Miracle-dz/UniFAR-FTUs huggingface dataset:
Investigation of the interaction between the atypical agonist c[YpwFG] and MOR

Endogenous and exogenous opiates are currently considered the drugs of choice for treating different kinds of pain. However, their prolonged use produces several adverse symptoms, and in addition, many forms of pain are resistant to any kind of therapy. Therefore, the discovery of compounds active towards μ‐opioid receptors (MORs) by alternative pharmacological mechanisms could be of value for developing novel classes of analgesics. There is evidence that some unusual molecules can bind opioid receptors, albeit lacking some of the typical opioid pharmacophoric features. In particular, the recent discovery of a few compounds that showed agonist behavior even in the absence of the primary pharmacophore, namely a protonable amine, led to a rediscussion of the importance of ionic interactions in stabilizing the ligand–receptor complex and in activating signal transduction. Very recently, we synthesized a library of cyclic analogs of the endogenous, MOR‐selective agonist endomorphin‐1 (YPWF‐NH2), containing a Gly5 bridge between Tyr1 and Phe4. The cyclopeptide c[YpwFG] showed good affinity and agonist behavior. This atypical MOR agonist does not have the protonable Tyr amine. In order to gain more information about plausible mechanisms of interaction between c[YpwFG] and the opioid receptor, we synthesized a selected set of derivatives containing different bridges between Tyr1 and Phe4, and tested their affinities towards μ‐opioid receptors. We performed conformational analysis of the cyclopeptides by NMR spectroscopy and molecular dynamics, and investigated plausible, unprecedented modes of interaction with the MOR by molecular docking. The successive quantum mechanics/molecular mechanics investigation of the complexes obtained by the molecular docking procedure furnished a more detailed description of the binding mode and the electronic properties of the ligands. The comparison with the binding mode of the potent agonist JOM‐6 seems to indicate that the cyclic endomorphin‐1 analogs interact with the receptor by way of an alternative mechanism, still maintaining the ability to activate the receptor.
The Chemical Synthesis of Amino Acyl Adenylates

‘I’hc present papcr deals with a description of the mcthod of preparation and partial purification of several amino arid adenylates. Two proccclurcs for the synthesis of these c o m ~ ~ o u ~ i d s have previously been ticscrihd, but these h a w certiiiii disarlv:int.ages for gcncriil aplilication. The first of tlicse iiic.t. liodi-: (I) wliicli lends to tl1e s~~ritllc of the lciicyl, aiaiiyl, cind plicnylnlanyl atlenylates in J.ieltls :tLout 10 per cent, involveti tlic rc1:rction of t,hc xiniiio acid :iryI chloride \\. it11 the silvcr salt of ndcnosinc 5’-phosphate (A5P). ’ In another method, I\-ieland et til. (2) used Ix-valine tliiopiirnol hytlroclil~ride as the :Lcti\-attLcl viiiino acid and they ivere abk to cffcct LL transfer of the i-aline moiety to A5P in yields or 10 to 20 ~ J W c w t . lleccntl y the usefulness of S ~ ~’-clicyclolics~-lcarbocliiniitle for the synthesis of nuclcosidc pyrophosphate derivatives was elegant,ly demonstrated b Khoraiia et ul. (3-5). Earlicr, Zetzclic aiitl Fredrich (ti j had u d thc carbodiimirlcs for tlic synthesis of ca.rbosylic acid anhydr cs. I t seemed, therefore, t , h t the carhodiimides might offer :t ~isrfnl rc.ageiit> for coupling tlic amino acids to A5P by an acyl p1iosph:tte 1iiik:rgc. Soon after our studies wcrc unrlcr way ( 5 ) TnlIwrt, and HuennPkeiis (S) Icported t,hc synthesis of butyryl itdenylatc with DCC. T h e incthod to lie dcscribed here involves the use of DCC to effect a condensntion of thc cnrhosyl group of a free amino acid with the phosphate of adenylic acid in aqueous pyridine. Vsing this procedure the nrlcnjlate derivatives of nand L-methionine, L-iilieii)-lslaiiiiie, L-t,ryptoplian, i ~ n d L-scrine have been prepared and purified.
Re-orientation and faster, directed migration of lens epithelial cells in a physiological electric field.

