gebhart/patrepeval huggingface dataset:
Molecular cloning and nucleotide sequence of cDNA for mRNA of mitochondrial cytochrome P-450(SCC) of bovine adrenal cortex. (1984)

We have isolated cDNA clones of the mRNA for cytochrome P-450(SCC), which catalyzes the side-chain cleavage reaction of cholesterol in bovine adrenal cortex mitochondria, by using synthetic oligonucleotides as probes. Sequence analysis of the cloned cDNAs enabled us to deduce the primary structure of the precursor form of P-450(SCC), which consisted of 520 amino acids and contained an extrapeptide of 39 amino acids at the NH2 terminus. The amino acid sequence from the 40th to 55th amino acid residue in the predicted structure completely coincided with the sequence of the NH2-terminal portion of purified P-450(SCC). The amino acid composition calculated from the predicted structure showed an excellent agreement with that determined with the purified protein. The extrapeptide of the precursor molecule resembles those of a few nuclear-encoded yeast mitochondrial proteins reported so far. Although P-450(SCC) is a component of mitochondria, comparison of its primary structure with those of other forms of cytochrome P-450 shows that P-450(SCC) is structurally more related to microsomal cytochrome P-450s than to a bacterial cytochrome P-450, P-450cam. A homologous sequence observed with various forms of cytochrome P-450 is also highly conserved in the P-450(SCC) molecule. Only two cysteinyl residues are present in the mature form of P-450(SCC), one of which is located in the middle of the conserved sequence, confirming the function of this cysteinyl residue as the fifth ligand of the heme.
Heavy water effects on certain energetic processes in retina. (1979)

Heavy water effects on ATP concentration in frog retina were followed up. A substantial (more than 50%) decrease of ATP pools was found in the retina immersed in 2H2O-Ringer as compared to that in H2O-Ringer, which revealed that protons are strongly involved in the cellular energy processes.
Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors (1998)

We constructed a double mutant version of the alpha subunit of Go that was regulated by xanthine nucleotides instead of guanine nucleotides (GoalphaX). We investigated the interaction between GoalphaX and G protein-coupled receptors in vitro. First, we found that the activated m2 muscarinic cholinergic receptor (MAChR) could facilitate the exchange of XTPgammaS for XDP in the GoalphaXbetagamma heterotrimer. Second, the GoalphaXbetagamma complex was able to induce the high affinity ligand-binding state in the N-formyl peptide receptor (NFPR). These experiments demonstrated that GoalphaX was able to interact effectively with G protein-coupled receptors. Third, we found that the empty form of GoalphaX, lacking a bound nucleotide and betagamma, formed a stable complex with the m2 muscarinic cholingeric receptor associated with the plasma membrane. Finally, we investigated the interaction of GoalphaX with receptor in COS-7 cells. The empty form of GoalphaX bound tightly to the receptor and was not activated because XTP was not available intracellularly. We tested the ability of GoalphaX to inhibit the activities of several different G protein-coupled receptors in transfected COS-7 cells and found that GoalphaX specifically inhibited Go-coupled receptors. Thus the modified G proteins may act as dominant-negative mutants to trap and inactivate specific subsets of receptors.
Immunologically Active and Structurally Similar Fragments of Protein A from Staphylococcus aureus (1975)

To study the active site(s) in protein A, partial tryptic digestions of the protein and of intact Staphylococcus aureus were performed. Fragments which bind to the Fc-part of human IgG were isolated by affinity chromatography on IgG-Sepharose 4B and purified by ion-exchange chromatography on phosphocellulose. From a partial tryptic digest of pure protein A at 30 degrees C, pH 8.2 for 30 min we have isolated and characterized six active fragments with molecular weights ranging from 6000 to 8000. Two active fragments, obtained in high yields by digestion at pH 7.2 of intact protein-A-containing bacteria, were shown to be similar to two of the six characterized fragments from the digest of pure protein A. All fragments appeared to have similar amino acid sequences, judged by peptide mapping, specific staining and amino acid analysis; some are very possibly overlapping peptides. Each fragment probably contains only one active site region since all are monovalent in the Fc-reaction when studied with a hemagglutination technique. The maximal molar yield of active fragments obtained from the digestion of pure protein A accounts for about 210% of the amount of protein A used. Thus protein A, suggested to consist of repeating units, should exhibit at least three similar if not identical active regions.
A Low-Power Fullband 802.11a/b/g WLAN Transceiver With On-Chip PA (2007)

