gebhart/patrepeval huggingface dataset:
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide:  A Selective α-Amino Amide Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes (2006)

A series of beta-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide (6), a potent, orally active DPP-4 inhibitor (IC(50) = 6.3 nM) with excellent selectivity, oral bioavailability in preclinical species, and in vivo efficacy in animal models. Compound 6 was selected for further characterization as a potential new treatment for type 2 diabetes.
Contrasting acute graft-versus-host disease effects of Tim-3/galectin-9 pathway blockade dependent upon the presence of donor regulatory T cells (2012)

T-cell immunoglobulin mucin-3 (Tim-3) is expressed on pathogenic T cells, and its ligand galectin-9 (gal-9) is up-regulated in inflamed tissues. When Tim-3(+) T cells encounter high gal-9 levels, they are deleted. Tim-3 is up-regulated on activated T cells during GVHD. Inhibition of Tim-3/gal-9 binding by infusion of a Tim-3-Ig fusion protein or Tim-3(-/-) donor T cells increased T-cell proliferation and GVHD lethality. When the Tim-3/gal-9 pathway engagement was augmented using gal-9 transgenic recipients, GVHD lethality was slowed. Together, these data indicate a potential for modulating this pathway to reduce disease by increasing Tim-3 or gal-9 engagement. Paradoxically, when Tim-3/gal-9 was inhibited in the absence of donor T-regulatory cells (Tregs), GVHD was inhibited. GVHD reduction was associated with decreased colonic inflammatory cytokines as well as epithelial barrier destruction. CD25-depleted Tim-3(-/-) donor T cells underwent increased activation-induced cell death because of increased IFN-γ production. To our knowledge, these studies are the first to show that although the absence of Tim-3/gal-9 pathway interactions augments systemic GVHD, concurrent donor Treg depletion paradoxically and surprisingly inhibits GVHD. Thus, although donor Tregs typically inhibit GVHD, under some conditions, such Tregs actually may contribute to GVHD by reducing activation-induced T-cell death.
Cryptanalysis of the New CLT Multilinear Maps. (2015)

Multilinear maps have many cryptographic applications. The first candidate construction of multilinear maps was proposed by Garg, Gentry, and Halevi (GGH13) in 2013, and soon afterwards, another candidate was suggested by Coron, Lepoint, and Tibouchi (CLT13) that works over the integers. However, both of these were found to be insecure in the face of a so-called zeroizing attack (HJ15, CHL15). To improve on CLT13, Coron, Lepoint, and Tibouchi proposed another candidate of new multilinear maps over the integers (CLT15). In this paper, we describe an attack against CLT15. Our attack shares the essence of the cryptanalysis of CLT13 and exploits low level encodings of zero, as well as other public parameters. As in CHL15, this leads to finding all the secret parameters of κmultilinear maps in polynomial time of the security parameter.
Phase conjugation by four-wave mixing in single-mode fibers (1994)

We present an exact solution to the coupled-mode equations, governing four-wave mixing in single-mode fibers, under the perfect phase-matching condition. The solution accounts for pump depletion and fiber absorption. Optimum length of fiber is derived and phase conjugation efficiency is calculated and discussed. The calculated results are in good agreement with the reported experimental results.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
A calorimetric study of self-heating in coffee and chicory (1982)

Abstract The technique of heat flow calorimetry was used to determine the specific heat of coffee and chicory products and to study their thermal behaviour above 20°C. Intensive exothermic reactions were particularly evident when measurements were made with sealed cells. The data obtained help in the understanding of how exothermic reactions (and self-heating) occurring in such foodstuffs can bring them above their minimum ignition temperature.
Techtile – Open 6G R&D Testbed for Communication, Positioning, Sensing, WPT and Federated Learning (2022)

