gebhart/patrepeval huggingface dataset:
Synthesis of self-immolative glucuronide spacers based on aminomethylcarbamate. Application to 5-fluorouracil prodrugs for antibody-directed enzyme prodrug therapy (1999)

The synthesis of three novel potential glucuronide-based prodrugs for antibody-directed enzyme prodrug therapy (ADEPT) is described. These prodrugs were designed to be activated at the tumour site by β-glucuronidase to afford the corrresponding anticancer agent, 5-FU. The structural pattern of these compounds includes a self-immolative spacer between the glucuronyl residue and the N1 of 5-FU. Three types of spacers have been elaborated which, after enzymic hydrolysis, spontaneously decompose to deliver an unstable N1 aminal 5-FU derivative and, from there, the cytotoxic drug. All potential prodrugs were stable and proved to be excellent substrates of E. coli in in vitro experiments.
Prevention of peroperative hypothermia in abdominal surgery (1986)

It is important to reduce or prevent heat loss during anaesthesia, especially in patients with restricted cardiopulmonary reserves. To test a specially developed esophageal thermal tube (GK-esophageal thermal tube) for this purpose, 33 patients were randomly divided into two groups: Group A were given heat transferred to the central core during operation, using the GK-tube with circulating 41.7 degrees C warm water. Group B received no active warming. All patients were scheduled for major abdominal operation. In both groups there was a temperature fall in the induction phase. In Group B the temperature continued to fall slowly during operation, resulting in a median end-temperature of 34.9 degrees C. In Group A the temperature rose slowly after induction of heat via the tube, resulting in a median end-temperature of 36.8 degrees C in this actively warmed group. The temperature difference is significant (P less than 0.001). The median operating time was 3h 30 min in both groups. After 2 h of anaesthesia the median temperature in Group A was 36.1 degrees C and in Group B 35.0 degrees C. This difference is also significant (P less than 0.001). The described method was easy to use and without complications. We recommend this method to prevent peroperative hypothermia in all patients suspected to have limited cardiopulmonary reserves. The possible hazards and how to avoid these are described.
Automatic UPDRS Evaluation in the Sit-to-Stand Task of Parkinsonians: Kinematic Analysis and Comparative Outlook on the Leg Agility Task (2015)

In this study, we first characterize the sit-to-stand (S2S) task, which contributes to the evaluation of the degree of severity of the Parkinson's disease (PD), through kinematic features, which are then linked to the Unified Parkinson's disease rating scale (UPDRS) scores. We propose to use a single body-worn wireless inertial node placed on the chest of a patient. The experimental investigation is carried out considering 24 PD patients, comparing the obtained results directly with the kinematic characterization of the leg agility (LA) task performed by the same set of patients. We show that i) the S2S and LA tasks are rather unrelated and ii) the UPDRS distributions (for both S2S and LA tasks) across the patients have a direct impact on the observed system performance.
Diffusion through colloidal shells under stress (2009)

The permeability of solids has long been associated with a diffusive process involving activated mechanism as originally envisioned by Eyring. Tensile stress can affect the activation energy but definitive experiments of the diffusion rate of species through a stressed solid are lacking. Here we use core-shell (liquid core-solid shell) colloidal particles that are sensitive to osmotic pressure to follow the permeation of encapsulated probes at various stresses. We unambiguously show that the tensile stress applied on colloidal shells linearly reduces the local energy barrier for diffusion.
Systematic Nanoengineering of Soft Matter Organic Electro-optic Materials (2010)

An overview of the development and utilization of organic electro-optic materials is presented with emphasis on the role played by quantum and statistical mechanical calculations in understanding critical structure/function relationships that have guided the improvement of such materials over the past two decades. This review concentrates largely on three classes of organic electro-optic materials prepared by electric field poling of materials near their glass transition temperature: (1) chromophore/polymer composite materials, (2) dendrimers and polymers containing covalently incorporated chromophores, and (3) matrix-assisted-poling (MAP) materials where specific spatially anisotropic interactions enhance poling efficiency. In particular, the role of chromophore shape, restrictions on chromophore motion associated with covalent bonds, and lattice dimensionality effects are reviewed. The role of device design and auxiliary properties (optical loss, thermal stability, photochemical stability, processability) in influencing the utilization of organic electro-optic materials is also briefly reviewed.
The central interactive region of human MxA GTPase is involved in GTPase activation and interaction with viral target structures (1999)

