gebhart/patrepeval huggingface dataset:
Kex2p: a model for cellular endoprotease processing human immunodeficiency virus type 1 envelope glycoprotein precursor (1994)

The endoproteolytic cleavage of the envelope glycoprotein precursor (gp160) of the human immunodeficiency virus type 1 (HIV-1) by a cellular protease is required for full activation of the virus. In this study, processing of gp160 was analyzed in vitro using the Kex2p endoprotease from the yeast Saccharomyces cerevisiae as a processing enzyme model. Endoproteolytic processing was examined using a synthetic peptide that mimics the cleavage site of HIV-1 glycoprotein, and a recombinant gp160 bearing the entire sequence of the env gene product, including the conserved cleavage site Arg508-Glu-Lys-Arg511. Coexpression in BHK-21 of Kex2p and gp160 by recombinant vaccinia viruses demonstrates that Kex2p can correctly process the HIV-1 glycoprotein to gp120 and gp41. Furthermore, recombinant gp160 and peptide were used as substrates and subjected to proteolysis with purified membranes from an S. cerevisiae strain overproducing the Kex2p endoprotease. Treatment of recombinant gp160, which has an apparent molecular mass of 127 kDa, with Kex2p and Western blot analysis showed that the precursor was cleaved into two products of about 101 and 34 kDa apparent molecular mass. Amino acid sequencing of the NH2-terminus of the 34-kDa product showed that the cleavage site of recombinant gp160 was between Arg511 and Ala512. Recombinant gp160 mutated at the sequence coding for the potential cleavage site, and mature recombinant gp120, however, were not cleaved when treated with Kex2p. In summary, our results show that Kex2p cleaves both the HIV-1 envelope glycoprotein precursor and a synthetic peptide mimicking the cleavage site of HIV-1 gp160 at the dibasic site, suggesting functional analogy between yeast Kex2p and the cellular protease responsible for the maturation of HIV-1 envelope glycoproteins in infected human cells.
Effects of the tyrosine protein kinase inhibitor genistein on the proliferation, activation of cultured rat hepatic stellate cells (2002)

Genistein influences proliferation of HSC, suppresses the expression of alpha-SMA in HSC and t inhibits the intensity of c-fos, c-jun and cyclin D(1) expression of HSCs. Genistein has therapeutic potential against liver fibrosis.
Proteomics analysis of malignant and benign prostate tissue by 2D DIGE/MS reveals new insights into proteins involved in prostate cancer (2015)

In addition to the identification of substantial number of proteins with known association with PCa, the proteomic approach in this study revealed proteins not previously clearly related to PCa, providing a starting point for further elucidation of their function in disease initiation and progression.
Uptake of N-(4'-pyridoxyl)amines and release of amines by renal cells: a model for transporter-enhanced delivery of bioactive compounds. (1991)

The importing of vitamin B6 by renal proximal tubular cells from the rat is facilitated and Na(+)-dependent and reflects specificity for the meta-phenolate pyridinium structure with a 5-hydroxymethyl function. This transporter can, however, accept competitively each of the natural nonphosphorylated vitamers (pyridoxine, pyridoxamine, and pyridoxal) and other B6 analogues differing only in the groups at position 4. A series of N-(4'-pyridoxyl)amines was synthesized by sodium borohydride or boro[3H]hydride reduction of aldimines formed by condensing the amines with pyridoxal. The unlabeled B6-secondary amine compounds were found to competitively inhibit the uptake of [4'-3H]pyridoxine by the renal cells. Moreover, the 3H-labeled N-(4'-pyridoxyl)amines were shown to enter the cells by the process facilitated by the B6 transporter. Upon entry the labeled compounds were converted to N-(5'-phospho-4'-pyridoxyl)amines in a reaction catalyzed by pyridoxal kinase, an enzyme that tolerates considerable functional variation in position 4 of the B6 structure. The 5'-phosphates were subsequently converted within the cell to pyridoxal 5'-phosphate with liberation of the original amine in a reaction catalyzed by pyridoxamine (pyridoxine) 5'-phosphate oxidase, an enzyme with broad specificity for 4'-substituted amines on the 5'-phospho-B6 structure. This system illustrates how knowledge of transporter specificity can permit design of a compound with potential biologic activity. A drug or other intracellular effector may be piggybacked onto a transported solute (e.g., vitamin or other nutrient) that gains facilitated entry to a cell and is, thereafter, metabolized to release the active compound.
An Engineered Human IgG1 Antibody with Longer Serum Half-Life (2006)

