gebhart/patrepeval huggingface dataset:
Actions and Potential Therapeutic Applications of Growth Hormone–Releasing Hormone Agonists (2019)

Abstract In this article, we briefly review the identification of GHRH, provide an abridged overview of GHRH antagonists, and focus on studies with GHRH agonists. Potent GHRH agonists of JI and MR class were synthesized and evaluated biologically. Besides the induction of the release of pituitary GH, GHRH analogs promote cell proliferation and exert stimulatory effects on various tissues, which express GHRH receptors (GHRH-Rs). A large body of work shows that GHRH agonists, such as MR-409, improve pancreatic β-cell proliferation and metabolic functions and facilitate engraftment of islets after transplantation in rodents. Accordingly, GHRH agonists offer a new therapeutic approach to treating diabetes. Various studies demonstrate that GHRH agonists promote repair of cardiac tissue, producing improvement of ejection fraction and reduction of infarct size in rats, reduction of infarct scar in swine, and attenuation of cardiac hypertrophy in mice, suggesting clinical applications. The presence of GHRH-Rs in ocular tissues and neuroprotective effects of GHRH analogs in experimental diabetic retinopathy indicates their possible therapeutic applications for eye diseases. Other effects of GHRH agonists, include acceleration of wound healing, activation of immune cells, and action on the central nervous system. As GHRH might function as a growth factor, we examined effects of GHRH agonists on tumors. In vitro, GHRH agonists stimulate growth of human cancer cells and upregulate GHRH-Rs. However, in vivo, GHRH agonists inhibit growth of human cancers xenografted into nude mice and downregulate pituitary and tumoral GHRH-Rs. Therapeutic applications of GHRH analogs are discussed. The development of GHRH analogs should lead to their clinical use.
Physical Adversarial Attacks Against End-to-End Autoencoder Communication Systems (2019)

We show that end-to-end learning of communication systems through deep neural network (DNN) autoencoders can be extremely vulnerable to physical adversarial attacks. Specifically, we elaborate how an attacker can craft effective physical black-box adversarial attacks. Due to the openness (broadcast nature) of the wireless channel, an adversary transmitter can increase the block-error-rate of a communication system by orders of magnitude by transmitting a well-designed perturbation signal over the channel. We reveal that the adversarial attacks are more destructive than jamming attacks. We also show that classical coding schemes are more robust than autoencoders against both adversarial and jamming attacks. The codes are available at [1].
Alstonerine, a new indole alkaloid from Alstonia muelleriana (1969)

J. M. Cook, P. W. Le Quesne and R. C. Elderfield, J. Chem. Soc. D, 1969, 1306 DOI: 10.1039/C29690001306
Tandem Systems for Two‐Photon Uncaging of Bioactive Molecules (2019)

Photodeprotection of biological ligands with the combination of photolabile protecting groups (PPGs) and two-photon (2P) excitation techniques offers the possibility to control physiological phenomena with utmost spatial and temporal precision. Yet, designing PPGs with sufficient 2P photosensitivity still remains challenging. Direct enhancement of the 2P absorption properties usually relies on modifications of the PPG structure, which sometimes results in unpredictable and counterproductive effects on the uncaging quantum yield. In that respect, combining known PPGs with a suitable two-photon light-harvesting antenna within a modular architecture offers a promising alternative. In this Minireview, we highlight this versatile strategy, with a discussion of different tandem 2P uncagers, relying on photoinduced electron transfer (PET), triplet- energy transfer (TT-ET), or Förster resonance energy transfer (FRET) sensitization to enhance the 2P sensitivity of PPGs.
ChemInform Abstract: Palladium‐Catalyzed Intramolecular α‐Arylation of α‐Amino Acid Esters. (2002)

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.
Multiple-input multiple-output cloud transmission for high data rate local contents delivery (2014)

A novel cloud transmission (CTxn) technique is proposed on the basis of the multiple-input multiple-output (MIMO) technique, called MIMO CTxn. Applying a MIMO technique to conventional SISO CTxn provides a very efficient way to support high-date-rate service for delivering local content, even for a negative SINR. Simulation results show that the performance of MIMO CTxn is better than that of SISO CTxn while supporting high-order modulation and a high code rate.
Bisnucleophilic Substitution as a Synthetic Tool for Ready Access to the Piperidine Alkaloids (+)-Connine, (+)-β-Conhydrine, (+)-8-Ethylnorlobelol, and (–)-Halosaline (2015)