A low-power fullband 802.11a/b/g WLAN transceiver in 0.15-mum CMOS technology is described. The zero-IF transceiver achieves a receiver noise figure of 4.4/4 dB for the 2.4-GHz/5-GHz bands, respectively. The corresponding sensitivity at 54-Mb/s operation is -72 dBm for 802.11g and -74 dBm for 802.11a using actual PER measurement. An on-chip PA delivers 20 dBm output P1-dB. A new I/Q compensation scheme is implemented in local oscillator (LO) and an image rejection of better than 52 dB is observed. The transmitter delivers 10/1.5 dBm (2.4-/5-GHz) EVM-compliant output power for a 64-QAM OFDM signal at 54-Mb/s. The power consumption is 117/135 mW (1.8-V) in the receive mode and 570/233.1 mW in the transmit mode for 2.4/5 GHz, respectively. The low power consumption, high integration and robustness (-40 to 140degC) make this transceiver suitable for portable applications
Angiogenesis and prostate cancer: identification of a molecular progression switch. (2001)

To elucidate the sequence of molecular events intricate with angiogenesis and the initiation and progression prostate cancer, the temporal and spatial expression patterns of platelet endothelial cell adhesion molecule-1 (PECAM1/CD31), hypoxia-induced factor-1alpha (HIF-1alpha), vascular endothelial growth factor (VEGF), and the cognate receptors VEGFR1 and VEGFR2 were characterized. Immunohistochemical and in situ analyses of prostate tissue specimens derived from the spontaneous autochthonous transgenic adenocarcinoma of the mouse prostate (TRAMP) model identified a distinct early angiogenic switch consistent with the expression of PECAM-1, HIF-1alpha, and VEGFR1 and the recruitment of new vasculature to lesions representative of high-grade prostatic epithelial neoplasia (PIN). During progression of prostate cancer, the intraductal microvessel density (IMVD) was also observed to increase as a function of tumor grade. Immunoblot and in situ analyses further demonstrated a distinct late angiogenic switch consistent with decreased expression of VEGFR1, increased expression of VEGFR2, and the transition from a differentiated adenocarcinoma to a more poorly differentiated state. Analysis of clinical prostate cancer specimens validated the predictions of the TRAMP model. This resolution of prostate cancer-associated angiogenesis into distinct early and late molecular events establishes the basis for a "progression-switch" model to explain how the targets of antiangiogenic therapy might change as a function of tumor progression.
Electrophysiological effects of S 16257, a novel sino‐atrial node modulator, on rabbit and guinea‐pig cardiac preparations: comparison with UL‐FS 49 (1994)

1. S 16257 is a new bradycardic agent. Its electropharmacological profile has been compared to that of the known bradycardic compound UL-FS 49 (Zatebradine). Intracellular recordings of action potentials (APs) were performed with conventional glass microelectrodes. 2. In the rabbit isolated sino-atrial node (SAN) tissue, S 16257 and UL-FS 49 (1 microM, 3 microM and 10 microM) were equipotent in slowing spontaneous APs firing predominantly by decreasing the rate of diastolic depolarization (at 3 microM, -23.8 +/- 3.9% and -27.9 +/- 2.6%, respectively). For the two compounds a maximal effect was obtained at 3 microM. In these preparations, action potential duration at 50% of total repolarization (APD50) was more affected by UL-FS 49 than S 16257 at any concentration tested (at 3 microM, +8.9 +/- 2.9% and +29.1 +/- 3.7% for S 16257 and UL-FS 49, respectively; P < or = 0.01). 3. To estimate the direct effects on AP duration, driven cardiac preparations were exposed to these agents. In guinea-pig papillary muscles, paced at a frequency of 1 Hz, increasing concentrations of S 16257 or UL-FS 49 (0.1 to 10 microM, 30 min exposure for each concentration) slightly prolonged AP repolarization. This prolongation was more marked for UL-FS 49 (at 1 microM, +6.1 +/- 0.6% and +11.2 +/- 1.3% elevation of APD50, for S 16257 and UL-FS 49, respectively). 4. Application of UL-FS 49 (3 microM) to rabbit Purkinje fibres, triggered at a frequency of 0.25 Hz, induced a marked prolongation of APD50 and APD90 (+149.4 +/- 51.2% and +86.0 +/- 15.4%, respectively). S 16257 (3 MicroM) induced only a weak prolongation of AP (+ 14.1 +/- 5.0% and + 14.8 +/- 3.3% for APD50 and APD90, respectively) significantly smaller than in the case of UL-FS 49.5. These results show that S 16257 slows the rate of spontaneous AP firing in isolated SAN mainly by a reduction of the diastolic depolarization of the cells, which suggests an inhibition of the pace-maker current (If). S 16257 and UL-FS 49 are equipotent in their bradycardic effect but S 16257 is more specific as it induces less increase in myocardial repolarization time.
Reproductive Assessment by Continuous Breeding: Evolving Study Design and Summaries of Ninety Studies (1997)

