gebhart/patrepeval huggingface dataset:
Balaglitazone: A Second Generation Peroxisome Proliferator-Activated Receptor (PPAR) Gamma (&#947;) Agonist (2012)

Balaglitazone (DRF-2593) is a novel partial agonist of PPAR-gamma (γ), which is developed by Dr. Reddy's laboratories India. Balaglitazone is a second generation peroxisome proliferator-activated receptor (PPAR) gamma agonist with only partial agonistic properties. Balaglitazone is currently being evaluated in phase III clinical trial in United States and Europe. Selective PPAR-γ modulators bind in distinct manners to the ligand-binding pocket of PPAR-γ, leading to alternative receptor conformations, differential cofactor recruitment/displacement, differential gene expression, and ultimately differential biological responses. Based on this concept, new and improved novel antidiabetic agents are in current development. Clinical studies conducted with 409 subjects of randomized, double blind, parallel-group placebo and active comparator-controlled subject groups to determine the efficacy and safety of Balaglitazone. The study showed that the trial met its primary endpoint. Balaglitazone treated groups shown significantly reduce of HbA1c (%), FSG (mmol/L), postprandial glucose as comparison to pioglitazone. Phase III clinical studies data clearly shows that Balaglitazone provides robust glycemic control as an add-on to insulin therapy. Balaglitazone 10 mg and 20 mg show the similar magnitudes of the effects which comparable to the effects seen in the pioglitazone 45 mg group. The incidence of fluid retention and fat accumulation fewer than those observed with pioglitazone 45 mg. Hence, Balaglitazone is prominent candidate of new glitazone which requires fewer doses as comparison pioglitazone and shows better safety profile less incidence of special adverse effect like heart failure, peripheral oedema, and myocardial infarction. Unlike other marketed PPAR gamma agonists, Balaglitazone shows less fluid retention, less heart enlargement and no reduction of bone formation than full PPAR gamma agonists in preclinical studies. In present review, we have tried to cover classification PPARs various ligands, chemistry, physical properties, commercial synthesis, current patent status, polymorphic information, receptor interaction, pharmacophore rational, mechanism, adverse effect and clinical status of Balaglitazone, giving emphasis on medicinal chemistry aspect.
Redundant and on-line CORDIC: application to matrix triangularization and SVD (1990)

Several modifications to the CORDIC method of computing angles and performing rotations are presented: (1) the use of redundant (carry-free) addition instead of a conventional (carry-propagate) one; (2) a representation of angles in a decomposed form to reduce area and communication bandwidth; (3) the use of on-line addition (left-to-right, digit-serial addition) to replace shifters by delays; and (4) the use of online multiplication, square root, and division to compute scaling factors and perform the scaling operations. The modifications improve the speed and the area of CORDIC implementations. The proposed scheme uses efficiently floating-point representations. The application of the modified CORDIC method to matrix triangularization by Givens' rotations and to the computation of the singular value decomposition (SVD) are discussed.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Understanding the Mechanism of Prosegment-catalyzed Folding by Solution NMR Spectroscopy (2013)

Multidomain protein folding is often more complex than a two-state process, which leads to the spontaneous folding of the native state. Pepsin, a zymogen-derived enzyme, without its prosegment (PS), is irreversibly denatured and folds to a thermodynamically stable, non-native conformation, termed refolded pepsin, which is separated from native pepsin by a large activation barrier. While it is known that PS binds refolded pepsin and catalyzes its conversion to the native form, little structural details are known regarding this conversion. In this study, solution NMR was used to elucidate the PS-catalyzed folding mechanism by examining the key equilibrium states, e.g. native and refolded pepsin, both in the free and PS-bound states, and pepsinogen, the zymogen form of pepsin. Refolded pepsin was found to be partially structured and lacked the correct domain-domain structure and active-site cleft formed in the native state. Analysis of chemical shift data revealed that upon PS binding refolded pepsin folds into a state more similar to that of pepsinogen than to native pepsin. Comparison of pepsin folding by wild-type and mutant PSs, including a double mutant PS, indicated that hydrophobic interactions between residues of prosegment and refolded pepsin lower the folding activation barrier. A mechanism is proposed for the binding of PS to refolded pepsin and how the formation of the native structure is mediated.
Microwave Setup Design for Continuous Fine‐Chemicals Synthesis (2014)