Correction to: Bisnucleophilic Substitution as a Synthetic Tool for Ready Access to the Piperidine Alkaloids (+)-Connine, (+)-β-Conhydrine, (+)-8-Ethylnorlobelol, and (–)-HalosalineSynlett 2015; 26(07): 937-941DOI: 10.1055/s-0034-1380151
Schlieren imaging of shock waves from a trumpet (2003)

A sensitive, large-aperture schlieren optical instrument is applied to observe gas-dynamic phenomena at the exit of a trumpet. Shock waves are seen, especially for loud, high-pitched trumpet notes, and several illustrations are given. Microphone waveforms are given for representative examples. These shock waves arise from the shock-tube-like effect of the performer's intermittent breath pressure driving the cylindrical duct of the trumpet, and are the result of cumulative nonlinear acoustic propagation inside the trumpet bore. They are, however, very weak, traveling only marginally above the acoustic speed. In the 118-124 peak dB(A) range, they are near the weak limit of shock wave visibility by schlieren optics. The schlieren evidence confirms that the frequency of the emitted shock waves corresponds to the frequency of the note being played. Ancillary laminar and turbulent jet phenomena associated with the performer's breath are also visible in the images.
Cycloaddition products of 3-oxido-1-phenylpyridinium and 1-cyanoacenaphthylene (1998)

Cycloaddition of 3-oxido-1-phenylpyridinium 8a to 1-cyanoacenaphthylene 9a affords three isomeric adducts (13, 14 and 15). Structures for these compounds resulted from a comparative NMR study, as well as an X-ray crystallographic determination of isomer 15. Attempts to eliminate HCN from compounds 13–15 resulted only in cycloreversion to 1-cyanoacenaphthylene.
Genome-wide DNA methylome and transcriptome changes induced by inorganic nanoparticles in human kidney cells after chronic exposure (2022)

The unique physicochemical properties make inorganic nanoparticles (INPs) an exciting tool in diagnosis and disease management. However, as INPs are relatively difficult to fully degrade and excrete, their unintended accumulation in the tissue might result in adverse health effects. Herein, we provide a methylome-transcriptome framework for chronic effects of INPs, commonly used in biomedical applications, in human kidney TH-1 cells. Renal clearance is one of the most important routes of nanoparticle excretion; therefore, a detailed evaluation of nanoparticle-mediated nephrotoxicity is an important task. Integrated analysis of methylome and transcriptome changes induced by INPs (PEG-AuNPs, Fe<sub>3</sub>O<sub>4</sub>NPs, SiO<sub>2</sub>NPs, and TiO<sub>2</sub>NPs) revealed significantly deregulated genes with functional classification in immune response, DNA damage, and cancer-related pathways. Although most deregulated genes were unique to individual INPs, a relatively high proportion of them encoded the transcription factors. Interestingly, FOS hypermethylation inversely correlating with gene expression was associated with all INPs exposures. Our study emphasizes the need for a more comprehensive investigation of INPs' biological safety, especially after chronic exposure.
Role of natriuretic peptides in regulation of conduit artery distensibility (2004)

