gebhart/patrepeval huggingface dataset:
Design and Synthesis of Peptidomimetic Protein Farnesyltransferase Inhibitors as Anti-Trypanosoma brucei Agents (2003)

On the basis of the structure of the CVIM tetrapeptide substrate of mammalian protein farnesyltransferase, a series of imidazole-containing peptidomimetics was designed and synthesized, and their inhibition activity against Trypanosoma brucei protein farnesyltransferase (TbPFT) was evaluated. Peptidomimetics where the 5-position of the imidazole ring was linked to the hydrophobic scaffold showed over 70% inhibition activity at 50 nM in the enzyme assay, whereas the corresponding C-4 regioisomers were less potent. The ester prodrug 23 was found to be a potent inhibitor against cultured Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense cells with ED(50) values of 0.025 and 0.0026 microM, respectively. Furthermore, introducing a second imidazole group into 23 led to 31, which showed the highest inhibition activity against the parasite with an ED(50) of 0.0015 microM. The potency of the TbPFT inhibitors and the cytotoxicity of the corresponding esters to T. brucei cells were shown to be highly correlated. These studies validate TbPFT as a target for the development of novel therapeutics against African sleeping sickness.
Monotone Multiscale Finite Volume Method for Flow in Heterogeneous Porous Media (2014)

Summary The MultiScale Finite-Volume (MSFV) method is known to produce non-monotone solutions. The causes of the non-monotone solutions are identified and connected to the local flux across the boundaries of primal coarse cells induced by the basis functions. We propose a monotone MSFV (m-MSFV) method based on a local stencil-fix that guarantees monotonicity of the coarse-scale operator, and thus the resulting approximate fine-scale solution. Detection of non-physical transmissibility coefficients that lead to non-monotone solutions is achieved using local information only and is performed algebraically. For these ‘critical’ primal coarse-grid interfaces, a monotone local flux approximation, specifically, a Two-Point Flux Approximation (TPFA), is employed. Alternatively, a local linear boundary condition is used for the basis functions to reduce the degree of non-monotonicity. The local nature of the two strategies allows for ensuring monotonicity in local sub-regions, where the non-physical transmissibility occurs. For practical applications, an adaptive approach based on normalized positive off-diagonal coarse-scale transmissibility coefficients is developed. Based on the histogram of these normalized coefficients, one can remove the large peaks by applying the proposed modifications only for a small fraction of the primal coarse grids. Though the m-MSFV approach can guarantee monotonicity of the solutions to any desired level, numerical results illustrate that employing the m-MSFV modifications only for a small fraction of the domain can significantly reduce the non-monotonicity of the conservative MSFV solutions.
Supplementary Figure from Pan-Cancer Analysis of Canonical and Modified miRNAs Enhances the Resolution of the Functional miRNAome in Cancer (2023)

Supplementary Figure from Pan-Cancer Analysis of Canonical and Modified miRNAs Enhances the Resolution of the Functional miRNAome in Cancer
Comparison of the Fracture Toughness and Stress Corrosion Behaviour of Four Aluminium Alloys (1974)

The fracture toughness and stress corrosion properties of forgings in four aluminium alloys (AA2014–T6, AA7075–T73, L83 WP and DTD 5084WP) have been compared, using precracked specimens to define KIscc (the critical stress intensity for stress corrosion cracking) for each alloy in the short transverse direction when tested in 3% sodium chloride solution. In the T73 condition of heat-treatment, alloy AA7075 was resistant to stress corrosion whereas the other three alloys all showed susceptibility to stress corrosion, the ratio KIscc to KIc being about 0·5 for the L83 WP and about 0·7 for the other two alloys.
An InGaP-GaAs HBT MMIC smart power amplifier for W-CDMA mobile handsets (2003)

We demonstrate a new linearized monolithic microwave integrated circuit smart power amplifier of extraordinary high power-added efficiency (PAE), especially at the most probable transmission power of wide-band code-division multiple-access handsets. A PAE of 21% at 16 dBm of output power, which is the maximum bound of the most probable transmission power in IS-95 systems, was obtained, as well as 40% at 28 dBm, the required maximum output power, with a single-chip MMIC power amplifier. The power amplifier has been devised with two InGaP-GaAs heterojunction bipolar transistor amplifying chains parallel connected, each chain being optimized for a different P/sub 1dB/ (1-dB compression point) value: one for 16 dBm for the low-power mode, targeting the most probable transmission power, and the other for 28 dBm for the high-power mode. The high-power mode operation shows 40% of PAE and -30 dBc of adjacent channel leakage power ratio (ACLR) at the maximum output power of 28 dBm. The low-power mode operation exhibits -34 dBc of ACLR at 16 dBm with 14 mA of a quiescent current. This amplifier improves power usage efficiency and, consequently, the battery lifetime of the handset by a factor of three.
A theoretical study on the interaction of dinitrogen with rhodium (1994)

