates. Severe acute peritonitis was accompanied by a 10-fold increase in NGAL plasma levels and the NGAL level in peritoneal exudates, which reached about 40 mg l-1. There was a good linear correlation between the concentrations of NGAL, leucocyte elastase and NP4 (neutrophil proteinase 4 = P3).
Nanocrystal-Based Light-Emitting Diodes Utilizing High-Efficiency Nonradiative Energy Transfer for Color Conversion (2006)

We report a practical implementation of high-efficiency color conversion in an electrically pumped light-emitting diode (LED) using nonradiative energy transfer. On the basis of a new LED design that offers both strong energy-transfer coupling and efficient carrier injection, we show that a hybrid structure comprising a single monolayer of CdSe nanocrystals assembled on top of an InGaN/GaN quantum well provides nearly 10% color conversion efficiency. This value is significantly higher than that for a traditional absorption-re-emission color-conversion scheme in a similar device structure. Furthermore, these hybrid devices can also provide improved efficiencies, compared not only to phosphor-based structures but also to stand-alone LEDs.