gebhart/patrepeval huggingface dataset:
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011:  Opener of Large-Conductance Ca2+-Activated Potassium (Maxi-K) Channels, Identification, Solubility, and SAR (2007)

Compound 8a (BMS-191011), an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. However, 8a suffered from poor aqueous solubility, which complicated elucidation of SAR during in vitro evaluation. The activity of 8a in in vivo stroke models and studies directed toward improving its solubility are reported herein. Enhanced solubility was achieved by appending heterocycles to the 8a scaffold, and a notable observation was made that inclusion of a simple amino group (anilines 8k and 8l) yielded excellent in vitro maxi-K ion channel opening activity and enhanced brain-to-plasma partitioning compared to the appended heterocycles.
Assessment of a capsid-modified E1B 55-kDa protein-deficient adenovirus vector for tumor treatment (2005)

ONYX-015 and H101 are E1B 55-kDa protein-deficient replicating C group adenoviruses that are currently in clinical trials as antitumor agents. However, their application in cancer gene therapy is limited by the native tropism of C group adenoviruses. This is in part due to low expression of the C group adenovirus receptor (coxsackievirus-adenovirus receptor, CAR) on malignant tumors. An H101-based chimeric virus vector containing sequences encoding the Ad35 fiber domain instead of the Ad5 fiber (H101-F35) was constructed. This modification allowed infection of tumor cells through CD46, a membrane protein over-expressed on tumors. The CAR and CD46 RNA expression was evaluated by RT-PCR method. H101-F35 conferred a stronger cytocidal effect than H101 and ONYX-015 in tumor cell lines that lacked CAR expression (MDA-MB-435 and MCF-7), while the cytocidal effect of H101-35, H101 and ONYX-015 was similar in high-level CAR expressing cancer cell lines (A549, NCI-H446, Hep3B, LNCaP, ZR-75-30 and Bcap-37). In an MDA-MB-435 xenograft mouse tumor model, tumor growth in mice receiving H101-F35 was significantly inhibited compared with mice injected with H101. These results suggest that the chimeric oncolytic adenovirus H101-F35 vector might be a useful candidate for gene therapy of cancer.
Novel Optical Sensors for High Temperature Measurement in Harsh Environments (2003)

Accurate measurement of temperature is essential for the safe and efficient operation and control of a vast range of industrial processes. Many of these processes involve harsh environments, such as high temperature, high pressure, chemical corrosion, toxicity, strong electromagnetic interference, and high-energy radiation exposure. These extreme physical conditions often prevent conventional temperature sensors from being used or make them difficult to use. Novel sensor systems should not only provide accurate and reliable temperature measurements, but also survive the harsh environments through proper fabrication material selections and mechanical structure designs. This dissertation presents detailed research work on the design, modeling, implementation, analysis, and performance evaluation of novel optical high temperature sensors suitable for harsh environment applications. For the first time to our knowledge, an optical temperature sensor based on the broadband polarimetric differential interferometric (BPDI) technology is proposed and tested using single crystal sapphire material. With a simple mechanically structured sensing probe, in conjunction with an optical spectrum-coded interferometric signal processing technique, the proposed single crystal sapphire optical sensor can measure high temperature up to 1600 oC in the harsh environments with high accuracy, corrosion resistance, and long-term measurement stability. Based on the successfully demonstrated sensor prototype in the laboratory, we are confident of the next research step on sensor optimization and scale-up for full field implementations. The goal for this research has been to bring this temperature sensor to a level where it will become commercially viable for harsh environment applications associated with industries.
Acute hepatitis and Brucella melitensis infection: clinicopathological findings (1988)

The clinical and pathological findings in a patient who had acute hepatitis caused by Brucella melitensis are described. Antibiotic therapy induced a good clinical and biochemical response, although a relapse occurred. Brucellosis must be considered in the differential diagnosis of pyrexia of unknown origin, particularly if associated hepatic involvement is present. A careful occupational and travel history is essential.
Perspectives on morphological complexity (2012)

