gebhart/patrepeval huggingface dataset:
Recent advances towards the discovery of ORL-1 receptor agonists and antagonists (2005)

AbstractSince their discovery a decade ago, remarkable progress has been made toward understanding the biological function and significance of the opioid receptor-like-1 (ORL-1) receptor and its endogenous peptide ligand, nociceptin. The human nociceptin receptor, herein referred to as ORL-1, but also known as OP4 (the fourth member of opioid peptide receptor family) or nociceptin/orphanin FQ peptide (NOP) receptor, was first identified as an orphan opioid receptor with close homology to the classical μ-, κ-, and δ-opioid receptors. ORL-1 does not bind endogenous ligands of the other opioid receptors with high affinity, but instead prefers the 17 amino acid peptide nociceptin. The obvious homologies of ORL-1 to opioid receptors, and its ligand nociceptin to opioid peptide ligands, led to a period of intense investigation that resulted in a number of significant reports describing the biology of the receptor and ligand. The emerging pharmacological evidence from these reports suggests that ORL-1 agonists may be clinically useful for treatment of stress, anxiety, substance abuse (opioid and alcohol), anorexia, cachexia, cough, asthma, and possibly neuropathic pain/allodynia. The peripheral effects of nociceptin suggest that agonists may have utility in the treatment of gastrointestinal motility disorders, water retention, and hypertension. ORL-1 antagonists may be useful in enhancing cognitive function and treating locomotor disorders such as Parkinsonism. In addition to research into the fundamental biology of ORL-1 and nociceptin, noteworthy advances have been made in the discovery of new peptide and non-peptide agonists and antagonists of the ORL-1 receptor leading to a better understanding of its involvement in a variety of biological processes. This review highlights the rationale for the development of ORL-1 ligands and recent progress made by different research groups towards the development of peptidic and non-peptidic ORL-1 agonists or antagonists over the last four years. To add perspective on the commercial potential of this research area, the development status of advanced new molecules is addressed together with any pharmacological characterisation of these entities.Keywordsanxietyaryl-piperidinesbenzimidazolyl-piperidinescognitioncoughdiuresislearningmemorymorphinansnociceptinopioid receptor-like (ORL)ORL-1orphanin FQ (OFQ)N/OFQ peptide (NOP)painquinazolinesquinolinesspiro-piperidinesstress
Sound Field Analysis along a Circle and Its Applications to HRTF Interpolation (2008)

In this paper, we are discussing the sampling and interpolation of the sound field in two and three dimensions along a circle. The Fourier domain representation of the sound field is used and an angular sampling theorem is developed for the sampling of the sound field along a circle. Based on these results, HRTF sampling and interpolation are discussed. As recently presented in [2], HRTF interpolation can be looked at in terms of sound field sampling. This method achieves very precise interpolation in terms of mean square error. However, these results are only possible if very finely spaced HRTF measurements are available. In this paper, we are proposing a method to improve interpolation results when the HRTF measurements are more coarsely spaced than dictated by the angular Nyquist theorem. The proposed method interpolates the HRTFs in a subband domain. In subbands where small angular aliasing occurs, the previous method is applied. In the other subbands, interpolation is carried out in a complex temporal envelope domain to avoid aliasing. Simulations with models and measured data show that the proposed algorithm performs significantly better than previous methods in a mean square error sense. 1
Optical System Identification for Passive Electro-Optical Imaging (2019)

A statistical inverse-problem approach is presented for jointly estimating camera blur from aliased data of a known calibration target. Specifically, a parametric Maximum Likelihood (ML) PSF estimate is derived for characterizing a camera's optical imperfections through the use of a calibration target in an otherwise loosely controlled environment. The unknown parameters are jointly estimated from data described by a physical forward-imaging model, and this inverse-problem approach allows one to accommodate all of the available sources of information jointly. These sources include knowledge of the forward imaging process, the types and sources of statistical uncertainty, available prior information, and the data itself. The forward model describes a broad class of imaging systems based on a parameterization with a direct mapping between its parameters and physical imaging phenomena. The imaging perspective, ambient light-levels, target-reflectance, detector gain and offset, quantum-efficiency, and read-noise levels are all treated as nuisance parameters. The Cram'{e}r-Rao Bound (CRB) is derived under this joint model, and simulations demonstrate that the proposed estimator achieves near-optimal MSE performance. Finally, the proposed method is applied to experimental data to validate both the fidelity of the forward-models, as well as to establish the utility of the resulting ML estimates for both system identification and subsequent image restoration.
The crystal and molecular structures of a novel tricyclic cylindrical polyether in uncomplexed and complexed forms (1981)