The vertebrate lens drives current through itself in a pattern which concentrates current efflux at the lens equator. Lens epithelial cells (LECs) move into this region where they change shape and differentiate into lens fibre cells. The mechanisms underpinning these cell behaviors are unclear. We have attempted to mimic, in isolation, the effects which such electrical signals have on LEC behaviors, by culturing LECs in a physiological DC electric field (EF) similar to that in lens. Primary human (PHLECs), primary bovine (PBLECs) and a transformed human cell line (THLECs) all changed shape to lie perpendicular to the EF, the same orientation which LECs adopt with respect to the equatorial EF as they differentiate into lens fibre cells. Exposure to an EF also significantly increased the migration rate of all three LEC types. All three LECs also showed directed cell migration although, curiously, different cell types moved in different directions. PBLECs and THLECs showed voltage-dependent, anode-directed migration, with a response threshold between 100-150 mV mm(-1)and 25-50 mV mm(-1), respectively. Small sheets of THLECs also migrated anodally. By contrast PHLECs migrated cathodally with a response threshold below 100 mV mm(-1). Reversing the polarity reversed the migration direction for each cell type. These observations raise three possibilities: (1) that small electric field may be one of the cues regulating lens epithelial cell behaviors in vivo; (2) that altering the in vivo electric field by lens replacement may contribute to the aberrant migration of epithelial cells in conditions such as posterior capsule opacification and (3) that applying electric fields may be one way of controlling aberrant lens epithelial cell behaviors.
Management practice in Malaysian Smart School: tasks and support analysis of the ICT implementation

This study elucidates the type of management practice carried out and the support received by the Malaysian Smart Schools in the implementation of ICT in their school management. The results revealed that the management tasks related to the students' assessments, time table scheduling, administrative records and financial accounting contributed to most of the ICT usage. The results also showed that the Smart Schools Initiative received considerable support from the relevant governmental agencies, parents and private companies and such continuous support was important to maintain the effective and efficient management practice of the Malaysian Smart Schools.
Assessment of Grape Yield and Composition Using Reflectance‐Based Indices in Rainfed Vineyards

Spectral vegetation indices such as the normalized difference vegetation index (NDVI) have proved to be useful in estimating berry yield and composition in irrigated vineyards that usually experience mild to moderate water deficits. However, their performance is not clear under rainfed conditions. This study explores the relationships between NDVI and berry yield and composition in rainfed vineyards experiencing mild to moderate water stress with respect to the timing of water deficits. The study was conducted on grape (Vitis vinifera L. ‘Chardonnay’). Biophysical variables such as predawn water potential (Ψₚ), canopy minus air temperature difference (ΔTₘ), fractional intercepted photosynthetic active radiation (fIPAR) and canopy reflectance measurements were acquired at veraison and were related to berry yield, total soluble solids (TSS), titratable acidity (TA), and maturity index (IMAD) at harvest. In our study, while NDVI provided consistent estimates of TSS (r² = 0.81) and IMAD (r² = 0.89) when water deficit conditions had a larger incidence before veraison, the water index (WI)–a reflectance-based index of water status–was related to TA (r² = 0.62) and IMAD (r² = 0.67) under post-veraison water deficits. Since early and late water deficits (i.e., before and after veraison) have a differential impact on the determinants of vine photosynthetic activity (i.e., leaf area and stomatal conductance), the capability of NDVI to estimate berry yield and composition might be subject to the extent and timing of water deficits in these rain-fed vineyards.
Habitat-specific effects of food abundance on the condition of ovenbirds wintering in Jamaica.

