gebhart/patrepeval huggingface dataset:
New Disulfide Route to 3-(1-Piperazinyl)-1,2-benzisothiazole. Nucleus for Atypical Antipsychotic Drugs (1999)

A new, one-step commercial process for the preparation of 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride, a key intermediate for the syntheses of some new, “atypical antipsychotic” drugs, was developed. Reaction of bis(2-cyanophenyl) disulfide with excess piperazine at 120−140 °C for 3−24 h in the presence of small amounts of DMSO and 2-propanol formed 3-(1-piperazinyl)-1,2-benzisothiazole in 75−80% yields. The DMSO oxidized the liberated 2-mercaptobenzonitrile to regenerate bis(2-cyanophenyl) disulfide, thereby enabling the utilization of both halves of the symmetrical disulfide to generate product. The reaction mechanism for the conversion of the bis(2-cyanophenyl) disulfide to 3-amino-1,2-benzisothiazole involves the formation of ring-opened sulfenamide and benzamidine intermediates and then their subsequent ring closure to regenerate the 1,2-benzisothiazole nucleus. A safe, efficient, and robust process to prepare 3-(1-piperazinyl)-1,2-benzisothiazole under very concentrated reaction conditions was developed and successfully scaled up in the pilot plant to support the development of ziprasidone.
Doping of SiC by Implantation of Boron and Aluminum (1997)

Experimental studies on aluminum (Al) and boron (B) implantation in 4H/6H SiC are reported; the implantation is conducted at room temperature or elevated temperatures (500 to 700 °C). Both Al and B act as “shallow” acceptors in SiC. The ionization energy of these acceptors, the hole mobility and the compensation in the implanted layers are obtained from Hall effect investigations. The degree of electrical activity of implanted Al/B atoms is determined as a function of the annealing temperature. Energetically deep centers introduced by the Al+/B+ implantation are investigated. The redistribution of implanted Al/B atoms subsequent to anneals and extended lattice defects are monitored. The generation of the B-related D-center is studied by coimplantation of Si/B and C/B, respectively.
Amino acid consensus sequence of UDP-glycosyltransferases taken from the PROSITE database of protein families and domains, which was used to identify the 107 UGT genes 7 (2011)

<b>Copyright information:</b>Taken from "Higher plant glycosyltransferases"Genome Biology 2001;2(2):reviews3004.1-reviews3004.6.Published online 7 Feb 2001PMCID:PMC138907.Copyright © 2001 BioMed Central Ltd Letters in brackets denote alternative amino acids at a particular position; X denotes any amino acid.
Authentication of fingerprint scanners (2011)

Fingerprint scanners have unique patterns that can be used to distinguish one scanner from another one. The pattern, which we call scanner pattern, stems from the variability of device characteristics at silicon level and is caused by imperfections of the conversion from the input to the scanner (i.e., the object applied to it) to its output (i.e., the digital image). The scanner pattern is a sufficiently unique and persistent intrinsic characteristic of the fingerprint scanners even to those of the same technology, manufacturer, and model. We propose a simple and extremely accurate algorithm that is able to distinguish the pattern of one scanner from the pattern of another scanner of exactly the same model by extracting the pattern from a single image, acquired with each scanner. In this way, the scanner pattern can be used to enhance the security of a bio metric system by authenticating the scanner, used to acquire a particular fingerprint image, and thus detect attacks on the scanner. Combining the biometric authentication with a scanner authentication leads to a two-part authentication, which we call bipartite authentication, that verifies both the identity of the user and the "identity" of the fingerprint scanner.
Gelation of Colloidal Crystals without Degradation in Their Transmission Quality and Chemical Tuning (2005)

A single-domain colloidal crystal with high transmission quality, prepared by a shear-induced process, was fixed as a hydrogel film by photopolymerization. Upon gelation, the original optical quality was almost perfectly preserved. By replacing the solvent, the gelled crystal could be converted to smaller lattice constant crystals without significant degradation in its transmission characteristics. The conversion results in a stop-band wavelength coverage across the entire visible light range.
Advances in Theory of Photonic Crystals (2006)