The strapped porphyrin 7, 17-diethyl-2,8, 12, 18-tetramethyl-3, 13-nonamethylene porphyrin was prepared by 11 2 + 2 synthesis" of the appropriate dipyrromethane. It 11as expected the nine-carbon "strap" would cause non-planarity of the porphyrin core, thus providing a model to examine the importance of doming in the metalloporphyrin oxygenation process.
Real-time dynamic planning to maintain network connectivity in a team of unmanned air vehicles (2011)

As technology progresses, the capability provided by teams of unmanned systems will span all operational domains and become increasingly important in many applications. Teams of unmanned systems can be composed of agents with different capabilities, and must often operate in dynamic environments where the state of tasks is always changing. Effective real-time task allocation is paramount in these situations. Constraints on connectivity of a network of unmanned agents, such as those required to provide realtime remotely sensed data for exploitation, are a major challenge in this planning process. This paper presents the implementation of research performed to extend a real-time task planning approach called the Consensus Based Bundle Algorithm (CBBA), to include planning for communication relays when facing potential network disconnects. The paper implements the algorithm in a flight test experiment with a team of 3 UAVs performing observation tasks out of communication range from the base station. Results show that planning for relays can be performed in real-time and offers increased mission performance over the baseline CBBA algorithm.
Supplementary Table 4 from Activating mTOR Mutations in a Patient with an Extraordinary Response on a Phase I Trial of Everolimus and Pazopanib (2023)

&lt;p&gt;XLSX file 451K, Somatic mutations identified by whole exome sequencing&lt;/p&gt;
A Dithienosilole‐Benzooxadiazole Donor–Acceptor Copolymer for Utility in Organic Solar Cells (2011)

A systematic evaluation of a novel conjugated polymer, bearing alkyl side chains on both the donor and acceptor units, is conducted using nanoscale characterization techniques and device fabrication. How to manage the use of solvent additives to achieve power-conversion efficiencies of up to 3.7% is demonstrated.
Inside Cover: CONFECT: Conformations from an Expert Collection of Torsion Patterns (ChemMedChem 10/2013) (2013)

The inside cover picture shows the conformational ensemble of AMP generated by CONFECT, a novel knowledge-based conformer generator. Conformations are generated by using lists of “usual” torsion angles derived from CSD-based frequency histograms (top left). One of the bioactive conformations of AMP is shown in the binding site of the protein from PDB complex 3TV2 (bottom right). For more details, see the Full Paper by Matthias Rarey et al. on p. 1690 ff.
A multi-level, multi-phase buck converter with shared flying capacitor for VRM applications (2018)

This paper introduces a multiphase high step-down DC-DC converter that is suitable for voltage regulator module (VRM) applications. In particular, this converter is derived from the conventional flying capacitor multilevel converter. Despite being a multiphase topology, the converter contains just a single flying capacitor that reduces voltage swing at the inductor switching nodes. Furthermore, all switches experience a maximum voltage stress of half the input voltage providing benefits such as the use of transistors with better figures of merit (FOM), as well as reduced switching losses. The converter is well suited for high conversion ratios and high load output required by VRMs as the freewheeling path of each phase contains only one switch. The effectiveness of this topology is verified with an experimental prototype with wide input voltage 12V/24V, and load V <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">out</sub> = 1.2 V, I <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">out</sub> ≤ 40 A operating at 500 kHz switching frequency. Peak efficiencies of 93.2% at 16A, and 89.4% at 28A, are attained with inputs at 12 V and 24V, respectively.
Arylcinnamido-propionone conjugates as tubulin polymerization inhibitors and apoptotic inducers (2016)