The serum half-life of IgG Abs is regulated by the neonatal Fc receptor (FcRn). By binding to FcRn in endosomes, IgG Abs are salvaged from lysosomal degradation and recycled to the circulation. Several studies have demonstrated a correlation between the binding affinity of IgG Abs to FcRn and their serum half-lives in mice, including engineered Ab fragments with longer serum half-lives. Our recent study extended this correlation to human IgG2 Ab variants in primates. In the current study, several human IgG1 mutants with increased binding affinity to human FcRn at pH 6.0 were generated that retained pH-dependent release. A pharmacokinetics study in rhesus monkeys of one of the IgG1 variants indicated that its serum half-life was approximately 2.5-fold longer than the wild-type Ab. Ag binding was unaffected by the Fc mutations, while several effector functions appeared to be minimally altered. These properties suggest that engineered Abs with longer serum half-lives may prove to be effective therapeutics in humans.
Purification and characterization of GDP‐D‐mannose 4,6‐dehydratase from porcine thyroid (1985)

The enzyme GDP-D-mannose 4,6-dehydratase has been purified 1500-fold from porcine thyroid tissue. The enzyme exhibits a molecular mass of 251000 Da as determined by sedimentation techniques. Its subunit size was determined as 41500 Da by dodecyl sulfate gel electrophoresis. The enzyme has a Km of 3.3 microM with respect to GDP-D-mannose and appears specific with respect to this substrate. The enzyme appears to be inhibited by guanine nucleotides and by guanine nucleotide sugars. It is particularly susceptible to inhibition by GDP-L-fucose. It is suggested that this compound may have a physiological function as an end-product feedback inhibitor.
Polymer Films on Electrodes: VII . Electrochemical Behavior at Polypyrrole‐Coated Platinum and Tantalum Electrodes (1982)

Polypyrrole films were deposited on platinum and tantalum and used as electrodes. The results indicate that these films are porous to solvent and electrolyte ions, and this porosity is responsible for the apparent reversible electrochemical behavior previously observed with many redox couples at polypyrrole on Pt. These electrochemically conducting films do exhibit electron transfer reactions with solution species, although less reversibly than at naked or film‐covered Pt. The films are unstable to oxidative conditions such as potentials > 0.6V vs. SCE or the presence of halogens.
Platelet-Derived Growth Factor-D Overexpression Contributes to Epithelial-Mesenchymal Transition of PC3 Prostate Cancer Cells (2008)

Abstract The majority of human malignancies are believed to have epithelial origin, and the progression of cancer is often associated with a transient process named epithelial-mesenchymal transition (EMT). EMT is characterized by the loss of epithelial markers and the gain of mesenchymal markers that are typical of “cancer stem-like cells,” which results in increased cell invasion and metastasis in vivo. Therefore, it is important to uncover the mechanistic role of factors that may induce EMT in cancer progression. Studies have shown that platelet-derived growth factor (PDGF) signaling contributes to EMT, and more recently, PDGF-D has been shown to regulate cancer cell invasion and angiogenesis. However, the mechanism by which PDGF-D promotes invasion and metastases and whether it is due to the acquisition of EMT phenotype remain elusive. For this study, we established stably transfected PC3 cells expressing high levels of PDGF-D, which resulted in the significant induction of EMT as shown by changes in cellular morphology concomitant with the loss of E-cadherin and zonula occludens-1 and gain of vimentin. We also found activation of mammalian target of rapamycin and nuclear factor-κB, as well as Bcl-2 overexpression, in PDGF-D PC3 cells, which was associated with enhanced adhesive and invasive behaviors. More importantly, PDGF-D-overexpressing PC3 cells showed tumor growth in SCID mice much more rapidly than PC3 cells. These results provided a novel mechanism by which PDGF-D promotes EMT, which in turn increases tumor growth, and these results further suggest that PDGF-D could be a novel therapeutic target for the prevention and/or treatment of prostate cancer. Disclosure of potential conflicts of interest is found at the end of this article.
Ultrawideband temperature-dependent dielectric properties of animal liver tissue in the microwave frequency range (2006)