In this paper, the authors review some of the recent advances in the theory of photonic crystals, drawing examples from their own work in magnetooptical and dynamic photonic crystals. The combination of theory and simulations shows that these crystal structures exhibit rich optical physics effects and can provide new ways to accomplish sophisticated optical information-processing tasks
Statistical modeling for unit selection in speech synthesis (2004)

Traditional concatenative speech synthesis systems use a number of heuristics to define the target and concatenation costs, essential for the design of the unit selection component. In contrast to these approaches, we introduce a general statistical modeling framework for unit selection inspired by automatic speech recognition. Given appropriate data, techniques based on that framework can result in a more accurate unit selection, thereby improving the general quality of a speech synthesizer. They can also lead to a more modular and a substantially more efficient system.We present a new unit selection system based on statistical modeling. To overcome the original absence of data, we use an existing high-quality unit selection system to generate a corpus of unit sequences. We show that the concatenation cost can be accurately estimated from this corpus using a statistical n-gram language model over units. We used weighted automata and transducers for the representation of the components of the system and designed a new and more efficient composition algorithm making use of string potentials for their combination. The resulting statistical unit selection is shown to be about 2.6 times faster than the last release of the AT&T Natural Voices Product while preserving the same quality, and offers much flexibility for the use and integration of new and more complex components.
Solar reactor combustion chamber. [chlorine, hydrogen, and oxygen reactions] (1978)

The 3D structure of pancreatic lipase (PL) consists of two functional domains. The N-terminal domain belongs to the alpha/beta hydrolase fold and contains the active site, which involves a catalytic triad analogous to that present in serine proteases. The beta-sandwich C-terminal domain of PL plays an important part in the binding process between the lipase and colipase, the specific PL cofactor. Recent structure-function studies have suggested that the PL C-terminal domain may have an extra role apart from that of binding colipase. This domain contains an exposed hydrophobic loop (beta5') which was found to be located on the same side as the hydrophobic loops surrounding the active site, and it may be involved in the lipid binding process. Indirect evidence for this new function of the PL C-terminal domain has been provided by studies with monoclonal antibodies directed against the beta5' loop. The catalytic activity of the PL-antibody complexes on water insoluble substrates decreased drastically, whereas their esterase activity on a soluble substrate remained unchanged. During the last few years, a number of protein structures (15-lipoxygenase, alpha-toxin from Clostridium perfringens) have been determined that contain domains with close structural homologies with the beta-sandwich C-terminal domain of PL. Generally speaking, these domains show structural homologies with the C2 domains occurring in a wide range of proteins involved in signal transduction (e.g. phosphoinositide-specific phospholipase C, protein kinase C, cytosolic phospholipase A2), membrane traffic (e.g. synaptotagmin I, rabphilin) and membrane disruption (e.g. perforin). Here it is proposed to review the structure and function of the C2 domains, based on the recent 3D structures and improved sequence alignments.
Modification of Calcium Phosphate Cement with α-Hydroxy Acids and Their Salts (2005)

Calcium phosphate cements (CPCs) are usually modified by organic/inorganic additives to improve their mechanical performance and to adjust their rheological and setting properties to clinical requirements. In this work we used several nontoxic and biocompatible α-hydroxylated organic acids (glycolic, lactic, malic, tartaric, and citric acids) and their calcium and sodium salts for the modification of CPC. The unmodified cement used in this study consisted of an equimolar powder mixture of tetracalcium phosphate (TTCP) and dicalcium phosphate anhydrous (DCPA) mixed with water at a powder mass/liquid volume ratio of 3.3 g/mL. It had a compressive strength of 38 MPa and an initial setting time of 8 min. The free acids as cement liquids had mainly a detrimental effect on the strength of the cement and led to a decreased setting time around 2−4 min, while the calcium salts did not significantly alter the cement properties. However, the sodium salts of the oligocarboxylic acids (malic, tartaric, and citric acids) resulted in a liquefying effect combined with a strong reinforcement of the mechanical strength, such that compressive strength increased to 78−99 MPa. The liquefying effect and prolonged setting time of these compounds was thought to derive from a strong increase in the surface charge of both reactants and the reaction product hydroxyapatite as determined by ζ potential, which increased from about −15 and −18 mV in pure water for TTCP and DCPA, respectively, to values around −40 to −50 mV. In contrast, the calcium salts did not alter ζ potentials due to the formation of neutral and stable complexes in aqueous solution.
Detection probability using relative clutter in infrared images (1998)