To define domains of the human MxA GTPase involved in GTP hydrolysis and antiviral activity, we used two monoclonal antibodies (mAb) directed against different regions of the molecule. mAb 2C12 recognizes an epitope in the central interactive region of MxA, whereas mAb M143 is directed against the N-terminal G domain. mAb 2C12 greatly stimulated MxA GTPase activity, suggesting that antibody-mediated crosslinking enhances GTP hydrolysis. In contrast, monovalent Fab fragments of 2C12 abolished GTPase activity, most likely by blocking intramolecular interactions required for GTPase activation. Interestingly, intact IgG molecules and Fab fragments of 2C12 both prevented association of MxA with viral nucleocapsids and neutralized MxA antiviral activity in vivo. mAb M143 had no effect on MxA function, indicating that this antibody binds outside functional regions. These data demonstrate that the central region recognized by 2C12 is critical for regulation of GTPase activity and viral target recognition.
A 40-Gb/s PAM-4 Transmitter Based on a Ring-Resonator Optical DAC in 45-nm SOI CMOS (2017)

The next generations of large-scale data-centers and supercomputers demand optical interconnects to migrate to 400G and beyond. Microring modulators in silicon-photonics VLSI chips are promising devices to meet this demand due to their energy efficiency and compatibility with dense wavelength division multiplexed chip-to-chip optical I/O. Higher order pulse amplitude modulation (PAM) schemes can be exploited to mitigate their fundamental energy-bandwidth tradeoff at the system level for high data rates. In this paper, we propose an optical digital-to-analog converter based on a segmented microring resonator, capable of operating at 20 GS/s with improved linearity over conventional optical multi-level generators that can be used in a variety of applications such as optical arbitrary waveform generators and PAM transmitters. Using this technique, we demonstrate a PAM-4 transmitter that directly converts the digital data into optical levels in a commercially available 45-nm SOI CMOS process. We achieved 40-Gb/s PAM-4 transmission at 42-fJ/b modulator and driver energies, and 685-fJ/b total transmitter energy efficiency with an area bandwidth density of 0.67 Tb/s/mm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> . The transmitter incorporates a thermal tuning feedback loop to address the thermal and process variations of microrings' resonance wavelength. This scheme is suitable for system-on-chip applications with a large number of I/O links, such as switches and general-purpose and specialized processors in large-scale computing and storage systems.
Nitric Oxide and Nitroxides Can Act as Efficient Scavengers of Protein-Derived Free Radicals (2008)

Nitric oxide ((*)NO) may act as either a pro-oxidant or an antioxidant in biological systems. Although (*)NO and nitroxide radicals react slowly with most molecules, they react at near diffusion-controlled rates with other radicals and may therefore be efficient protective agents. This study assessed the ability of (*)NO and nitroxides to intercept specific protein-derived radicals and compared the efficacy of these species. Three protein radical systems were investigated as follows: BSA-derived radicals generated via radical transfer from H(2)O(2)-activated horseradish peroxidase, radicals formed on myoglobin via reaction with H(2)O(2), and carbon-centered radicals formed from amino acid hydroperoxides on exposure to Fe(2+)-EDTA. In each case, radicals were generated in the absence or presence of (*)NO or nitroxides of different size and charge. Concentration-dependent loss of the protein radicals was detected by electron paramagnetic resonance with both (*)NO and nitroxides and time-dependent consumption of (*)NO using an (*)NO electrode. The protein oxidation product dityrosine was significantly reduced by (*)NO and nitroxides, and 3,4-dihydroxyphenylalanine levels were reduced by nitroxides but not (*)NO. Overall, these studies demonstrate that (*)NO and nitroxides are efficient near-stoichiometric scavengers of protein radicals and, hence, are potential protective agents against protein oxidation reactions and resulting damage. These reactions show little dependence on nitroxide structure or charge.
Highly Selective Recognition of Cytosine over Uracil and Adenine by a Guanine Analogue, 2-N-Acetyl-3-deazaguanine, in 2‘-O-Methyl-RNA/RNA and DNA Duplexes (2007)

