gebhart/patrepeval huggingface dataset:
Dibenzo[b,f]thiepin-10-carbonitrile, its 10,11-dihydro derivative, some transformation products and related compounds (1983)

Reactions of 10-bromodibenzo[ b,f ]thiepin ( IIIa ), its 2-chloro derivative IIIb and 2,8-dichloro derivative IIIc with cuprous cyanide in boiling dimethylformamide gave the carbonitriles Iabc out of which the first two were reduced with sodium borohydride to the 10,11-dihydro derivatives IVab ; the amides VIIab were obtained as by-products. Alkaline hydrolysis of the nitriles IVab or their mixtures with the amides VIIab afforded the acids VIIIab . By the addition of 3-dimethylaminopropylmagnesium chloride to the nitrile Ia cis and trans -11-(3-dimethylaminopropyl)-10,11-dihydrodibenzo[ b,f ]thiepin-10-carbonitriles ( XVIII ) were obtained. Alkylation of the nitrile IVa with 2-dimethylaminoethyl chloride and 3-dimethylaminopropyl chloride resulted in the 10-(dimethylaminoalkyl) derivatives XX and XXI . A reaction of the crude cyano alcohol XXIII with phosphorus tribromide afforded the 2-bromoethyl derivative XXIV as a by-product only. The main product was the hydrobromide of the spirocyclic imidate XXX which affords by acid hydrolysis the spirocyclic lactone XXXI . An analogous sequence proceeding via the ether XXVI and the alcohol XXVII leads to the 10-(3-bromopropyl) derivative XXVIII as the main product. An attempt at preparing the same substance by alkylation of the nitrile IVa with 1,3-dibromopropane gave stereoisomeric dinitriles XXXII . At high doses the amides VIIab reveal an anticonvulsant effect, the acids VIIIab antiinflammatory actions, the basic nitrile cis-XVIII antireserpine activity and the basic nitriles XX and XXI a central depressant and pseudo-analgesic activity in addition to further peripheral and cardiovascular effects.
5′‐Secondary structure formation, in constrast to a short string of non‐preferred codons, inhibits the translation of the pyruvate kinase mRNA in yeast (1989)

The effects of poor codon bias and secondary structure formation upon the translation of the pyruvate kinase (PYK1) mRNA have been investigated in Saccharomyces cerevisiae. Following insertion mutagenesis at the 5'-end of the PYK1 coding region, the gene was transformed into yeast, and translation assessed directly in vivo by determining the distribution of the modified PYK1 mRNAs across polysomes fractionated by sucrose density gradient centrifugation. The chromosomally-encoded (wild-type) PYK1 mRNA, and the actin, ribosomal protein L3 and glyceraldehyde-3-phosphate dehydrogenase mRNAs were used to control for minor differences between polysome preparations. An insertion containing 13 non-preferred codons at the 5'-end of the coding region was found to have no significant effect upon PYK1 mRNA translation. In contrast, translation was inhibited by an insertion which increased the formation of secondary structures at the 5'-end of the mRNA (overall delta G = -36.6 kcal/mol). Control insertions were also analysed to exclude the possibility that alterations to the amino acid sequence of pyruvate kinase affect the translation of its mRNA. These insertions, which introduced preferred codons or restored wild-type levels of secondary structure formation, did not significantly influence PYK1 mRNA translation.
[Afferent stimulation of the tibial nerve in patients with hyperactive bladder]. (2002)

36 patients with overactive bladder (24 with idiopathic detrusor instability; 12 with detrusor hyperreflexia due to multiple sclerosis) underwent percutaneous afferent neuromodulation. The treatment consisted of percutaneous insertion of a 34-gauge solid stainless steel needle at a point of 5 cm cephald from the medial malleolus. The patients were treated weekly for 12 weeks for 30 minutes. A subjective effect was assessed using a dairy. An objective effect was analysed by urodynamic studies. We noticed a decrease in the average voiding frequency, number of leakage episodes and pad use per 24 hours after 12 sessions of the stimulation. Symptomatic improvement of more than 50% was achieved in 28 of 36 patients. No significant adverse events related to the treatment were observed. Thus, stimulation of the posterior tibial nerve is effective in patients with overactive bladder.
REVERSAL OF DIABETES IN RATS USING FETAL PANCREASES STORED AT −196 ,C (1978)

