gebhart/patrepeval huggingface dataset:
Rigid Dipeptide Surrogates:  Syntheses of Enantiopure Quinolizidinone and Pyrroloazepinone Amino Acids from a Common Diaminodicarboxylate Precursor (2000)

A versatile and practical approach for synthesizing azabicyclo[X.Y.0]alkane amino acids of different ring sizes from a common diaminodicarboxylate precursor has been developed as a means for mimicking different peptide conformations. (2S,9S)-1-tert-Butyl 10-benzyl 5-oxo-2-[N-(PhF)amino] 9-[N-(BOC)amino]dec-4-enedioate (18) was first prepared in 83% yield by the Horner-Wadsworth-Emmons olefination of N-(PhF)aspartate beta-aldehyde 8 with pyroglutamate-derived beta-keto phosphonate 12 (PhF = 9-phenylfluoren-9-yl). The practicality of this approach for making azabicyclo[X.Y.0]alkane amino acids was then illustrated by the first synthesis of enantiopure quinolizidin-2-one amino acid 6 in seven steps and 40% overall yield from L-pyroglutamic acid. Hydrogenation of delta-keto alpha,omega-diaminosebacate 18, followed by lactam cyclization and protection, gave quinolizidin-2-one amino acid 6 as a single diastereomer. The versatility of this approach was next demonstrated by the synthesis of both ring-fusion isomers of pyrroloazepin-2-one amino acid 6 in 11 steps and 13% overall yield from pyroglutamic acid. Hydride reduction of 18, followed by methanesulfonate displacement, gave 5-alkylproline 22. Protective group manipulations, lactam cyclization, and removal of the ester group afforded readily separable pyrroloazepinone amino acids (7S)- and (7R)-7 in a 1:2 diastereomeric ratio. By introducing two new azabicycloalkane amino acids using our olefination approach, we have expanded the diversity of these important heterocycles for studying the conformational requirements for peptide biological activity.
Applicability of the Van Vleck formula for polynuclear complexes (1968)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTApplicability of the Van Vleck formula for polynuclear complexesColin G. Barraclough, Harry B. Gray, and L. DubickiCite this: Inorg. Chem. 1968, 7, 4, 844–845Publication Date (Print):April 1, 1968Publication History Published online1 May 2002Published inissue 1 April 1968https://pubs.acs.org/doi/10.1021/ic50062a052https://doi.org/10.1021/ic50062a052research-articleACS PublicationsRequest reuse permissionsArticle Views92Altmetric-Citations13LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Reelin supports Glycoprotein VI and integrin outside-in signaling of platelets (2021)

Objective Reelin is known as an extracellular matrix protein mediating cell migration upon brain development. Recent studies provide evidence for reelin to be expressed in platelets, to co-localize to F-actin and to bind to amyloid precursor protein (APP) and apolipoprotein E receptor 2 (ApoER2) at the platelet surface. Furthermore, reelin is important for glycoprotein Ib (GPIb) mediated platelet adhesion and thrombus formation under high shear. Consequently, defective thrombus formation protects reelin-deficient mice (reeler) against arterial thrombosis.
Controlled Synthesis of Monodispersed Cerium Oxide Nanoparticle Sols Applicable to Preparing Ordered Self-Assemblies (2008)

Abstract Highly dispersed metal oxide nanoparticle sols are of great interest in science and engineering because of their broad potential applications in optics, electronics, sensors, catalysis, biomedicines, and even in cosmetics. Here, we report the size-controlled synthesis of cerium oxide nanoparticle sols by a reflux method with poly(vinylpyrrolidone) as a coating agent to afford stable monodispersions of spherical particles with size of 50–120 nm. The size of nanoparticles can be easily controlled by appropriate adjustment of the molecular weight of the added polymer. Colloidal crystals of cerium oxide are also obtained by evaporation of the cerium oxide sol. As cerium oxide has a larger refractive index than silica and polymers typically used for the preparation of colloidal crystals, the present sols are expected to be useful for the fabrication of high-performance photonic crystals.
Concentration of enzymatically active prostate‐specific antigen (PSA) in the extracellular fluid of primary human prostate cancers and human prostate cancer xenograft models (2001)

Prostate cancers obtained directly from patients produce and secrete large amounts of PSA, the majority of which is highly enzymatically active. In contrast, while PSA was detected in the sera, none of this PSA was enzymatically active. This is also the case for the human PC-82 prostate cancer xenografts. In contrast, LNCaP and LAPC-4 human prostate cancer xenograft models secrete approximately 70-300-fold less PSA in the ECF than prostate cancers from patients and the majority of this PSA is enzymatically inactive. Also, the serum from these animals had detectable PSA, but none of this PSA was enzymatically active. Thus, these latter two prostate cancer models define the least and the PC-82, the most, optimized xenograft model for screening PSA targeted prodrugs.
Expression and isolation of antimicrobial small molecules from soil DNA libraries. (2001)

