gebhart/patrepeval huggingface dataset:
Pharmacophore/Receptor Models for GABAA/BzR Subtypes (α1β3γ2, α5β3γ2, and α6β3γ2) via a Comprehensive Ligand-Mapping Approach (1999)

Pharmacophore/receptor models for three recombinant GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) have been established via an SAR ligand-mapping approach. This study was based on the affinities of 151 BzR ligands at five distinct (alpha1-3,5,6beta3gamma2) recombinant GABA(A)/BzR receptor subtypes from at least nine different structural families. Examination of the included volumes of the alpha1-, alpha5-, and alpha6-containing subtypes indicated that region L(2) for the alpha5-containing subtype appeared to be larger in size than the analogous region of the other receptor subtypes. Region L(Di), in contrast, appeared to be larger in the alpha1 subtype than in the other two subtypes. Moreover, region L(3) in the alpha6 subtype is either very small or nonexistent in this diazepam-insensitive subtype (see Figure 16 for details) as compared to the other subtypes. Use of the pharmacophore/receptor models for these subtypes has resulted in the design of novel BzR ligands (see 27) selective for the alpha5beta3gamma2 receptor subtype. alpha5-Selective ligand 27 when injected directly into the hippocampus did enhance memory in one paradigm (Bailey et al., unpublished observations); however, systemic administration of either 9 or 27 into animals did not provide an observable enhancement. This result is in complete agreement with the observation of Liu (1996). It has been shown (Liu, 1996; Wisden et al., 1992) that in the central nervous system of the rat (as well as monkeys and pigeons) there are several native subtypes of the GABA(A) receptor which exhibit different functions, regional distributions, and neuronal locations. Although 27 binds more potently at alpha5beta3gamma2 receptor subtypes and is clearly an inverse agonist (Liu et al., 1996; Liu, 1996), it is possible that this ligand acts as an agonist at one or more subtypes. Liu (1996) clearly showed that a number of imidazobenzodiazepines were negative modulators at one subtype and agonists at another. Therefore, selectivity for a particular subtype at this point is not sufficient to rule out some physiological effect at other GABA(A)/BzR subtypes. The inability of 27 to potentiate memory when given systemically is again in support of this hypothesis, especially since alpha1beta2gamma2 subtypes are distributed throughout the brain (Wisden et al., 1992). A drug delivered systemically is far more likely to interact with all subtypes than one delivered to a specific brain region. This observation (systemic vs intrahippocampal) provides further support for the design of more subtype-specific ligands at the BzR to accurately define their pharmacology, one key to the design of new drugs with fewer side effects.
Chemokine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019)

Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [417, 416, 31]) comprise a large subfamily of 7TM proteins that bind one or more chemokines, a large family of small cytokines typically possessing chemotactic activity for leukocytes. Additional hematopoietic and non-hematopoietic roles have been identified for many chemokines in the areas of embryonic development, immune cell proliferation, activation and death, viral infection, and as antibiotics, among others. Chemokine receptors can be divided by function into two main groups: G protein-coupled chemokine receptors, which mediate leukocyte trafficking, and "Atypical chemokine receptors", which may signal through non-G protein-coupled mechanisms and act as chemokine scavengers to downregulate inflammation or shape chemokine gradients [31].Chemokines in turn can be divided by structure into four subclasses by the number and arrangement of conserved cysteines. CC (also known as β-chemokines; n= 28), CXC (also known as α-chemokines; n= 17) and CX3C (n= 1) chemokines all have four conserved cysteines, with zero, one and three amino acids separating the first two cysteines respectively. C chemokines (n= 2) have only the second and fourth cysteines found in other chemokines. Chemokines can also be classified by function into homeostatic and inflammatory subgroups. Most chemokine receptors are able to bind multiple high-affinity chemokine ligands, but the ligands for a given receptor are almost always restricted to the same structural subclass. Most chemokines bind to more than one receptor subtype. Receptors for inflammatory chemokines are typically highly promiscuous with regard to ligand specificity, and may lack a selective endogenous ligand. G protein-coupled chemokine receptors are named acccording to the class of chemokines bound, whereas ACKR is the root acronym for atypical chemokine receptors [32]. There can be substantial cross-species differences in the sequences of both chemokines and chemokine receptors, and in the pharmacology and biology of chemokine receptors. Endogenous and microbial non-chemokine ligands have also been identified for chemokine receptors. Many chemokine receptors function as HIV co-receptors, but CCR5 is the only one demonstrated to play an essential role in HIV/AIDS pathogenesis. The tables include both standard chemokine receptor names [657] and aliases.
Climate and biodiversity impacts of low-density polyethylene production from CO2 and electricity in comparison to bio-based polyethylene (2023)