Robert E. Chapin, Richard A. Sloane, Reproductive Assessment by Continuous Breeding: Evolving Study Design and Summaries of Ninety Studies, Environmental Health Perspectives, Vol. 105, Supplement 1 (Feb., 1997), pp. 199-205
1.5–1.6 μm GaInAsP/InP Integrated twin-guide lasers with first-order distributed Bragg reflectors (1980)

The room-temperature operation of 1.5–1.6 μm GaInAsP/InP integrated twin-guide lasers with first-order distributed Bragg reflectors is reported. Single-longitudinal-mode oscillation was observed up to 1.4 times the threshold current. The temperature dependence of lasing wavelength was only 0.8 Å/degree.
Cell surface-localized matrix metalloproteinase-9 proteolytically activates TGF-β and promotes tumor invasion and angiogenesis (2000)

We have uncovered a novel functional relationship between the hyaluronan receptor CD44, the matrix metalloproteinase-9 (MMP-9) and the multifunctional cytokine TGF-β in the control of tumor-associated tissue remodeling. CD44 provides a cell surface docking receptor for proteolytically active MMP-9 and we show here that localization of MMP-9 to cell surface is required for its ability to promote tumor invasion and angiogenesis. Our observations also indicate that MMP-9, as well as MMP-2, proteolytically cleaves latent TGF-β, providing a novel and potentially important mechanism for TGF-β activation. In addition, we show that MMP-9 localization to the surface of normal keratinocytes is CD44 dependent and can activate latent TGF-β. These observations suggest that coordinated CD44, MMP-9, and TGF-β function may provide a physiological mechanism of tissue remodeling that can be adopted by malignant cells to promote tumor growth and invasion.
Crystalline L-Ribulose 5-Phosphate 4-Epimerase from Escherichia coli (1968)

Abstract l-Ribulose 5-phosphate 4-epimerase has been crystallized from l-arabinose-induced cells of Escherichia coli B/r strain F' araB-24/araB-24 after a 40-fold purification. The enzyme is homogeneous in the ultracentrifuge and 98% pure by acrylamide gel disc electrophoresis. The molecular weight determined by sedimentation equilibrium is 1.03 ± 0.01 x 105. The enzyme is free of d-ribulose 5-phosphate 3-epimerase activity, does not exhibit any cofactor requirement, and shows maximal activity from pH 7 to 10. An amino acid analysis is presented.
Efficient Nucleic Acid Detection by Templated Reductive Quencher Release (2009)

RNA-templated fluorescence activation is a nucleic acid detection strategy that offers the possibility of direct visual detection of genetic information in living cells. Here we describe a new reaction strategy for fluorescence activation in which a phosphine on one DNA probe reduces an azide group in a linker on a second probe, resulting in linker cleavage and release of a fluorescence quenching group. These "Q-STAR" probes are shown to yield a strong fluorescence turn-on signal in approximately 20 min, with very low background and substantial amplification by turnover on the template. A green/red pair of such probes allowed the discrimination of two bacterial species by a single nucleotide difference in their 16S rRNA. The beneficial properties of the reductive quencher release design make these probes promising candidates for widespread application in the detection of nucleic acids in vitro and in cells.
Design of Networked Visual Monitoring Systems (1999)

ABSTRACT

We design and implement a networked visual monitoring system for surveillance. Instead of the usual periodical monitoring, the proposed system has an auto-tracking feature which captures the important characteristics of intruders. We integrate two schemes, namely, image segmentation and histogram comparison, to accomplish auto-tracking. The developed image segmentation scheme is able to separate moving objects from the background in real time. Next, the corresponding object centroid and boundary are computed. This information is used to guide the motion of tracking camera to track the intruders and then to take a series of shots, by following a predetermined pattern. We have also developed a multiple objects tracking scheme, based on object color histogram comparison, to overcome object occlusion and disocclusion issues. The designed system can track multiple intruders or follow any particular intruder automatically. To achieve efficient transmission and storage, the captured video is compressed in the H.263 format. Query based on time as well as events are provided. Users can access the system from web browsers to view the monitoring site or manipulate the tracking camera on the Internet. These features are of importance and value to surveillance.
Alterations in 3-Hydroxyisobutyrate and FGF21 Metabolism Are Associated With Protein Ingestion–Induced Insulin Resistance (2017)

