gebhart/patrepeval huggingface dataset:
Macromolecule-drug conjugates in targeted cancer chemotherapy. (1984)

Although clinical trials using macromolecular conjugates of cytotoxic drugs in a treatment of malignant disease are fragmentary at best, a number of carrier systems that have been examined in vitro, in tissue culture, and in vivo animal experiments demonstrate great promise and warrant further extensive examination. The optimal drug delivery and, consequently, maximum therapeutic effect will be accomplished when all available information from diverse disciplines can be integrated. This review has attempted to point out some of the limitations of taking an optimistic view of the question of targeting drug delivery using macromolecule-drug conjugates. For example, a strategy for the development of macromolecular conjugates can be established based on characteristics of the targeted tumors and the drugs in prospect of great success. Biological and physiological features of the tumor such as a cell type, site, and the pharmacological and physicochemical properties of chemical agents such as site of action and chemical stability must be considered at the first step. Selection of the optimum carrier system will be accompanied when all these problems are carefully considered. Similarly, the optimum method of conjugation is likely to vary as a function of the carrier, the chemotherapeutic agent, and the delivery site or site of action of the agent. The stability of the bond must adopt itself to the mode and site of action of the agent, the necessity for release, and the availability of hydrolytic enzymes which break the linkage and release the agent. On the other hand, the success of such conjugates synthesized according to this strategy will depend on physicochemical properties of the conjugates such as molecular size, electric charge, and solubility; chemical and biological stability of active components of conjugates and linkages; interaction with the tumor cells; cytotoxicity in tissue culture system; pharmacokinetics in the body such as absorption profile, localization, and elimination manner; in vivo antitumor activity; and biodegradability and antigenicity of the conjugates. The practitioners of macromolecular conjugate research find themselves in the interesting, but difficult, position of being at the interface between basic information on the drugs and biological systems and an expanding clinical demand for more sophisticated therapeutic agents. Consequently, knowledge is demanded not only of the chemical, physical, and pharmaceutical properties of macromolecules, but also of pathophysiology of the condition being treated.(ABSTRACT TRUNCATED AT 400 WORDS)
An assessment of the ability of a silver‐releasing device to prevent bacterial contamination of urethral catheter drainage systems (1996)

Objective To investigate the ability of a silver‐releasing device to protect the catheterized bladder from infection by blocking the ascending migration of bacteria from contaminated urine‐drainage bags. Materials and methods A simple physical model of the catheterized bladder and drainage system was used with the device located in the drainage‐tube just below the sampling port. Urine was supplied to the model at 1.0 mL/min and the drainage bag was contaminated with Pseudomonas aeruginosa, Escherichia coli and Proteus mirabilis. Over 10 days, urine from the bag, catheter sampling‐port and bladder were examined for contamination. Results Bacteriological analysis showed that the mean time for test organisms to reach the sampling ports of four different control bag systems ranged from 5.7 to 7.7 days. Urine from the sampling ports of the test systems incorporating the silver device remained sterile for 10 days. The device also prevented the growth of the large populations of bacteria (10 8 colony‐forming units per mL) that occurred in the control bags. While scanning electron microscopy showed the formation of bacterial biofilm throughout the control drainage systems, no bacterial colonization was visible on the surfaces of the test systems. Chemical analysis established that the devices consistently generated concentrations of silver in urine ranging from 1.0 to 2.0 μg/mL. Conclusion The incorporation of the silver‐releasing device into the drainage systems produced an antibacterial barrier which protected the catheterized bladder from intraluminal contamination for at least 10 days. These in vitro tests suggest a useful role for the device in controlling infection in patients undergoing short‐term indwelling bladder catheterization.
Yield and speed optimization of a latch-type voltage sense amplifier (2004)