Plastics are essential materials for modern societies, but their production contributes to significant environmental issues. Power-to-X processes could produce plastics from captured CO<sub>2</sub> and hydrogen with renewable electricity, but these technologies may also face challenges from environmental perspective. This paper focuses on environmental sustainability assessment of CO<sub>2</sub>-based low-density polyethylene (LDPE) compared to bio-based LDPE. Life cycle assessment has been applied to study climate impacts and land use related biodiversity impacts of different plastic production scenarios. According to the climate impact results, the carbon footprint of the produced plastic can be negative if the energy used is from wind, solar, or bioenergy and the carbon captured within the plastic is considered. In terms of biodiversity, land-use related biodiversity impacts seem to be lower from CO<sub>2</sub>-based polyethylene compared to sugarcane-based polyethylene. Forest biomass use for heat production in CO<sub>2</sub>-based polyethylene poses a risk to significantly increase biodiversity impacts. Taken together, these results suggest that CO<sub>2</sub>-based LDPE produced with renewable electricity could reduce biodiversity impacts over 96 % while carbon footprint seems to be 6.5 % higher when compared to sugarcane-based polyethylene.
Sampling field sensor with anisotropic fan-out (2002)

We describe a new common-path, phase-shift, and shearing interferometric device capable of single-shot detection of optical phase profiles. It samples the input field and uses birefringent plates to fan out phase-shifted copies of the samples in the empty space between them. The phase shifts are given by the thickness of the plates and not by the relative position of the components, as in classical interferometers. This makes the device insensitive to vibrations. We recorded repeatability better than lambda/100, even though strong shocks were applied to the air table in proximity to the system. We recorded better than lambda/1000 repeatability under quiet conditions and estimated the accuracy to be better than lambda/3000 at the shot-noise limit. In addition, the device is compact and easy to integrate in a variety of setups that require the measurement of optical phase profiles.
Mid-Infrared Generation by Frequency Down-Conversion Across 1.2 Octaves in a Normally-Dispersive Silicon Wire (2013)

Using four-wave mixing in normally-dispersive mid-infrared silicon nanophotonic waveguides, we demonstrate the conversion of light across more than 1.2 octaves, from the telecom band to a wavelength of 3630 nm.
Smart antennas: state of the art (2006)

Aim of this contribution is to illustrate the state of the art of smart antenna research from several perspectives. The bow is drawn from transmitter issues via channel measurements and modeling, receiver signal processing, network aspects, technological challenges towards first smart antenna applications and current status of standardization. Moreover, some future prospects of different disciplines in smart antenna research are given
Photogenerated Base as Catalyst for Imidization Reactions: Design of Photosensitive Polyimides (1992)

The photogeneration of free amines or diamines from soluble organic precursors such as photoactive 2-nitrobenzyl carbamates is useful for the imidization of polymers containing amic acid or amic ester groups as part of their main-chain or their side-chain. The base-catalyzed reaction occurs at lower temperatures than the noncatalyzed thermal process and is applicable to the patterning of thin film coatings.
Suboptimal control techniques for networked hybrid systems (2004)

In this paper we discuss a feasible solution to the hybrid optimal switching problem, where the measurement and feedback signals are communicated via a network and undergo a constant delay. We utilize the concept of model prediction to compensate for the induced delay and periodic update of state measurements. A bound on the resulting estimation error is provided, and an example is provided to illustrate the method.
Miniaturization of the Diameter of an Integrated ECF Micro Motor (2004)

This paper reports the development of micro motors using Electro-Conjugate Fluids (ECFs). ECF is a kind of dielectric fluids, which produces jet-flow by applying high DC voltage between electrodes inserted in the fluid. By applying the phenomena of ECFs to motor driving principle, simple structure and lightweight micro motors can be realized. We call these motors ECF micro motors. In this study, we designed and fabricated φ5mmI.D. 4-layered and 8-layered DP-RE-type ECF micro motors are miniaturized in order to improve the output power density. Also we investigated the characteristics by experiment in the case of using high performance ECF in order to confirm possibility of improvement of output characteristics. In conclusion, it is confirmed that it is effective to miniaturize ECF micro motor and use high performance ECF for improvement of output characteristics.
Modulation of the Cell Cycle and Induction of Apoptosis in Human Cancer Cells by Synthetic Bile Acids (2006)