The development of ultrawideband (UWB) microwave diagnostic and therapeutic technologies, such as UWB microwave breast cancer detection and hyperthermia treatment, is facilitated by accurate knowledge of the temperature- and frequency-dependent dielectric properties of biological tissues. To this end, we characterize the temperature-dependent dielectric properties of a representative tissue type-animal liver-from 0.5 to 20 GHz. Since discrete-frequency linear temperature coefficients are impractical and inappropriate for applications spanning wide frequency and temperature ranges, we propose a novel and compact data representation technique. A single-pole Cole-Cole model is used to fit the dielectric properties data as a function of frequency, and a second-order polynomial is used to fit the Cole-Cole parameters as a function of temperature. This approach permits rapid estimation of tissue dielectric properties at any temperature and frequency.
Isothiazolone Derivatives Selectively Inhibit Telomerase from Human and Rat Cancer Cells in Vitro (1999)

The telomere hypothesis postulates stabilization of telomere length and telomerase activation as key events in cellular immortalization and carcinogeneses. Accordingly, telomerase has been suggested as a novel and highly selective target for design of antitumor drugs. Screening of a chemical library including 16 000 synthetic compounds yielded six that strongly inhibited telomerase activity in extracts of cultured human cells, including four isothiazolone derivatives and two unrelated compounds. The most potent inhibitor was 2-[3-(trifluoromethyl)phenyl]isothiazolin-3-one (TMPI), a concentration of 1.0 microM inhibited telomerase activity by 50% according to a telomere repeat amplification protocol (TRAP) assay. Analysis using partially purified telomerase from AH7974 rat hepatoma cells demonstrated noncompetitive inhibition with the telomere-repeat primer and mixed inhibition with the dNTPs; the inhibition constant was 2.5 microM. TMPI did not inhibit eukaryotic DNA polymerase alpha, beta, or human immunodeficiency virus reverse transcriptase (HIV RT). Thus, inhibition by TMPI was highly selective for telomerase. Inhibition by TMPI was quenched by 1 mM of dithiothreitol or glutathione, suggesting that TMPI inhibits telomerase by acting at a cysteine residue. TMPI inhibition of this enzyme may find application as an antineoplastic agent.
The effect of environmental exposure upon the mechanical properties of coir or oil palm fiber reinforced composites (2000)

Polyester matrix composites reinforced using nonwoven coir or oil palm empty fruit bunch fiber mats were manufactured. Fibers were used unmodified, chemically modified by acetylation, or treated with silane or titanate coupling agents. Composite test pieces were exposed to decay fungi in unsterile soil for up to 12 months, along with samples made of unreinforced, or glass fiber reinforced, resin. Water exposure tests were also performed. The effect of such exposure on the mass loss, tensile and flexural properties of the samples was evaluated. Mechanical properties deteriorated as a result of exposure. However, acetylation of fibers, or treatment with silane coupling agent was found to afford a significant degree of protection. © 2000 John Wiley & Sons, Inc. J Appl Polym Sci 77: 1322–1330, 2000
No overall change in the rate of weight gain after switching to an integrase-inhibitor in virologically suppressed adults with HIV (2019)

We found no clear evidence of an overall increase in rate of weight gain following switch to INSTI in virologically suppressed individuals.
Synthetic approaches to long-wavelength-absorbing photosensitizers: porphyrinone and derivatives (1990)