Fetal rat pancreases frozen to and stored at -196 C were used for transplantation into streptozotocin-induced diabetic syngeneic adult recipients. Transplantation was carried out either directly after thawing from -196 C, or after a 21-day growth period in a syngeneic, normoglycemic adult carrier. All transplants were placed under the kidney capsule. A single, frozen fetal rudiment was sufficient to restore blood glucose, urine volume, and urine glucose to normal, provided it had first been grown for 21 days in a normal carrier. It vitro perfusion studies showed that fetal pancreases stored at -196 C were equivalent to fresh rudiments in their responses to a glucose stimulus.
Acquisition of TGF-beta 1 resistance: an important progression factor in human renal cell carcinoma. (1997)

The balance of growth regulation in tumors can be profoundly disturbed by defects in the transforming growth factor-beta 1 (TGF-beta 1) system. Thus far, investigations into the secretion of TGF-beta 1, the expression of its type I, II, and III receptors, as well as the functional intactness of the TGF-beta 1 signal transduction pathways in human renal cell carcinomas (RCC) have been lacking. The objective of the present study, therefore, was to elucidate the role of the TGF-beta 1 system in RCC. We were able to determine the status of this system in 20 primary RCC and in 30 newly established human RCC cell lines of all major histologic types. All primary RCC showed expression of TGF-beta 1 and its type I and II receptors by immunohistochemistry, irrespective of histologic type. In vitro, all RCC cell lines secreted TGF-beta 1 protein as a biologically inactive complex, which cannot interact with cell-surface receptors. Type I ALK-5-receptor mRNA and protein were detected in 29 RCC cell lines, whereas type I ALK-2-receptor mRNA was found in all cell lines. Type II-receptor mRNA and protein could be demonstrated in all cell lines analyzed, and type III-receptor mRNA was observed in five RCC cell lines. Exogenously added, biologically active TGF-beta 1 (1 ng/ml) resulted in significant (p < 0.05) inhibition of proliferation in 14 of 30 RCC cell lines. Sixteen of thirty RCC cell lines, however, proved to be TGF-beta 1-resistant. This resistance could not be explained by mutations in two "hot spot" regions of the type II-receptor gene (bp 622 to 795 and bp 1868 to 2019), as was demonstrated by DNA sequencing in the TGF-beta 1-resistant RCC cell lines. In conclusion, our observations are the first to provide evidence of an "escape" from the negative growth control of TGF-beta 1 by a significant proportion of RCC, suggesting that the acquisition of TGF-beta 1 resistance is an important progression factor for human RCC.
Fall Incidents Detection for Intelligent Video Surveillance (2006)

We present in this paper an intelligent video surveillance system to detect human fall incidents for enhanced safety in indoor environments. The system consists of two main parts: a vision component which can reliably detect and track moving people in the view of a camera, and an event-inference module which parses observation sequences of people features for possible falling behavioral signs. In particular, we extract the aspect ratio of a person as observation feature, based on which fall incidents are detected as abrupt changes in the feature space. Our experiments show that the proposed approach can robustly detect human falls in real time.
A luminescent multicomponent species made of fullerene and Ir(iii) cyclometallated subunits (2007)

The first system containing a luminescent Ir(m) cyclometallated species and a functionalized C60 unit has been prepared; triplet-triplet energy transfer from the Ir-based MLCT state to the C60 triplet state occurs, leading to phosphorescence (lifetime, 4.8 ms) of the derivatized-C60 at 77 K.
Support Vector Machine Technique for the Short Term Prediction of Travel Time (2007)

A vast majority of urban transportation systems in North America are equipped with traffic surveillance systems that provide real time traffic information to traffic management centers. The information from these are processed and provided back to the travelers in real time. However, the travelers are interested to know not only the current traffic information, but also the future traffic conditions predicted based on the real time data. These predicted values inform the drivers on what they can expect when they make the trip. Travel time is one of the most popular variables which the users are interested to know. Travelers make decisions to bypass congested segments of the network, to change departure time or destination etc., based on this information. Hence it is important that the predicted values be as accurate as possible. A number of different forecasting methods have been proposed for travel time forecasting including historic method, real-time method, time series analysis, and artificial neural networks (ANN). This paper examines the use of a machine learning technique, namely support vector machines (SVM), for the short-term prediction of travel time. While other machine learning techniques, such as ANN, have been extensively studied, the reported applications of SVM in the field of transportation engineering are very few. A comparison of the performance of SVM with ANN, real time, and historic approach is carried out. Data from the TransGuide Traffic Management center in San Antonio, Texas, USA is used for the analysis. From the results it was found that SVM is a viable alternative for short-term prediction problems when the amount of data is less or noisy in nature.
Minimal Clinically Important Difference for the UCSD Shortness of Breath Questionnaire (2005)