New concepts for next-generation wireless systems are being developed. It is expected that these 6G and beyond systems will incorporate more than only communication, but also sensing, positioning, (deep) edge computing, and other services. The discussed measurement facility and approach, named Techtile, is an open, both in design and operation, and unique testbed to evaluate these newly envisioned systems. Techtile is a multi-functional and versatile testbed, providing fine-grained distributed resources for new communication, positioning and sensing technologies. The facility enables experimental research on hyper-connected interactive environments and validation of new algorithms and topologies. The backbone connects 140 resource units equipped with edge computing devices, software-defined radios (SDRs), sensors, and LED sources. By doing so, different network topologies and local-versus-central computing can be assessed. The introduced diversity of i) the technologies (e.g., RF, acoustics and light), ii) the distributed resources and iii) the interconnectivity allows exploring more degrees and new types of diversity, which can be investigated in this testbed.
The northwest frontier: Spectroscopy of N ∼ Z nuclei below mass 100 (2009)

The spectroscopy and structure of excited states of N similar to Z nuclei in the mass 70-100 region has been investigated using two techniques. In the A similar to 70-80 region fusion evaporation reactions coupled with the recoil-beta-tagging method have been employed at Jyvaskyla to study low-lying states in odd-odd N = Z nuclei. Results from these and other data for known odd-odd nuclei above mass 60 will be discussed. In the heavier mass 90 region a fragmentation experiment has been performed using the RIS-ING/FRS setup at GSI. This experiment was primarily aimed at searching for spin gap isomers in nuclei around A similar to 96. The objectives of the latter experiment will be discussed.
Etude moléculaire des voies d'oxydation et de réduction du glycérol chez Clostridium butyricum (2003)

C. Butyricum est une bacterie sporulante, strictement anaerobie et capable d'assimiler le glycerol. Les genes et les enzymes de la voie d'oxydation du glycerol, la glycerol deshydrogenase, codee par le gene dhaD1, et la DHA kinase codee par les trois genes dhaK1, dhaK2 et dhaK3 ont ete caracterises. L'organisation genomique de la DHA kinase est differente de celle decrite chez les autres micro-organismes, ce qui met en evidence l'originalite de cette enzyme chez C. Butyricum. La voie de reduction du glycerol a mis en evidence une organisation genomique en operon des genes dhaB1 et dhaB2 codant respectivement pour une glycerol deshydratase atypique, sa proteine activatrice et dhaT codant pour une 1,3-propanediol deshydrogenase. Une regulation au niveau transcriptionnel par un systeme putatif de transduction du signal a deux composants (TCS) est egalement suggeree pour les deux voies metaboliques. La caracterisation moleculaire et biochimique des proteines DhaB1 et DhaB2 a permis de confirmer que la glycerol deshydratase de C. Butyricum est d'un type entierement nouveau puisqu'elle est coenzyme B12-independante contrairement a toutes les glycerol deshydratases decrites a ce jour. Par ailleurs, les donnees biochimiques suggerent un mecanisme radicalaire pour cette enzyme analogue a celui decrit pour les autres enzymes a radical SAM. L'analyse structurale de DhaB1 initiee lors de ce travail permettra de la comparer aux pyruvate formate lyases, enzymes a radical SAM les mieux caracterisees. Enfin, les divers outils moleculaires et biochimiques developpes pour cette etude pourront ulterieurement etre utilises pour des experiences d'ingenierie proteique afin d'accroitre nos connaissances sur le mecanisme d'action de cette enzyme
ChemInform Abstract: Cu(I)‐Mediated Intramolecular Conjugate Addition of Alkenyltrimethylstannane Functions to α,β‐Unsaturated Ketones: A Convenient Preparation of Functionalized cis‐Fused Bicyclo[4.3.0]non‐8‐en‐3‐ones and Bicyclo[3.3.0]oct‐6‐en‐3‐ones. (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.
Exposure Time Optimization for Highly Dynamic Star Trackers (2014)

Under highly dynamic conditions, the star-spots on the image sensor of a star tracker move across many pixels during the exposure time, which will reduce star detection sensitivity and increase star location errors. However, this kind of effect can be compensated well by setting an appropriate exposure time. This paper focuses on how exposure time affects the star tracker under highly dynamic conditions and how to determine the most appropriate exposure time for this case. Firstly, the effect of exposure time on star detection sensitivity is analyzed by establishing the dynamic star-spot imaging model. Then the star location error is deduced based on the error analysis of the sub-pixel centroiding algorithm. Combining these analyses, the effect of exposure time on attitude accuracy is finally determined. Some simulations are carried out to validate these effects, and the results show that there are different optimal exposure times for different angular velocities of a star tracker with a given configuration. In addition, the results of night sky experiments using a real star tracker agree with the simulation results. The summarized regularities in this paper should prove helpful in the system design and dynamic performance evaluation of the highly dynamic star trackers.
Implementation of a 2D motion vector detection on image sensor focal plane (2003)