1. Food availability has been considered one of the most important factors limiting bird populations, yet the effects of food abundance on non-breeding insectivores has rarely been investigated. We studied the effects of food abundance on the body condition of ovenbirds (Seiurus aurocapillus L.), a sexually monomorphic, ground-foraging, Neotropical-Nearctic migrant warbler during two winters in three habitats on their wintering grounds in Jamaica. 2. Prey biomass decreased from early to late winter in all habitats. Concurrently, ovenbird body mass, corrected for differences in structural size, decreased significantly in five of six habitat-year combinations. Only in second growth scrub habitat in the 1995-96 winter did ovenbirds show no decrease in corrected body mass, and during this period there was no significant decrease in ant biomass, the dominant prey item of ovenbirds in all habitats. 3. Significant positive correlations were found between ovenbirds' rate of feather regrowth and the biomass of ants on their home ranges in early winter, and between overwinter change in ovenbird body mass and the biomass of ants on their home ranges in late winter. 4. The results of both the habitat- and home-range-based analyses suggest a similar threshold of ant biomass (2·5-3·0 mg m-2 ), below which ovenbirds did not maintain their body mass. 5. The results suggest that late winter rainfall mediates the biomass of prey abundance, which in turn affects the ovenbirds' overwinter body condition.
Sialic Acid Mutarotation Is Catalyzed by the Escherichia coli β-Propeller Protein YjhT*

The acquisition of host-derived sialic acid is an important virulence factor for some bacterial pathogens, but in vivo this sugar acid is sequestered in sialoconjugates as the α-anomer. In solution, however, sialic acid is present mainly as the β-anomer, formed by a slow spontaneous mutarotation. We studied the Escherichia coli protein YjhT as a member of a family of uncharacterized proteins present in many sialic acid-utilizing pathogens. This protein is able to accelerate the equilibration of the α- and β-anomers of the sialic acid N-acetylneuraminic acid, thus describing a novel sialic acid mutarotase activity. The structure of this periplasmic protein, solved to 1.5Å resolution, reveals a dimeric 6-bladed unclosed β-propeller, the first of a bacterial Kelch domain protein. Mutagenesis of conserved residues in YjhT demonstrated an important role for Glu-209 and Arg-215 in mutarotase activity. We also present data suggesting that the ability to utilize α-N-acetylneuraminic acid released from complex sialoconjugates in vivo provides a physiological advantage to bacteria containing YjhT.
Nonlinear sliding surface based adaptive sliding mode control for industrial emulator

The control of an industrial emulator is one of the interesting problems to look into. In this paper, a high performance nonlinear sliding surface based strategy is combined with an adaptive tuning algorithm to achieve low overshoot, short settling time, robustness against disturbance, chattering reduction, as well as minimum control effort where the prior knowledge of uncertainty bound is not required. The designed sliding surface increases the damping ratio of the closed-loop system as the states approach the setpoint. Initially the system is lightly damped resulting in a quick response and as the states approach the setpoint, the system is overdamped to avoid overshoot. In adaptive sliding mode strategy, control gain is dynamically adapted, to be as small as possible but sufficient enough to counteract the uncertainties. Since chattering magnitude is proportional to the controller gain, using the adaptive gain, chattering can be further reduced. Effectiveness of the proposed method is validated in simulation as well as by experiment.
An isochore map of human chromosomes data

data Supplementary http://www.genome. org/cgi/content/full/16/4/536/DC1 "Supplemental Research Data" References http://www.genome. org/cgi/content/full/16/4/536#References This article cites 40 articles, 8 of which can be accessed free at: IOA Freely available online through the Genome Research Open Access option. service Email alerting click here top right corner of the article or Receive free email alerts when new articles cite this article sign up in the box at the
Intestinal mucoadhesive devices for oral delivery of insulin

Abstract Oral delivery of proteins such as insulin has been a long‐lasting challenge owing to gastrointestinal degradation and poor permeability of therapeutic macromolecules across biological membranes. We have developed mucoadhesive intestinal devices for oral delivery of insulin to address this challenge. Here we demonstrate a combination of intestinal devices and a permeation enhancer, dimethyl palmitoyl ammonio propanesulfonate (PPS), for oral delivery of insulin. The devices were delivered from a capsule coated with a pH‐responsive enteric coating. The devices adhere to intestinal mucosa, release their protein load unidirectionally, and prevent enzymatic degradation in the gut. Devices were found to completely release their drug load within 3–4 hr and showed excellent strength of mucoadhesion to porcine intestine. Devices loaded with insulin and PPS significantly decreased blood glucose levels by 30 and 33% in diabetic and nondiabetic rats, respectively. These studies demonstrate that intestinal mucoadhesive devices are a promising oral alternative to insulin injections and therefore should be further explored for the treatment of diabetes.
Impact of anti-poaching approaches for the success of Rhino conservation in Chitwan National Park, Nepal

