gebhart/patrepeval huggingface dataset:
Concepts for the design of 5‐HT1A serotonin agonists and antagonists (1992)

Abstract The accessibility and use of a standard 5‐HT 1A agonist radioligand ([ 3 H]8‐hydroxy‐2‐(dipropylaminotetralin) has resulted in the availability of a large amount of binding data on various serotonergic agents. This, in turn, has permitted the formulation of structure—affinity relationships (SAFIR). By contrast, much less information is available concerning the agonist and antagonist activity of these agents. This is primarily due to a lack of standard evaluation procedures, controversy regarding the presynaptic versus postsynaptic nature of certain models, and the recent realization that many 5‐HT 1A agents are partial agonists. Thus, it has been difficult to formulate structure—activity relationships (SAR) for these agents. The present review examines the various classes of 5‐HT 1A serotonergic agents and the available data on their 5‐HT 1A agonist and antagonist activity with the aim of formulating SAR. These SAR should provide useful information for the subsequent design of 5‐HT 1A ‐selective agonists and antagonists. © 1992 Wiley‐Liss, Inc.
Low-complex adaptive post filter for enhancement of coded video (2007)

In this paper an adaptive filter that removes de-blocking and de-ringing artifacts and also enhances the sharpness of decoded video, which may be caused by zeroing high-frequency DCT coefficients, is presented. The solution is designed with consideration of mobile equipment with limited computational power and memory. Also, the solution is computationally scalable to be able to handle limited computational resources in different user cases. In the paper it is shown that the adaptive filter always keeps or increases the image quality, compared to the original decoded sequences, and that the amount of sharpening decreases with an decrease of bit-rate to limit amplification of coding artifacts or noise.
Expression of NAD glycohydrolase activity by rat mammary adenocarcinoma cells transformed with rat T cell alloantigen RT6.2 (1994)

RT6.2 is a 26-kDa alloantigen expressed only on post-thymic T cells and attached to the cell membrane through a glycosylphosphatidylinositol (GPI) anchor. It has been reported that expression of RT6.2 in animal models may correlate with lymphopenia and genetically-induced insulin-dependent diabetes mellitus. Its physiological function is unclear. Since RT6.2 has significant amino acid identity with a GPI-anchored rabbit muscle NAD:arginine ADP-ribosyltransferase, RT6.2 was expressed in rat mammary adenocarcinoma cells and the ability of the expressed protein to catalyze ADP-ribose transfer reactions was examined. Cells transformed with the RT6.2 gene expressed NAD glycohydrolase activity that was released from intact cells by phosphatidylinositol-specific phospholipase C, consistent with its presence on the cell surface. A similar activity was not detected with vector-transformed cells. RT6.2 did not ADP-ribosylate simple guanidino compounds. The molecular weight of the phosphatidylinositol-specific phospholipase C-released NAD glycohydrolase, determined by SDS-polyacrylamide gel electrophoresis, was 22,000-24,000, in good agreement with that of native RT6.2. These results strongly suggest that the rat T cell alloantigen RT6.2 is a GPI-anchored NAD glycohydrolase.
Exact synthesis of single-qubit unitaries over Clifford-cyclotomic gate sets (2015)

We generalize an efficient exact synthesis algorithm for single-qubit unitaries over the Clifford+T gate set which was presented by Kliuchnikov, Maslov, and Mosca [Quantum Inf. Comput. 13(7,8), 607–630 (2013)]. Their algorithm takes as input an exactly synthesizable single-qubit unitary—one which can be expressed without error as a product of Clifford and T gates—and outputs a sequence of gates which implements it. The algorithm is optimal in the sense that the length of the sequence, measured by the number of T gates, is smallest possible. In this paper, for each positive even integer n, we consider the “Clifford-cyclotomic” gate set consisting of the Clifford group plus a z-rotation by πn. We present an efficient exact synthesis algorithm which outputs a decomposition using the minimum number of πn z-rotations. For the Clifford+T case n = 4, the group of exactly synthesizable unitaries was shown to be equal to the group of unitaries with entries over the ring Z[eiπn,1/2]. We prove that this characterization holds for a handful of other small values of n but the fraction of positive even integers for which it fails to hold is 100%.
Cyclic Peptides of the Nocardamine Class from a Marine-Derived Bacterium of the GenusStreptomyces (2005)

