gebhart/patrepeval huggingface dataset:
Syntheses and Biological Properties of Brefeldin Analogues (2010)

Abstract Total and partial syntheses of brefeldin analogues are described. (6 R )‐Hydroxy‐BFA ( 5 ) was obtained through a total synthesis from (1 S ,2 R )‐2‐[(trityloxy)methyl]cyclopent‐3‐ene‐1‐carbonitrile ( cis ‐ 8 ) in 13 steps. The BFA lactam analogue 6 was prepared via the key building block 25 , which was accessed in four steps from BFA ( 1 ). (7 S )‐Amino‐BFC ( 7 ) was obtained from 7‐dehydro‐BFA ( 3 ) by reductive amination. The structures of the brefeldin analogues were determined by X‐ray analyses. The activities of the brefeldin analogues in blocking protein traffic between the endoplasmatic reticulum and the Golgi apparatus were determined both for mammalian cells and for plant cells. Molecular mechanics calculations and docking into the Arf1‐GEF protein complex, an established receptor of BFA, were carried out.
Recent Results in State Estimation of Dynamical Systems with Inputs under Bandwidth Constraints (2018)

Finding the minimal bit rate needed for state estimation of a dynamical system is a fundamental problem in control theory. We present two notions of topological entropy, one to lower bound the bit rate needed to estimate the state of a nonlinear dynamical system, with unknown bounded inputs, up to a constant error ε. The other is to do the same but to estimate the state of a switched system with unknown switching signal up to an error that is bounded by ε for τ seconds after each switch and then decays exponentially at a rate of α till the next switch. Since computation of entropy is hard in general, we present upper bounds on both notions of entropy. Finally, we present preliminary results on the relation between the two notions. Note that most of the ideas presented in this abstract are from our papers [4] and [5].
Figure S4 from Low-pass Whole-genome Sequencing of Circulating Cell-free DNA Demonstrates Dynamic Changes in Genomic Copy Number in a Squamous Lung Cancer Clinical Cohort (2023)

&lt;p&gt;Comparison of CNV landscapes in tumor tissue and cfDNA of the FIGARO squamous NSCLC patients.&lt;/p&gt;
Elevated Expression of DecR1 Impairs ErbB2/Neu-Induced Mammary Tumor Development (2007)

Tumor cells utilize glucose as a primary energy source and require ongoing lipid biosynthesis for growth. Expression of DecR1, an auxiliary enzyme in the fatty acid beta-oxidation pathway, is significantly diminished in numerous spontaneous mammary tumor models and in primary human breast cancer. Moreover, ectopic expression of DecR1 in ErbB2/Neu-induced mammary tumor cells is sufficient to reduce levels of ErbB2/Neu expression and impair mammary tumor outgrowth. This correlates with a decreased proliferative index and reduced rates of de novo fatty acid synthesis in DecR1-expressing breast cancer cells. Although DecR1 expression does not affect glucose uptake in ErbB2/Neu-transformed cells, sustained expression of DecR1 protects mammary tumor cells from apoptotic cell death following glucose withdrawal. Moreover, expression of catalytically impaired DecR1 mutants in Neu-transformed breast cancer cells restored Neu expression levels and increased mammary tumorigenesis in vivo. These results argue that DecR1 is sufficient to limit breast cancer cell proliferation through its ability to limit the extent of oncogene expression and reduce steady-state levels of de novo fatty acid synthesis. Furthermore, DecR1-mediated suppression of tumorigenesis can be uncoupled from its effects on Neu expression. Thus, while downregulation of Neu expression may contribute to DecR1-mediated tumor suppression in certain cell types, this is not an obligate event in all Neu-transformed breast cancer cells.
I The synthesis of papyracillic acids: Application of the tandem chain extension-acylation reaction II Diastereoselective synthesis of beta-methyl-gamma-keto esters through the utility of an L-serine auxiliary (2011)