In this paper, we will outline the current understanding of cell cycle modulation and induction of apoptosis in cancer cells by natural and synthetic bile acid. Bile acid homeostasis is tightly regulated in health, and their cellular and tissue concentrations are restricted. However, when pathophysiological processes impair their biliary secretion, hepatocytes are exposed to elevated concentrations of bile acids which trigger cell death. In this context, we developed several newly synthesized bile acid derivatives. These synthetic bile acids modulated the cell cycle and induced apoptosis in several human cancer cells similar to natural bile acids. In human breast and prostate cancer cells with different tumor suppressor p53 status, synthetic bile acid-induced growth inhibition and apoptosis were associated with up-regulation of Bax and p21(WAF1/CIP1) via a p53-independent pathway. In Jurkat human T cell leukemia cells, the synthetic bile acids induced apoptosis through caspase activation. In addition to this, the synthetic bile acids induced apoptosis in a JNK dependent manner in SiHa human cervical cancer cells, via induction of Bax and activation of caspases in PC3 prostate cancer cells and induction of G1 phase arrest in the cell cycle in HT29 colon cancer cells. Moreover, they induced apoptosis in four human glioblastoma multiform cell lines (i.e., U-118MG, U-87MG, T98G, and U-373MG) and one human TE671 medulloblastoma cells. In addition to this, a chenodeoxycholic acid derivative, called HS-1200, significantly decreased the growth of TE671 medulloblastoma tumor size and increased life span in non-obese diabetic and severe combined immunodeficient (NOD/SCID) mice. Therefore, these new synthetic bile acids, which are novel apoptosis mediators, might be applicable to the treatment of various human cancer cells.
ICAM-1 Targeted Nanogels Loaded with Dexamethasone Alleviate Pulmonary Inflammation (2014)

Lysozyme dextran nanogels (NG) have great potential in vitro as a drug delivery platform, combining simple chemistry with rapid uptake and cargo release in target cells with "stealth" properties and low toxicity. In this work, we study for the first time the potential of targeted NG as a drug delivery platform in vivo to alleviate acute pulmonary inflammation in animal model of LPS-induced lung injury. NG are targeted to the endothelium via conjugation with an antibody (Ab) directed to Intercellular Adhesion Molecule-1(ICAM-NG), whereas IgG conjugated NG (IgG-NG) are used for control formulations. The amount of Ab conjugated to the NG and distribution in the body after intravenous (IV) injection have been quantitatively analyzed using a tracer isotope-labeled [125I]IgG. As a proof of concept, Ab-NG are loaded with dexamethasone, an anti-inflammatory therapeutic, and the drug uptake and release kinetics are measured by HPLC. In vivo studies in mice showed that: i) ICAM-NG accumulates in mouse lungs (∼120% ID/g vs ∼15% ID/g of IgG-NG); and, ii) DEX encapsulated in ICAM-NG, but not in IgG-NG practically blocks LPS-induced overexpression of pro-inflammatory cell adhesion molecules including ICAM-1 in the pulmonary inflammation.
Silicon-on-insulator polarization splitter using two horizontally slotted waveguides (2010)

We propose and analyze a short-length silicon-on-insulator polarization splitter using two horizontally slotted silicon waveguides. A polarization splitter with a 46.7 microm length and a 22 dB extinction ratio (ER) is achieved. Around 1550 nm, it also exhibits an 18 nm bandwidth for ER>20 dB. The effects of the slot thickness, the waveguide spacing, and the refractive index of the slot on the splitting length and ER are investigated.
Reverse flow in compliant vessels and its implications for the Fontan procedure: numerical studies. (2002)

The Total Cavopulmonary Connection (TCPC), a variant of the Fontan operation used for palliative cardiovascular repair of patients with single ventricle physiology, creates a passive system of blood flow into the pulmonary circulation for which energy efficiency may be critical to long term outcome. Clinical studies have shown that reverse flow in the TCPC is an indication of poor clinical status in these patients. Using numerical simulations, we demonstrate that reverse flow leads to increased energy losses in compliant vessels. Such an effect can potentially set off a series of spiraling negative events with decreased ventricular function leading to reverse flow, which causes decreased energy efficiency, which in turn leads to worsening function, and so forth, thereby suggesting one cause of progressive heart failure in this patient group.
Predictors of postoperative bleeding after vitrectomy for vitreous hemorrhage in patients with diabetic retinopathy (2017)

Abstract Aims/Introduction To clarify the association between perioperative variables and postoperative bleeding in pars plana vitrectomy for vitreous hemorrhage in diabetic retinopathy. Materials and Methods The present retrospective study enrolled 72 eyes of 64 patients who were admitted to Osaka University Hospital between April 2010 and March 2014, and underwent vitrectomy for vitreous hemorrhage as a result of diabetic retinopathy. Results Postoperative bleeding developed in 12 eyes. Using binomial logistic regression analysis, we found that the duration of operation was the only significant variable associated with postoperative bleeding within 12 weeks after vitrectomy. Furthermore, Poisson regression analysis identified fasting blood glucose just before vitrectomy, no treatment with antiplatelet drugs and treatment with antihypertensive drugs, as well as duration of operation, to be significantly associated with the frequency of bleeding within 52 weeks after vitrectomy. Conclusions Long duration of operation can be used to predict bleeding within both 12 and 52 weeks after vitrectomy. In addition, fasting blood glucose just before vitrectomy, no treatment with antiplatelet drugs and treatment with antihypertensive drugs might be risk factors for postoperative bleeding up to 1 year after vitrectomy.
Performance of Silicon Carbide Avalanche Photodiode Arrays and Photomultipliers (2010)