Two new cyclic peptides (2 and 3) along with the previously reported nocardamine (1) were isolated from the culture broth of an actinomycete of the genus Streptomyces isolated from an unidentified marine sponge. On the basis of the results of combined spectral analyses, the structures of the new compounds were defined to be the dehydroxy and desmethylenyl derivatives of nocardamine, respectively. The new compounds exhibited weak inhibition against the enzyme sortase B.
Dynamic scheduling in antenna array packet radio (2003)

Efficient exploitation of the spatial diversity is fundamentally important to resource critical wireless applications. In this paper, a scheduling protocol for space-division multiple-access (SDMA) wireless packet networks is proposed. The new protocol is "channel-aware" in the sense that it performs scheduling based on terminal spatial characteristics to achieve throughput multiplication and reduction of packet delays. Performance of the system is evaluated and compared to the throughput zipper and lower bounds derived in the paper. Our analytic results show that with scheduling the throughput of the 2-antenna SDMA approaches its upper bound for a large terminal population.
In Vitro Characterization of Conditions for Amyloid-β Peptide Oligomerization and Fibrillogenesis (2003)

Extensive research causally links amyloid-beta peptide (A beta) to Alzheimer's disease, although the pathologically relevant A beta conformation remains unclear. A beta spontaneously aggregates into the fibrils that deposit in senile plaques. However, recent in vivo and in vitro reports describe a potent biological activity for oligomeric assemblies of A beta. To consistently prepare in vitro oligomeric and fibrillar forms of A beta 1-42, a detailed knowledge of how solution parameters influence structure is required. This manuscript represents the first study using a single chemically and structurally homogeneous unaggregated starting material to demonstrate that the formation of oligomers, fibrils, and fibrillar aggregates is determined by time, concentration, temperature, pH, ionic strength, and A beta species. We recently reported that oligomers inhibit neuronal viability 10-fold more than fibrils and approximately 40-fold more than unaggregated peptide, with oligomeric A beta 1-42-induced neurotoxicity significant at 10 nm. In addition, we were able to differentiate by structure and neurotoxic activity wild-type A beta1-42 from isoforms containing familial mutations (Dahlgren, K. N., Manelli, A. M., Stine, W. B., Jr., Baker, L. K., Krafft, G. A., and LaDu, M. J. (2002) J. Biol. Chem. 277, 32046-32053). Understanding the biological role of specific A beta conformations may define the link between A beta and Alzheimer's disease, re-focusing therapeutic approaches by identifying the pernicious species of A beta ultimately responsible for the cognitive dysfunction that defines the disease.
Molecular n‐Type Doping of 1,4,5,8‐Naphthalene Tetracarboxylic Dianhydride by Pyronin B Studied Using Direct and Inverse Photoelectron Spectroscopies (2006)

Abstract Molecular n‐type doping of 1,4,5,8‐naphthalene tetracarboxylic dianhydride (NTCDA) by pyronin B (PyB) is investigated using ultraviolet photoelectron spectroscopy (UPS), inverse photoelectron spectroscopy (IPES), and current–voltage ( I–V ) measurements. Deposition of small amounts (&lt; 2 Å) of PyB on pristine NTCDA films leads to a shift of all the molecular levels away from the Fermi level by nearly 0.20 eV, indicative of n‐type doping of NTCDA by PyB. Interface and bulk energy levels of films formed by co‐evaporation of host and dopant show similarly efficient n‐doping. The spectroscopic measurements are confirmed by I–V measurements, which show a four‐orders‐of‐magnitude increase in current in doped films. The comparison of data obtained from UPS of the neat PyB film with the results of density functional theory calculations confirm that two species of PyB are evaporated and condensed into the solid state, with one species primarily responsible for doping.
Metal and Metal Oxide Nanoparticles in Chemiresistors: Does the Nanoscale Matter? (2005)