Ab initio theoretical computations have been performed for RhN 2 , Rh + N 2 , Rh(N 2 ) 2 , and Rh + (N 2 ) 2 species. The computed vibrational frequencies and binding-energy trends are in qualitative accord with prior FTIR studies of N 2 interacting with supported Rh films. Computations of the type described herein should be useful in aiding the assignment of observed infrared bands to specific surface species in future work.
IL-6 Mediates the Intestinal Microvascular Thrombosis Associated with Experimental Colitis (2016)

Inflammatory bowel diseases are associated with increased risk for thrombus formation both within the inflamed bowel and at distant sites. Although the increased propensity for distant organ thrombus development has been recapitulated in animal models of colitis and linked to interleukin-6 (IL-6), it remains unclear whether experimental colitis results in accelerated thrombus development within the inflamed bowel and whether IL-6 contributes to a local thrombogenic response. These issues related to thrombus formation within the inflamed bowel were addressed in mice with dextran sodium sulfate-induced colitis. Wild-type (WT) mice, IL-6 deficient (IL-6(-/-)) mice, and bone marrow chimeras (WT→WT and IL-6(-/-)→WT) were used. The effects of treatment with either an IL-6-blocking, IL-6Rα-blocking or gp130-blocking antibody were also evaluated. Disease activity index and colonic weight-to-length ratio (W/L) were used to monitor the development of colitis. Intravital videomicroscopy was used to study thrombus development (induced with the light/dye method) in mucosal vessels of the ascending colon. Thrombus development was significantly enhanced in WT colitic mice. Neither genetic deficiency nor immunoblockade of IL-6 significantly altered the disease activity index and W/L responses to dextran sodium sulfate treatment. However, colitis-induced thrombogenesis was attenuated in IL-6(-/-) mice and in WT mice treated with either the IL-6-blocking, IL-6Rα-blocking or gp130-blocking antibody. IL-6(-/-)→WT, but not WT→WT chimeras, exhibited a blunted thrombosis response to dextran sodium sulfate. These results indicate that experimental colitis is associated with accelerated thrombus development within the inflamed colon and that IL-6, derived from bone marrow-derived blood cells, is largely responsible for this response.
Pitfalls in HLA Ligandomics—How to Catch a Li(e)gand (2021)

Knowledge about the peptide repertoire presented by human leukocyte antigens (HLA) holds the key to unlock target-specific cancer immunotherapies such as adoptive cell therapies or bispecific T cell engaging receptors. Therefore, comprehensive and accurate characterization of HLA peptidomes by mass spectrometry (immunopeptidomics) across tissues and disease states is essential. With growing numbers of immunopeptidomics datasets and the scope of peptide identification strategies reaching beyond the canonical proteome, the likelihood for erroneous peptide identification as well as false annotation of HLA-independent peptides as HLA ligands is increasing. Such "fake ligands" can lead to selection of nonexistent targets for immunotherapeutic development and need to be recognized as such as early as possible in the preclinical pipeline. Here we present computational and experimental methods that enable the identification of "fake ligands" that might be introduced at different steps of the immunopeptidomics workflow. The statistics presented herein allow discrimination of true HLA ligands from coisolated HLA-independent proteolytic fragments. In addition, we describe necessary steps to ensure system suitability of the chromatographic system. Furthermore, we illustrate an algorithm for detection of source fragmentation events that are introduced by electrospray ionization during mass spectrometry. For confirmation of peptide sequences, we present an experimental pipeline that enables high-throughput sequence verification through similarity of fragmentation pattern and coelution of synthetic isotope-labeled internal standards. Based on these methods, we show the overall high quality of existing datasets but point out limitations and pitfalls critical for individual peptides and how they can be uncovered in order to identify true ligands.
Time-Resolved Spray-Droplet Velocity and Size Measurements via Single Camera Laser Sheet Imaging and Planar DPIV (2002)