We present recent results on 4H-SiC avalanche photodiode arrays and SiC-based solid-state photomultiplier arrays suitable for ultraviolet and solar-blind light detection. A novel SiC-based photomultiplier array was demonstrated. An additional solar-blind filter enabled a solar photon rejection ratio of more than 106 in combination with 40% quantum efficiency at 280 nm.
Metal-Organic Frameworks: New Fire Retardant for Polymeric Material (2017)

International audience
Equity for Open-Access Journal Publishing (2010)

Scholars write articles to be read--the more access to their articles the better--so one might think that the open-access approach to publishing, in which articles are freely available online to all without interposition of an access fee, would be an attractive competitor to traditional subscription-based journal publishing. But open-access journal publishing is currently at a systematic disadvantage relative to the traditional model. I propose a simple, cost-effective remedy to this inequity that would put open-access publishing on a path to become a sustainable, efficient system, allowing the two journal publishing systems to compete on a more level playing field. The issue is important, first, because academic institutions shouldn’t perpetuate barriers to an open-access business model on principle and, second, because the subscription-fee business model has manifested systemic dysfunctionalities in practice. After describing the problem with the subscription-fee model, I turn to the proposal for providing equity for open-access journal publishing--the open-access compact.
Understanding the User (2017)

Document engineering is all about building systems and tools that allow people to work with documents and document collections. A key aspect is the usefulness and usability of these tools. In this tutorial, we will look at the many different kinds of user studies and user evaluations that can be used to inform the design and improve utility and usability of document engineering applications. The tutorial will be based on actual studies and will also give participants a chance to explore how they might use these techniques in their research or system development.
Concentrated photovoltaics system costs and learning curve analysis (2013)

An extensive set of costs in $/W for the installed costs of CPV systems has been amassed from a range of public sources, including both individual company prices and market reports. Cost reductions over time are very evident, with current prices for 2012 in the range of 3.0 0.7 $/W and a predicted cost of 1.5 $/W for 2020. Cost data is combined with deployment volumes in a learning curve analysis, providing a fitted learning rate of either 18.5% or 22.3% depending on the methodology. This learning rate is compared to that of PV modules and PV installed systems, and the influence of soft costs is discussed. Finally, if an annual growth rate of 39% is assumed for deployed volumes, then, using the learning rate of 20%, this would predict the achievement of a cost point of 1.5 $/W by 2016.
Active Damping Using Distributed Anisotropic Actuators (2010)

A helicopter structure experiences substantial high-frequency mechanical excitation from powertrain components such as gearboxes and drive shafts. The resulting structure-borne vibration excites the windows which then radiate sound into the passenger cabin. In many cases the radiated sound power can be reduced by adding damping. This can be accomplished using passive or active approaches. Passive treatments such as constrained layer damping tend to reduce window transparency. Therefore this paper focuses on an active approach utilizing compact decentralized control units distributed around the perimeter of the window. Each control unit consists of a triangularly shaped piezoelectric actuator, a miniature accelerometer, and analog electronics. Earlier work has shown that this type of system can increase damping up to approximately 1 kHz. However at higher frequencies the mismatch between the distributed actuator and the point sensor caused control spillover. This paper describes new anisotropic actuators that can be used to improve the bandwidth of the control system. The anisotropic actuators are composed of piezoelectric material sandwiched between interdigitated electrodes, which enables the application of the electric field in a preferred in-plane direction. When shaped correctly the anisotropic actuators outperform traditional isotropic actuators by reducing the mismatch between the distributed actuator and point sensor at high frequencies. Testing performed on a Plexiglas panel, representative of a helicopter window, shows that the control units can increase damping at low frequencies. However high frequency performance was still limited due to the flexible boundary conditions present on the test structure.
1A2-I01 Gripping Strategy of Industrial Robot with Abundant Degrees of Freedom : Wrist Control in Consideration of Compensation of Gravity(Robot Hand Mechanism and Grasping Strategy(2)) (2012)

In previous research, we have developed the pneumatic robot arm driven by pneumatic actuators as the versatile end effector of a material handling system. The arm consists of the hand and wrist parts. The hand can grasp various objects without force sensors and feedback control. In industrial fields, the wrist must be able to be controlled with the object held. Therefore we aim to control the wrist motions with the object held. We construct the experimental models of the drive system of the pneumatic robot wrist. We design the control systems using simulations with the constructed models. After that, we try to control the wrist motions with constructed controllers. As a result, we can control the wrist motions with constructed PI controllers. The wrist models are coincident with the motions of the wrist accurately. Therefore, we can get the experimental results that meet the simulation conditions.