This paper discusses the notion of morphological complexity and differentiates language external complexity (E-complexity) from language internal complexity (I-complexity). While E-complexity is measurable on the basis of the statistical occurrences of affixes and their combinations with roots, I-complexity can be measured on the basis of the number of operations applying in the derivation of morphological forms. The author compares results from studies classifying languages based on their E-complexity to results from studies showing similarities between languages with respect to I-complexity. The comparison reveals that languages with different E-complexity may have similar I-complexity. The author revisits results from psycholinguistic and parsing experiments and discusses how the two sorts of complexity can be reduced. Finally, the role of I- and E-complexity for the understanding of the relation between the language faculty and the external systems is considered.
The Relationship between Structural and Electrical Characteristics in Perylenecarboxydiimide‐Based Nanoarchitectures (2015)

The controlled assembly of the prototypical n‐type organic semiconductor N,N′‐1H,1H‐perfluorobutyl dicyanoperylenecarboxydiimide (PDIF‐CN 2 ) into ordered nanoarchitectures and the multiscale analysis of the correlation between their structural and their electrical properties is reported. By making use of the Langmuir–Blodgett (LB) technique, monolayers of PDIF‐CN 2 arranged in upright standing molecular packing on different substrates are formed. Postdeposition thermal treatment makes it possible to trigger a reorganization into layered ultrathin crystalline nanostructures, exhibiting structural and photophysical properties similar to those of microscopic crystals obtained by solvent‐induced precipitation. The controlled engineering of these molecular architectures on surfaces enables us to identify both a dependence of the monolayer resistance on the molecular tilt angle in vertical junctions and a pronounced charge‐transport anisotropy with enhanced transport along the π–π stacking direction of the PDI core. While a charge carrier mobility for electrons as high as 10 –2 cm 2 V –1 s –1 is determined in monolayer field‐effect transistors for the in‐plane direction, being the highest yet reported value for a n‐type LB monolayer, the out‐of‐plane mobility measured by conductive atomic force microscopy in multilayered structures is found to be one order of magnitude lower.
Guideline on network security testing (2003)

The Information Technology Laboratory (ITL) at the National Institute of Standards and Technology (NIST) promotes the U.S. economy and public welfare by providing technical leadership for the Nation's measurement and standards infrastructure. ITL develops tests, test methods, reference data, proof of concept implementations, and technical analysis to advance the development and productive use of information technology. ITL's responsibilities include the development of technical, physical, administrative, and management standards and guidelines for the cost-effective security and privacy of sensitive unclassified information in Federal computer systems.
Novel dibenzo[a,e]pentalene-based conjugated polymers (2013)

Dibenzo[a,e]pentalene (DBP), a ladder-type fused-ring system with 16π anti-aromatic nature, is integrated into conjugated polymers with oligothiophene building blocks to examine the potential of DBP as a new building block for semiconducting polymers. Depending on the incorporation manner of the DBP unit in the polymer backbone, via the 5,10- or 2,7-positions, the polymers show distinct colours, reflecting the different electronic structures, though the HOMO and LUMO energy levels estimated from cyclic voltammograms are almost the same. Interestingly, the impact of the incorporation manner was observed in the characteristics of their field-effect transistors (FETs). For PDTDBP2Ts, in which the DBP units are integrated into the polymer backbone via the 5,10-positions, the DBP units behave like a “dibenzo-annulated 1,3-butadiene” moiety, and their FET characteristics are strongly affected by orientational ordering and crystallinity, similar to ordinary “donor-only” polymers such as P3HT. On the other hand, iPDTDBP2Ts, in which the whole 16π DBP unit is integrated into the polymer backbone via the 2,7-positions, behave like a certain kind of donor-acceptor polymers, and the FET characteristics are independent of orientational order: the field-effect mobilities are higher than 0.1 cm2 V−1 s−1 regardless of the polymer orientation in the thin film. From these results, we can recognize the 16π anti-aromatic DBP unit as a useful building block with transmutable nature for the development of new conjugated polymers.
A broadband local area network using the intelligent head-end (2003)

A broadband local area network system call is illustrated using the previously developed intelligent head-end. The head-end provides the advantages of dynamical channel exchange and network configuration control facility. The head-end exchanges analog information in a manner similar to the digital exchange. A novel LAN architecture is described, which is based on the open system interconnection for the broadband network, to which the digital/analog devices are connected. A prototype model experiment is presented.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Dual-mode endoscopic probe combining OCT and autofluorescence imaging for inner ear hearing loss diagnosis and therapy guidance (Conference Presentation) (2020)