Arterial distensibility, assessed by the pulse-wave velocity (PWV), is an independent predictor of cardiovascular risk. We investigated whether natriuretic peptides, acting locally, modify conduit artery distensibility in vivo. All studies were conducted in anesthetized sheep (n = 18) by using a validated ovine hindlimb model. In brief, the PWV was calculated, with the use of the foot-to-foot methodology, from two pressure waveforms recorded simultaneously with a high-fidelity dual pressure-sensing catheter placed in the common iliac artery. Drugs were infused either proximally, via the catheter to perfuse the segment of artery under study, or distally, via the sheath to control for any reflex changes in flow or sympathetic activation. First, the effects of atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP) were studied. Second, the role of endogenous ANP was investigated by infusing the natriuretic peptide receptor type A (NPRA)-selective receptor antagonist A71915. Third, A71915 was coinfused with ANP. Fourth, the NPRC-selective agonist cANF was infused. Infusion of CNP or des-[Gln18Ser19Gly20Leu21Gly22]-ANF-(4-23)-NH2 (cANF) had no effect on iliac PWV. However, infusion of ANP, and to a lesser degree BNP, resulted in a reduction in PWV (-9%; P < 0.01 and -6%; P < 0.05, respectively). A71915 increased iliac PWV from 2.97 +/- 0.13 to 3.06 +/- 0.13 m/s; P < 0.01. Coinfusion of A71915 with ANP completely abolished the effects of ANP (P < 0.01). Importantly, ANP-BNP infusion via the sheath did not alter PWV. In conclusion, ANP, and to a lesser extent BNP, modify large artery distensibility via the NPRA receptor. Neither CNP nor cANF altered PWV, suggesting that the NPRB and NPRC receptors do not acutely influence distensibility in vivo.
Mechanism of IGF-I-Stimulated Glucose Transport in Human Adipocytes: Demonstration of Specific IGF-I Receptors Not Involved in Stimulation of Glucose Transport (1989)

We demonstrate the presence of specific insulinlike growth factor I (IGF-I) receptors in human adipocytes. Competition studies with 125I-labeled IGF-I and unlabeled IGF-I, IGF-II, and insulin showed the specificity of 125I-IGF-I binding to the IGF-I receptors in adipocytes, membranes, and partially purified detergent-solubilized extracts. The monoclonal antibody to the IGF-I receptor (alpha-IR3) inhibits 125I-IGF-I binding and immunoprecipitates the IGF-I receptor. In addition, the alpha-subunit of IGF-I receptor is approximately 10,000 Mr larger than the alpha-subunit of insulin receptor, and IGF-I stimulates phosphorylation of the beta-subunit of the IGF-I receptor. IGF-I stimulates basal glucose transport in human adipocytes, but the concentrations of IGF-I required for half-maximal and maximal stimulation of glucose transport are 800- and 1000-fold greater than that of insulin. The possibility of IGF-I stimulating glucose transport by interacting predominantly with insulin receptors is suggested by data showing that 1) IGF-I competes with insulin-binding sites, 2) there is a lack of an additive effect with IGF-I and insulin in stimulating glucose transport, 3) alpha-IR3, which specifically inhibits IGF-I binding, does not inhibit IGF-I or insulin-stimulated glucose transport, 4) insulin-receptor antibody MA-10 inhibits IGF-I and insulin-stimulated glucose transport, and 5) IGF-I stimulates insulin-receptor autophosphorylation, although its effect is markedly decreased compared with insulin. In summary, human adipocytes possess specific IGF-I receptors. However, IGF-I stimulates glucose transport predominantly by interacting with the insulin receptor.
Rewarding Smatch: Transition-Based AMR Parsing with Reinforcement Learning (2019)

Our work involves enriching the Stack-LSTM transition-based AMR parser (Ballesteros and Al-Onaizan, 2017) by augmenting training with Policy Learning and rewarding the Smatch score of sampled graphs. In addition, we also combined several AMR-to-text alignments with an attention mechanism and we supplemented the parser with pre-processed concept identification, named entities and contextualized embeddings. We achieve a highly competitive performance that is comparable to the best published results. We show an in-depth study ablating each of the new components of the parser
Radiofrequency electromagnetic radiation from Wi-fi and its effects on human health, in particular children and adolescents. Review (2020)

Radiofrequency electromagnetic radiation emitted from Wi-Fi devices is nonionizing radiation. The frequencies used in wireless technology are similar to those applied in mobile telephony. Due to the much lower output power of devices using Wi-Fi compared to mobile phones, the degree of exposure to radiation is also lower. Most of the research on Wi-Fi has been carried out in less favorable or adverse conditions, involving higher power values of devices (peak values instead of average values) and smaller distances of working devices from measuring points. None of the studies conducted so far have indicated that there were the exceedances of the permissible values of radiofrequency electromagnetic radiation contained in the Polish and global legal regulations. Similar to the research related to the impact of mobile telephony on human health, the studies conducted until now focusing on exposure to Wi-Fi are considered ambiguous as they do not give a definitive answer on the possible negative (including carcinogenic) effects on human health. Because of the continuous development of wireless networks, there is a need for further research on this topic. Moreover, due to the high popularity of devices using Wi-Fi among children and adolescents, whose period of exposure to electromagnetic radiation is longer compared to adults, it is necessary to continuously observe these populations and subject them to careful analysis.
Role of Growth Hormone (GH) in Liver Regeneration (2004)