This paper describes a first effort to investigate the feasibility of droplet size and shape characterization by direct laser sheet imaging using time resolved Digital Particle Image Velocimetry. A 60-degree conical, high-pressure spray generated a poly-dispersed droplet distribution. Measurements were preformed for seven planes parallel to the spray axis, and separated by 4mm. A CMOS camera recorded the DPIV images at sampling rate of 10 KHz. Advanced image processing techniques were employed to identify the droplets and individually resolve their velocity using a hybrid cross-correlation particle-tracking algorithm. Subsequently, the size distribution of each droplet was quantified using geometric optics theory to convert the droplet image information to the true droplet size. Finally, the entire volume of the spray velocity and size distributions was reconstructed in a time-averaged sense. The droplet sizes from our direct imaging DPIV system were validated using a Phase Doppler Particle Analyzer (PDPA). The calculated sizes from the direct imaging methodology were found to agree with the measured PDPA results for droplets images larger than the diffraction limited diameter. Resolution limitations introduced inaccuracy for smaller droplets. In addition, the shedding frequency of the spray ligament was observed to be on the order of 1KHz, demonstrating the feasibility of using a high speed, direct imaging system in the characterization of unsteady, liquid sheet breakup properties. This preliminary effort illustrates the potential of performing global time resolved velocity and size measurements using a simple DPIV configuration based on CMOS imaging technology.
Conventional administration and scoring procedures suppress the diagnostic accuracy of a performance-based test designed to assess balance ability in lower limb prosthesis users (2019)

Scoring a clinical balance test using conventional procedures that do not mitigate practice effects reduced its diagnostic accuracy. Changing administration and scoring procedures to accommodate practice effects should be considered to improve the diagnostic accuracy of other performance-based balance tests.
INHIBITION OF THE RENAL TUBULAR EFFECTS OF PARATHYROID HORMONE ON PHOSPHATE TRANSPORT BY PROSTAGLANDIN E2 (1981)

The infusion of PGE2 into TPTX dogs abolishes the phosphaturic action of PTH in vivo. This effect occurs only if PGE2 infusion precedes the administration of PTH. The infusion of PGE2 in vivo induces a state of refractoriness of PTH-sensitive adenylate cyclase in renal middle medulla from TPTX dogs in vitro. These results suggest that PGE2 inhibits the biological effects of PTH, in part by altering the events related to PTH activation of renal adenylate cyclase. These effects of PGE2, a local mediator, suggest that the renal tubular cell may modulate its responses to multiple and antagonistic stimuli by altering local renal prostaglandins.
Meaningful evaluation of plastisol gelation and fusion temperatures by dynamic mechanical analysis (1986)

Abstract In most PVC plastisol processing operations, gelation and fusion characteristics of the plastisol are critically important. For example, in chemically foamed plastisols, plastisol fusion temperature and blowing agent decomposition temperature must be carefully coordinated. In rotomolded parts, rates of gelation may determine the quality of the finished parts. For plastisol products made by any process, the final fusion temperature determines the processing temperatures required to give the finished product acceptable mechanical properties. For a variety of reasons, the methods commonly used to characterize plastisol gelation and fusion (hot bar test, resin in plasticizer clear point, torque rheometer measurements, etc.) provide comparisons between plastisols but do not provide temperatures that are easily related to actual industrial processes. With dynamic mechanical analysis (DMA), one can characterize, under low shear conditions, the temperatures at which gelation begins, gelation ends, and complete fusion occurs. Additionally, it is possible to record plastisol viscosities (and other dynamic mechanical properties) over the processing temperature range. We used a multiple linear regression program to analyze the DMA data for plastisols heated from 30 to 210°C and containing either 70, 80 or 90 phr of Jayflex dihexyl phthalate (DHP) or Jaylflex di‐isodecyl phthalate (DIDP). Further, we determined the plasticizer phr dependence and the reproducibility of gel and fusion temperatures given by data analyzed in this manner. Finally, for comparison, we analyzed the reproducibility of initial and final plastisol gel temperatures and fusion temperatures, which were determined by visually analyzing the DMA data for plastisols containing 70, 80, and 90 phr of Jyflex plasticizers DHP, Jayflex 77, diisononyl phthalate (DINP), and DIDP. Precise characterization of plastisol gelation and fusion behavior will, undoubtedly, facilitate substitution of plastisol ingredients as is often required by those who manufacture and process plastisols.
Understanding the role of grain boundaries in sulfide thin film solar cells with scanning probe microscopy (2012)