Clutter plays a very important role in the area of machine and human-in-the-loop target acquisition. A great deal of interest has recently been shown in assessing several different definitions of clutter. In spite of so many definitions available, no single clutter definition has been agreed on by the target acquisition modeling community as being the best. Here we develop a new clutter metric, called relative clutter, based on factor analysis which is extensively used for statistical analysis. This relative clutter combines many definitions of clutter. Different methods for calculating the relative clutter based on the magnitude of the eigenvalues obtained from the correlation matrix are suggested. The relative clutter of many images is analyzed. The relative clutter is used to calculate probability of detection on Night Vision Lab (NVL) Terrain Board Infrared images.
Extending Antibody Fragment Half-Lives with Albumin (2009)

Albumin is the most abundant protein in serum and acts as a multifunctional carrier for many endogenous small molecules, as diverse as fatty acids, metals, bilirubin, amino acids, and vitamins that ensure wide biodistribution of these compounds throughout the body. In addition, its remarkably long half-life of 19 days in humans makes albumin a versatile and preferred carrier for small molecule and protein therapeutics. A receptor-mediated pathway controlled by the neonatal Fc receptor (FcRn) has recently been shown to be essential for regulation of the long half-life of albumin as well as IgG. This new discovery will strongly influence the further development of albumin-fused and albumin-targeting diagnostics and therapeutics.
Waldenström’s Macroglobulinemia/Lymphoplasmacytic Lymphoma, Version 2.2013 (2012)

These NCCN Guidelines Insights highlight the important updates/changes specific to the management of Waldenström's Macroglobulinemia/Lymphoplasmacytic Lymphoma. These include the addition of regimens containing novel agents as primary and salvage therapy options, inclusion of the updated summary of response categories and criteria from the sixth international workshop on Waldenström's Macroglobulinemia, and a section on management of peripheral neuropathy in the accompanying discussion.
Signing on elements in bilinear groups for modular protocol de-sign. (2010)

A signature scheme is called structure-preserving if its verification keys, messages, and signatures are group elements and the verification predicate is a conjunction of pairing product equations. We answer to the open problem of constructing a constant-size structure-preserving signature scheme. The security is proven in the standard model based on a novel non-interactive assumption that can be justified and has an optimal bound in the generic bilinear group model. We also present efficient structure-preserving signature schemes with advanced properties including signing unbounded number of group elements, allowing simulation in the common reference string model, signing messages from mixed groups in the asymmetric bilinear group setting, and strong unforgeability. Among many applications, we show two examples; an adaptively secure round optimal blind signature scheme and a group signature scheme with efficient concurrent join. As a bi-product, several homomorphic trapdoor commitment schemes and one-time signature schemes are presented, too. In combination with the Groth-Sahai non-interactive proof system, these schemes contribute to give efficient instantiations to modular constructions of cryptographic protocols.
Immunization with Porphyromonas (Bacteroides) gingivalis fimbriae protects against periodontal destruction (1992)

Adhesive fimbriae from Porphyromonas gingivalis are cell surface structures which may be important in the virulence of this oral pathogen and thus may serve as a critical or target antigen. Immunization with highly purified 43-kDa fimbrial protein protected against periodontal tissue destruction when tested in the P. gingivalis-infected gnotobiotic rat model. A similarly highly purified 75-kDa cell surface component did not provide protection. Heat-killed whole-cell and sonicated cell surface extracts which contain the 43-kDa protein as well as the 75-kDa component were protective also. This study indicates that the fimbrial protein may serve as a model for the development of effective vaccines against periodontitis, a major human oral disease.
Generating High-Power Short Terahertz Electromagnetic Pulses with a Multifoil Radiator (2013)