This study presents a novel technology for in vivo cochlear imaging in sensorineural hearing loss (SNHL). SNHL is the most common type of permanent hearing loss and is associated with damaged hair cells of the cochlea. State of the art clinical imaging does not have sufficient resolution to show inner ear microstructure. We are developing and testing a dual-modal endoscopic instrument that combines optical coherence tomography (OCT) and autofluorescence imaging (AFI) for dynamic cochlear imaging. If successful, this approach will improve our understanding of the cellular basis of SNHL and enable the development of targeted therapies for inner ear disorders.
UNDERWATER MARINE APPLICATIONS OF COATINGS AND ADHESIVES (1974)

This paper describes two types of plastics formulation, one used for metal surface coating, the other for bonding in applications. There are two basic types of coatings that have been investigated. The first type investigated was the high viscosity, epoxy-polyamide material commonly called splash-zone compound. Later investigations concerned lower viscosity materials of brushable consistency. Each of these types is discussed separately. Results of experiments aimed at the development of rapidly curing adhesives that could be applied under seawater for construction and repair are tabulated and evaluated. Formulations for underwater adhesive with optimal properties are included in this report.
Growth regulators in connective tissue. Systemic administration of an aortic extract inhibits tumor growth in mice. (1978)

A low-molecular-weight fraction prepared from extracts of bovine aorta inhibits the growth of a transplantable mammary tumor and a fibrosarcoma in mice when injected systemically. It also inhibits the growth of the fibrosarcoma in cell culture. The effect on the fibrosarcoma is much more marked than on the mammary tumor. Since the extract is more effective against the fibrosarcoma and is known to inhibit the growth of endothelial cells, it appears that the enhanced effect on this tumor is due to its activity on the endothelial cells of the host and the tumor cells themselves. The material injected is enriched in an antiproteinase we have previously isolated, which has anticollagneolytic activity and is presumed to be the effector molecule.
Synthesis of Novel α,β-Unsaturated Sulfonic Acid Derivatives Containing Dithiocarbamate/Xanthate Groups by Ring Opening of an α,β-Unsaturated γ-Sultone (2020)

An efficient method is disclosed for the synthesis of novel α,β-unsaturated sulfonic acid derivatives containing dithiocarbamate/xanthate groups through ring opening of an α,β-unsaturated γ-sultone with dithiocarbamic acid salts or xanthates prepared in situ. Treatment of the primary products with hydrochloric acid afforded the corresponding β-chloro-γ-(dithiocarbamato)propanesulfonic acids in excellent yields.
Acute Intermittent Porphyria: Expression of Mutant and Wild-Type Porphobilinogen Deaminase in COS-1 Cells (2000)

The results confirm the causality of mutations for the half normal enzyme activity measured in the patients' erythrocytes. In contrast to the decreased enzyme activity, the majority of the mutations produced a detectable polypeptide, and the stability and the intracellular processing of the mutated polypeptides were both comparable to that of the wild-type PBGD and independent of the cross-reacting immunological material (CRIM) class.
Exploring Li distribution in Li-ion batteries with FIB-SEM and TOF-SIMS (2018)

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Producción en reactores de membrana de hidrolizados enzimáticos de proteínas lácteas para nutrición enteral (2011)

En esta tesis doctoral se estudia el proceso de produccion encontinuo de hidrolizados enzimaticos de proteinas para nutricion enteral. En primer lugar se seleccionan el sustrto y la enzima mas adecuados. Por su alto valor biologico, el sustrato utilizado ha sido un concentrado de proteinas de lactosuero con un 76% en proteina. Para la hidrolisis de este sustrato, la proteasa bacteriana protex 6L ha resultado ser la mas eficaz a pH8,5 y T50oC. Seguidamente se ha puesto a punto la metodologia necesaria para el segumiento continuo del proceso. La determinacion del grado de hidrolisis se realiza por medidas del volumen de base necesario para nmantener constante el pH en el reactor y por medidas del descenso del punto de congelacion de la mezcla reaccionante. Sin embargo para relacionar ambas variables con el grado de hidrolisis ha sido necesario determinar el valor de pK medio de los grupos a-amino liberados. El proceso de reaccion se ha controlado tambien por la medida del indice de solubilidad de los peptidos en TCA. El producto se ha caracterizado mediante la determinacion de la distribucion de los pesos moleculares de los peptidos por cromatografia liquida de exclusion y por medidas del potencial antigenico. Se ha realizaco el estudio cinetico del proceso de hidrolisis. La variable intensiva del tratamiento enzimatico es e t/s que permite optimizar las condiciones de operacion. El proceso se ha llevado a cabo en un reactor discontinuo agitado y en un reactor concitnuo de membrana, en el que el modulo de filtracion seleccionado ha sido un modulo de ultrafiltracion tangencial de poliestersulfona d e3000Da. Se ha comprobado que la realizaciond e la hidrolisis en el reactor de membrana permite incrementar la capacidad del proceso (masa de nitrogeno/masa de enzima tiempo) de 5 a 6 veces respecto a los resultados obtenidos en el proceso discontinuo. Ademas los hidrolizados obtenidos cum
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from Mycobacterium tuberculosis to overcome kanamycin resistance (2021)