The development of the zinc-mediated tandem chain extension-acylation reaction for the synthesis of spiro-fused ketals was successfully accomplished. The incorporation of a methyl-substituent into the gamma-keto ester backbone, through a methyl substituted carbenoid, allowed for the synthesis of papyracillic acid B and 4-epi-papyracillic acid C. Comparison between the reported and experimental spectral data for papyracillic acid B and 4- epi-papyracillic acid C permitted structural and stereochemical reassignment. Diastereoselective syntheses of beta-methyl-gamma-keto esters were achieved through the utility of an L-serine auxiliary. Preparation of a series of L-serine derived precursors were prepared and studied.
Localization of material defects using nonlinear resonant ultrasound spectroscopy under asymmetric boundary conditions (2010)

The position of microscopic defects in a one-dimensional bar is analyzed by means of the nonlinear resonant ultrasound spectroscopy technique under asymmetric boundary conditions. Experimental results on cementitious material confirm the feasibility of the method to locate nonlinear scatterers. Good agreement between the real damage position and the inferred experimental prediction is obtained based on information about the nonlinear frequency shift and about the amplitude ratio of the third and fifth harmonic for the fundamental resonance mode.
10D1F, an Anti-HER3 Antibody That Uniquely Blocks the Receptor Heterodimerization Interface, Potently Inhibits Tumor Growth Across a Broad Panel of Tumor Models (2020)

In recent years, HER3 has increasingly been implicated in the progression of a variety of tumor types and in acquired resistance to EGFR and HER2 therapies. Whereas EGFR and HER2 primarily signal through the MAPK pathway, HER3, as a heterodimer with EGFR or HER2, potently activates the PI3K pathway. Despite its critical role, previous attempts to target HER3 with neutralizing antibodies have shown disappointing efficacy in the clinic, most likely due to suboptimal and indirect mechanisms of action that fail to completely block heterodimerization; for example, tumors can escape inhibition of ligand binding by upregulating ligand-independent mechanisms of HER3 activation. We therefore developed 10D1F, a picomolar affinity, highly specific anti-HER3 neutralizing antibody that binds the HER3 heterodimerization interface, a region that was hitherto challenging to raise antibodies against. We demonstrate that 10D1F potently inhibits both EGFR:HER3 and HER2:HER3 heterodimerization to durably suppress activation of the PI3K pathway in a broad panel of tumor models. Even as a monotherapy, 10D1F shows superior inhibition of tumor growth in the same cell lines both <i>in vitro</i> and in mouse xenograft experiments, when compared with other classes of anti-HER3 antibodies. This includes models demonstrating ligand-independent activation of heterodimerization as well as constitutively activating mutations in the MAPK pathway. Possessing favorable pharmacokinetic and toxicologic profiles, 10D1F uniquely represents a new class of anti-HER3 neutralizing antibodies with a novel mechanism of action that offers significant potential for broad clinical benefit.10D1F is a novel anti-HER3 antibody that uniquely binds the receptor dimerization interface to block ligand-dependent and independent heterodimerization with EGFR/HER2 and thus more potently inhibits tumor growth than existing anti-HER3 antibodies.
Phase II study of cisplatin, etoposide and concurrent radiation therapy with maintenance chemotherapy with cisplatin and gemcitabine for unresectable non-small cell lung cancer (2004)

7290
Consciousness monitoring using near-infrared spectroscopy (NIRS) during high +Gz exposures (2004)

The relationship between human consciousness and oxygen saturation (rSO(2)) in cerebral tissue under high +Gz stress was non-invasively monitored by near-infrared multiple wavelength spectroscopy (NIRS). We studied the drop in rSO(2) levels in human subjects during exposure to various head-to-foot acceleration (+Gz) profiles. These profiles included sustained +Gz plateaus and repeated short duration +Gz pulses of varying duration. The end point in this study was +Gz-induced loss of consciousness (G-LOC). The rSO(2) levels under normal (asymptomatic), almost loss of consciousness (A-LOC) and G-LOC conditions were recorded. Correlations among decrease in rSO(2), +Gz pulse duration, +Gz stress level and incapacitation time (ICAP) after G-LOC were also investigated. It was found that once rSO(2) fell to a certain level, G-LOC occurred. This threshold was repeatable and independent of the +Gz level or duration. It was also observed that the total ICAP after G-LOC was dependent on the length of time that rSO(2) remained below the G-LOC threshold level, i.e. the longer the rSO(2) level remained below the G-LOC induction level, the longer the subject remained unconscious. These results may prove to be useful in designing closed loop control systems for personal protective gear for pilots of high performance aircraft.
The Sources of Tax Complexity: How Much Simplicity Can Fundamental Tax Reform Achieve (1997)