Systemic hyperaminoacidemia, induced by either intravenous amino acid infusion or protein ingestion, reduces insulin-stimulated glucose disposal. Studies of mice suggest that the valine metabolite 3-hydroxyisobutyrate (3-HIB), fibroblast growth factor 21 (FGF21), adiponectin, and nonesterified fatty acids (NEFAs) may be involved in amino acid-mediated insulin resistance. We therefore measured in 30 women the rate of glucose disposal, and plasma 3-HIB, FGF21, adiponectin, and NEFA concentrations, under basal conditions and during a hyperinsulinemic-euglycemic clamp procedure (HECP), with and without concomitant ingestion of protein (<i>n</i> = 15) or an amount of leucine that matched the amount of protein (<i>n</i> = 15). We found that during the HECP without protein or leucine ingestion, the grand mean ± SEM plasma 3-HIB concentration decreased (from 35 ± 2 to 14 ± 1 µmol/L) and the grand median [quartiles] FGF21 concentration increased (from 178 [116, 217] to 509 [340, 648] pg/mL). Ingestion of protein, but not leucine, decreased insulin-stimulated glucose disposal (<i>P</i> < 0.05) and prevented both the HECP-mediated decrease in 3-HIB and increase in FGF21 concentration in plasma. Neither protein nor leucine ingestion altered plasma adiponectin or NEFA concentrations. These findings suggest that 3-HIB and FGF21 might be involved in protein-mediated insulin resistance in humans.
Characterising plant surfaces for spray adhesion and retention (2005)

A simple measurement of static contact angle of aqueous acetone droplets on surfaces has been developed for characterising leaf surfaces It allows leaves to be compared and grouped by their surface roughness factor and it differentiates between easy difficult and very difficulttowet species This paper describes how the method has been used to survey a large number of plant species including weeds and crops fruit and foliage High contact angles indicate difficulttowet surfaces The quantitative measure of contact angle is a useful tool to predict spray droplet adhesion and rank plant surfaces for retention properties It can also indicate whether surfactant addition is likely to be beneficial for agrochemical sprays targeted at fruit or foliage on different crops Surfactants were most useful for improving spray droplet adhesion and retention on difficulttowet surfaces but results varied with surface wettability surfactant type and concentration and with plant architecture
Transformation of Salmonella typhimurium by Plasmid Deoxyribonucleic Acid (1974)

A modified transformation procedure that is effective for the introduction of plasmid deoxyribonucleic acid at high frequency into Salmonella typhimurium, as well as into Escherichia coli, is described. Transformed bacteria acquire a circular deoxyribonucleic acid species having the genetic and molecular characteristics of the transforming plasmid.
Evaluation of 3-mm diameter intravenous tubing for the rapid infusion of fluids. (1987)

The use of intravenous administration systems incorporating 3-mm internal diameter tubing is becoming more common in hospital practice. The maximum flow-rate of crystalloid solutions through 3-mm-diameter tubing is compared to that through conventional 4-mm tubing when connected to standard large-gauge intravenous cannulae. Lengths of intravenous tubing between 80 cm and 200 cm were tested in combination with 16 gauge, 14 gauge and 13 gauge intravenous cannulae. The results demonstrated that the use of 3-mm-diameter infusion sets, or the inclusion of even short lengths of 3-mm tubing in an infusion system, limits the maximum flow that can be delivered through a cannula of size 16 gauge or larger. The reduced performance of the 3-mm tubing makes administration systems incorporating even short lengths of this diameter of tubing unsuitable in emergency situations and locations where rapid infusion of fluids is vital.
Bax-induced Caspase Activation and Apoptosis via Cytochromec Release from Mitochondria Is Inhibitable by Bcl-xL (1999)