Liver regeneration is a fundamental mechanism by which the liver responds to injury. This process is regulated by endogenous growth factors and cytokines, and it involves proliferation of all mature cells that exist within the intact organ. To understand the role of the GH/IGF-I axis in liver regeneration, we performed partial hepatectomies in three groups of mice: GH antagonist (GHa) transgenic mice, in which the action of GH is blocked; liver IGF-I-deficient mice that lack IGF-I specifically in the liver and also lack the acid-labile subunit (ALS; LID+ALSKO mice), in which IGF-I levels are very low and GH secretion is increased; and control mice. Interestingly, the survival rate of GHa transgenic mice was dramatically reduced after partial hepatectomy (57%) compared with the survival rate of controls (100%) or LID+ALSKO mice (88%). In control mice, the liver was completely regenerated after 4 d, whereas liver regeneration required 7 d in LID+ALSKO mice. In contrast, in GHa mice, liver regeneration reached only 70% of the original liver mass after 4 d and did not improve thereafter. Strikingly, 36 and 48 h after hepatectomy, the livers of control and LID+ALSKO mice, respectively, exhibited intense 5-bromo-2'-deoxyuridine (BrdU) staining, whereas BrdU staining was dramatically decreased in the livers of GHa-treated mice. These results suggest that GH plays a critical role in liver regeneration, although whether it acts directly or indirectly remains to be determined.
Dual-Purpose Lenticular Locking Hinges for Actuation and Stiffening of Deployable Origami Arrays (2022)

Abstract Deployable origami arrays have been used to increase the aperture areas of spacecraft instruments. Folds within these patterns allow the arrays to fold compactly, but can also cause un-desired folding when in the deployed state. In addition, there is a need to deploy them with mechanisms that are light and small. This paper introduces a strain-energy storing joint that can be used to deploy and stiffen foldable origami arrays, called the Lenticular Lock (LentLock). The LentLock hinge design includes compliant flexures with geometry based on the Euler spiral. When panels are folded, the flexures are deflected flat and lie in-plane with the panels, storing strain energy. During deployment, the panels are released and the stored strain energy in the flexures opens the folded hinge. Simultaneously, the out-of-plane displacement of the deployed flexures is used to create beneficial interference to stabilize the array and prevent undesired refolding of the mechanism. In this paper, the geometry of the LentLock is introduced and performance of the joint is shown. The Lent-Lock is integrated into several folding mechanisms including a single fold, a single origami vertex, a Z-fold, and a multi-vertex origami array. Proof-of-concept prototypes of each folding pattern are shown.
Brown adipose tissue dysfunction promotes heart failure via a trimethylamine N-oxide-dependent mechanism (2022)

Low body temperature predicts a poor outcome in patients with heart failure, but the underlying pathological mechanisms and implications are largely unknown. Brown adipose tissue (BAT) was initially characterised as a thermogenic organ, and recent studies have suggested it plays a crucial role in maintaining systemic metabolic health. While these reports suggest a potential link between BAT and heart failure, the potential role of BAT dysfunction in heart failure has not been investigated. Here, we demonstrate that alteration of BAT function contributes to development of heart failure through disorientation in choline metabolism. Thoracic aortic constriction (TAC) or myocardial infarction (MI) reduced the thermogenic capacity of BAT in mice, leading to significant reduction of body temperature with cold exposure. BAT became hypoxic with TAC or MI, and hypoxic stress induced apoptosis of brown adipocytes. Enhancement of BAT function improved thermogenesis and cardiac function in TAC mice. Conversely, systolic function was impaired in a mouse model of genetic BAT dysfunction, in association with a low survival rate after TAC. Metabolomic analysis showed that reduced BAT thermogenesis was associated with elevation of plasma trimethylamine N-oxide (TMAO) levels. Administration of TMAO to mice led to significant reduction of phosphocreatine and ATP levels in cardiac tissue via suppression of mitochondrial complex IV activity. Genetic or pharmacological inhibition of flavin-containing monooxygenase reduced the plasma TMAO level in mice, and improved cardiac dysfunction in animals with left ventricular pressure overload. In patients with dilated cardiomyopathy, body temperature was low along with elevation of plasma choline and TMAO levels. These results suggest that maintenance of BAT homeostasis and reducing TMAO production could be potential next-generation therapies for heart failure.
Development and Testing of a Cylindrical LED Lighting Unit for a Conveyer-Type Salad Production System (2004)