The complexity of the federal income tax exacts obvious social costs.It leads to wasteful compliance and administrative activity and deters productive activities that would otherwise be undertaken.But if tax complexity is undesirable, why has it thrived?In this Article, Professor Paul argues that the desire for equitable distribution of tax liabilities and the desire for certainty of application cause tax complexity.Pressure to achieve those goals comes to bear on the federal income tax and would come to bear on possible replacements, such as a federal tax on human consumption, causing complexity in both the current system and possible alternatives.Professor Paul applies her model of complexity to the debate over adoption of a consumption tax and challenges the prevailing wisdom that consumption taxes are simpler than income taxes.
Controlled and targeted drug delivery strategies towards intraperiodontal pocket diseases (2000)

Advances in the understanding of the aetiology, epidemiology, pathogenesis and microbiology of periodontal pocket flora have revolutionized the strategies for the management of intraperiodontal pocket diseases. Intra-pocket, sustained release, drug delivery devices have been shown to be clinically effective in the treatment of periodontal infections. Several degradable and non-degradable devices are under investigation for the delivery of antimicrobial agents into the periodontal pocket including non-biodegradable fibres, films (biodegradable and non-biodegradable), bio-absorbable dental materials, biodegradable gels/ointments, injectables and microcapsules. With the realization that pocket bacteria accumulate as biofilms, studies are now being directed towards eliminating/killing biofilm concentrations rather than their planktonic (fluid phase) counterparts. Intraperiodontal pocket drug delivery has emerged as a novel paradigm for the future research. Similarly, bioadhesive delivery systems are explored that could significantly improve oral therapeutics for periodontal disease and mucosal lesions. A strategy is to target a wide range of molecular mediators of tissue destruction and hence arrest periodontal disease progression. Research into regenerating periodontal structures lost as a result of disease has also shown substantial progress in the last 25 years.
Mesenchymal Stem Cells &ndash; Sources and Clinical Applications (2008)

SUMMARY: Although mesenchymal stem cells (MSC) from different tissue sources share many characteristics and generally fulfill accepted criteria for MSC (plastic adherence, certain surface marker expression, and ability to differentiate into mesenchymal tissues), we are increasingly learning that they can be distinguished at the level of cytokine production and gene expression profiles. Their ability to differentiate into different tissues including endodermal and ectodermal lineages, also varies according to tissue origin. Importantly, MSC from fetal sources can undergo more cell divisions before they reach senescence than MSC from adult tissue such as bone marrow or adipose tissue. As we learn more about the differentiation and plasticity of MSC from different sources, health care providers in the future will use them tailored to different medical indications.
Data reduction of friction factor, permeability and inertial coefficient for a compressible gas flow through a milli-regenerator (2021)

A regenerator of a Stirling machine alternately absorbs and releases heat from and to the working fluid which allows to recycle rejected heat during theoretical isochoric processes. This work focuses on a milli-regenerator fabricated with a multiple jet molding process. The regenerator is a porous medium filled with a dense pillar matrix. The pillars have a geometrical lens shape. Two metallic layers (chromium and copper) are deposited on the polymer pillars to increase heat transfer inside the regenerator. We performed experiments on different milli-regenerators corresponding to three porosities (ε = 0.80, 0.85 and 0.90) under nitrogen steady and oscillating compressible flows (oscillating Reynolds number in the range 0 &lt; Re ω &lt; 60 and Reynolds number based on the hydraulic diameter Re Dh,max &lt;6000) for different temperature gradients (Δ T &lt; 100°C). Temperature, velocity and pressure experimental measurements are performed with microthermocouples (type K with 7,6 µm diameter), hotwires and miniature pressure sensors, respectively. We identified a threeterm composite correlation equation for the friction factor based on a Darcy-Forchheimer flow model that best-fit the experimental data. In steady and oscillating flows permeabilities and inertial coefficients are of the same magnitude order. Inertial coefficients decrease when the porosities increase.
Histopathology following electrode insertion and chronic electrical stimulation (1985)