A series of cinnamido-propionone conjugates (4–6a-h and 7a-f) has been designed, synthesized and evaluated for their anticancer potential against some human cancer cell lines. Among them, conjugates 6d and 6g have shown significant cytotoxic activity against prostate cancer cells (DU-145) displaying IC50 of 7.48 and 8.91 μM respectively. Studies to understand the mechanism of action of 6d and 6g indicate that they inhibit the tubulin polymerization thereby arresting the cell cycle in G2/M phase. Furthermore, studies such as mitochondrial membrane potential and Annexin V-FITC assay suggested that these conjugates 6d and 6g induced cell death by apoptosis. The molecular docking studies suggested that the binding by these conjugates takes place at the colchicine site of the tubulin protein.
Analysis of Endovascular Graft Treatment for Aortoiliac Occlusive Disease (1999)

Endovascular grafts can often be used when conventional procedures are contraindicated or technically impractical. These grafts are a valuable alternative to extraanatomic and aortofemoral bypasses in high-risk patients with aortoiliac occlusive disease and critical ischemia.
Lithographically defined microporous carbon-composite structures (2023)

A microporous carbon scaffold is produced by lithographically patterning a carbon-containing photoresist, followed by pyrolysis of the developed resist structure. Prior to exposure, the photoresist is loaded with a nanoparticulate material. After pyrolysis, the nanonparticulate material is dispersed in, and intimately mixed with, the carbonaceous material of the scaffold, thereby yielding a carbon composite structure.
Ultrafast carrier relaxation dynamics in InN films (2009)

Ultrafast and slow photo-carrier dynamics in InN films were investigated using femtosecond transient measurements. We found the slow component disappears under the optimized condition due to the equilibrium of band filling and bandgap renormalization effects.
Modelling and mitigation of time-zero variability in sub-16nm finfet-based STT-MRAM memories (2014)

Spin-transfer torque magnetic RAM (STT-MRAM) is one of the most promising non-volatile memory technologies and shows potential as an SRAM replacement. However, targeted for advanced CMOS technologies such as the 14nm FinFET node, time-zero variability is a major concern for these memory technologies. In this paper, we investigate the STT-MRAM variability with respect to different technology scenarios. We show the impact of these variations on the bit error rate of the emerging STT-MRAM memories.
Cache Coherency and Storage Management in a Persistent Object System. (1990)

A distributed architecture for the support of programs written in the persistent programming language Napier is described. The architecture consists of a central server containing the stable persistent store and a collection of clients, each executing Napier processes. Since each client has a cache of objects, some of which may be shared with other clients, a protocol is required to ensure that the caches are coherent and that any access of an object will be to the most up-todate copy. This architecture is explicated by following the lifecycle of an object from its &amp;apos;birth&amp;apos; inside a client, through its life in the persistent store and its migration into other clients. Using this vehicle, the coherency protocol and client/server architecture are illustrated and explained.
Measuring the interference at an RFID tag: Where does it have an impact? (2011)

In this paper we consider reader collisions in an Radio Frequency IDentification (RFID) system, especially how interference impacts the ability of a passive UHF tag to respond. We propose two innovative applications for using interference: 1) Blocking a tag response, and 2) cooperative reading of a tag. In order to investigate their applicability we focus on the experimental evaluation, where we impose interference on the download and uplink, respectively, and on both links simultaneously. The results are positive with respect to blocking the tag, where modulated Co-Channel Interference (CCI) shows most effective. Based on the measurements it is however not possible to read a tag cooperatively, i.e. the tag is unable to utilize the interference as an additional energy source.
Temporin B forms hetero-oligomers with Temporin L, modifies its membrane activity and increases the cooperativity of its antibacterial pharmacodynamic profile (2022)