A vision chip for very fast detection of motion vector is presented. It consists of a pixel array and parallel block matching processors. Each pixel of the pixel array contains a photodetector, an edge detector and a 4-bit memory. The image data is firstly binarized by the edge detector and then the binary edge data is used in the block matching. The block matching is performed in local pixel parallel and global column parallel way. We can obtain a dense motion field in which a motion vector is assigned to each pixel by overlapping 2/spl times/2 target blocks. The prototype with 16/spl times/16 pixels and four block matching processors is designed and implemented. Test results obtained by the prototype are shown.
Structure-Property Relationships of Perfectly Alternating Polycarbonate-Polydimethylsiloxane Block Copolymers, Part II (1984)

Abstract The relationships between the properties and microstructures of two series of perfectly alternating bisphenol A-polycarbonate-polydimethylsiloxane block copolymers were studied. In the first series, the polycarbonate (PC) block length was kept constant while the block length of polydimethylsiloxane (PDMS) was varied. The tensile properties of these block copolymers were found to be a function of composition. Dynamic mechanical properties measured as a function of temperature revealed the two-phase nature of these materials. Transmission electron micrographs showed that all samples had a sponge-like morphology independent of composition. The rheological maximum viscosity for the sample containing PC and PDMS blocks of equal molecular weight and extrudate swells increased with PC content. Takayamagi's mechanical coupling model was used to predict the maximum loss tangent at the glass transition temperature of PDMS using the known properties of pure components. The predictions agreed fairly well with the experimental results. In a second series of block copolymers, the block molecular weights of both PC and PDMS were varied to keep the composition constant. The tensile strength of these samples was found to increase with block molecular weights, except for the sample having the highest block molecular weights. The lower tensile strength of this material was attributed to its lamellar type morphology. Cold crystallization of PDMS blocks was found for samples having high PDMS block molecular weight (greater than 8000 g/mole). The T g of PC blocks followed the Fox-Flory equation with a higher K value than expected. The PDMS content in PC domains was calculated to range from 11% for material of low block molecular weights to about 1.3% for high block molecular weight material.
Bacterial Ice Nucleation in Monodisperse D2O and H2O-in-Oil Emulsions (2016)

Ice nucleation is of fundamental significance in many areas, including atmospheric science, food technology, and cryobiology. In this study, we investigated the ice-nucleation characteristics of picoliter-sized drops consisting of different D2O and H2O mixtures with and without the ice-nucleating bacteria Pseudomonas syringae. We also studied the effects of commonly used cryoprotectants such as ethylene glycol, propylene glycol, and trehalose on the nucleation characteristics of D2O and H2O mixtures. The results show that the median freezing temperature of the suspension containing 1 mg/mL of a lyophilized preparation of P. syringae is as high as -4.6 °C for 100% D2O, compared to -8.9 °C for 100% H2O. As the D2O concentration increases every 25% (v/v), the profile of the ice-nucleation kinetics of D2O + H2O mixtures containing 1 mg/mL Snomax shifts by about 1 °C, suggesting an ideal mixing behavior of D2O and H2O. Furthermore, all of the cryoprotectants investigated in this study are found to depress the freezing phenomenon. Both the homogeneous and heterogeneous freezing temperatures of these aqueous solutions depend on the water activity and are independent of the nature of the solute. These findings enrich our fundamental knowledge of D2O-related ice nucleation and suggest that the combination of D2O and ice-nucleating agents could be a potential self-ice-nucleating formulation. The implications of self-nucleation include a higher, precisely controlled ice seeding temperature for slow freezing that would significantly improve the viability of many ice-assisted cryopreservation protocols.
ChemInform Abstract: New Generation Dopaminergic Agents. Part 4. Exploiting the 2‐Methyl Chroman Scaffold. Synthesis and Evaluation of Two Novel Series of 2‐(Aminomethyl)‐3,4,7,9‐tetrahydro‐2H‐pyrano[2,3‐e]indole and Indol‐8‐one Derivatives. (1998)