A quantitative yield analysis of a latch-type voltage sense amplifier with a high-impedance differential input stage is presented. It investigates the impact of supply voltage, input DC level, transistor sizing, and temperature on the input offset voltage. The input DC level turns out to be most significant. Also, an analytical expression for the sensing delay is derived which shows low sensitivity on the input DC bias voltage. A figure of merit indicates that an input dc level of 0.7 V/sub DD/ is optimal regarding speed and yield. Experimental results in 130-nm CMOS technology confirm that the yield can be significantly improved by lowering the input DC voltage to about 70% of the supply voltage. Thereby, the offset standard deviation decreases from 19 to 8.5 mV without affecting the delay.
AL preincubation inhibits calcification of bioprosthetic heart valve tissue in the rat subdermal model. (1989)

To date, the clinical usefulness of bioprosthetic heart valves (BPV) fabricated from glutaraldehyde pretreated porcine aortic valves or bovine pericardium has been limited because leaflet calcification (CALC) leads to valvular stenosis and/or regurgitation and subsequent valve failure. The present study was designed to test the hypothesis that preincubation of glutaraldehyde pretreated pericardial BPV leaflets in a solution containing the trivalent cation, AL , inhibits BPV calcification. BPV tissue was preincubated in 0.1 M ALCL3 for 24 hours (T = 25 degrees C), then subdermally implanted in rats (weanling, male, CD, Sprague-Dawley) for 21 days. Compared to the control group (tissue Ca++ = 143.81 +/- 25.49 micrograms/mg), calcification was markedly inhibited in the group pretreated with AL (tissue Ca++ = 4.1 +/- 1.03 micrograms/mg) after a 21 day implant. No adverse effects on rat growth or bone morphology were detected. It is concluded that the trivalent cation AL provided a marked anticalcification effect for BPV tissue implanted subdermally in the rat for 21 days.
Synthesis of π-Conjugated Polymers Containing Fluorinated Arylene Units via Direct Arylation: Efficient Synthetic Method of Materials for OLEDs (2012)

Polycondensation via direct arylation of tetrafluorobenzene or octafluorobiphenyl was investigated for the synthesis of π-conjugated polymers consisting of fluorinated arylene units. The optimization of reaction conditions revealed that a combination of Pd(OAc)2 and PtBu2Me-HBF4 is the most efficient catalytic system for the polycondensation reactions. The polycondensation reactions produced four types of π-conjugated polymers having low highest occupied molecular orbital (HOMO) levels due to the strong electron-withdrawing nature of the fluorine substituents. Owing to the low HOMO levels, the synthesized polymers served as an efficient hole-blocking layer (HBL) in OLEDs.
MALDI-TOF/MS analysis of archaebacterial lipids in lyophilized membranes dry-mixed with 9-aminoacridine (2010)

A method of direct lipid analysis by MALDI mass spectrometry in intact membranes, without prior extraction/separation steps, is described. The purple membrane isolated from the extremely halophilic archaeon Halobacterium salinarum was selected as model membrane. Lyophilized purple membrane were grinded with 9-aminoacridine (9-AA) as dry matrix, and the powder mixture was crushed in a mechanical die press to form a thin pellet. Small pieces of the pellet were then attached to the MALDI target and directly analyzed. In parallel, individual archaebacterial phospholipids and glycolipids, together with the total lipid extract of the purple membrane, were analyzed by MALDI-TOF/MS using 9-AA as the matrix in solution. Results show that 9-AA represents a suitable matrix for the conventional MALDI-TOF/MS analysis of lipid extracts from archaeal microorganisms, as well as for fast and reliable direct dry lipid analysis of lyophilized archaebacterial membranes. This method might be of general application, offering the advantage of quickly gaining information about lipid components without disrupting or altering the membrane matrix.
1,2,4‐Trisubstituted Cyclopentanes as Platforms for Diversity (2012)

Despite their simplicity, relatively few examples of 1,2,4 (1,3,4)-amino-, azido-, and hydroxy-substituted cyclopentanes are reported in the literature. We found that cyclopent-3-en-1-ol can be transformed into a significant variety of compounds of this class by relatively common and efficient synthetic procedures. Stereochemical control of epoxidation of the cyclopentene double bond can be achieved by varying the substitutents at C4. The C4 substituent and epoxide functional group can be converted into a variety of intermediates with differential protection designed for use in applications requiring regiospecific control for further elaboration of the cyclopentane scaffold.
Impaired cardiopulmonary baroreflex control of renal nerves in renal hypertension. (1985)