ABSTRACT The pharmacodynamic profile of antimicrobial peptides (AMPs) and their in vivo synergy are two factors that are thought to restrict resistance evolution and ensure their conservation. The frog Rana temporaria secretes a family of closely related AMPs, temporins A-L, as an effective chemical dermal defence. The antibacterial potency of temporin L has been shown to increase synergistically in combination with both temporins B and A but this is modest. Here we show that the less potent temporin B enhances the cooperativity of the in vitro antibacterial activity of the more potent temporin L against EMRSA-15 and that this may be associated with an altered interaction with the bacterial plasma membrane, a feature critical for the antibacterial activity of most AMPs. Addition of buforin II, a histone H2A fragment, can further increase the cooperativity. Molecular dynamics simulations indicate temporins B and L readily form hetero-oligomers in models of Gram-positive bacterial plasma membranes. Patch-clamp studies show transmembrane ion conductance is triggered with lower amounts of both peptides and more quickly, when used in combination, but conductance is of a lower amplitude and pores are smaller. Temporin B may therefore act by forming temporin L/B hetero-oligomers that are more effective than temporin L homo-oligomers at bacterial killing and/or by reducing the probability of the latter forming until a threshold concentration is reached. Exploration of the mechanism of synergy between AMPs isolated from the same organism may therefore yield antibiotic combinations with advantageous pharmacodynamic properties.
Figure S1 from An AIB1 Isoform Alters Enhancer Access and Enables Progression of Early-Stage Triple-Negative Breast Cancer (2023)

&lt;p&gt;A) Sequence alignment of PCR amplicons of genomic DNA spanning exon 4 of AIB1 (UCSC genome browser). Black filled boxes are the sequences that align to the genome and dotted lines represent the missing/deleted sequences. AIB1 in the DCIS-Î"4 cell line is missing part of intron 3 and exon 4. Two deleted regions around exon 4 of AIB1 were identified in the 10A-Î"4 cell line; both are missing exon 4 acceptor site. B) Sanger sequencing of PCR amplicons spanning exons 2, 3, 4, 5 splice junctions. C) AIB1 mRNA between exon 2 and exon 5 in the MCFDCIS-Î"4 cell clones and the parental MCFDCIS cells. D) Western blot shows AIB1 isoforms' protein expression in MCFDCIS-Î"4 cell clones and the parental MCFDCIS cells. E) Schematic of the migration, trans-endothelial invasion and proliferation assays using real time electric cell impedance sensing (ECIS) to detect migrating cells, invasion across an endothelial monolayer or proliferation rate. F) Invasion of DCIS-Î"4-hy across an endothelial monolayer using ECIS compared to parental control DCIS cells. G) Cell proliferation of MCFDCIS (DCIS), DCIS-Î"4 and DCIS-Î"4-hy measured by electric cell impedance sensing (ECIS). A single well coated with electrodes was used to measure real time change in cell impedance as they proliferate over 80 hours (See diagram in S1E). H) Cell proliferation of MCFDCIS and MCF10A parental lines and their AIB1Î"4 expressing counterpart. ***p&lt;0.001.&lt;/p&gt;
Mechanisms of IL-8-induced Ca2+ signaling in human neutrophil granulocytes (1999)

Interleukin-8 (IL-8) plays an important role in the activation of neutrophil granulocytes. Although intracellular Ca2+ signals are essential in this process, they have not been studied in great detail so far. Here, we have measured IL-8-induced Ca2+ signals in single human neutrophil granulocytes using the Ca2+ indicator dye FURA-2 AM and we have investigated the signal transduction that leads to these Ca2+ signals with various pharmacological tools. Our results indicate that IL-8-induced Ca2+ signals consist of at least two components. An initial fast component was followed by a smaller and more persistent one. The initial Ca2+ signal was independent of extracellular Ca2+ . It required the activation of phospholipase C via a pertussis toxin sensitive G-protein and was due to activation of IP3 receptor-coupled Ca2+ release channels. The late phase of the Ca2+ signal was suppressed when extracellular Ca2+ was removed suggesting that it was generated by Ca2+ influx through Ca2+ release-activated Ca2+ (CRAC) channels. This Ca2+ influx may prolong IL-8-induced Ca2+ signals during granulocyte activation.
Real-time estimation of solar irradiation (2023)