&lt;div class="htmlview paragraph"&gt;A cylindrical plant growth chamber (PGC) referred to as PHYTOCYCLE-SD was designed and developed as a conveyor-type cultivation system for continuous production of salad crops. The volume of the plant growth chamber is 0.19 m&lt;sup&gt;3&lt;/sup&gt;, and the illuminated crop area is 0.86 m&lt;sup&gt;2&lt;/sup&gt;. The PGC is comprised of a convex cylindrical planting surface with a spiral cylindrical light unit (LU) above the planting surface. The LU consists of 15 light-emitting diode (LED) panels distributed on the spiral cylindrical surface with adjustable operating currents between 10 to 35 mA. The average photosynthetic photon flux (PPF, 400–700 nm wavelengths) level at the crop surface (3 cm below the light bar) is 350 μmol m&lt;sup&gt;−2&lt;/sup&gt; s&lt;sup&gt;−1&lt;/sup&gt; and the LU power consumption is approximately 440 W. Leaf area as a function of the radius of the cylindrical growth chamber has been determined experimentally. Light intensity and distribution inside cylindrical growth chamber has been measured and modeled. These models can be used to estimate the productivity of various species crops in a spiral growth chamber compared to a flat surface.&lt;/div&gt;
Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer’s Disease (2017)

A mini-HTS on 4000 compounds selected using 2D fragment-based similarity and 3D pharmacophoric and shape similarity to known selective tau aggregate binders identified N-(6-methylpyridin-2-yl)quinolin-2-amine 10 as a novel potent binder to human AD aggregated tau with modest selectivity versus aggregated β-amyloid (Aβ). Initial medicinal chemistry efforts identified key elements for potency and selectivity, as well as suitable positions for radiofluorination, leading to a first generation of fluoroalkyl-substituted quinoline tau binding ligands with suboptimal physicochemical properties. Further optimization toward a more optimal pharmacokinetic profile led to the discovery of 1,5-naphthyridine 75, a potent and selective tau aggregate binder with potential as a tau PET tracer.
P-Val: Antifuse-Based Package-Level Defense Against Counterfeit ICs (2015)

The rapidly growing incidences of counterfeit integrated circuits (ICs) pose a significant threat to the semiconductor industry. These ICs may suffer from functional, performance, or reliability issues and can affect chip manufacturers, system designers as well as end users. The standard chip/package level structural and functional tests are often inadequate in detecting various forms of counterfeit ICs. Moreover, existing design for security approaches are usually not attractive due to additional design modifications, hardware overhead, test cost, and inadequate robustness. In this paper, we propose a novel, low-overhead package-level IC integrity validation approach, referred to as P-Val, for unified protection against two primary forms of counterfeiting attacks: 1) recycling and 2) cloning. Protection against recycled/remarked chips is achieved through a unique active defense that inserts antifuses (AFs) (one-time programmable) to few select pins inside the package. It effectively disables the functionality or “locks” these pins, which need to be programmed before first-time use to make a chip functional in a system. To protect against cloned ICs, intrinsic random variations in programmed resistances of AFs connected to some of the remaining IC pins are exploited to create unique chip-specific signatures for authentication. P-Val requires no die-level design modifications and remains effective for legacy designs. Moreover, we show that it is effective for small chips with just few pins including analog ICs, where common authentication approaches fail to work. We discuss optimal choice of AF structure and program parameters; their integration in IC packages; and the signature generation/verification process. Through mathematical analysis and simulation results, we demonstrate that the proposed mechanism provides high level of protection against counterfeiting attacks at ultralow overhead (<0.05% package area).