We describe a multifoil cone radiator capable of generating high-field short terahertz pulses using short electron bunches. Round flat conducting foil plates with successively decreasing radii are stacked, forming a truncated cone with the z axis. The gaps between the foil plates are equal and filled with some dielectric (or vacuum). A short relativistic electron bunch propagates along the z axis. At sufficiently high particle energy, the energy losses and multiple scattering do not change the bunch shape significantly. When passing by each gap between the foil plates, the electron bunch emits some energy into the gap. Then, the radiation pulses propagate radially outward. For transverse electromagnetic waves with a longitudinal (along the z axis) electric field and an azimuthal magnetic field, there is no dispersion in these radial lines; therefore, the radiation pulses conserve their shapes (time dependence). At the outer surface of the cone, we have synchronous circular radiators. Their radiation field forms a conical wave. Ultrashort terahertz pulses with gigawatt-level peak power can be generated with this device.
Light-activated shape memory of glassy, azobenzene liquid crystalline polymer networks (2011)

Rapidly reconfigurable, adaptive materials are essential for the realization of “smart”, highly engineered technologies sought by aerospace, medicine, and other application areas. Shape memory observed in metal alloys and polymers (SMPs) is a primary example of shape change (adaptation). To date, nearly all shape adaptations in SMPs have been thermally triggered. A desire for isothermal, remotely cued shape adaptations of SMP has motivated examinations of other stimuli, such as light. Only a few reports document so-called light-activated SMP, in both cases exploiting photoinduced adjustments to the crosslink density of a polymer matrix with UV light of 365 nm (crosslinking) and <260 nm (decrosslinking). This work presents a distinctive approach to generating light-activated SMP by employing a glassy liquid crystal polymer network (LCN) material that is capable of rapid photo-fixing with short exposures (<5 min) of eye-safe 442 nm light. Here, linearly polarized 442 nm light is used to photo-fix temporary states in both cantilever and free-standing geometries which are then thermally or optically restored to the permanent shape. The combination of thermal and photo-fixable shape memory presented here yields substantial functionality in a single adaptive material that could reduce part count in applications. As a demonstration of the opportunities afforded by this functional material, the glassy, photoresponsive LCN is thermally fixed as a catapult and subsequently used to transduce light energy into mechanical work, demonstrated here in the “photo-fueled” launching of an object at a rate of 0.3 m s−1.
Riboflavin Analogues: A Novel Class of Antihypertensive Drugs (1982)

1. Riboflavin analogues were tested in three hypertensive rat models: the DOCA-salt hypertensive rat, spontaneously hypertensive rats (SHR) and Dahl S rats. 2. When 1.6 mg of 7,8-dimethyl-10-formyl-methylisoalloxazine (FMI) or 7,8-dimethyl-10-(2′-hydroxyethyl)isoalloxazine (HEI) was administered with 3.0 mg of DOCA twice weekly for 9 weeks, the systolic blood pressure (SBP) of the unanaesthetized rats rose to only 136 ± 5 mmHg compared with 165 ± 5 mmHg during DOCA treatment alone. The analogues blunted the retention of iliopsoas muscle Na+ and water due to DOCA. 3. In subsequent studies, the more potent riboflavin analogue 7,8-dimethyl-10-(3-chlorobenzyl)isoalloxazine (CBI) was employed. Administration of 0.5 mg of CBI/100 g body wt. twice weekly for 7 weeks lowered the SBP of the unanaesthetized SHR from 188 ± 7 mmHg to 148 ± 2 mmHg. The rats tolerated the medication well. CBI was more effective than hydrochlorothiazide, which at 2.2 mg/100 g body wt. daily only lowered the SBP to 167 ± 5 mmHg. The combined administration of CBI and hydrochlorothiazide produced an additive effect in that the SBP was reduced to 126 ± 4 mmHg. 4. CBI treatment resulted in a 36% and 11% decrease in the iliopsoas muscle Na+ concentration and water content respectively, suggesting that the untreated SHR is retaining Na+. The hydrochlorothiazide-treated SHR exhibited elevated levels of serum aldosterone. There was a profound suppressive effect of CBI on the secondary hyperaldosteronism generated by hydrochlorothiazide which was also reflected in the iliopsoas muscle K+ concentration. 5. In contrast to the SHR, the administration to the Dahl S rats of CBI for 8 weeks at 0.5 mg/100 g body wt. twice weekly reduced neither their SBP nor their iliopsoas muscle Na+ and water contents. 6. These results are consistent with our hypothesis that the antihypertensive actions of the riboflavin analogues are closely associated with their ability to modify the effects of mineralocorticoids on Na+ balance. These data suggest that riboflavin analogues also decrease aldosterone production and may function as dual-mechanism diuretic agents with K+ sparing properties and thus act as a novel class of antihypertensive drugs.
Therapeutic targeting truncated adenomatous polyposis coli (APC) proteins for the selective killing of colorectal cancer cells (2014)