Abstract A feasibility study in state‐of‐the‐art multi‐ and monomode microwave cavities was conducted to outline important functionalities necessary in a microwave setup for continuous fine‐chemicals synthesis. For multimode operation, the heating efficiency depends on the position as well as on the volume distribution of the load. For monomode operation, the heating efficiency does not depend on the axial position and has a maximum with respect to the load diameter. Based on this study, a microwave setup consisting of four cavities was designed and constructed. The setup provided a defined microwave field pattern and allowed focusing of the microwave power. A near‐uniform distribution of microwave energy in all four cavities of the setup was achieved at reduced grid to applicator losses.
Short- and Long-Term Black Tea Consumption Reverses Endothelial Dysfunction in Patients With Coronary Artery Disease (2001)

Short- and long-term black tea consumption reverses endothelial vasomotor dysfunction in patients with coronary artery disease. This finding may partly explain the association between tea intake and decreased cardiovascular disease events.
The impact of step and flash imprint lithography for nano-manufacturing applications (2004)

Summary form only given, as follows. Step and Flash Imprint Lithography (S-FILTM) process is a step and repeat nano-replication technique based on UV curable low viscosity liquids. Investigation by this group and others has shown that the resolution of replication by imprint lithography is limited only be the size of the structures that can be created on the template (mold). S-FIL uses field-to-field drop dispensing of the W curable liquids for the step and repeat patterning. This approach allows for nanomanufacturing of devices with widely varying pattern densities and complicated structures. There are numerous bio applications for imprint lithography. One of the more interesting is to imprint small posts to manage cell =-growth. Images will be shown of distortion free 100 to 60 nm posts that are replicated by SFIL processing. Process data for repeatability, process control, effects and etch pattern transfer of sub 100 nm posts and other features will also be shown.
SilhoNet-Fisheye: Adaptation of A ROI-Based Object Pose Estimation Network to Monocular Fisheye Images (2020)

There has been much recent interest in deep learning methods for monocular image based object pose estimation. While object pose estimation is an important problem for autonomous robot interaction with the physical world, and the application space for monocular-based methods is expansive, there has been little work on applying these methods with fisheye imaging systems. Also, little exists in the way of annotated fisheye image datasets on which these methods can be developed and tested. The research landscape is even more sparse for object detection methods applied in the underwater domain, fisheye image based or otherwise. In this work, we present a novel framework for adapting a ROI-based 6D object pose estimation method to work on full fisheye images. The method incorporates the gnomic projection of regions of interest from an intermediate spherical image representation to correct for the fisheye distortions. Further, we contribute a fisheye image dataset, called UWHandles, collected in natural underwater environments, with 6D object pose and 2D bounding box annotations.
Life Stress and Cervical Squamous Intraepithelial Lesions in Women With Human Papillomavirus and Human Immunodeficiency Virus (2003)

These findings suggest that life stress may constitute an independent risk factor for SIL progression and/or persistence in HIV-infected women. Stress management interventions may decrease risk for SIL progression/persistence in women living with HIV.
Lowering blood pressure to prevent myocardial infarction and stroke: a new preventive strategy (2003)

The evidence presented indicates that three drugs in combination may reduce stroke by about two-thirds and ischaemic heart disease by half. The report suggests that the term hypertension should be avoided because it is not a disease and it implies another category (normotensives) who would not benefit from lowering blood pressure. Blood pressure reduction using combinations of safe, well-established drugs is effective in preventing cardiovascular events. It is therefore suggested that such preventive therapy be considered more widely in people who by virtue of existing disease or simply age are at risk of a heart attack or stroke regardless of initial blood pressure.
ChemInform Abstract: Synthesis and Structural Examination of Complexes of Am(IV) and Other Tetravalent Actinides with Lacunary Heteropolyanion α2‐P2W17O6110‐. (2009)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Zirconia - an overview (1981)