Sensor technology is one of the most important key technologies of the future with a constantly increasing number of applications, both in the industrial and in the private sectors. More and more gas sensors are used for the control of technical processes, in environment monitoring, healthcare, and automobiles. Consequently, the development of fast and sensitive gas sensors with small cross sensitivity is the subject of intense research, propelled by strategies based on nanoscience and -technology. Established systems can be improved and novel sensor concepts based on bottom-up approaches show that the sensor properties can be controlled by molecular design. This Review highlights the recent developments and reflects the impact of nanoscience on sensor technology.
A small element from the Mason-Pfizer monkey virusgenome makes human immunodeficiency virus type 1 expression and replicationRev-independent. (1994)

Replication of human immunodeficiency virus type 1 (HIV-1) is dependent on the viral Rev protein. This protein acts in concert with the cis-acting rev-responsive element present in intron-containing RNAs to facilitate nuclear export of these RNAs. Here we show that a cis-acting 219-nucleotide sequence from an unrelated "simple" retrovirus, Mason-Pfizer monkey virus (MPMV), enables Rev-independent HIV-1 replication. This sequence is present in an untranslated region near the 3' end of the MPMV genome. The MPMV element is also able to efficiently substitute for Rev in expression of Gag/Pol and Env proteins from subgenomic constructs. We hypothesize that the MPMV element functions by interacting with a cellular factor that plays a role in mRNA transport analogous to that of the Rev protein. It might be possible to exploit this element in the development of an HIV vaccine.
Disease Control Priorities in Developing Countries (1993)

This first edition provides information on disease control interventions for the most common diseases and injuries in developing countries to help them define essential health service packages. Life expectancy in developing countries increased from forty to sixty-three years between 1950 and 1990 with a concommitant rise in the incidence of noncommunicable diseases of adults and the elderly. It is still necessary to deal with under nutrition and communicable childhood diseases. Also, new epidemic diseases like AIDS are emerging, and the health of the poor during economic crisis is a growing concern. These health developments intensify the need for better information on the effectiveness and cost of health interventions. The information is intended for health practitioners at every level. Individual chapters offer preventive and case management guidelines critical to improving the quality of care. The need for health sector reform is global. Both developed and developing countries, and centrally planned and market oriented health systems share basic dissatisfaction with the present organization and financing of health care delivery and a conviction that there are better ways to obtain results with the available resources. This book attempts to assist health sector reformers to review existing services and adapt them to provide the most cost effective interventions available.
Hepatic alpha 1-adrenergic receptor alteration in a rat model of chronic sepsis. (1986)

Catecholamine therapy is often ineffective in reversing the peripheral vasodilatation and hypotension of septic shock. This suggests that catecholamines might not be able to activate alpha 1-adrenergic receptors to cause vasoconstriction. Despite elevations in endogenous catecholamines, hypoglycemia is also a complication of human sepsis, suggesting that among many other causes, hepatic alpha 1-receptors might be altered. To better understand the pathophysiologic basis for this pharmacologic dilemma, we studied the effect of experimental sepsis on alpha 1-adrenergic receptors in hepatic tissue, a rich source of alpha 1-receptors, from septic and control Sprague-Dawley rats. alpha 1-adrenergic receptors were measured with [3H]-prazosin and data analyzed by a computerized nonlinear least-square regression algorithm. Twenty-four hours following cecal ligation with puncture, a decreased number of alpha 1-adrenergic receptors was noted in crude and purified plasma membrane fractions (23 and 40% reductions respectively) from septic animals. No changes in either agonist or antagonist affinity for receptors from septic animals were noted. These data indicate that the catecholamine refractoriness seen in septic shock may be a result of alterations in alpha 1-adrenergic receptor number or receptor-effector coupling.
Next generation of immune checkpoint therapy in cancer: new developments and challenges (2018)