In this paper, we report a new modified base, 2-N-acetyl-3-deazaguanine (a2c3G), and the synthesis of the 2‘-O-methyl-RNA incorporating a2c3G. It should be noted that a2c3G is the first example of guanine analogues that recognize cytosine more selectively than guanine, keeping the stability of the Watson−Crick base pair essentially unchanged. The higher selectivity might be attributed to the relatively weak hydrogen bonding ability of a2c3G to U in comparison to that of a2c3G−C pair as suggested by the ab initio calculations. Moreover, incorporation of a2c3G destabilized a tandem GA mismatch in a certain sequence probably because, due to the lack of the nitrogen atom, the sheared-type GA pairing was avoided. In combination with the previously reported highly selective artificial nucleobases, such as 2-thiouracil, the a2c3G must become a useful material to develop new hybridization probes or antisense molecules having higher sequence selectivity.
Aging abolishes the renal response to L-arginine infusion in essential hypertension. (1996)

A defect in the endothelium-dependent vasorelaxation could contribute to the development of arterial hypertension through the facilitation of renal vasoconstriction and sodium retention. In this study, we tested the hypothesis that aging impairs kidney function in essential hypertension through a derangement of nitric oxide-dependent renal mechanisms. To this end, we compared the renal response to an intravenous infusion of the precursor of nitric oxide synthesis, L-arginine, in young and aged essential hypertensives. In young hypertensives, L-arginine induced a significant increase in renal plasma flow, glomerular filtration rate, natriuresis and kaliuresis, without changes in filtration fraction. These effects were not observed in aged hypertensives. Neither PRA nor PA were affected by L-arginine infusion in any group. These results indicate that aging produces a derangement of endothelial function in essential hypertension.
Polyphenol‐enriched extract of oil palm fronds (Elaeis guineensis) promotes vascular relaxation via endothelium‐dependent mechanisms (2002)

Plant-based polyphenolic compounds have been reported to possess cardiovascular health benefits. Several dietary sources, including herbs and spices, fruits and vegetables, and tea and wine, contain an array of biologically active compounds that have been shown to be effective in retarding oxidation of low-density lipoproteins (LDL) and promoting vascular relaxation. In the present study four different plant sources, both edible and non-edible, were evaluated for potential activity. Organic extracts enriched in polyphenols were prepared from palm fronds (Elaesis guineensis); lemongrass (Cymbopogon citrates); papaya shoots (Carica papaya) and green chilli (Capsicum frutescenes) and tested for their ability to prevent in vitro oxidation of LDL, and for potential vascular relaxation actions. Rings of rat thoracic aorta and isolated perfused mesenteric vascular beds were mounted in organ baths, contracted using a half-maximal dose of noradrenaline and exposed to cumulative additions of test extracts. Palm frond extract resulted in considerable relaxation (>75%) in both preparations and was found to be endothelium-dependent as removal of endothelium or inhibition of endogenous nitric oxide (NO) led to a total loss in relaxant activity. Lemongrass extract caused a greater relaxation action in the mesenteric preparation compared to aortic rings, and appears to be mediated via NO-independent and non-prostanoid mechanisms. Of the extracts tested, palm fronds also demonstrated the highest antioxidant capacity, as determined by the ferric reducing activity/potential assay, and resulted in a significant delay (P < 0.05) in the oxidation of LDL. Collectively, these preliminary findings lend further support to the potential cardiovascular actions of plant polyphenols and also identify oil palm fronds as containing constituents that promote vascular relaxation via endothelium-dependent mechanisms.
Map‐based cloning of a fertility restorer gene, Rf‐1, in rice (Oryza sativa L.) (2004)

Summary A rice nuclear gene, Rf‐1 , restores the pollen fertility disturbed by the BT‐type male sterile cytoplasm, and is widely used for commercial seed production of japonica hybrid varieties. Genomic fragments carrying Rf‐1 were identified by conducting chromosome walking and a series of complementation tests. Isolation and analysis of cDNA clones corresponding to the fragments demonstrated that Rf‐1 encodes a mitochondrially targeted protein containing 16 repeats of the 35‐aa pentatricopeptide repeat (PPR) motif. Sequence analysis revealed that the recessive allele, rf‐1 , lacks one nucleotide in the putative coding region, presumably resulting in encoding a truncated protein because of a frame shift. Rice Rf‐1 is the first restorer gene isolated from cereal crops that has the property of reducing the expression of the cytoplasmic male sterility (CMS)‐associated mitochondrial gene like many other restorer genes. The present findings may facilitate not only elucidating the mechanisms of male sterility by the BT cytoplasm and its restoration by Rf‐1 but also isolating other restorer genes from cereal crops, especially rice.
Use of polymerase chain reaction for detection of Chlamydia trachomatis (1990)