A historical perspective is provided through bench marks in the development of zirconia. The crystal structures of the three polymorphs-cubic, tetragonal and monoclinic-are reviewed. The martensitic nature of the monoclinic-tetragonal transformation is substantiated. Enhancement of strength and toughness through the phase transformation in partially stabilized zirconia, which led to important applications as extrusion dies and tool bits, is discussed. The process of stabilization, which enabled refractory applications of zirconia, is covered, followed by a discussion of the defect structure and consequent ionic conductivity of doped zirconia. The use of stabilized zirconia in oxygen sensors, fuel cells, etc., is based on its high oxygen ion conduction. Cubic zirconia, because of its high refractive index, is widely used as jewellery. The state of knowledge in each area is reviewed, and gaps in present understanding are highlighted for future studies.
Model Experiment on the Formation of the Cohesive Zone in the Blast Furnace (1982)

In order to clarify the dynamic behavior of the cohesive zone in the blast furnace, a simulation model experiment was carried out.One-sixth scale sector model unit was built. Quasi are and coke were charged at the top and hot air (180°C) was injected from the tuyeres. The formation process of the cohesive zone was observed via a glass wall fitted on the front of the unit.(1) The cohesive zone is found to be classified into inverted U, inverted V and normal W types, each of which seems to be attributable to the characteristics of gas flow around the root of the cohesive zone. Among them, inverted V type is most desirable for its efficient heat exchange and low thermal load.(2) As concerns burden distribution, a high ore/coke ratio in the periphery makes the cohesive zone inverted U type and a low ore/coke ratio results in W type. In order to obtain inverted V type, an appropriate permeability of the root, especially at the wall side, is necessary.(3) The cohesive zone tends to become inverted U type with a decrease in the thermal flow ratio. An increase in the blast volume raises the level of the cohesive zone and causes its width to become broad. The permeability of the cohesive layers also exerts a large effect on their formation.The mechanism of the cohesive-zone formation has been discussed.
ChemInform Abstract: Synthesis of 2(3H)‐Benzoxazolone and 2(3H)‐Benzothiazolone Derivatives as Potential Beta‐3‐adrenergic Receptor Ligands. Part 2. (2001)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Rheology Guided Rational Selection of Processing Temperature To Prepare Copovidone–Nifedipine Amorphous Solid Dispersions via Hot Melt Extrusion (HME) (2016)

The production of amorphous solid dispersions via hot melt extrusion (HME) relies on elevated temperature and prolonged residence time, which can result in potential degradation and decomposition of thermally sensitive components. Herein, the rheological properties of a physical mixture of polymer and an active pharmaceutical ingredient (API) were utilized to guide the selection of appropriate HME processing temperature. In the currently studied copovidone-nifedipine system, a critical temperature, which is substantially lower (∼13 °C) than the melting point of crystalline API, was captured during a temperature ramp examination and regarded as the critical point at which the API could molecularly dissolve into the polymer. Based on the identification of this critical point, various solid dispersions were prepared by HME processing below, at, and above the critical temperature (both below and above the melting temperature (T<sub>m</sub>) of crystalline API). In addition, the resultant extrudates along with two control solid dispersions prepared by physical mixing and cryogenic milling were assessed by X-ray diffraction, differential scanning calorimetry, hot stage microscopy, rheology, and solid-state NMR. Physicochemical properties of resultant solid dispersions indicated that the identified critical temperature is sufficient for the polymer-API system to reach a molecular-level mixing, manifested by the transparent and smooth appearance of extrudates, the absence of API crystalline diffraction and melting peaks, dramatically decreased rheological properties, and significantly improved polymer-API miscibility. Once the critical temperature has been achieved, further raising the processing temperature only results in limited improvement of API dispersion, reflected by slightly reduced storage modulus and complex viscosity and limited improvement in miscibility.
Antiepileptic Drugs in Patients With HIV Infection/AIDS (2015)