Natural products have been a critically important source of clinically relevant small molecule therapeutics. However, the discovery rate of novel structural classes of antimicrobial molecules has declined. Recently, increasing evidence has shown that the number of species cultivated from soil represents less than 1% of the total population, opening up the exciting possibility that these uncultured species may provide a large untapped pool from which novel natural products can be discovered. We have constructed and expressed in E. coli a BAC (bacterial artificial chromosome) library containing genomic fragments of DNA (5-120kb) isolated directly from soil organisms (S-DNA). Screening of the library resulted in the identification of several antimicrobial activities expressed by different recombinant clones. One clone (mg1.1) has been partially characterized and found to express several small molecules related to and including indirubin. These results show that genes involved in natural product synthesis can be cloned directly from S-DNA and expressed in a heterologous host, supporting the idea that this technology has the potential to provide novel natural products from the wealth of environmental microbial diversity and is a potentially important new tool for drug discovery.
Calcitonin and Calcitonin-Related Peptide Genes (1987)

The neuroendocrine system serves critical regulator and communicative functions during development and in the maintenance of physiological homeostasis. To serve these functions with requisite specificity and nuance, many diverse regulatory peptides are produced by various strategies. Complex regulatory mechanisms operate to restrict the expression of genes encoding neuroendocrine peptides to precise groups in neurons in the neural tissues and in specific cell types in peripheral organs. An understanding of the mechanisms by which expression of neuroendocrine genes is regulated is critical to achieve insights into the molecular mechanisms important in developmental processes.
A novel quality model for HTTP adaptive streaming (2016)

HTTP Adaptive Streaming (HAS) has become a popular trend for multimedia delivery nowadays. Because of throughput variations, video quality strongly fluctuates during a session. Therefore, a main challenge in HAS is how to evaluate the overall video quality of a session. In this paper, we explore the impact of quality variations on the perceptual quality of a video in HAS. We propose to use the histogram of segment quality values and the histogram of quality gradients in a session to model the overall video quality. Subjective test results show that the proposed model can capture the segment quality variations and accurately predict the overall quality of a session.
GaAs/AlGaAs Colliding Pulse Mode-Locked Lasers with Non-Absorbing Mirrors (2010)

We use quantum well intermixing to monolithically integrate non-absorbing mirrors in 3.7mm long GaAs/AlGaAs colliding-pulse mode-locked lasers and improve their output power by 40% by increasing the threshold for catastrophic optical mirror damage.
Biological evaluation of a new C-xylopyranoside derivative (C-Xyloside) and its role in glycosaminoglycan biosynthesis (2011)

The mechanical properties of skin are determined primarily by the extracellular matrix of the dermis. These mechanical and biological properties change significantly as a function of age. Key components of the extracellular matrix are proteoglycans, which are molecules composed of a core protein and covalently attached glycosaminoglycans. Proteoglycans and their constituent glycosaminoglycans are involved in many biological processes which are important for dermal function, such as proper formation of the collagen network. A recently developed compound, C-xylopyranoside derivative (C-Xyloside), was designed to mimic β-xylosides, which are known initiators of glycosaminoglycan biosynthesis. C-Xyloside was found, by several criteria, to act like β-xylosides, such as in the eliciting of an increase in glycosaminoglycan synthesis by human dermal fibroblasts in culture. This increase may lead to the preservation of matrix integrity and thereby contribute to the firmness of skin. Thus, C-Xyloside may be useful in improving the quality of skin.
Abstract 4527: p53-Reactivating Small Molecules Induce Apoptosis in Head and Neck Cancer (2010)

Abstract Novel small molecules have been reported to restore the p53 tumor suppressor function inducing cell cycle arrest and apoptosis. The p53-targeting therapy may overcome the resistance to chemotherapeutic agents. This study evaluated whether small molecules induce p53-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) lines. PRIMA-1, CP-31398, RITA, and nutlin-3 were tested in 6 HNSCC cell lines with different p53 status and MDM2 expression levels. Cell growth, viability, cell cycle, and apoptosis after the treatment or combined treatment with common chemotherapeutic agents were assessed. The p53 reactivation was observed in mutant TP53-carrying cell lines by PRIMA-1 or CP-31398 treatment and in wild-type TP53-carrying cell lines by nutlin-3 treatment. The cell cycle arrest and apoptosis by the small molecules was associated with up-regulation of p21, Bax, and cleaved caspase-3. PRIMA-1 or CP-31398 induced also significant apoptosis in cell lines without p53 protein expression. Nutlin-3 or RITA showed maximal suppression in tumors with MDM2-induced tumor degradation. The small molecules enhanced the antitumor activity of the cell lines with a combination of cisplatin, 5-fluorouracil, paclitaxel, or erlotinib. The small molecules effectively restored p53 tumor suppressive function in HNSCC with mutant or wild-type p53. The p53 reactivating agents may be used for HNC with a combination of commonly-used chemotherapeutic agents. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 4527.
In tumor cells, thyroid hormone analogues non-immunologically regulate PD-L1 and PD-1 accumulation that is anti-apoptotic (2018)