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.
Synthesis and anti-tumour activity of some new derivatives of flavone-8-acetic acid (1995)

A robust six-step synthesis of substituted flavone-8-acetic acid sodium salts has been developed and optimised to allow preparation of a wide variety of products for testing as anti-tumour agents. The condensation and cyclisation steps have been combined in an efficient one-pot procedure and efficient procedures for subsequent oxidative cleavage of an allyl group and salt formation have been developed. Using this method a total of 18 derivatives bearing substituents on the 2-phenyl ring have been prepared. Based on encouraging activity from methoxy substituted compounds, attention has been concentrated on these and various mono-, di-, tri- and tetramethoxy compounds have been prepared, most for the first time. Activity of these against MAC15A, both in vitro and in vivo has been determined by collaborators at Bradford and several compounds have comparable or greater activity than the unsubstituted prototype. The presence of a 2'-methoxyl substituent appears to be particularly favourable to activity. Five different heterocyclic analogues with furyl, thienyl and benzothienyl groups at the 2-position have been obtained and these also show good activity with the 3-methyl-2-thienyl compound showing the highest in vivo activity of any compound examined. Attempts to prepare pyridyl and quinolyl derivatives were unsuccessful. The 2-benzyl and 2-diphenylmethyl compounds have also been prepared and while the former shows good activity in vitro, it is inactive in vivo probably due to metabolic breakdown. The latter compound is completely inactive probably due to a requirement for planarity in the 2- substituent. An extended derivative has been obtained by an unexpected mode of reaction encountered in an attempt to prepare the 2-phenylethynyl compound. Both this and a dimeric ether analogue show significant activity, thereby adding to our understanding of the structural requirements for activity. Variation in the 8-acetic acid substituted has been examined by synthesis of three compounds with CH₂C(O)CH₂OH at this position and, by a separate multi-stage synthesis, the compound with tetrazolylmethyl. The former compounds are too insoluble for activity to be measured, while the latter is inactive. A comparison of electron density, as reflected by ¹H and ¹³C NMR shifts, against activity in vitro has been made for all the compounds prepared, and while some trends may be discerned, the correlation is generally poor. A suitable single crystal of flavone acetic acid was prepared and its X-ray structure was obtained by the SERC Crystallography Unit, Cardiff. The structure, which proved to be of the monohydrate showed the preferred orientation of the 2- and 8-substituents and provided accurate dimensions for future theoretical work.
Supplementary Figure S6 from A Drug Repositioning Approach Identifies Tricyclic Antidepressants as Inhibitors of Small Cell Lung Cancer and Other Neuroendocrine Tumors (2023)

&lt;p&gt;- PDF file 980K, Expression levels of the ligands of the GPCRs targeted by the TCAs and the enzymes required for their biosynthesis in SCLC cells&lt;/p&gt;
Rationally designed inhibitors as tools for comparing the mechanism of squalene‐hopene cyclase with oxidosqualene cyclase (2000)

The inhibition of squalene-hopene cyclase (SHC) (E.C. 5.4.99.-), an enzyme of bacterial membranes catalyzing the formation of pentacyclic sterol-like triterpenes, was studied by using different classes of compounds originally developed as inhibitors of oxidosqualene cyclase (OSC) (E.C. 5.4.99.7), the enzyme of eukaryotes responsible for the formation of tetracyclic precursors of sterols. The mechanism of cyclization of squalene by SHC, beginning with a protonation of the 2,3 double bond by an acidic residue of the enzyme, followed by a series of electrophilic additions of the carbocationic intermediates to the double bonds, is similar to the mechanism of cyclization of 2,3-oxidosqualene by OSC. The inhibitors studied included: (i) analogs of the carbocationic intermediates formed during cyclization, such as aza-analogs of squalene and 2,3-oxidosqualene; (ii) affinity-labeling inhibitors bearing a methylidene reactive group; and (iii) vinyldioxidosqualenes and vinylsulfide derivatives of the substrates. Comparison of the results obtained with the two enzymes, SHC and OSC, showed that many of the most effective inhibitors of OSC were also able to inhibit SHC, while some derivatives acted as specific inhibitors. Differences could be easily explained on the basis of the different substrate specificity of the two enzymes.
Applying extracellular vesicles based therapeutics in clinical trials – an ISEV position paper (2015)