We recently reported that arterial baroreflex control of renal nerve traffic is impaired in renal hypertensive rabbits. The purpose of this study was to determine if vagal cardiopulmonary baroreflex control of renal nerve traffic is also impaired. Experiments were performed in 10 hypertensive (mean arterial pressure +/- SE in conscious state, 110 +/- 3 mm Hg) and 10 normotensive (79 +/- 1 mm Hg) chloralose-anesthetized rabbits. Responses to graded blood volume expansion (+5, +10, +15 ml/kg) with dextran in saline were recorded with all baroreflexes intact, after sinoaortic baroreceptor denervation, and after vagotomy. With arterial and cardiopulmonary baroreflexes intact, volume expansion resulted in decreases in renal nerve traffic of -12 +/- 2%/mm Hg increase in left atrial pressure in normotensive rabbits, but of only -5 +/- 2%/mm Hg in the hypertensive rabbits (P less than 0.05). This difference is particularly striking in view of the larger maximum increases in arterial (25 +/- 7 vs. 12 +/- 3 mm Hg) and left atrial pressure (9 +/- 1 vs. 6 +/- 1 mm Hg) during volume expansion in hypertensive vs. normotensive rabbits. After sinoaortic baroreceptor denervation, the responses of normotensive rabbits were preserved (-11 +/- 3%/mm Hg), while those of hypertensive rabbits were impaired further (-2 +/- 1%/mm Hg). Vagotomy abolished responses of renal nerves to volume expansion in both groups. These data demonstrate striking impairment of vagal cardiopulmonary baroreflex control of renal nerve traffic in renal hypertension. Even though arterial baroreflexes have been shown to be abnormal in renal hypertension, they still may partially compensate for markedly impaired cardiopulmonary baroreflex control of the renal nerves.
Empirical Generalizations and Marketing Science: A Personal View (1995)

Marketing has matured to the point where it seems desirable to take stock of where we are, what we have learned, and fruitful directions for extending the knowledge base that has developed. Science is a process involving the interaction between empirical generalizations and theory. An empirical generalization is “a pattern or regularity that repeats over different circumstances and that can be described simply by mathematical, graphic, or symbolic methods.” One of the purposes of the Empirical Generalizations Conference held at Wharton on February 16–18, 1994 was to develop a list of examples of such empirical generalizations in marketing. Empirical generalization can precede a theory to explain it or it can be predicted by a theory. Science is the process of interaction between theory and data that leads to higher level theories. Examples are provided here of empirical generalizations in marketing and their theoretical counterparts. One example is provided of a higher level theory.
Bistability in non-Newtonian flow: Rheology of lyotropic liquid crystals (1998)

We study the rheological properties of self-assembled surfactant structures: lyotropic liquid crystals exhibiting plane lamellar and ``onion'' (concentric bilayer) textures. Both systems behave similarly: they are gel-like and exhibit extreme shear-thinning behavior. We demonstrate that this results in a hysteresis in the stress-strain curve when the stress is imposed. Controlled shear-rate experiments reveal the origin of the hysteresis by demonstrating the existence of two extrema in the stress-strain curve. The bistability leads to the formation of shear bands in the system and is illustrated by demonstrating the existence of sudden jumps in the viscosity of the fluid, following the viscosity of the fluid in time.
View dependent fluid dynamics (2006)

This thesis presents a method for simulating fluids on a view dependent grid structure to\nexploit level-of-detail with distance to the viewer. Current computer graphics techniques,\nsuch as the Stable Fluid and Particle Level Set methods, are modified to support a nonuniform\nsimulation grid. In addition, infinite fluid boundary conditions are introduced that\nallow fluid to flow freely into or out of the simulation domain to achieve the effect of\nlarge, boundary free bodies of fluid. Finally, a physically based rendering method known\nas photon mapping is used in conjunction with ray tracing to generate realistic images of\nwater with caustics. These methods were implemented as a C++ application framework\ncapable of simulating and rendering fluid in a variety of user-defined coordinate systems.
SWORD Financing of Innovation in the Biotechnology Industry (1993)