The adenomatous polyposis coli (APC) gene is a multifunctional tumor suppressor mutated in over 80% of colorectal cancers (CRC). Mutations in APC are believed to be one of the earliest events that contribute to CRC initiation. APC has been implicated in the negative regulation of the canonical Wnt signaling pathway, cell cycle control, cell migration, differentiation, and apoptosis. However, there remain many unanswered questions about the precise roles of APC in CRC progression. For example, over 90% of APC mutations result in truncated proteins, among which termination mutations at codons 1309 and 1450 occur the most frequently. It is completely unclear why the vast majority of human colon cancers would retain truncated APC proteins unless there was some survival/growth advantage to the emerging tumor. We hypothesized that these truncated APC proteins may actually play a dominant (gain of function) role in the initiation and/or progression of CRC and have conducted experiments to test this idea. Our rationale for these experiments is there are no disease-specific targeted treatments for CRC and therapeutic agents targeting APC truncations could be beneficial.

We developed a unique series of telomerase (TERT) and CDK4 immortalized human colonic epithelial cell (HCEC) lines and experimentally made isogenic derivatives by ectopic expression of the most commonly observed APC truncations found in patients. In addition, we made TERT and CDK4 expressing HCECs with TP53 and APC knockdowns as well as ectopic expression of oncogenic KRASv12. We have completed a cell-based high-throughput screen within UT Southwestern's 200,000 compound library utilizing the most cancer progressed isogenic cell line and tested the initial hits against the TERT immortalized normal diploid HCECs. A small molecule lead compound, TASIN-1 (truncated APC selective inhibitor), was identified from this screen that is selectively toxic towards a panel of colon cancer cell lines with APC truncations while sparing normal diploid HCECs and cancer cells with wild type APC. TASIN-1 and its analogs (with IC50s from 0.01nM to 5µM) represent a novel strategy for the treatment of colon cancer. In vitro and in vivo preclinical results will be presented.
Production of large-particle-size monodisperse latexes (1984)

The research program achieved two objectives: (1) it has refined and extended the experimental techniques for preparing monodisperse latexes in quantity on the ground up to a particle diameter of 10 microns; and (2) it has demonstrated that a microgravity environment can be used to grow monodisperse latexes to larger sizes, where the limitations in size have yet to be defined. The experimental development of the monodisperse latex reactor (MLR) and the seeded emulsion polymerizations carried out in the laboratory prototype of the flight hardware, as a function of the operational parameters is discussed. The emphasis is directed towards the measurement, interpretation, and modeling of the kinetics of seeded emulsion polymerization and successive seeded emulsion polymerization. The recipe development of seeded emulsion polymerization as a function of particle size is discussed. The equilibrium swelling of latex particles with monomers was investigated both theoretically and experimentally. Extensive studies are reported on both the type and concentration of initiators, surfactants, and inhibitors, which eventually led to the development of the flight recipes. The experimental results of the flight experiments are discussed, as well as the experimental development of inhibition of seeded emulsion polymerization in terms of time of inhibition and the effect of inhibitors on the kinetics of polymerization.