Grain boundaries (GBs) in Cu(In,Ga)Se <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> (CIGS) and CdTe thin film solar cells are known to be beneficial for achieving high conversion efficiencies. In this work, we will show that Cu <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> ZnSnS <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sub> (CZTS) and Cu <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> ZnSn(S,Se) <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sub> (CZTSSe) solar cells have the same GB electronic properties as CIGS and CdTe. Scanning Kelvin Probe Microscopy (SKPM) measurements reveal a higher positive surface potential at the GBs as compared to the grain while Conductive Atomic Force Microscopy (C-AFM) measurements show higher current flow in the vicinity of the GBs. These two measurement results are similar to those obtained for CIGS and CdTe and together they demonstrate the enhanced minority carrier collection taking place at the GBs of CZTS and CZTSSe. This implies that CZTS and CZTSSe solar cells have the potential to achieve the high efficiencies that CIGS and CdTe solar cells enjoy.
[A Case of Gastric Cancer Performed Curative Operation after Nivolumab]. (2022)

A 69-year-old man was admitted for the severe anemia. Upper gastrointestinal endoscopy revealed type 3 gastric cancer (por1, HER2 negative)that spread from EG junction to the lesser curvature of lower gastric body. CT revealed LNs metastasis and the direct invasion to the diaphragm. We diagnosed the locally advanced gastric cancer(T4bN[+]M0, Stage ⅣA) and planed neoadjuvant chemotherapy. After 3 courses of S-1 plus CDDP therapy, serum CEA level increased. And the invasion to diaphragm was unclear although the tumor shrunk. After 3 courses of nab-PTX plus RAM therapy as the second- line, the tumor was PD. As the third-line chemotherapy, nivolumab therapy was repeated up to a total of 15 courses. As the tumor was PR, the patient underwent total gastrectomy with D2 lymphadenectomy. The histopathological examination revealed that the cancer invaded into the muscle layer without lymph nodes metastasis. The cancer was diagnosed as pT2 (MP)N0M0, Stage ⅠB. The cancer cells were EB virus positive and MSI-high. CD 8 positive T lymphocytes infiltrated into the stroma. The patient is alive 26 months without adjuvant chemotherapy. The curative operation was able to perform because the infiltrative CD8 positive T lymphocytes reactivated with nivolumab responded remarkably.
Magnetic Resonance Imaging of Knee Cartilage Repair (1998)

Gold, Garry E. M.D.; Bergman, A. Gahrielle M.D.; Pauly, John M. Ph.D.; Lang, Philipp M.D.; Butts, R. Kim Ph.D.; Beaulieu, Christopher F. M.D., Ph.D.; Hargreaves, Brian M.S.; Frank, Lawrence Ph.D.; Boutin, Robert D. M.D.; Macovski, Albert Ph.D.; Resnick, Donald M.D. Author Information
Highly Enantioselective Rh‐Catalysed Hydrogenation of 1‐Alkyl Vinyl Esters Using Phosphine–Phosphoramidite Ligands (2013)

MatPhos, a good mate for hard tasks: The asymmetric hydrogenation of 1-alkyl vinyl esters, thwarted so far by mediocre ee values and low activities, can now be achieved with MatPhos/Rh catalysts with ee values of 96-99% for a variety of substrates at low catalyst loadings (0.1-1 mol %) and under mild conditions (5-20 bar H2, room temperature). After hydrolysis, the corresponding chiral secondary alkyl alcohols can be obtained in high enantiopurities providing a general and practical route to this important product class.
ChemInform Abstract: Catalysis as an Important Tool of Green Chemistry (2010)

Abstract Review: 248 refs.
A luminescent gold complex: bis-μ-[bis(dicyclohexylphosphino)ethane-P,P']-digold bis(hexafluorophosphate) (1991)

Tableau 2. Distances interatomiques (A) et angles ( 0 ) Rh-Rh' 2,3829 (6) 0(1)-C(I) 1,260 (5) Rh-0(1) 2,031 (3) C(l}-C(2) 1,498 (7) Rh-0(2) 2,043 (3) C(l)-D(4') 1,266 (5) Rh-0(3) 2,030 (3) 0(2)-C(3) 1,265 (5) Rh-0(4) 2,038 (3) C(3}-C(4) 1,495 (8) Rh-N(l3) 2,241 (4) C(3)-D(3') 1,270 (5) S(ll)-c(l2 1,722 (4) S(2 I )-c(22) 1,716 (5) S(l l)-c(l5) 1,730(5) S(2 I )-c(25) 1,699 (7) C(l2}-N(J3) 1,310 (5) C(22)-C(23) 1,389 (7) C(l2)-N(28) 1,360(6) C(22)-C(26) 1,461 (7) N(l3)-c(14) 1,365 (6) C(23)-c(24) 1,390 (8) C(l4)-c(l5) 1,332 (7) C(24)-c(25) 1,356 (9) C(l5)-N(16) 1,434 (6) C(26)-D(27) 1,219 (6) N(l6)-D(l7) 1,219 (6) C(26)-N(28) 1,369 (6) N(l6)-D(l8) 1,223 (6) C(30)-Cl(31) 1,753 (9) C(30)-Cl(32) 1,753 (9)
Allyl End‐Functionalized Poly(ethylene oxide)‐block‐poly(methylidene malonate 2.1.2) Block Copolymers: Synthesis, Characterization, and Chemical Modification (2005)