There has been considerable interest in the development of photosensitizers having increased absorption in the red or near infrared region for PDT applications. It is known that porphyrin absorptions can be shifted to longer wavelengths by expanding the n-conjugation of the macrocycle and by introducing electron-withdrawing groups at the ring. This principle has been applied to a number of porphyrinone (oxochlorin), porphyrintriones (dioxobacteriochlorins and dioxoisobacteriochlorins), as well as a porphyrintrione. The oxo group in this class of compounds has been transformed into sulfido-, imino, and methide derivatives, i.e., the ring system contains at least one exocyclic double bond connected to S, N-CN, and C(CN)2 using suitable reaction conditions. Many of these compounds exhibit absorption maxima longer than 700 nm, some even in the 800 nm region. Since the porphyrinones are generally photodynamically active to in vitro cells, they are attractive for PDT drug use.
An asynchronous 2-D discrete cosine transform chip (2002)

This paper describes a fully asynchronous two-dimensional discrete cosine transform chip. The chip has a fixed block size of 8/spl times/8 pixels and uses bit-serial arithmetic. The chip was fabricated through MOSIS using a 0.8 /spl mu/ double-metal CMOS process. The 49.5 mm/sup 2/ core uses /spl sim/162,000 transistors. The chip operates from 0.65 V to 7.0 V, but its pixel rate at 5.0 V, 17 MHz, is significantly below the 27 MHz simulated because none of the signal's capacitances were backextracted. In order to design a completely asynchronous chip, a FIFO-based transposition memory was used, even though it used more area than RAM-based memory. The most interesting aspects of the design are presented here: the memory control structure, the pipelining structures, the use of Xilinx FPGAs and a Quickturn emulation system for emulation, and a comparison with other synchronous and asynchronous designs.
The making of the dominant MHC class I ligand SYFPEITHI (1998)

The proteasome contributes to the generation of most of the peptide ligands of MHC class I molecules. To compare the identity of the peptides generated by the proteasome with those finally presented by MHC class I molecules, we generated a monoclonal antibody recognizing the C-terminal part of the dominant H2-Kd ligand SYFPEITHI derived from the JAK1 tyrosine kinase. Immunoprecipitations of lysates from H2-Kd-expressing or non-expressing cells revealed that only in the presence of H2-Kd SYFPEITHI could be isolated. No longer potential precursor peptide containing SYFPEITHI could be detected. Surprisingly, a peptide lacking the first two amino acids, FPEITHI, was isolated independently of the presence of H2-Kd molecules. The detection of only SYFPEITHI and FPEITHI in cell lysates corresponded with the strong generation of these two peptides in in vitro digests of elongated SYFPEITHI-containing peptides with purified 20S proteasomes. Our results indicate that MHC ligands can be generated directly by the proteasome in vivo and that at least for SYFPEITHI the expression of the corresponding MHC molecule is critical for protection of the ligand in vivo.
Considerations for Successful Cognitive Radio Systems in US TV White Space (2008)

On February 17, 2009, the United States will complete the transition to digital television. The FCC is in the process of establishing rules to allow unlicensed secondary use of the TV "white space" that this transition creates. This television white space (TVWS) opens vital new portions of limited radio spectrum and enables delivery of new communication services, particularly wireless broadband, to millions of underserved Americans. In some rural markets, up to 250 MHz of spectrum could be utilized. Expected initial system deployments in TVWS include wireless Internet service providers (WISPs) and broadband coverage systems for business enterprises. It is critical that these early services are successful, both technically in protecting incumbent licensed users as well as financially in being commercially viable. Cognitive radio technologies are available that enable radio systems operating in the TVWS spectrum to reliably protect the incumbent licensed users. These technologies include geolocation, augmented by sensing, and beaconing. Existing protocols, such as WiMax, WiFi, and proprietary protocols, rebanded to the UHF frequency ranges, will provide broadband data throughput at adequate ranges to allow practical services. It is important to develop and deploy early viable solutions into this band that protect incumbent licensed users so that cycles of learning can start. Lessons from these early systems will allow the industry to accept more aggressive cognitive radio technologies and services, will offer greater comfort to critics of the technology, and will provide regulatory agencies worldwide with data for future rulemaking.
Strengthening the Prevention of Periodontal Disease: The WHO Approach (2005)