We have examined a number of safety issues associated with cochlear implants. This work has been primarily designed to evaluate the histopathological effects of intracochlear electrode implantation and chronic electrical stimulation. The results of these studies may be summarized as follows: 1) The insertion of the banded free-fit scala tympani array into human cadaver temporal bones produces minimal damage, occurring primarily to a localized region of the spiral ligament. This damage would not result in significant neural degeneration and thus, would not compromise the efficacy of the multiple channel device; 2) chronic intracochlear electrical stimulation for continuous periods of 500 to 2000 hours, using charge balanced biphasic current pulses developing charge densities of 18-32 }?C/cm2. geom./phase, does not adversely affect the spiral ganglion cell population; 3) labyrinthine infection severely reduces the viable spiral ganglion cell population; 4) the formation of new bone present in approximately half of the animals we have implanted --is not associated with electrical stimulation per se; 5) scanning electron microscope studies of electrodes subjected to long periods of intracochlear electrical stimulation reveals minimal platinum dissolution when compared with unstimulated control electrodes, and electrodes that have been stimulated for similar periods in inorganic saline.
Model-Free Based Automated Trajectory Optimization for UAVs toward Data Transmission (2019)

In this paper, we consider an unmanned aerial vehicle (UAV) enabled wireless network with a set of ground devices that are randomly distributed in an area and each having a certain amount of data for transmission. The UAV flies over this region from a starting point to a destination. During its flight, the UAV wants to communicate to the ground devices for maximizing the cumulative collected data by optimizing the trajectory of the UAV subject to its flight time constraint. Due to uncertainty in the locations of the ground devices and the communication dynamics, an accurate system model is difficult to acquire and maintain. With the help of stochastic modelling, we present a reinforcement learning based automated trajectory optimization algorithm. By dividing the considered region into small grids with finite state space and action space, we apply the Q-learning based automated trajectory optimization approach for maximizing the cumulative collected data during its flight time. Simulation results demonstrate that the reinforcement learning approach can find an optimal strategy under the flight time constraint.
Salient features of the ciliated organ of asymmetry (2014)

Many internal organs develop distinct left and right sides that are essential for their functions. In several vertebrate embryos, motile cilia generate an asymmetric fluid flow that plays an important role in establishing left-right (LR) signaling cascades. These 'LR cilia' are found in the ventral node and posterior notochordal plate in mammals, the gastrocoel roof plate in amphibians and Kupffer's vesicle in teleost fish. I consider these transient ciliated structures as the 'organ of asymmetry' that directs LR patterning of the developing embryo. Variations in size and morphology of the organ of asymmetry in different vertebrate species have raised questions regarding the fundamental features that are required for LR determination. Here, I review current models for how LR asymmetry is established in vertebrates, discuss the cellular architecture of the ciliated organ of asymmetry and then propose key features of this organ that are critical for orienting the LR body axis.
Turbine meters for liquid measurement (1984)

Turbine meters presently used for liquid measurement are presented here. Through the evolution of technology, the turbine meter has maintained its reliability and ruggedness while attaining a high degree of accuracy. The paper attempts to explain the basic principles involved with the utilization of turbine meters, as well as the application of the meter by the aerospace industry, petroleum industry, and petrochemical industry. The use of turbine meters for custody transfer of refined products and pipeline systems, tankers and barge loading or unloading of crude oil has brought the turbine meter to worldwide recognition as a primary register for the exchange of energy.
Evaluating anycast in the domain name system (2013)

IP anycast is a central part of production DNS. While prior work has explored proximity, affinity and load balancing for some anycast services, there has been little attention to third-party discovery and enumeration of components of an anycast service. Enumeration can reveal abnormal service configurations, benign masquerading or hostile hijacking of anycast services, and help characterize anycast deployment. In this paper, we discuss two methods to identify and characterize anycast nodes. The first uses an existing anycast diagnosis method based on CHAOS-class DNS records but augments it with traceroute to resolve ambiguities. The second proposes Internet-class DNS records which permit accurate discovery through the use of existing recursive DNS infrastructure. We validate these two methods against three widely-used anycast DNS services, using a very large number (60k and 300k) of vantage points, and show that they can provide excellent precision and recall. Finally, we use these methods to evaluate anycast deployments in top-level domains (TLDs), and find one case where a third-party operates a server masquerading as a root DNS anycast node as well as a noticeable proportion of unusual DNS proxies. We also show that, across all TLDs, up to 72% use anycast.
Rapid Microwave‐Promoted Synthesis of Functionalized Benzophenones. (2002)