Abstract The incidence of seizures may be as high as 11% in HIV-infected patients. The combination regimens used to treat HIV infection often include substrates, inducers, and inhibitors of several cytochrome P-450 isoenzymes. Complex interactions may occur when some AEDs are administered to patients receiving treatment for HIV infection.
Rescue and Salvage Excavation (2010)

Immediately hailed as the standard work and one of the most widely used archaeological field manuals, this survey of current excavation techniques, now in its third edition, remains an in-dispensible guide for archaeologists. his text has been written by an experienced excavator about the inadequacies of excavation techniques and the possible ways of refining them and should serve as a valuable introduction to the subtleties and spirit of modern archaeology.
Port Control Protocol (PCP) Server Selection (2015)

This document specifies the behavior to be followed by a Port Control Protocol (PCP) client to contact its PCP server(s) when one or several PCP server IP addresses are configured.
Transceiver cascade system analysis and design via a contribution method (2006)

An approach to the design of cascade receiver and transmitter systems for maximum spurious-free dynamic range (SFDR) is introduced. The contribution method developed here provides a good initial assignment of noise figure, gain, and linearity requirement to individual stages and enables informed assessment of trade-offs during system design. Application of the approach to the design of a receiver preselector cascade for maximum SFDR is discussed. © 2006 Wiley Periodicals, Inc. Int J RF and Microwave CAE, 2006.
Induction of genes for the stress proteins PR‐10 and PAL in relation to growth, visible injuries and stomatal conductance in birch (Betula pendula) clones exposed to ozone and/or drought (1998)

Well watered (WW) or drought-stressed (DS) saplings of ozone-sensitive and ozone-tolerant (less sensitive) birch (Betula pendula Roth) clones were exposed for 43 d to 0 nl l<sup>-1</sup> or 100 nl l<sup>-1</sup> ozone. Relative growth rates of leaves, stem, and roots, leaf discolouration, stomatal conductance and induction of genes encoding stress-related proteins PR-10, PAL and a LEA-group protein BP8 were determined. In general, both ozone and drought stress, singly and in combination, increased transcript levels of PR-10 in both clones. This was related to lower induction of PAL (except in older leaves of the tolerant clone), and increased proportions of visibly injured and yellowed leaves in ozone-exposed plants. The clones differed in their stomatal conductance and growth responses. In the less sensitive clone 2, ozone did not affect growth rates, but high stomatal conductance was observed in WW ozone-exposed plants. The more sensitive clone 5 showed, on the contrary, reduced growth rates and low stomatal conductance in WW ozone plants. Interestingly, clone 2 was sensitive to drought stress alone, whereas clone 5 was highly sensitive to ozone and drought stress experienced together. The results show that appearance of visible injuries (necrotic flecks) and enhanced yellowing of leaves coincided with the induction of genes for stress proteins PR-10 and PAL. The short-term growth responses, however, seemed to be separate processes. Additionally, stomatal conductance was related to leaf injuries and growth rates in a complicated manner, emphasizing the complex nature of ozone sensitivity/tolerance mechanisms in birch.
CYP2R1Mutations Impair Generation of 25-hydroxyvitamin D and Cause an Atypical Form of Vitamin D Deficiency (2015)

These studies confirm that CYP2R1 is the principal 25-hydroxylase in humans and demonstrate that CYP2R1 alleles have dosage-dependent effects on vitamin D homeostasis. CYP2R1 mutations cause a novel form of genetic vitamin D deficiency with semidominant inheritance.
Sustainability research: Organizational challenge for intermediary research institutes (2013)