Tuberculosis (TB), caused by <i>Mycobacterium tuberculosis</i> (<i>Mtb</i>), is a deadly bacterial disease. Drug-resistant strains of <i>Mtb</i> make eradication of TB a daunting task. Overexpression of the enhanced intracellular survival (Eis) protein by <i>Mtb</i> confers resistance to the second-line antibiotic kanamycin (KAN). Eis is an acetyltransferase that acetylates KAN, inactivating its antimicrobial function. Development of Eis inhibitors as KAN adjuvant therapeutics is an attractive path to forestall and overcome KAN resistance. We discovered that an antipsychotic drug, haloperidol (HPD, <b>1</b>), was a potent Eis inhibitor with IC<sub>50</sub> = 0.39 ± 0.08 μM. We determined the crystal structure of the Eis-haloperidol (<b>1</b>) complex, which guided synthesis of 34 analogues. The structure-activity relationship study showed that in addition to haloperidol (<b>1</b>), eight analogues, some of which were smaller than <b>1</b>, potently inhibited Eis (IC<sub>50</sub> ≤ 1 μM). Crystal structures of Eis in complexes with three potent analogues and droperidol (DPD), an antiemetic and antipsychotic, were determined. Three compounds partially restored KAN sensitivity of a KAN-resistant <i>Mtb</i> strain K204 overexpressing Eis. The Eis inhibitors generally did not exhibit cytotoxicity against mammalian cells. All tested compounds were modestly metabolically stable in human liver microsomes, exhibiting 30-60% metabolism over the course of the assay. While direct repurposing of haloperidol as an anti-TB agent is unlikely due to its neurotoxicity, this study reveals potential approaches to modifying this chemical scaffold to minimize toxicity and improve metabolic stability, while preserving potent Eis inhibition.
Important Drop Rate of Acute Diabetes Complications in People With Type 1 or Type 2 Diabetes After Initiation of Flash Glucose Monitoring in France: The RELIEF Study (2021)

&lt;b&gt;Objective&lt;/b&gt; &lt;p&gt;The RELIEF study assessed rates of hospitalization for acute diabetes complications in France, before and after initiating the FreeStyle Libre system. &lt;/p&gt; &lt;p&gt;&lt;b&gt;Research Design and Methods&lt;/b&gt;&lt;/p&gt; &lt;p&gt;74,011 patients with type 1 diabetes or type 2 diabetes who initiated the FreeStyle Libre system were identified from the French national claim database (SNDS) using ICD-10 codes, from hospitalizations with diabetes as a contributing diagnosis, or the prescription of insulin. Patients were sub-classified based on SMBG strip-acquisition prior to starting FreeStyle Libre. Hospitalizations for DKA, severe hypoglycemia, diabetes-related coma and hyperglycemia were recorded for the 12 months before and after initiation. &lt;/p&gt; &lt;p&gt;&lt;b&gt;Results&lt;/b&gt;&lt;/p&gt; &lt;p&gt;Hospitalizations for acute diabetes complications fell in type 1 diabetes (-49.0%) and in type 2 diabetes (-39.4%) following FreeStyle Libre initiation. DKA fell in type 1 diabetes (-56.2%,) and in type 2 diabetes (-52.1%), as did diabetes-related comas in type 1 diabetes (-39.6%) and in type 2 diabetes (-31.9%). Hospitalizations for hypoglycemia and hyperglycemia decreased in type 2 diabetes (-10.8% and -26.5%, respectively). Before initiation, hospitalizations were most marked for people non-compliant with SMBG and for those with highest acquisition of SMBG, which fell by -54.0% and 51.2% respectively following FreeStyle Libre initiation. Persistence with FreeStyle Libre at 12 months was 98.1%.&lt;/p&gt; &lt;p&gt;&lt;b&gt;Conclusions&lt;/b&gt;&lt;/p&gt; &lt;p&gt;This large retrospective study on hospitalizations for acute diabetes complication shows that a significantly lower incidence of admissions for DKA and for diabetes-related coma is associated with use of flash glucose monitoring. This study has significant implications for patient-centered diabetes care and potentially for long-term health economic outcomes.&lt;/p&gt; &lt;br&gt; &lt;p&gt; &lt;/p&gt;
TRAIL-Mediated Apoptosis in Breast Cancer Cells Cultured as 3D Spheroids (2014)