A financing arrangement known as stock warrant off-balance sheet research and development (SWORD) has been used recently in the biotechnology industry to finance innovation. Innovation is important to biotech firms because it provides the competitive edge necessary for survival, yet it is very risky because of the uncertainty about the commercial viability and regulatory approval of new products and technologies. Biotech firms are so small that they cannot diversify this risk internally across projects, and conventional internal financing of innovation is generally not possible because biotech firms tend to be lacking in both profitability and cash resources. Since a SWORD is offered to the investment public, the innovation risk can be diversified across many investors and their portfolios. The SWORD technique may lead to a more efficient allocation of the risk of innovation over the financial markets.
Investigating a Catalytic Mechanism of Hyperthermophilic L-Threonine Dehydrogenase from Pyrococcus horikoshii (2008)

Based on our first structural data of L-threonine dehydrogenase (TDH) of Pyrococcus horikoshii (PhTDH), we examined its catalytic mechanism. The structural analysis indicated that a catalytic zinc atom at the active centre of PhTDH is coordinated by four residues (Cys42, His67, Glu68 and Glu152) with low affinity. These residues are highly conserved in alcohol dehydrogenases (ADHs) and TDHs. Several PhTDH mutants were prepared with respect to Glu152 and other residues, relating to the proton relay system that is substantially a rate-limiting step in ADH. It was found that the E152D mutant showed 3-fold higher turnover rate and reduced affinities toward L-threonine and NAD(+), compared to wild-type PhTDH. The kinetic analysis of Glu152 mutants indicated that the carboxyl group of Glu152 is important for expressing the catalytic activity. The results obtained from pH dependency of kinetic parameters suggested that Glu152 to Asp substitution causes the enhancement of deprotonation of His47 or ionization of zinc-bound water and threonine in the enzyme-NAD(+) complex. Furthermore, it was predicted that the access of threonine substrate to the enzyme-NAD(+) complex induces a large conformational change in the active domain of PhTDH. From these results, we propose here that the proton relay system works as a catalytic mechanism of PhTDH.
The opposing effects of the flavonoids isoquercitrin and Sissotrin, isolated from <i>Pterospartum tridentatum</i>, on oral glucose tolerance in rats (2008)

The effect of an aqueous extract of Pterospartum tridentatum on the blood glucose levels of normal Wistar rats was investigated in a situation of oral glucose challenge. The extract at 300 mg/kg showed an antihyperglycaemic effect in the first 30 min after glucose challenge but then the blood glucose levels rose above those of the control group, indicating the presence of compounds with different effects on glucose tolerance. Nine compounds of isoflavone and flavonol skeletons were identified in the extract by HPLC-ESI-MS(n), four of them being identified for the first time in this species. The isoflavone sissotrin and the flavonol derivative, isoquercitrin, were selected for the oral glucose tolerance test. Isoquercitrin (100 mg/kg) showed time-dependent antihyperglycaemic activity by delaying the post-oral glucose load glycaemic peak at 30 min, as did the sodium-dependent glucose transporter inhibitor phloridzin (100 mg/kg). In contrast, sissotrin (100 mg/kg) showed an opposite effect, impairing glucose tolerance. In conclusion, these preliminary results indicate that the effect of the extract on blood glucose may be either antihyperglycaemic or hyperglycaemic. Additionally, as far as is known, these are the first in vivo results on the acute antihyperglycaemic potential of isoquercitrin.
Localization of the phosphocholine-binding sites on C-reactive protein by immunoelectron microscopy. (1983)