The agricultural sustainability challenge is often formulated in terms of meeting the increasing demand for food of a growing and wealthier world population while simultaneously reducing environmental impacts. Strategies to meet this challenge include increasing agricultural yields, saving land and diverting agricultural produce from use for feed and fuel. The paper compares such strategies based on natural sciences with alternatives captured under the umbrella of sustainability sciences, based on systems and mixed sciences approaches. Theoretical and methodological foundations of various branches of sustainability have been developed over the last decades at academia, but although experimentation -putting theory into action- has been carried out a in The Netherlands to a considerable degree, this has hardly led to institutional change of research constellation itself. It is argued that intermediary research institutes by their position in between academia, practice and between government and society are in principle well positioned to incorporate sustainability science. This requires boundary management beyond the traditional boundaries of biological and technical disciplines and their fields of application and retention of methodology and knowledge within with units of scientists with complementary knowledge and skills. To become effective doing sustainability science can probably only be achieved after a prolonged period of experimentation and evaluation, while the shared base of theories, methods and networks form the core of such a knowledge system, as contrasted to disciplinary groups.
Yüksek dinamik ölçekli fotoğraf ve monitörlerin aydınlatma araştırma projelerinde kullanımı (2011)

Bu calismanin amaci, Yuksek Dinamik Olcekli (YDO) goruntuleme tekniginin kullanildigi YDO monitorlerin aydinlatma muhendisligi problemlerinin cozumunde kullanilabilecegini gostermektedir. Bu makalede sunulan ilk deney, YDO monitorde goruntulenen YDO fotograflarin, LCD ekranda goruntulenen (tek pozlamadan olusan) geleneksel fotograflardan daha gercekci oldugu hipoteziyle tasarlanmistir. Alti adet hacmin detayli parilti olcumleri noktasal olcum yapabilen bir parilti olcer ve parilti kamerasi kullanilarak yapildiktan sonra, bu parilti degerleri YDO ekrana yansitilmistir. Deney sonuclari YDO fotograf teknigi ile uretilen fotograflarin YDO ekrandaki goruntulerinin, LCD ekranda goruntulenen tek pozlamadan olusan fotograflardan daha gercekci algilandigini gostermistir. Calismanin ikinci bolumunde, YDO goruntuleme tekniginden faydalanilarak bir acik plan ofisteki aydinlatma kalitesi incelenmistir. Bu calismada, goruntu karakteristikleri (ortalama parilti, parilti dagilimi ve dogal isigi hacme alan pencere buyuklugu) ile hacmin aydinlatma kalitesi arasindaki baginti incelenmistir. Calismanin sonuclari, YDO ekranda sergilenen YDO fotograflarin ozellikle dogal isik iceren goruntulerde aydinlatma kalitesi analizi yapmak amaciyla gercek hacim yerine kullanilabilecegini gostermektedir. Henuz insa edilmemis binalarin grafik simulasyonlarinin, gercek hacimde saglanmasi ongorulen parilti degerleriyle YDO ekranda goruntulenmesi, aydinlatma projesine iliskin karar asamasinda faydali olacaktir. YDO teknolojisi kullanilarak elde edilen sonuclar literaturdeki calismalarla tutarli olmasi, YDO teknolojisinin aydinlatma muhendisligi problemlerinin cozumunde kullanilmasina iliskin guveni arttirmaktadir. Anahtar Kelimeler: Aydinlatma tasarimi, Yuksek Dinamik Olcekli fotograflama teknigi, Yuksek Dinamik Olcekli monitor, aydinlatma kalitesi, ofis aydinlatmasi.
Probing PARP1-inhibitor complexes for the development of novel inhibitors. (2014)

Poly (ADP-ribose) polymerase 1 (PARP1) is the most important member of the PARP family which has been shown to have a direct involvement in the development of cancer. A strategy to rationalize the structure based drug discovery of PARP1 inhibitors has been discussed. So far studies regarding varied scaffold PARP1 inhibitors have been done, however the current study focus on how the available data from potent PARP1 inhibitors could be combined and utilized for developing a robust model for the development of novel inhibitors. Through detailed analyses of PARP1-inhibitor binding, a pharmacophore model has been developed followed by a virtual screen of potential inhibitors. The resulting high-affinity binding hits following the defined pharmacophore model and making the critical interactions were selected as final potential leads. Hence, using the approaches of pharmacophore design, docking based virtual screening and conformation alignment, we have identified important leads which satisfy all parameters of the screening process. The developed pharmacophore model as well as the strategy is very straightforward for screening novel inhibitors and could thus be used as a prototype for PARP1 structure based drug discovery.