Discovery of GPR183 Agonists Based on an Antagonist Scaffold

The G protein-coupled receptor GPR183/EBI2, which is activated by oxysterols, is a therapeutic target for inflammatory and metabolic diseases where both antagonists and agonists are of potential interest. Using the piperazine diamide core of the known GPR183 antagonist (E)-3-(4-bromophenyl)-1-(4-(4-methoxybenzoyl)piperazin-1-yl)prop-2-en-1-one (NIBR189) as starting point, we identified and sourced 79 structurally related compounds that were commercially available. In vitro screening of this compound collection using a Ca²⁺ mobilization assay resulted in the identification of 10 compounds with agonist properties. To enable establishment of initial structure-activity relationship trends, these were supplemented with five in-house compounds, two of which were also shown to be GPR183 agonists. Taken together, our findings suggest that the agonist activity of this compound series is dictated by the substitution pattern of one of the two distal phenyl rings, which functions as a molecular efficacy-switch.     

A transimpedance CMOS multichannel amplifier with a 50 Ω-wideoutput range buffer for high counting rate applications

A fast transimpedance multichannel amplifier has been designed, fabricated in CMOS 1.2-μm technology and tested. Each channel consists of a current sensitive preamplifier followed by a voltage amplification stage and an on-chip buffer able to drive 50 Ω loads with an output range of ±800 mV. Measured peaking time at the output is 40 ns and the circuit recovers to baseline in 90 ns. This results in a counting capability of more than 10⁷ hits/s, Signals of both polarities can be handled. The first two stages consume a total of 2 mW per channel and the 50 Ω buffer consumes another 17 mW. The equivalent noise charge (ENC) is 1100 e^- rms with a slope of 40e^-/pF. The IC is intended for use in gas and solid-state detectors with high particle rate and extensive charge release as in high energy calorimetry     

Labelling 2-D geometric primitives using probabilistic relaxation:reducing the computational requirements

In previous work, an algorithm for matching geometric features was developed. Although the method worked well, it was demanding in computational resources when applied to large problems. The authors now present methods for reducing the computational requirements, without significantly affecting the reliability of the algorithm     

A Scheduling Technique Wireless Personal for Bandwidth Communication Allocation in Networks

Future generation wireless personalcommunication networks (PCN) are expected to providemultimedia capable wireless extensions of fixedATM/B-ISDN. This paper presents a scheduling techniquefor PCN based on TDMA and the leaky bucket regulator, thewell known bandwidth enforcement mechanism for fixedATM. The main objective of the proposed technique is toensure fair and efficient treatment of various types oftraffic on the air interface, includingconstant-bit-rate (CBR) voice and variable-bit-rate(VBR) video. Two alternative priority mechanisms areintroduced and their performance is evaluated. Theperformance comparison of the alternatives reveals aninteresting tradeoff between fairness and quality ofservice (QoS).     

Purification of alcohol dehydrogenase from four genotypes of the olive fruit fly Bactrocera (Dacus) oleae

Two forms of a sampling theorem for concentric circles are established for a bandlimited two-dimensional (2-D) function. The location of the samples is prescribed either on equidistant circles or on the roots of the Bessel function J0( ). Both methods give comparable results, however, the number of samples required for their numerical evaluation is significantly less for the root-sampling formulation.     

Classification of sets of mixed pixels with the hypothesis-testingHough transform

A new method is presented for mixed pixel classification where the classification of groups of mixed pixels is achieved by using the hypothesis-testing Hough transform. The motivation of the work is that some other estimation methods based on robust statistics, such as the standard Hough transform, have been criticised that, although they can cope with the presence of outliers, they give poor performance in the absence of outliers in comparison to the least-squares-error method. The method proposed in the paper is demonstrated using simulated data and proved to perform equally well in the presence and in the absence of outliers. It is also applied to real Landsat TM data     

A Water Balance Derived Drought Index for Pinios River Basin, Greece

This study estimates hydrological drought characteristics using a water balance derived drought index in Pinios river basin, Thessaly, Greece. The concept of hydrological management at subwatershed scale has been adopted because it encompasses the areal extent of a drought event. Fourteen (14) sub-watersheds of Pinios river basin were delineated according to the major tributaries of Pinios river using GIS. For the assessment of hydrological drought, because none of the sub-watersheds have flow gauge stations at their outlets, a six-parameter monthly conceptual water balance model (UTHBAL model), has been applied regionally to simulate runoff for the period October 1960?CSeptember 2002. The synthetic runoff was normalized through Box-Cox transformation and standardized to the mean runoff to produce the water balance derived drought index for hydrological drought assessment. The standardized precipitation index (SPI) at multiple time scales and four indices of the Palmer method (i.e. PDSI, WPLM, PHDI and the Palmer moisture anomaly Z-index) were also calculated to assess hydrological droughts. The results showed that the water balance derived drought index is a good indicator of hydrological drought in all sub-watersheds, since is capable to quantify drought severity and duration. Furthermore, the drought index provides guidance on the selection of an appropriate meteorological drought index for operational hydrological drought monitoring. Hence, SPI at 3- and 6-month timescales and the WPLM could be used along with the water balance derived drought index in risk and decision analyses at the study area.     

2.5D Elastic graph matching

In this paper, we propose novel elastic graph matching (EGM) algorithms for face recognition assisted by the availability of 3D facial geometry. More specifically, we conceptually extend the EGM algorithm in order to exploit the 3D nature of human facial geometry for face recognition/verification. In order to achieve that, first we extend the matching module of the EGM algorithm in order to capitalize on the 2.5D facial data. Furthermore, we incorporate the 3D geometry into the multiscale analysis used and build a novel geodesic multiscale morphological pyramid of dilations/erosions in order to fill the graph jets. We show that the proposed advances significantly enhance the performance of EGM algorithms. We demonstrate the efficiency of the proposed advances in the face recognition/verification problem using photometric stereo.