TNF-alpha-related-apoptosis-inducing-ligand (TRAIL) has been explored as a therapeutic drug to kill cancer cells. Cancer cells in the circulation are subjected to apoptosis-inducing factors. Despite the presence of these factors, cells are able to extravasate and metastasize. The homotypic and heterotypic cell-cell interactions in a tumor are known to play a crucial role in bestowing important characteristics to cancer cells that leave the primary site. Spheroid cell culture has been extensively used to mimic these physiologically relevant interactions. In this work, we show that the breast cancer cell lines BT20 and MCF7, cultured as 3D tumor spheroids, are more resistant to TRAIL-mediated apoptosis by downregulating the expression of death receptors (DR4 and DR5) that initiate TRAIL-mediated apoptosis. For comparison, we also investigated the effect of TRAIL on cells cultured as a 2D monolayer. Our results indicate that tumor spheroids are enriched for CD44hiCD24loALDH1hi cells, a phenotype that is predominantly known to be a marker for breast cancer stem cells. Furthermore, we attribute the TRAIL-resistance and cancer stem cell phenotype observed in tumor spheroids to the upregulation of cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE₂) pathway. We show that inhibition of the COX-2/PGE₂ pathway by treating tumor spheroids with NS-398, a selective COX-2 inhibitor, reverses the TRAIL-resistance and decreases the incidence of a CD44hiCD24lo population. Additionally, we show that siRNA mediated knockdown of COX-2 expression in MCF7 cells render them sensitive to TRAIL by increasing the expression of DR4 and DR5. Collectively, our results show the effect of the third-dimension on the response of breast cancer cells to TRAIL and suggest a therapeutic target to overcome TRAIL-resistance.
Bioinspired Preparation of Ultrathin SiO2 Shell on ZnO Nanowire Array for Ultraviolet-Durable Superhydrophobicity (2009)

ZnO nanowire (NW) array was conformally coated with an ultrathin SiO(2) shell by a bioinspired layer-by-layer deposition in order to obtain ultraviolet (UV)-durable superhydrophobic property. Uniform SiO(2) shell was prepared on ZnO NW by alternative reactive deposition of polyethylenimine and silicic acid. Despite the highly curved morphology of ZnO NW array, the thickness of SiO(2) shell increased linearly with the number of deposition cycles, with a thickness increment being of approximately 4.17 nm per deposition cycle. The SiO(2) shell only had a slight influence on the superhydrophobic property of ZnO NW array after modification with a monolayer of octadecyltrimethoxysilane (OTS). However, it greatly improved the UV durability of the superhydrophobic property of ZnO NW array due to the confinement effect of insulating SiO(2) layer on the photogenerated electron-hole pairs in ZnO NW.
2-(2-Alkylai-nino-4-aminothiazol-5-oyl)-N-methylbenzimidazoles: Synthesis and the effect of intra molecular H-bonding in 1H NMR (2009)

2-(2-Alkylamino-4-aminothiazol-5-oyl)-N-methylbenzimidazoles, as the analogs of the cytotoxic marine alkaloid dendrodoine, is synthesized and characterized by elemental analysis, IR, NMR and mass spectral data. The thiourea derivatives provide four ring atoms for the thiazole ring construction and thus act as [C-N-C-S] synthons. The remaining carbon of the thiazole is sourced from 2-(2-bromoacetyl)-N-methylbenzimidazole. This [4+1] heterocyclization reaction is adopted for the synthesis of novel benzimidazole derivatives. The presence of two signals in the 1 H NMR spectrum arising from the NH 2 hydrogens shows that the two hydrogens are not exchanging rapidly on the chemical shift time scale and they arc in two different chemical environments due to II-bonding.