Nepal has succeeded in granting better protection for its Asian rhino population that has become exemplary in the world. Effective law enforcement along with community participation has been acclaimed as a reason for this achievement. However, there have been very few studies to assess the effectiveness of current anti-poaching strategies. In this study, we assessed the performance of SMART patrolling and population trend of rhino in Chitwan National Park (CNP). The patrol data collected through patrolling logbooks were used to visualize the coverage of SMART in the CNP and its Buffer Zone by dividing it into 1km*1km grid cell. Logistic regression models were used to analyze whether or not the patrol effort and patrol frequency correlate with the reduction in occurrences of illegal activities. A total of 6,593 patrols were conducted within the last fifteen months. Logistic regression models revealed that sites with a greater frequency of patrols, rather than the combined distance walked, had a lower probability of occurrence of illegal activities (βPatrol.frequency= -8.6428 & βPatrol.effort= -4.1804). This implies that patrol frequency was found more significant than patrol efforts in reducing prevalence of illegal activities in and around the CNP. The poaching activities were found high during insurgency period. The trend in rhino poaching was found to be decreased with increase in number of security posts, Community-based Anti-poaching Unit formation, conservation education and sweeping/camping operations. To maintain the continuous success in the long-run, it is crucial to regulate and enhance effective law enforcement capability and more advance techno-based modality in close coordination with stakeholders including community institutions.
Investigation on Boundary Layer Ingestion Propulsion for UAVs

Power reduction is one of the most current important issues. One promising way is to use boundary layer ingestion propulsion. In order to evaluate the benefits of using boundary layer ingestion propulsion in reduction of power consumption and to understand the difference between the propeller placed behind and in front of a fuselage, a comparison is made between propeller placed behind and in front of a fuselage. It is found that the backward position has less drag and power consumption. Power saving coefficient reached 21.7% compared to the forward position and drag coefficient is 28.5% less. Also it shows tendency to stabilize and prevent separation of the boundary layer.
Intelligent adaptation for UEC video/voice over IP with access control

In this paper, we introduce a high-performance real-time video/voice over IP VVoIP application implemented by Ubuntu enterprise cloud UEC, denoted UEC-VVoIP. It is much easer to use than the earlier work of P2P connection VVoIP called P2P-VVoIP does. This is because user does not need to key-in a real IP and a web interface using TCP-based RMTP protocol achieves a friendly GUI. Furthermore, computation load has been moved to cloud computing server rather than in user device. Thus, this approach reduces computation load and power consumption dramatically at user device. Meanwhile, we have employed adaptive network-based fuzzy inference system ANFIS together with particle swarm optimisation PSO to properly tune seamless handoff and analyse network traffic over time. As a result, it takes around 1.589 sec for the seamless handoff among different base stations in wireless mobile network. Cloud computing server with access control accomplishes rapid face recognition and fingerprint identification successfully within 2.15 seconds to identify the permitted user. Finally, the experiment result shows that the performance of our proposed approach is better than the earlier work of Hadoop-VVoIP and P2P-VVoIP.
Outbreak of cryptosporidiosis in a day-care center.

An outbreak of diarrhea due to infection with Cryptosporidium occurred in a day-care center. During a period of 2 months, 23 of 53 (43%) children attending the day-care center and 15 of 104 (14%) household contacts had diarrhea. Cryptosporidium oocysts were identified in 13 of 20 (65%) symptomatic children tested compared with three of 27 (11%) asymptomatic children (chi 2 = 12.56, P less than .001). Enteropathogenic bacteria, enteroviruses, rotavirus, and other protozoan parasites were ruled out as the cause of the diarrhea. A history of diarrhea in household contacts was associated with excretion of Cryptosporidium oocysts by the children. Human-to-human transmission of the infection was suggested by the epidemiology.
Factors affecting wildlife – vehicle collision on the expressway in a suburban area in northern Poland