The MCID calculated using an SEM approach for the SOBQ, CRQ, and QWB meets clinical expectations for these instruments. HRQOL measures provide information that is complementary and distinct from physiological measures.
De novo chromosome formation in rodent cells. (1991)

A hybrid cell line was produced by the fusion of an EC3/7 mouse cell with a Chinese hamster ovary cell. The EC3/7 cell carries a dicentric chromosome with a functional marker centromere. This marker centromere contains human, lambda, and bacterial vector DNA sequences and a dominant selectable gene (aminoglycoside 3'-phosphotransferase type II; neo). In the hybrid, the marker centromere separated from the dicentric chromosome and formed a full-sized chromosome (lambda neo). The newly formed chromosome is stable, even under nonselective culture conditions. This functional chromosome, which is the result of an amplification process, is composed of seven large, different-sized amplicons. Each amplicon contains multiple copies of human, lambda, neo, and mouse telomeric DNA sequences. Individual amplicons are separated from each other by mouse major satellite DNA sequences. The marker centromere was localized to a terminal amplicon by anticentromere immunostaining. The number of amplicons in the newly formed chromosome is remarkably consistent. This finding suggests that the length of the newly formed chromosome is highly constrained.
The transmembrane domain of N-glucosaminyltransferase I contains a Golgi retention signal. (1992)

The enzyme N-acetylglucosaminyltransferase I (NT, EC 2.4.1.101) is a resident type II transmembrane protein of the Golgi apparatus. To delineate the portion of its primary sequence that is responsible for the Golgi retention of this protein, we constructed chimeras containing different N-terminal portions of NT joined to a reporter sequence, the ectodomain of a type II surface membrane protein. These chimeric proteins were found to be retained in the Golgi apparatus as assessed by cell surface biotinylation and immunofluorescence. We found that the transmembrane domain of NT is sufficient to confer Golgi retention of the fusion proteins and propose that it contains the Golgi retention signal of the parent molecule.
Progression of Glomerular Filtration Rate Reduction Determined in Conscious Dahl Salt-Sensitive Hypertensive Rats (2013)

Sequential changes in glomerular filtration rate during development of hypertension in the conscious Dahl salt-sensitive rats were determined using a new method for measurement. Using a miniaturized device, disappearance curves of fluorescein isothiocyanate-sinistrin were measured by transcutaneous excitation and real-time detection of the emitted light through the skin. Rats with implanted femoral venous catheters (dye injection and sampling) and carotid catheters (mean arterial pressure by telemetry) were studied, while maintained on a 0.4% NaCl diet and on days 2, 5, 7, 14, and 21 after switching to 4.0% (high-salt [HS]) diet. A separate group of rats were maintained on 0.4% for 21 days as a time control. Mean arterial pressure rose progressively from the last day of 0.4% (130±2 mm Hg) reaching significance by day 5 of HS and averaged 162±7 mm Hg by day 21. Urine albumin excretion was significantly elevated (×3) by day 7 of HS in Dahl salt-sensitive rats. Glomerular filtration rate reduced on day 14 of HS falling from 1.53±0.06 mL/min per 100 g body weight to 1.27±0.04. By day 21, glomerular filtration rate had fallen 28% to 1.1±0.04 mL/min per 100 g (t(1/2) 28.4±1.1 minute.) No significant reductions of creatinine clearance were observed throughout the study in response to HS demonstrating the insensitivity of creatinine clearance measurements even with creatinine measured using mass spectrometry. We conclude that the observed reduction of glomerular filtration rate was a consequence and not a cause of the hypertension and that this noninvasive approach could be used in these conscious Dahl salt-sensitive rats for a longitudinal assessment of renal function.
HMG2 Interacts with the Nucleosome Assembly Protein SET and Is a Target of the Cytotoxic T-Lymphocyte Protease Granzyme A (2002)