Extracellular vesicles (EVs), such as exosomes and microvesicles, are released by different cell types and participate in physiological and pathophysiological processes. EVs mediate intercellular communication as cell-derived extracellular signalling organelles that transmit specific information from their cell of origin to their target cells. As a result of these properties, EVs of defined cell types may serve as novel tools for various therapeutic approaches, including (a) anti-tumour therapy, (b) pathogen vaccination, (c) immune-modulatory and regenerative therapies and (d) drug delivery. The translation of EVs into clinical therapies requires the categorization of EV-based therapeutics in compliance with existing regulatory frameworks. As the classification defines subsequent requirements for manufacturing, quality control and clinical investigation, it is of major importance to define whether EVs are considered the active drug components or primarily serve as drug delivery vehicles. For an effective and particularly safe translation of EV-based therapies into clinical practice, a high level of cooperation between researchers, clinicians and competent authorities is essential. In this position statement, basic and clinical scientists, as members of the International Society for Extracellular Vesicles (ISEV) and of the European Cooperation in Science and Technology (COST) program of the European Union, namely European Network on Microvesicles and Exosomes in Health and Disease (ME-HaD), summarize recent developments and the current knowledge of EV-based therapies. Aspects of safety and regulatory requirements that must be considered for pharmaceutical manufacturing and clinical application are highlighted. Production and quality control processes are discussed. Strategies to promote the therapeutic application of EVs in future clinical studies are addressed.
Distinct X chromosomal rearrangements in four haemophilia B patients with entire F9 deletion (2015)

We identified diverse X chromosomal rearrangements in four haemophilia B patients, which might be caused by distinct mechanisms of genomic rearrangement.
Introduction (2008)

No AccessPlastics Testing and CharacterizationMar 2008IntroductionAlberto Naranjo, María del Pilar Noriega E., Tim A. Osswald, Alejandro Roldán-Alzate, Juan Diego SierraAlberto Naranjo, María del Pilar Noriega E., Tim A. Osswald, Alejandro Roldán-Alzate, Juan Diego Sierrahttps://doi.org/10.3139/9783446418530.001SectionsAboutPDF ToolsAdd to FavoritesDownload CitationTrack CitationsCopy LTI LinkPDF key 'share (en)' returned an object instead of string.FacebookTwitterEmailLinkedIn previous chapternext chapter FiguresReferencesRelatedDetails 2008Pages: 1-6Print ISBN: 978-3-446-41315-3eISBN: 978-3-446-41853-0 Copyright & Permissions© 2008 Carl Hanser Verlag GmbH & Co. KGPDF downloadLoading ...
Design and Implementation of Vertically Emitting Distributed Feedback Lasers for Biological Sensing (2011)

This chapter contains sections titled: Introduction DFB Laser Biosensor Design Fabrication and Instrumentation Experimental Results Conclusions Acknowledgements References
Enteric type adenocarcinoma of the upper tract urothelium associated with ectopic ureter and renal dysplasia: an oncological rationale for complete extirpation of this aberrant developmental anomaly. (1996)

Our experience demonstrates that this anomaly is another scenario in which closed spaced nonfunctional urothelium can undergo malignant degeneration. Since monitoring such units for tumor progression does not seem to be possible presently, conservative treatment appears hazardous. This new recognition of the risk of malignant metaplastic degeneration is an additional rationale to consider complete extirpation of these lesions as the most appropriate treatment in young men.
Serial Observations of Muscle and Fat Mass as Prognostic Factors for Deceased Donor Liver Transplantation (2020)

A large reduction in preoperative SMI was significantly associated with reduced survival after DDLT. Therefore, changes in muscle mass during the preoperative period can be considered as a prognostic factor for survival after DDLT.