Aspects relate to methods, systems, and computer program products for estimating future levels of solar power received at a sensor including receiving, by a processor, a first measured power value at a first time from the sensor, calculating a first value of a dynamic correction factor based on the first measured power value associated with the first time, applying the first value of the calculated dynamic correction factor to a power estimation model, generating a first power estimation value for a second time using the power estimation model, wherein the second time is later than the first time, receiving a second measured power value at the second time, and calculating a second value of a dynamic correction factor based on the second measured power value associated with the second time and the first value of the dynamic correction factor.
VISUAL OUTCOMES FROM PARS PLANA VITRECTOMY VERSUS COMBINED PARS PLANA VITRECTOMY, PHACOEMULSIFICATION, AND INTRAOCULAR LENS IMPLANTATION IN PATIENTS WITH DIABETES (2014)

In diabetic patients, equivalent visual acuity improvement over 4 years was observed after PPV or PPVCE. Visual outcomes and retinopathy progression rates were not significantly different after either intervention, suggesting that PPVCE may be appropriate when indicated in patients with diabetes.
Hosting Byzantine Fault Tolerant Services on a Chord Ring (2010)

In this paper we demonstrate how stateful Byzantine Fault Tolerant services may be hosted on a Chord ring. The strategy presented is fourfold: firstly a replication scheme that dissociates the maintenance of replicated service state from ring recovery is developed. Secondly, clients of the ring based services are made replication aware. Thirdly, a consensus protocol is introduced that supports the serialization of updates. Finally Byzantine fault tolerant replication protocols are developed that ensure the integrity of service data hosted on the ring.
Homomorphic encryption and secure comparison (2008)

We propose a protocol for secure comparison of integers based on homomorphic<br/>encryption.We also propose a homomorphic encryption scheme that can be used in our protocol,<br/>makes it more efficient than previous solutions, and can also be used as the basis of efficient and<br/>general secure Multiparty Computation (MPC). We show how our comparison protocol can be<br/>used to improve security of online auctions, and demonstrate that it is efficient enough to be used<br/>in practice. For comparison of 16 bits numbers with security based on 1024 bits RSA (executed<br/>by two parties), our implementation takes 0.28 sec including all computation and communication.<br/>Using precomputation, one can save a factor of roughly 10.<br/>
Electronic structure, vibrational spectrum, and thermal properties of yttrium nitride: A first-principles study (2011)

Yttrium nitride (YN) is a promising semiconductor for use in metal/semiconductor superlattices for thermoelectric applications. We determine its electronic structure, vibrational spectrum, and thermal properties using first-principles density functional theory (DFT) based simulations with a generalized gradient approximation (GGA) of the exchange correlation energy. We employ GGA+U and GW approximations in our calculations to (a) improve the accuracy of the calculation of bandgaps and (b) determine specific features of its electronic structure relevant to transport properties, such as transverse (mt*) and longitudinal (m1*) conduction band effective mass. To evaluate consequences of forming alloys of YN with other materials to its electronic properties, we have determined the volume deformation potentials. Our results for phonons show a large longitudinal optical (LO) and transverse optical (TO) splitting at the Γ point in the vibrational spectrum with a gap of 325 cm−1 arising from long- range dipole-dipole interactions. We estimate temperature dependent lattice specific heat and lattice thermal conductivity based on Boltzmann transport theory to assess YN’s potential for thermoelectric applications.
Attachment of Polybutadienes to Hydrogen-Terminated Silicon and Post-Derivatization of the Adsorbed Species (2009)

We report the first attachment of polymers with pendant vinyl groups to hydrogen-terminated silicon(111) (Si(111)-H); 1,2-polybutadiene (M(w) = 3200-3500 g/mol) was attached to Si(111)-H under mild conditions at room temperature with visible light. We also report the partial functionalization, in solution, of 1,2-polybutadiene with various thiols using thiol-ene chemistry and the subsequent attachments of these compounds to Si(111)-H. The partially functionalized or unfunctionalized polybutadienes allow further functionalization at the surface through their unreacted carbon-carbon double bonds. We present this as a useful strategy for silicon surface modification. Surfaces were characterized with contact angle goniometry, spectroscopic ellipsometry, X-ray photoelectron spectroscopy (XPS), time-of-flight secondary ion mass spectrometry (ToF-SIMS), and atomic force microscopy (AFM).