A polymerase chain reaction (PCR) assay was developed for detection of Chlamydia trachomatis DNA. From the published sequence of the common C. trachomatis plasmid, two primer sets were selected. Detection of amplified sequences was done by agarose gel electrophoresis of cleaved or uncleaved amplified sequences, Southern hybridization, or dot blot analysis. The PCR assay was optimized and, after 40 cycles of amplification with primer set II, demonstrated a sensitivity of 10(-17) g of DNA, which corresponds to the detection of one copy of the plasmid. Because of the high sensitivity, we developed a closed system in which airborne contamination was minimized. Analysis of 228 clinical samples tested by cell culture, IDEIA enzyme immunosorbent assay (Medico-Nobel, Boots-Celltech Ltd., Berkshire, United Kingdom), and PCR showed a sensitivity of 100%, a specificity of 93% when PCR was compared with cell culture, and a corrected specificity of 99% when PCR was compared with cell culture or IDEIA.
Resistance to arginine deiminase treatment in melanoma cells is associated with induced argininosuccinate synthetase expression involving c-Myc/HIF-1α/Sp4 (2009)

Arginine deiminase (ADI)-based arginine depletion is a novel strategy under clinical trials for the treatment of malignant melanoma with promising results. The sensitivity of melanoma to ADI treatment is based on its auxotrophy for arginine due to a lack of argininosuccinate synthetase (AS) expression, the rate-limiting enzyme for the de novo biosynthesis of arginine. We show here that AS expression can be transcriptionally induced by ADI in melanoma cell lines A2058 and SK-MEL-2 but not in A375 cells, and this inducibility was correlated with resistance to ADI treatment. The proximal region of the AS promoter contains an E-box that is recognized by c-Myc and HIF-1alpha and a GC-box by Sp4. Through ChIP assays, we showed that under noninduced conditions, the E-box was bound by HIF-1alpha in all the three melanoma cell lines. Under arginine depletion conditions, HIF-1alpha was replaced by c-Myc in A2058 and SK-MEL-2 cells but not in A375 cells. Sp4 was constitutively bound to the GC-box regardless of arginine availability in all three cell lines. Overexpressing c-Myc by transfection upregulated AS expression in A2058 and SK-MEL-2 cells, whereas cotransfection with HIF-1alpha suppressed c-Myc-induced AS expression. These results suggest that regulation of AS expression involves interplay among positive transcriptional regulators c-Myc and Sp4, and negative regulator HIF-1alpha that confers resistance to ADI treatment in A2058 and SK-MEL-2 cells. Inability of AS induction in A375 cells under arginine depletion conditions was correlated by the failure of c-Myc to interact with the AS promoter.
The effect of the nature of the polymer backbone on the stability and the analytical response of polymer‐modified electrodes (1995)

Abstract The synthesis, characterization, and sensor application of the novel redox polymer [Os(bipy) 2 (PS) 7.5 (DMAP) 2.5 Cl]Cl, where bipy = 2,2′‐bipyridyl, PS = polystyrene, and DMAP = poly[4‐( N ‐methyl‐ N ‐ p ‐vinylbenzylamino) pyridine], are described. The charge transport properties of electrodes modified with the redox material are investigated using cyclic voltammetry and chronoamperometry. The modified electrode behaves as an efficient electrocatalyst for the outer‐sphere reduction of Fe III , with the cross‐exchange reaction occurring at the surface of the polymer ( Sk ″) at concentrations less than 1.0 × 10 −3 mol dm −3 Fe III , with a change over to the St e , kinetic regime at higher substrate concentrations. Direct agreement was observed between the kinetic behavior at rotating disk electrodes and in thin‐layer flow cells. Application of the modified electrodes for the determination of iron in pharmaceutical formulations and the long term stability of the electrodes are investigated. The results obtained are compared with those reported for the analogous metallopolymer [Os(bipy) 2 (PVP) 10 Cl]Cl, where PVP is poly‐4‐vinylpyridine.
Potential bile acid metabolites: IV. Inversion of 7α‐hydroxyl; ursodeoxycholic acid (1981)