Immune checkpoints consist of inhibitory and stimulatory pathways that maintain self-tolerance and assist with immune response. In cancer, immune checkpoint pathways are often activated to inhibit the nascent anti-tumor immune response. Immune checkpoint therapies act by blocking or stimulating these pathways and enhance the body's immunological activity against tumors. Cytotoxic T lymphocyte-associated molecule-4 (CTLA-4), programmed cell death receptor-1 (PD-1), and programmed cell death ligand-1(PD-L1) are the most widely studied and recognized inhibitory checkpoint pathways. Drugs blocking these pathways are currently utilized for a wide variety of malignancies and have demonstrated durable clinical activities in a subset of cancer patients. This approach is rapidly extending beyond CTLA-4 and PD-1/PD-L1. New inhibitory pathways are under investigation, and drugs blocking LAG-3, TIM-3, TIGIT, VISTA, or B7/H3 are being investigated. Furthermore, agonists of stimulatory checkpoint pathways such as OX40, ICOS, GITR, 4-1BB, CD40, or molecules targeting tumor microenvironment components like IDO or TLR are under investigation. In this article, we have provided a comprehensive review of immune checkpoint pathways involved in cancer immunotherapy, and discuss their mechanisms and the therapeutic interventions currently under investigation in phase I/II clinical trials. We also reviewed the limitations, toxicities, and challenges and outline the possible future research directions.
Kinetic deuterium isotope effects in enzymic formate oxidation (1964)

Abstract
On the Nanoparticle to Molecular Size Transition:  Fluorescence Quenching Studies (2001)

Semiconductor nanoparticles, NPs, exhibit fluorescence properties that are closely related to the nature of their surface. CdSe NPs that range in size from 2 to 15 nm in diameter fluoresce with both near-band-edge emission and deep-trap emission, depending on the quality of the surface. When butylamine is added to colloidal solutions of NPs in this size range, the amine is thought to bind to the NP surface and eliminate radiant recombination pathways that lead to luminescence. Since the amine binds to the NP surface, the decrease in fluorescence intensity does not follow standard molecular models of collisional fluorescence quenching. NPs that are smaller than ∼2 nm are composed entirely of a discontinuous arrangement of atoms that are all in constant chemical contact with capping material, solvent, and contaminants. When butylamine is added to solutions of these smaller NPs, the fluorescence quenching follows more standard collisional quenching models. Thus, by monitoring the interaction between NPs and a hole acceptor such as butylamine, one can observe the transition from NP, with atoms both in the core and on the surface, to molecular cluster, with no core atoms to dominate the electron density, but with only surface atoms that can participate in molecular processes such as electron transfer.
Classroom lessons of astronomy using the Internet and its multimedia applications (2002)

Although a lot of people are interested in astronomical objects, it is difficult to teach astronomy in school. One of the reasons for the difficulty is that students can not observe astronomical objects in school. We consider that the Internet and its multimedia applications can resolve this problem. On November 19th, 1995, we had a very unusual astronomical phenomenon. We broadcasted the real time video of this astronomical phenomenon to the Internet. This experiment shows that the Internet has the advantages for classroom lessons in astronomy. We consider classroom lessons of astronomy using the Internet and its multimedia applications.
Modified technetium-99m heparin for the imaging of acute experimental myocardial infarcts. (1980)

We have reported previously that technetium-99m heparin (TcH) accumulates in, and allows scintigraphic identification of, damaged canine myocardium occurring with temporary occlusion and reperfusion of the left anterior descending (LAD) coronary artery. A recent modification consists of using heparin from sheep lung, with stannous phosphate as the reducing agent. In 12 dogs with permanent LAD occlusion, six were injected intravenously with TcH (3--6 mCi) at 24 hr after occlusion, and six at 48 hr. Each experimental animal demonstrated relatively high TcH uptake in the left-ventircular infarct region as compared with normal myocardium. The in vivo scintigrams in all animals with gross myocardial infarcts were positive. The results suggest that this modified TcH has value for identifying experimental myocardial infarcts and that the reduced bone uptake, compared with that occurring with Tc-99m phosphates, may be an advantage for scintigraphic infarct detection.
A possible near-ballistic collection in an AlGaAs/GaAs HBT with a modified collector structure (1988)