The cytotoxic T-lymphocyte protease granzyme A induces caspase-independent cell death in which DNA single-stranded nicking is observed instead of oligonucleosomal fragmentation. A 270- to 420-kDa endoplasmic reticulum-associated complex (SET complex) containing the nucleosome assembly protein SET, the tumor suppressor pp32, and the base excision repair enzyme APE can induce single-stranded DNA damage in isolated nuclei in a granzyme A-dependent manner. The normal functions of the SET complex are unknown, but the functions of its components suggest that it is involved in activating transcription and DNA repair. We now find that the SET complex contains DNA binding and bending activities mediated by the chromatin-associated protein HMG2. HMG2 facilitates assembly of nucleoprotein higher-order structures by bending and looping DNA or by stabilizing underwound DNA. HMG2 is in the SET complex and coprecipitates with SET. By confocal microscopy, it is observed that cytoplasmic HMG2 colocalizes with SET in association with the endoplasmic reticulum, but most nuclear HMG2 is unassociated with SET. This physical association suggests that HMG2 may facilitate the nucleosome assembly, transcriptional activation, and DNA repair functions of SET and/or APE. HMG2, like SET and APE, is a physiologically relevant granzyme A substrate in targeted cells. HMG1, however, is not a substrate. Granzyme A cleavage after Lys65 in the midst of HMG box A destroys HMG2-mediated DNA binding and bending functions. Granzyme A cleavage and functional disruption of key nuclear substrates, including HMG2, SET, APE, lamins, and histones, are likely to cripple the cellular repair response to promote cell death in this novel caspase-independent death pathway.
The small molecule tyrosine kinase inhibitor NVP-BHG712 antagonizes ABCC10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study (2014)

Paclitaxel exhibits clinical activity against a wide variety of solid tumors. However, resistance to paclitaxel significantly attenuates the response to chemotherapy. The ABC transporter subfamily C member 10 (ABCC10), also known as multi-drug resistance protein 7 (MRP7) efflux transporter, is a major mediator of paclitaxel resistance. Here, we determine the effect of NVP-BHG712, a specific EphB4 receptor inhibitor, on 1) paclitaxel resistance in HEK293 cells transfected with ABCC10, 2) the growth of tumors in athymic nude mice that received NVP-BHG712 and paclitaxel systemically and 3) the pharmacokinetics of paclitaxel in presence or absence of NVP-BHG712. NVP-BHG712 (0.5 μM), in HEK293/ABCC10 cells, significantly enhanced the intracellular accumulation of paclitaxel by inhibiting the efflux activity of ABCC10 without altering the expression level of the ABCC10 protein. Furthermore, NVP-BHG712 (25 mg/kg, p.o., q3d x 6), in combination with paclitaxel (15 mg/kg, i.p., q3d x 6), significantly inhibited the growth of ABCC10-expressing tumors in athymic nude mice. NVP-BHG712 administration significantly increased the levels of paclitaxel in the tumors but not in plasma compared to paclitaxel alone. The combination of NVP-BHG712 and paclitaxel could serve as a novel and useful therapeutic strategy to attenuate paclitaxel resistance mediated by the expression of the ABCC10 transporter.
Human T Cell Leukemia Virus Type 1 Oncoprotein Tax Targets the Human Mitotic Checkpoint Protein MAD1 (1998)

In searching for cellular targets of the HTLV-I oncoprotein Tax, we identified TXBP181, which we characterized as the human homolog of yeast mitotic checkpoint MAD1 protein. Evidence supporting TXBP181 as HsMAD1 includes sequence conservation with yeast MAD1, hyperphosphorylation during S/G2/M phases and upon treatment of cells with nocodazole, and binding to HsMAD2. HsMAD1 functions as a homodimer. It localizes to the centrosome during metaphase and to the spindle midzone and the midbody during anaphase and telophase. Expression of either Tax or a transdominant-negative TXBP181 results in multinucleated cells, a phenotype consistent with a loss of HsMAD1 function. We propose a model of viral transformation in which Tax targets TXBP181, thereby abrogating a mitotic checkpoint.
The putative centromere-forming sequence CM8 is a single copy sequence and is not a component of most human centrnmeres (1992)

Journal Article The putative centromere-forming sequence λCM8 is a single copy sequence and is not a component of most human centrnmeres Get access Katrina F. Cooper, Katrina F. Cooper CRC Cromosome Molecular Biology Group, Department of Biochemistry, University of OxfordSouth Parks Road, Oxford OX1 3QU, UK Search for other works by this author on: Oxford Academic PubMed Google Scholar Chris Tyler-Smith Chris Tyler-Smith * CRC Cromosome Molecular Biology Group, Department of Biochemistry, University of OxfordSouth Parks Road, Oxford OX1 3QU, UK * To whom correspondence should be addressed Search for other works by this author on: Oxford Academic PubMed Google Scholar Human Molecular Genetics, Volume 1, Issue 9, December 1992, Pages 753–754, https://doi.org/10.1093/hmg/1.9.753 Published: 01 December 1992 Article history Received: 23 September 1992 Revision received: 02 October 1992 Accepted: 02 October 1992 Published: 01 December 1992
Increased amounts of double-stranded RNA in the cytoplasm of rat liver following treatment with carcinogens. (1982)