Wildlife–vehicle collisions (WVC) pose a serious socio-economic and traffic safety issue. We investigated factors affecting the location and number of WVC on the expressway “Tri-City Bypass” in a suburban area in N Poland. We analysed WVC with large-sized (LSM; ungulates; 54% of roadkills) and small-sized mammals (SSM; mainly carnivores; 46% of roadkills) and both groups combined (AM). We identified WVC hotspots and analysed factors affecting their spatial distribution with Poisson regression based on four sets of landscape and road-related features (area, patchiness, presence and other features). The most frequent mammal victims of WVCs were wild boar Sus scrofa (31%), roe deer Capreolus capreolus (21%) and European badger Meles meles (13%), among LSM, and red fox Vulpes vulpes (27%) among SSM. In general, our results indicated that most WVCs occurred in areas with a higher number of forest patches and a higher total length of forest edge (AM, LSM), in curvy sections of the road (LSM). The number of WVCs was lower in locations covered by urbanized areas and grassland (LSM), in the sections with fences, exits and overpasses (LSM, AM). The road sections where there is a higher risk of severe collisions (involving large species) are situated in areas where the Tri-City Bypass bisects a highly forested area, which serve as movement corridors for LSM between fragmented forest complexes. We conclude that the number of WVCs can be reduced by preventing animals from accessing the road and ensuring a safe road crossing. This could be achieved by extending fencing and retrofitting some existing underpasses.
ASSESSMENT OF A VIRTUAL POWER AND STORAGE PLANT FOR PROVISION OF MARKET-DRIVEN AND REGULATED ACTIVITIES

Distributed renewable generation challenge the traditional planning and operation paradigm of distribution networks, demanding strategies of active network management and operational flexibility. Distributed Energy Storage Systems (DESS) will play an important role under current and future renewables integration levels, providing multiple services within the electric sector structure, both regulated and marketdriven. In fact, performing a single service is often recognized as insufficient for DESS to surpass its costs. This work introduces the concept of Virtual Power and Storage Plant (VPSP) which represents an aggregator of renewables and DESS connected in the same medium voltage distribution network. The objective is to optimally coordinate the distributed storage systems to increase their operational and economic value.
Pushing the branch predictability limits with the multi-poTAGE+SC predictor

This paper describes the conditional branch predictor that the authors submitted to the unlimited-size track of the 4th Championship Branch Prediction. The multi-poTAGE+SC predictor which we submit combines the multi-poTAGE and TAGE-SC predictors that were submitted separately to CBP-4 by the first and second authors respectively. Both multi-poTAGE and TAGE-SC are based on the TAGE predictor. We combine them by replacing the TAGE component in TAGE-SC with the multi-poTAGE.
A comparative evaluation of Oratest with the microbiological method of assessing caries activity in children

Aims: The aim of this study is to find out whether Oratest can be used as a diagnostic tool in assessing the caries activity by evaluating its relationship to the existing caries status and the salivary streptococcus mutans level. Materials and Methods: The study sample consists of 90 students divided into two groups. Group I (test group) and Group II (control group) consisting of 30 children for control group and 60 children for test group. The sampling of unstimulated saliva for the estimation of streptococcus mutans was done as per the method suggested by Kohler and Bratthall. The plates were then incubated. Rough surface colonies were identified as streptococcus mutans on a pre-determined area of the tip (approximately 1.5 cm2) were counted for each side of spatula pressed against mitis salivarius bacitracin agar using digital colony counter. The results were expressed in colony forming units (CFU). Oratest was carried out in the same patients after the collection of salivary sample for the microbiological method to evaluate the relationship between the two tests. Statistical Analysis Used: The tests used were ANOVA, Pearson Chi-square test, Pearson′s correlation analysis, Mann-Whitney U test and Student′s independent t-test. Results: In the control group and test group, when the streptococcus mutans count (CFU) and Oratest time (minutes) were correlated using Pearson′s correlation analysis, the streptococcus mutans counts was found to be in a statistically significant negative linear relationship with the Oratest time. When the caries status of the children, participated in the test group were correlated with mutans count (CFU) and Oratest time, caries status were found to be in a statistically significant positive linear relationship with streptococcus mutans count and in a significant negative linear relationship with Oratest time. Conclusions: The test proved to be a simple, inexpensive and rapid technique for assessing caries activity since a significant relationship exists clinically with caries status and microbiologically with the streptococcus mutans count of the individual.