The PD-1/PD-L1 immune checkpoint involving tumor cells and host immune defense lymphocytes is a well-studied therapeutic target in oncology. That PD-1 and PD-L1 may have additional functions within tumor cells that are independent of the checkpoint is indicated by actions of a thyroid hormone analogue, L-thyroxine (T<sub>4</sub>), on these checkpoint components. Acting at a cell surface receptor on plasma membrane integrin αvβ3, T<sub>4</sub> stimulates intracellular accumulation of PD-L1 in cancer cells. In these thyroid hormone-treated cells, T<sub>4</sub>-induced PD-L1 is non-immunologically anti-apoptotic, blocking activation of p53. Several laboratories have also described accumulation of PD-1 in a variety of cancer cells, not just immune defense lymphocytes and macrophages. Preliminary observations indicate that T<sub>4</sub> stimulates intracellular accumulation of PD-1 in tumor cells, suggesting that, like PD-L1, PD-1 has non-immunologic roles in the setting of cancer. Where such roles are anti-apoptotic, thyroid hormone-directed cancer cell accumulation of PD-1 and PD-L1 may limit effectiveness of immunologic therapy directed at the immune checkpoint.
Generation and Detection of Very Short-Wavelength Surface Acoustic Waves at Nano-interfaces (2011)

Using an ultrafast laser to excite 2D nanostructures, and coherent extreme ultraviolet light to detect the resulting acoustic response, we observe and characterize the shortest-wavelength (35 nm) surface acoustic waves to date.
Supplementary Figure 2 from MiR-122/Cyclin G1 Interaction Modulates p53 Activity and Affects Doxorubicin Sensitivity of Human Hepatocarcinoma Cells (2023)

Supplementary Figure 2 from MiR-122/Cyclin G1 Interaction Modulates p53 Activity and Affects Doxorubicin Sensitivity of Human Hepatocarcinoma Cells
Metallization Technologies on a Smooth Resin Surface for the Next Generation of Flip Chip Packaging (2010)

To realize higher wiring density, both finer line/space resolution and a smoother resin-metal interface are needed. These requirements, however, conflict to each other: sufficiently fine lines are difficult to form on a rough surface, while a smooth surface generally results in poor peel strength. The feasibility of various metallization processes that promote adhesion on smooth resin surfaces is examined. Their practical applicability to manufacturing high wiring-density packages is also assessed and the related issues that need to be improved are discussed.
Preliminary characterization of a Tritrichomonas foetus-like protozoan isolated from preputial smegma of virgin bulls (1999)

Trichomonad isolates from 14 virgin beef bulls in 3 California herds were submitted to the California Veterinary Diagnostic Laboratory for confirmation of a diagnosis of bovine trichomoniasis. Specimens were submitted in self-contained diagnostic pouches and produced cultures with a protozoan like Tritrichomonas foetus. Under bright-field microscopy, large numbers of single-celled motile organisms, approximately 12 μm x 9 μm, with multiple anterior flagellae, a posterior flagellum, axostyle, and a clearly visible undulating membrane were detected. Motility was jerky and rolling. Air-dried smears of cultures stained with Giemsa or Diff-Quick/iodine revealed an organism similar to T. foetus, although somewhat more rounded (less spindle-shaped). Several organisms appeared to have 4 flagellae, and there were numerous dark-staining bodies in the cytoplasm. Scanning electron micrographs (5000 X) clearly showed four anterior flagellae and an undulating membrane on most organisms, and an axostyle that was consistently longer than that seen in T. foetus. Specific primers for T. foetus were used in a polymerase chain reaction (PCR) assay. No amplification product was detected from any of the "virgin bull" isolates, while positive control isolates of T. foetus all yielded an amplicon of the expected size. On the basis of this partial morphological and molecular characterization, it was tentatively concluded that the isolated organism is not T. foetus, and speculate that it may be a commensal organism of the lower bowel. The recovery of non T. foetus trichomonads in a commercially available diagnostic system suggests that more specific methods may be needed for discrimination among trichomonads isolated from the preputial cavity of bulls.
Derivation and Validation of a Biomarker-Based Clinical Algorithm to Rule Out Sepsis From Noninfectious Systemic Inflammatory Response Syndrome at Emergency Department Admission: A Multicenter Prospective Study* (2018)

We have developed and validated a high-performing, reproducible, and parsimonious algorithm to assist emergency department physicians in distinguishing sepsis/septic shock from noninfectious systemic inflammatory response syndrome.
Performance of decision-directed channel estimation using low-rate turbo codes for OFDM (2011)