Cytoplasmic RNA was isolated from control rats or at 48 hr following carcinogen administration. A significant quantity (0.6%) of double-stranded RNA was present in control preparations, as assessed by digestion with RNase III. Following carcinogen treatment of rats, this percentage increased significantly. The results suggest that the altered transport of repetitive sequences which is induced by carcinogen treatment involves alterations in the metabolism of double-stranded RNA sequences.
The structure, function and distribution of the mouse TWIK‐1 K+ channel (1997)

The two P domain K+ channel mTWIK-1 has been cloned from mouse brain. In Xenopus oocytes, mTWIK-1 currents are K+-selective, instantaneous, and weakly inward rectifying. These currents are blocked by Ba2+ and quinine, decreased by protein kinase C and increased by internal acidification. The apparent molecular weight of mTWIK-1 in brain is 81 kDa. A 40 kDa form is revealed after treatment with a reducing agent, strongly suggesting that native mTWIK-1 subunits dimerize via a disulfide bridge. TWIK-1 mRNA is expressed abundantly in brain and at lower levels in lung, kidney, and skeletal muscle. In situ hybridization shows that mTWIK-1 expression is restricted to a few brain regions, with the highest levels in cerebellar granule cells, brainstem, hippocampus and cerebral cortex.
Hemorrhagic Transformation of Ischemic Stroke: Prediction with CT Perfusion (2009)

http://radiology.rsnajnls.org/cgi/content/full/250/3/867/DC1.
Biological studies on 1,2-benzisothiazole derivatives VI Antimicrobial activity of 1,2-benzisothiazole and 1,2-benzisothiazolin-3-one derivatives and of some corresponding 1,2-benzisoxazoles. (1996)

Numerous 1,2-benzisothiazole and 1,2-benzisothiazolin-3-one derivatives, variously substituted in the different positions of the molecule, were tested for their in vitro antimicrobial activity. Some corresponding 1,2-benzisoxazoles and 1,2-benzisoxazolin-3-ones were also considered. Several compounds possess a potent and broad antibacterial and antifungal activity, particularly against Gram positive microorganisms, yeasts and dermatophytes. 1,2-Benzisothiazolin-3-ones were found to be the most active substances. On the contrary, the benzisoxazoles and the benzisoxazolin-3-ones considered were devoid of activity. The results obtained are discussed on the basis of structure-activity relationships.
Recombinant canditropsin, an extracellular aspartic protease from yeast Candida tropicalis. Escherichia coli expression, purification, zymogen activation, and enzymic properties. (1993)

A cDNA fragment which encodes the zymogen of canditropsin, the extracellular aspartic protease from the yeast Candida tropicalis (Togni,G., Sanglard, D., Falchetto, R., and Monod, M. (1991) FEBS Lett. 286, 181-185) was cloned into a T7 expression vector for the synthesis of the recombinant zymogen in Escherichia coli. Recombinant canditropsinogen (Ctg), which was expressed as inclusion bodies in the cytosol of E. coli, was refolded by dialysis from an 8 M urea solution and purified to homogeneity using chromatographies on Sephacryl S-300 and on MonoQ columns. The purified Ctg was converted into canditropsin by either acid activation or trypsin conversion. The specificity of the resulting recombinant canditropsin toward polypeptide substrates is significantly different from other aspartic proteases. Canditropsin hydrolyzes oxidized insulin B chain between Ala-Leu and many other minor cleavage sites. Canditropsin also hydrolyzes keratin and collagen, which are components of connective tissues known to be hydrolyzed by canditropsin during Candida infections. Canditropsin was strongly inhibited by the universal aspartic protease inhibitor pepstatin (Ki = 1.75 x 10(-8) M) and inactivated by two aspartic protease inactivators, DAN and EPNP. Canditropsin is weakly inhibited by leupeptin and antipain, with an apparent Ki of 1.74 x 10(-4)M and 1.5 x 10(-5) M, respectively.