Abstract Summary: Poly(ethylene oxide)‐ block ‐poly(methylidene malonate 2.1.2) block copolymer (PEO‐ b ‐PMM 2.1.2) bearing an allyl moiety at the poly(ethylene oxide) chain end was synthesized by sequential anionic polymerization of ethylene oxide (EO) and methylidene malonate 2.1.2 (MM 2.1.2). This allyl functional group was subsequently modified by reaction with thiol‐bearing functional groups to generate carboxyl and amino functionalized biodegradable block copolymers. These end‐group reactions, performed in good yields both in organic media and in aqueous micellar solutions, lead to functionalized PEO‐ b ‐PMM 2.1.2 copolymers which are of interest for cell targeting purposes. Synthetic route to α ‐allyl functionalized PEO‐ b ‐PMM 2.1.2 copolymers. magnified image Synthetic route to α ‐allyl functionalized PEO‐ b ‐PMM 2.1.2 copolymers.
Clinical Features and Long-Term Outcomes in Very Young Patients with Myocardial Infarction with Non-Obstructive Coronary Arteries (2022)

Very young patients with MINOCA had a poor prognosis at long-term follow-up, similar to patients with obstructive CAD. Focusing efforts on secondary prevention is essential in this population.
Analysis Software for Interplanetary Trajectories using Three Body Problem (2010)

International audience
A dynamic, linearly-shifted, fixed-slope digital-ramp control technique for improved transient response in DC - DC converters (2015)

A conventional Counter-Comparator Digital Pulse Width Modulator (DPWM) with a fixed slope is dynamically and linearly shifted upwards or downwards by a value proportional to the error signal. The shift is done through applying a positive or negative offset (shift) value depending on the direction of the transient. This control approach aims to improve the transient response and efficiency of an FPGA-based digitally controlled DC-DC converters in terms of shorter settling time with optimal over-and undershoots. The dynamic Ramp Shift design method presented in this work is a linear DC shift control achieving a better dynamics response through reducing the time required by the compensator to reach back to the steady state during a transient condition. Moreover, it utilizes existing system digital controller, and does not require any additional circuitry. This shifting will only occur during transients for the reason that the error (which basically formulates the shift value) is almost zero during steady state, while during transients; the positive or negative value of the error will shift the ramp downwards or upwards. The proposed digital technique is validated by computer simulation. Experimental result of a prototype on a Xilinix FPGA platform verifies the concept.
Table S1 from First-in-Human Phase I Study of ABBV-838, an Antibody–Drug Conjugate Targeting SLAMF7/CS1 in Patients with Relapsed and Refractory Multiple Myeloma (2023)

&lt;p&gt;Overall summary of treatment-emergent adverse events&lt;/p&gt;
Flavanols and Platelet Reactivity (2004)

Platelet activity and platelet-endothelial cell interactions are important in the acute development of thrombosis, as well as in the pathogenesis of cardiovascular disease. An increasing number of foods have been reported to have platelet-inhibitory actions, and research with a number of flavanol-rich foods, including, grape juice, cocoa and chocolate, suggests that these foods may provide some protection against thrombosis. In the present report, we review a series of in vivo studies on the effects of flavanol-rich cocoa and chocolate on platelet activation and platelet-dependent primary hemostasis. Consumption of flavanol-rich cocoa inhibited several measures of platelet activity including, epinephrine- and ADP-induced glycoprotein (GP) IIb/IIIa and P-Selectin expression, platelet microparticle formation, and epinephrine-collagen and ADP-collagen induced primary hemostasis. The epinephrine-induced inhibitory effects on GP IIb/IIIa and primary hemostasis were similar to, though less robust than those associated with the use of low dose (81 mg) aspirin. These data, coupled with information from other studies, support the concept that flavanols present in cocoa and chocolate can modulate platelet function through a multitude of pathways.