A low-rate turbo code can reduce the required average received signal-to-noise power ratio (SNR) that satisfies the target block error rate (BLER) due to its high coding gain. When a low-rate turbo code is used however, channel estimation (CE) error becomes a bottleneck in bringing out the potential coding gain. Therefore, this paper presents the average BLER performance using decision-directed channel estimation (DDCE) for a low-rate turbo code in orthogonal frequency division multiplexing (OFDM). In the proposed DDCE, we employ soft-decision symbol estimation based on the log-likelihood ratio (LLR) of an extrinsic probability at the Max-Log-MAP (maximum a posteriori probability) decoder output in addition to reference signals (RSs). The DDCE works synergistically with the low-rate turbo code, since the extrinsic LLR at the Max-Log-MAP decoder becomes more reliable due to the increasing coding gain. Computer simulation results show that when the turbo code with R = 1/15 (1/9) and the constraint length of K = 4 bits is used, the required average received SNR at the average BLER of 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-2</sup> using the DDCE is decreased by approximately 1.2 (1.2) dB compared to that for the RS based CE. As a result, the required average received SNR using the DDCE for R = 1/15 and 1/9 is decreased by approximately 6.0 and 4.4 dB, respectively, compared to that for R = 1/3.
A comparison of different methods to assess phase-locking in auditory neurons (2002)

Proposes a method to reconstruct acoustic signals from auditory nerve firings. This is a major step in order to improve cochlear implants by demonstrating what patients perceive with such a device. A computer model of the human cochlea transforms an acoustic test signal into a train of impulses, and the place- and volley-principle of cochlear frequency coding will be evaluated in order to invert this process, i.e. to reconstruct the original signal from the impulses. Phase-locking of the impulses to an acoustic stimulus is believed to be the main information carrier of loudness and frequency in the cochlea. Four different synchronization indices, which are used to assess phase-locking in the sensory receptor cells of the ear, will be presented and compared.
Efficient and targeted drug/siRNA co-delivery mediated by reversibly crosslinked polymersomes toward anti-inflammatory treatment of ulcerative colitis (UC) (2019)

Co-delivery of anti-inflammatory siRNA and hydrophilic drug provides a promising approach for the treatment of ulcerative colitis (UC). However, lack of a suitable and efficient co-delivery carrier poses critical challenge against their utilization. We herein developed macrophage-targeting, reversibly crosslinked polymersomes (TKPR-RCP) based on the TKPR-modified, poly(ethylene glycol)-b-poly(trimethylene carbonate-co-dithiolane trimethylene carbonate)-b-polyethylenimine (PEG-P(TMC-DTC)-PEI) triblock copolymer, which could efficiently encapsulate TNF-α siRNA and dexamethasone sodium phosphate (DSP) in their hydrophilic core. The cationic PEI segments provided additional electrostatic interactions with cargo molecules to promote the encapsulation, and disulfide crosslinking of the polymersome membrane endowed the TKPR-RCP with high colloidal stability. Because the cationic PEI was embedded in the hydrophilic core, the polymersomes displayed neutral surface charge and thus possessed high serum stability. The TKPR-RCP co-encapsulating TNF-α siRNA and DSP could be efficiently internalized by macrophages (∼ 98%) and undergo redox-responsive membrane de-crosslinking to accelerate cargo release in the cytoplasm, thus inducing efficient gene silencing and anti-inflammatory effect. Intravenous injection of the co-delivery TKPR-RCP mediated potent and cooperative anti-inflammatory effect in inflamed colons of UC mice, and significantly prevented animals from colonic injury. This study therefore provides a promising approach for the co-delivery of hydrophilic drug/siRNA toward the treatment of inflammatory bowel diseases.
W and Z boson production in p-Pb collisions at s N N = 5.02 $$ \sqrt{s_{\mathrm{NN}}}=5.02 $$ TeV (2017)

The W and Z boson production was measured via the muonic decay channel in proton-lead collisions at sNN−−−√=5.02 TeV at the Large Hadron Collider with the ALICE detector. The measurement covers backward (−4.46<ycms<−2.96) and forward (2.03<ycms<3.53) rapidity regions, corresponding to Pb-going and p-going directions, respectively. The Z-boson production cross section, with dimuon invariant mass of 60<mμμ<120 GeV/c2 and muon transverse momentum (pμT) larger than 20 GeV/c, is measured. The production cross section and charge asymmetry of muons from W-boson decays with pμT>10 GeV/c are determined. The results are compared to theoretical calculations both with and without including the nuclear modification of the parton distribution functions. The W-boson production is also studied as a function of the collision centrality: the cross section of muons from W-boson decays is found to scale with the average number of binary nucleon-nucleon collisions within uncertainties.