An AlGaAs/GaAs heterojunction bipolar transistor (HBT) structure with an n-p/sup +//sub 1/-i-p/sup +//sub 2/-n/sup +/ doping profile that enables electron collection in the Gamma -valley of GaAs is presented. In fabricated HBTs operating at low collector current density, f/sub T/ reaches its peak value when the potential variation in the i collector layer is around 0.4 V, which indicates that the electron transport is dominated by the Gamma -valley feature in GaAs. A high f/sub T/ value of 105 GHz obtained at a collector current density of 5*10/sup 4/ A/cm/sup 2/ also demonstrates the significance of the proposed near-ballistic collection structure.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Viscous drag measurements utilizing microfabricated cantilevers (1996)

The influence of viscous drag forces on cantilevers is investigated using standard atomic force microscope (AFM) cantilevers. Viscosity effects on several geometrically different cantilevers manifest themselves as variations in resonance frequencies, quality factors, and cantilever response amplitudes. With this novel measurement, a single cantilever can be used to measure viscosities ranging from η=10−2 to 102 g/cm s.
Specific dealkylation of phosphonate esters using iodotrimethylsilane (1978)

Phosphonic acid dialkyl esters are transformed in high yield into the corresponding bistrimethylsilyl esters on treatment with iodotrimethylsilane; subsequent hydrolysis of these products affords the parent phosphonic acids under mild conditions without influence on a variety of other functional groups.
Lubricin and surfacing of articular joints (2004)

Purpose of review: Understanding lubrication of articular cartilage, provided by synovial fluid, requires knowledge of tribology, cartilage mechanics, biochemistry, and now genetic factors. These advances have implications in the engineering of articular cartilage and in revisiting the importance of lubrication in chondroprotection as it relates to preventing osteoarthritis. Recent findings: Lubricin and superficial zone protein (SZP) share a common primary structure and are expressed by synovial fibroblasts and chondrocytes, respectively. SZP is also secreted by chondrocytes in vitro, cultured on molecular scaffolds in efforts to engineer articular cartilage. The concentration of expressed SZP is suitable to enable boundary lubrication and offers an important biophysical marker in tissue engineering efforts. Researchers have also reported that lubricin levels are diminished in patients with traumatic synovitis. These same patients show collagen type II degeneration, leading one to wonder whether lubricin/SZP is easily degraded during inflammatory events such as early osteoarthritis, thereby contributing to long-term catabolic consequences. Summary: The identification of lubricin and SZP as articular lubricants secreted by synovium and articular cartilage will herald a new venue of investigation into chondroprotection.
A ligand-reversible dimerization system for controlling protein–protein interactions (2000)

Chemically induced dimerization provides a general way to gain control over intracellular processes. Typically, FK506-binding protein (FKBP) domains are fused to a signaling domain of interest, allowing crosslinking to be initiated by addition of a bivalent FKBP ligand. In the course of protein engineering studies on human FKBP, we discovered that a single point mutation in the ligand-binding site (Phe-36 --> Met) converts the normally monomeric protein into a ligand-reversible dimer. Two-hybrid, gel filtration, analytical ultracentrifugation, and x-ray crystallographic studies show that the mutant (F(M)) forms discrete homodimers with micromolar affinity that can be completely dissociated within minutes by addition of monomeric synthetic ligands. These unexpected properties form the basis for a "reverse dimerization" regulatory system involving F(M) fusion proteins, in which association is the ground state and addition of ligand abolishes interactions. We have used this strategy to rapidly and reversibly aggregate fusion proteins in different cellular compartments, and to provide an off switch for transcription. Reiterated F(M) domains should be generally useful as conditional aggregation domains (CADs) to control intracellular events where rapid, reversible dissolution of interactions is required. Our results also suggest that dimerization is a latent property of the FKBP fold: the crystal structure reveals a remarkably complementary interaction between the monomer binding sites, with only subtle changes in side-chain disposition accounting for the dramatic change in quaternary structure.