A growing body of evidence supports a role for mitochondria and mitochondria-derived factors in the cell death process. In particular, much attention has focused on cytochrome c, a key component of the electron transport chain, that has been reported to translocate from the mitochondria to the cytosol in cells undergoing apoptosis. The mechanism for this release is, as yet, unknown. Here we report that ectopic expression of Bax induces apoptosis with an early release of cytochrome c preceding many apoptosis-associated morphological alterations as well as caspase activation and subsequent substrate proteolysis. A loss of mitochondrial transmembrane potential was detected in vivo, although no mitochondrial swelling or loss of transmembrane potential was observed in isolated mitochondria treated with Bax in vitro. Caspase inhibitors, such as endogenous XIAP and synthetic peptide benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone (zVAD-fmk), although capable of altering the kinetics and perhaps mode of cell death, had no influence on this release, suggesting that if cytochrome c plays a role in caspase activation it must precede this step in the apoptotic process. Mitochondrial permeability transition was also shown to be significantly prevented by caspase inhibition, indicating that the translocation of cytochrome c from mitochondria to cytosol is not a consequence of events requiring mitochondrial membrane depolarization. In contrast, Bcl-xL was capable of preventing cytochrome c release while also significantly inhibiting cell death. It would therefore appear that the mitochondrial release of factors such as cytochrome c represents a critical step in committing a cell to death, and this release is independent of permeability transition and caspase activation but is inhibited by Bcl-xL.
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors (2014)

A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and selective tetrahydropyrazolo[1,5-a]pyrazines. Use of PI3Kα mutants as ATR crystal structure surrogates was instrumental in providing cocrystal structures to guide the medicinal chemistry designs. Detailed DMPK studies involving cyanide and GSH as trapping agents during microsomal incubations, in addition to deuterium-labeled compounds as mechanistic probes uncovered the molecular basis for the observed CYP3A4 TDI in the series.
Inhibitory Effect of Fibronectin and Its Recombinant Polypeptides on the Adhesion of Metastatic Melanoma Cells to Laminin (1991)

We have utilized recombinant fibronectin fragments with cell-binding domain (C-274), heparin-binding domain (H-271) or CS1 peptide in type III connecting segment (IIICS) and their fusion polypeptides such as CH-296 (containing C-274, H-271 and CS1), CH-271 (containing C-274 and H-271) and C-CS1 (containing C-274 and CS1) to investigate the mechanism of the fibronectin-mediated inhibitory effect on tumor cell adhesion to laminin as well as fibronectin. These fragments retained cell adhesion-promoting and/or heparin-binding properties when they were immobilized on a surface. Pretreatment of tumor cells with CH-296 or CH-271 suppressed cell adhesion to both laminin and fibronectin. H-271 at the high concentration of 500 micrograms/ml slightly inhibited cell adhesion to laminin (but not to fibronectin), whereas C-274, C-CS1 or a mixture of C-274, H-271 and CS1 (similar molar ratio to CH-296) inhibited cell adhesion to fibronectin but not to laminin. On the other hand, tumor cell adhesion to laminin-substrate was also inhibited by heparin or heparan sulfate, which were able to bind to laminin, suggesting that heparin-like molecules on the cell surface may be included among the laminin receptors. These results indicated that the co-presence of cell- and heparin-binding domains of fibronectin may be required for the fibronectin-mediated inhibitory effect on tumor cell adhesion to laminin, and that the interaction of the heparin-binding domain of fibronectin with the cell surface leads to the inhibition of the cell adhesion to laminin.
Role of ADAMs in Cancer Formation and Progression (2009)

The ADAMs (a disintegrin and metalloproteinase) comprise a family of multidomain transmembrane and secreted proteins. One of their best-established roles is the release of biologically important ligands, such as tumor necrosis factor-alpha, epidermal growth factor, transforming growth factor-alpha, and amphiregulin. Because these ligands have been implicated in the formation and progression of tumors, it might be expected that the specific ADAMs involved in their release would also be involved in malignancy. Consistent with this hypothesis, emerging data from model systems suggest that ADAMs, such as ADAM-9, ADAM-12, ADAM-15, and ADAM-17, are causally involved in tumor formation/progression. In human cancer, specific ADAMs are up-regulated, with levels generally correlating with parameters of tumor progression and poor outcome. In preclinical models, selective ADAM inhibitors against ADAM-10 and ADAM-17 have been shown to synergize with existing therapies in decreasing tumor growth. The ADAMs are thus a new family of potential targets for the treatment of cancer, especially malignancies that are dependent on human epidermal growth factor receptor ligands or tumor necrosis factor-alpha.