C-reactive protein (CRP) was reacted with monoclonal IgG antibody or Fab antibody fragments directed against the phosphocholine- (PC) binding site or a second unrelated site. The resulting immune complexes were viewed by a negative stain immunoelectron microscopy technique. Monoclonal anti-PC-binding site antibody bound to a single epitope on each of the five CRP subunits. The orientation of the PC-binding sites was determined to be slightly medial to one of the planar faces (A-face) of the molecule. The second monoclonal antibody, which was not PC-binding site related, bound to epitopes (one per CRP subunit) that were located slightly lateral to the other planar face (B-face) of the CRP molecule, i.e., opposite of the PC-binding site. Thus, the PC-binding site and the non-PC-binding site are oriented nearly perpendicular but on opposite sides with respect to the plane of the CRP molecule. The functional significance of this configuration is discussed.
Adaptive torque-based control of a humanoid robot on an unstable platform (2010)

We are interested in performing dynamic tasks with humanoid robots. Using a model-based controller to perform these tasks can expose modeling errors that are not apparent when performing slower or less difficult tasks. To successfully perform a dynamic task with the Sarcos Primus humanoid, we augmented a model-based policy-mixing controller with automated model adaptation techniques. We conducted experiments to show that this augmented controller can balance the Sarcos Primus humanoid on an unstable seesaw platform in the presence of unexpected disturbances and significant model errors.
The Mechanism of Unresponsiveness to Circulating Tumor Antigen MUC1 Is a Block in Intracellular Sorting and Processing by Dendritic Cells (2000)

Immunity to tumor Ags in patients is typically weak and not therapeutic. We have identified a new mechanism by which potentially immunogenic glycoprotein tumor Ags, such as MUC1, fail to stimulate strong immune responses. MUC1 is a heavily glycosylated membrane protein that is also present in soluble form in sera and ascites of cancer patients. We show that this soluble protein is readily taken up by dendritic cells (DC), but is not transported to late endosomes or MHC class II compartments for processing and binding to class II MHC. MUC1 uptake is mediated by the mannose receptor, and the protein is then retained long term in early endosomes without degradation. Long-term retention of MUC1 does not interfere with the ability of DC to process and present other Ags. We also demonstrate inhibited processing of another important glycoprotein tumor Ag, HER-2/neu. This may, therefore, be a frequent obstacle to presentation of tumor Ags and an important consideration in the design of cancer vaccines. It should be possible to overcome this obstacle by providing DC with a form of tumor Ag that can be better processed. For MUC1 we show that a 140-aa-long synthetic peptide is very efficiently processed by DC.
Dynamic Management of Multiple Mobile Routers (2006)

Network mobility (NEMO) support is used to maintain the Internet connectivity of a group of terminals located into a network that changes its point of attachment to the Internet. The Internet access is made through a number of interfaces on a mobile router acting as a gateway of the mobile network. The overall bandwidth can be increased and redundancy can be provided by serving the mobile network through multiple mobile routers. However, this raises a number of issues related to multihoming. We therefore propose a multiple mobile router management (MMRM) system which allows nodes in the mobile network to be connected transparently to the Internet through multiple mobile routers. Mobile routers can dynamically join and leave the mobile network. They cooperate in order to share their Internet access within the entire mobile network. The proposed system is implemented and evaluated. Evaluation results show that the overhead of our system is negligible while redundancy and the overall bandwidth for the nodes in the mobile network are increased.
Effect of saponin on the surface properties of quinoa proteins (1999)

Abstract Quinoa seeds were cleaned, ground, and defatted using hexane. The defatted flour was dispersed and stirred in alkali to extract the proteins, one half of which was desaponized with methanol. The whole seed flour, protein, and desaponized protein fractions were compared for their functional properties. Removal of saponins increased water hydration capacity and lowered the fat binding capacity. The emulsion capacity was also reduced in the desaponized protein although emulsion the stability increased markedly. A slight decrease in buffer capacity was observed which was attributed to the removal of saponins. The foaming capacity and foam stability were affected in the similar manner to that of the emulsifying properties. The removal of saponins also lowered the total nitrogen solubility of quinoa proteins.