Abstract A new method for inversion of chenodeoxycholic to ursodeoxycholic acid which does not involve an intermediary ketone is described. Methyl chenodeoxycholate‐3‐cathylate‐7‐mesylate undergoes a mild reaction with potassium superoxide‐18‐crown ether‐6 in DMSO to give ursodeoxycholic acid in good yield.
Incoherent Ray Tracing without Acceleration Structures (2012)

Recently, a new family of dynamic ray tracing algorithms, called divide-and-conquer ray tracing, has been introduced. This approach partitions the primitives on-the-fly during ray traversal, which eliminates the need for an acceleration structure. We present a new ray traversal method based on this principle, which efficiently handles incoherent rays, and takes advantage of the SSE and AVX instruction sets of the CPU. Our algorithm offers notable performance improvements over similar existing solutions, and it is competitive with powerful static ray tracers.
Slippery Liquid-Infused Porous Surfaces Showing Marine Antibiofouling Properties (2013)

Marine biofouling is a longstanding problem because of the constant challenges placed by various fouling species and increasingly restricted environmental regulations for antifouling coatings. Novel nonbiocidal strategies to control biofouling will necessitate a multifunctional approach to coating design. Here we show that slippery liquid-infused porous surfaces (SLIPSs) provide another possible strategy to obtaining promising antifouling coatings. Microporous butyl methacrylate-ethylene dimethacrylate (BMA-EDMA) surfaces are prepared via UV-initiated free-radical polymerization. Subsequent infusion of fluorocarbon lubricants (Krytox103, Krytox100, and Fluorinert FC-70) into the porous microtexture results in liquid-repellent slippery surfaces. To study the interaction with marine fouling organisms, settlement of zoospores of the alga Ulva linza and cypris larvae of the barnacle Balanus amphitrite is tested in laboratory assays. BMA-EDMA surfaces infused with Krytox103 and Krytox100 exhibit remarkable inhibition of settlement (attachment) of both spores and cyprids to a level comparable to that of a poly(ethylene glycol) (PEG)-terminated self-assembled monolayer. In addition, the adhesion strength of sporelings (young plants) of U. linza is reduced for BMA-EDMA surfaces infused with Krytox103 and Krytox100 compared to pristine (noninfused) BMA-EDMA and BMA-EDMA infused with Fluorinert FC-70. Immersion tests suggest a correlation between the stability of slippery coatings in artificial seawater and fouling resistance efficacy. The results indicate great potential for the application of this concept in fouling-resistant marine coatings.
Chronic irradiation with 222-nm UVC light induces neither DNA damage nor epidermal lesions in mouse skin, even at high doses (2018)

Surgical site infections (SSIs) represent an important clinical problem associated with increased levels of surgical morbidity and mortality. UVC irradiation during surgery has been considered to represent a possible strategy to prevent the development of SSI. 254-nm UVC induces marked levels of DNA damage by generating cyclobutyl pyrimidine dimers (CPD) in microorganisms. However, this effect is elicited not only in microorganisms, but also in human cells, and chronic exposure to 254-nm UVC has been established to represent a human health hazard. In contrast, despite short wavelength-UVC light, especially 222-nm UVC, having been demonstrated to elicit a bactericidal effect, single irradiation with a high dose of 222-nm UVC energy has been reported to not induce mutagenic or cytotoxic DNA lesions in mammalian cells. However, the effect of chronic irradiation with a high dose of 222-nm UVC to mammalian cells has not been determined. In this study, it was demonstrated that large numbers of CPD-expressing cells were induced in the epidermis of mice following treatment with a small amount of single exposure 254-nm UVC, and then less than half of these cells reduced within 24 h. Chronic 254-nm UVC irradiation was revealed to induce sunburn and desquamation in mouse skin. Histological analysis demonstrated that small numbers of CPD-expressing cells were detected only in hyperkeratotic stratum corneum after chronic irradiation with a high dose of 254-nm UVC, and that significant hyperplasia and intercellular edema were also induced in the epidermis of mice. In contrast, chronic irradiation with 222-nm UVC light was revealed not to induce mutagenic or cytotoxic effects in the epidermis of mice. These results indicated that 222-nm UVC light emitted from the lamp apparatus (or device), which was designed to attenuate harmful light present in wavelengths of more than 230 nm, represents a promising tool for the reduction of SSI incidence in patients and hospital staff.