The vast majority of countries need to establish a surveillance system for measuring progress in the control of periodontal disease and promotion of oral health. WHO has designed approaches for the integration of oral disease prevention within the prevention of non-communicable chronic diseases, and global strategies are currently being implemented in all regions of the world.
Sensitivity of Osteoinductive Activity of Demineralized and Defatted Rat Femur to Temperature and Duration of Heating (1995)

For autogenous and allogeneic bone grafts, heat treatment has been thought to kill malignant cells and viruses such as human immunodeficiency virus. It is unclear whether heat treatment could preserve bone-inductive activity. Cortical bones from 6-week-old rat femurs were heated in a water bath at a temperature of 50 degrees-100 degrees C for periods of 15 minutes to 10 hours. After treatment, they were defatted and decalcified. Each sample was transplanted into the hamstring muscle of 3-week-old rats. Eleven days after transplantation, the samples were removed and messenger ribonucleic acids (mRNAs) were determined for alkaline phosphatase and collagens in the transplant. Twenty-one days after transplantation, actual bone formation was studied by histologic analysis and measurement of calcium content. Heat treatment at 60 degrees C for 10 hours and at 70 degrees C for 1 hour preserved bone-inductive activity, as indicated by the induction of mRNAs for alkaline phosphatase and Type I and Type II collagens. Significant decreased in Type II collagen mRNA and calcium content were observed at 70 degrees C when the transplants were heated for 10 hours, suggesting the importance of evaluating the duration of heat treatment.
Society for Ambulatory Anesthesia Consensus Statement on Preoperative Selection of Adult Patients with Obstructive Sleep Apnea Scheduled for Ambulatory Surgery (2012)

The suitability of ambulatory surgery for a patient with obstructive sleep apnea (OSA) remains controversial because of concerns of increased perioperative complications including postdischarge death. Therefore, a Society for Ambulatory Anesthesia task force on practice guidelines developed a consensus statement for the selection of patients with OSA scheduled for ambulatory surgery. A systematic review of the literature was conducted according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines. Although the studies evaluating perioperative outcome in OSA patients undergoing ambulatory surgery are sparse and of limited quality, they do provide useful information that can guide clinical practice. Patients with a known diagnosis of OSA and optimized comorbid medical conditions can be considered for ambulatory surgery, if they are able to use a continuous positive airway pressure device in the postoperative period. Patients with a presumed diagnosis of OSA, based on screening tools such as the STOP-Bang questionnaire, and with optimized comorbid conditions, can be considered for ambulatory surgery, if postoperative pain can be managed predominantly with nonopioid analgesic techniques. On the other hand, OSA patients with nonoptimized comorbid medical conditions may not be good candidates for ambulatory surgery. What other guidelines are available on this topic? The American Society of Anesthesiologists (ASA) practice guidelines for management of surgical patients with OSA published in 2006. Why was this guideline developed? The ASA guidelines are outdated because several recent studies provide new information such as validated screening tools for clinical diagnosis of OSA and safety of ambulatory laparoscopic bariatric surgery in OSA patients. Therefore, an update on the selection of patients with OSA undergoing ambulatory surgery is warranted. How does this guideline differ from existing guidelines? Unlike the ASA guidelines, this consensus statement recommends the use of the STOP-Bang criteria for preoperative OSA screening and considers patients' comorbid conditions in the patient selection process. Also, current literature does not support the ASA recommendations that upper abdominal procedures are not appropriate for ambulatory surgery. Why does this guideline differ from existing guidelines? This consensus statement differs from existing ASA guidelines because of the availability of new evidence.