Abstract For Abstract see ChemInform Abstract in Full Text.
The “FIFTY SHADOWS” of the RALES Trial: Lessons about the Potential Risk of Dietary Potassium Supplementation in Patients with Chronic Kidney Disease (2022)

Hyperkalaemia (HK) is one of the most common electrolyte disorders and a frequent reason for nephrological consultations. High serum potassium (K<sup>+</sup>) levels are associated with elevated morbidity and mortality, mainly due to life-threatening arrhythmias. In the majority of cases, HK is associated with chronic kidney disease (CKD), or with the use of renin-angiotensin-aldosterone system inhibitors (RAASis) and/or mineral corticoid antagonists (MRAs). These drugs represent the mainstays of treatment in CKD, HF, diabetes, hypertension, and even glomerular diseases, in consideration of their beneficial effect on hard outcomes related to cardiovascular events and CKD progression. However, experiences in relation to the Randomised Aldactone Evaluation Study (RALES) cast a long shadow that extends to the present day, since the increased risk for HK remains a major concern. In this article, we summarise the physiology of K<sup>+</sup> homeostasis, and we review the effects of dietary K<sup>+</sup> on blood pressure and cardiovascular risk in the general population and in patients with early CKD, who are often not aware of this disease. We conclude with a note of caution regarding the recent publication of the SSaSS trial and the use of salt substitutes, particularly in patients with a limited capacity to increase K<sup>+</sup> secretion in response to an exogenous load, particularly in the context of "occult" CKD, HF, and in patients taking RAASis and/or MRAs.
Direct torque control, induction motor vector control without an encoder (1997)

The basic evolution of direct torque control from other drive types is explained. Qualitative comparisons with other drives are included. The basic concepts behind direct torque control are clarified. An explanation of direct self control and the field-orientation concepts implemented in the adaptive motor model block is presented. The reliance of the control method on fast processing techniques is stressed. The theoretical foundations for the control concept are provided in summary format. Information on the ancillary control blocks outside the basic direct torque control is given. The implementation of special functions directly related to the control approach is described. Finally, performance data from an actual system are presented.
You Shouldn’t Trust Me: Learning Models Which Conceal Unfairness from Multiple Explanation Methods (2020)

Transparency of algorithmic systems is an important area of research, which has been discussed as a way for end-users and regulators to develop appropriate trust in machine learning models. One popular approach, LIME [23], even suggests that model expla- nations can answer the question “Why should I trust you?”. Here we show a straightforward method for modifying a pre-trained model to manipulate the output of many popular feature importance explana- tion methods with little change in accuracy, thus demonstrating the danger of trusting such explanation methods. We show how this ex- planation attack can mask a model’s discriminatory use of a sensitive feature, raising strong concerns about using such explanation meth- ods to check fairness of a model.
Kovalente Hämin‐DNA‐Addukte zur Herstellung einer neuartigen Klasse artifizieller Häm‐Enzyme (2005)

Wohldefinierte Konjugate aus DNA und Häm-Enzymen sind durch Rekonstitution der entsprechenden apo-Enzyme mit kovalenten DNA-Hämin-Addukten zugänglich (siehe Bild). Dieses Konzept bereitet den Weg zu neuartigen Redox-Katalysatoren mit programmierbaren Bindungseigenschaften, die in der Biokatalyse, der Sensorik oder als Biomaterialien Verwendung finden könnten.
Studies on the Friedel-Crafts Reaction of Diphenyl Ether Derivatives. VI (1954)

It was clarified that the application of acetyl chloride to 2-chloro-, 3-chloro-, or 4-chlorodiphenyl ether in the presence of aluminum chloride results in the introduction of the acetyl radical in the para-position of the ether linkage (4′-position).