gebhart/patrepeval huggingface dataset:
High level describable attributes for predicting aesthetics and interestingness (2011)

With the rise in popularity of digital cameras, the amount of visual data available on the web is growing exponentially. Some of these pictures are extremely beautiful and aesthetically pleasing, but the vast majority are uninteresting or of low quality. This paper demonstrates a simple, yet powerful method to automatically select high aesthetic quality images from large image collections. Our aesthetic quality estimation method explicitly predicts some of the possible image cues that a human might use to evaluate an image and then uses them in a discriminative approach. These cues or high level describable image attributes fall into three broad types: 1) compositional attributes related to image layout or configuration, 2) content attributes related to the objects or scene types depicted, and 3) sky-illumination attributes related to the natural lighting conditions. We demonstrate that an aesthetics classifier trained on these describable attributes can provide a significant improvement over baseline methods for predicting human quality judgments. We also demonstrate our method for predicting the “interestingness” of Flickr photos, and introduce a novel problem of estimating query specific “interestingness”.
Two peptides from the alpha 2A-adrenergic receptor alter receptor G protein coupling by distinct mechanisms (1991)

Peptides derived from various regions of the alpha 2A-adrenergic receptor (alpha 2A-AR) were used to study receptor-G protein interactions. Binding of the partial agonist [125I]-p-iodoclonidine and the full agonist [3H]bromoxidine (UK14,304) to membrane preparations from human platelet was potently reduced by peptides (12-14 amino acids) from the second cytoplasmic loop (A) and the C-terminal side of the third cytoplasmic loop (Q). Binding of the antagonist [3H]yohimbine was significantly less affected. Five other peptides had no significant effects on ligand binding at concentrations less than 100 microM. The IC50 values for peptides A and Q were 7 and 27 microM for [125I]-p-iodoclonidine binding at the platelet alpha 2A receptor, 15 and 71 microM for the neuroblastoma-glioma (NG108-15) alpha 2B receptor, and greater than 300 microM for yohimbine binding at both alpha 2A and alpha 2B receptors. Competition studies demonstrate that at concentrations of 100 microM, peptides A and Q reduce the affinity of bromoxidine for the platelet alpha 2A-AR and this effect was abolished in the presence of guanine nucleotide. Alpha 2A-AR-stimulated GTPase activity in platelet membranes was inhibited by peptide Q with an IC50 of 16 microM but A was inactive. These data suggest that both the second cytoplasmic loop and the C-terminal part of the third cytoplasmic loop of the alpha 2A-AR are important in the interaction between the alpha 2-AR and Gi protein. Peptide Q appears to destabilize the high affinity state of the alpha 2-AR by binding directly to Gi thus preventing it from coupling to the receptor under both binding and GTPase assay conditions. The peptide from the second cytoplasmic loop (A) also reduces high affinity agonist binding in a G protein-dependent manner but its interaction with receptor and G protein is distinct in that it does not prevent activation of the G protein. These results provide new information about regions of the alpha 2-adrenergic receptor involved in G protein coupling and high affinity agonist binding.
Discovery of Potent Antiproliferative Agents Targeting EGFR Tyrosine Kinase Based on the Pyrido[3′,2′:4,5]thieno[3,2-<i>d</i>]pyrimidin-4-amine Scaffold (2015)

A series of pyridothieno[3,2-d]pyrimidin-4-amines was designed and synthesized as congeners to the classical 4-anilinoquinazolines as ATP-competitive epidermal growth factor receptor (EGFR) inhibitors. Compound 5a exhibited the most potent and selective inhibitory activity against EGFR with an IC50 value of 36.7 nM. Moreover, compounds 4b and 5a showed remarkable cell growth inhibition against leukemia, central nervous system cancer, and non-small cell lung cancer cell lines that overexpress EGFR, with growth inhibition of 50% (GI50) values of around 10 nM in the full U.S. National Cancer Institute 60 cell panel assay. Cell cycle studies indicated that compounds 4b and 5a induced significant cell cycle arrest in the S-phase and G0/G1, respectively, in addition to boosting P27(kip) expression. Compound 5a did not alter the viability of placental trophoblasts, which reflects its safety for normal cells. The standard COMPARE analyses demonstrated considerable correlation levels between compounds 4b and 5a and erlotinib, with pyridinium chlorochromate (PCC) values of 0.707 and 0.727, respectively.
The steroid binding domain of porcine estrogen receptor (1987)

For the purpose of characterizing the estrogen binding domain of porcine estrogen receptor (ER), we have made use of affinity labeling of partially purified ER with [3H]tamoxifen aziridine. The labeling is very efficient and selective particularly after partial purification of ER. A 65,000-dalton (65-kDa) band was detected on the fluorogram of a sodium dodecyl sulfate-polyacrylamide gel, together with a 50-kDa band and a few more smaller bands. The 50-kDa protein appears to be a degradation product of the 65-kDa protein in view of the similar peptide map. ER was affinity labeled before or after controlled limited proteolysis with either trypsin, papain, or alpha-chymotrypsin. The labeling patterns of limited digests indicate that a fragment of about 30 kDa is relatively resistant to proteases and has a full and specific binding activity to estrogen, whereas smaller fragments have lost much of the binding activity. This fragment is very hydrophobic and probably corresponds to the carboxy half of ER.
System Issues Relating To Laser Diode Requirements For VLSI Holographic Optical Interconnects (1989)

Laser requirements and limitations for VLSI optical interconnect networks employing computer-generated holograms are discussed from a system point of view. For architectures with a collimating lens at the laser and a collector lens at the detector, the restrictions on laser wave-length stability are typically ± 10 A (thus requiring the laser's temperature to be regulated to approximately ± 5°C to 10°C). Diffraction limitations are shown to restrict the density of interconnects to the 104/cm2 range from many architectures (in particular, "space variant" architectures), rather than the 107/cm2 to 108/cm2 range frequently cited for "space invariant" architectures. Architectures with a mixture of space variance and invariance can lead to intermediate densities. Some architectures require low threshold, high efficiency lasers, whereas others require very high output power with much less concern for threshold and efficiency. A network with 3000 point-to-point interconnects per square centimeter, each transmitting at a 500 Mbit rate with a 10-11 bit-error rate, is analyzed. The best system performance is obtained if wavelength stabilized high power (10 W) laser arrays are available. Monolithic integration is discussed, and the need for uniform and/or tunable emission wavelength may be the greatest challenge in this area.
Continuously variable transmission control (1980)

A large gain in automobile fuel economy has been made by a continuously variable transmission under microcomputer control. The transmission, of toroid and roller type, has a very wide range of ratios and the controller makes full use of this range to minimise the fuel consumption of the vehicle. The controller also has to ensure that the vehicle responds rapidly and predictably to changes in the driver's demand. These gains in fuel economy have been possible because only about 10 to 40 per cent of the installed power is needed for medium speed cruising and that amount of power can be obtained for much less fuel than usual if the engine is run at very low speeds. The internal losses of the engine are largely speed related and not much affected by the higher torque needed to maintain the power output. To develop the controller a special test rig was built with mechanical simulation of all the major elements in the driveline. The controller was designed to use information from speed sensors and the carburettor butterfly angle to minimise fuel consumption while conforming smoothly to the driver's demands for performance. After tuning of the feedback loops and initial proving of the controller on the test rig the transmission was installed in a car. Some further development was needed to improve driveability. Fuel savings were very close to the predicted values.
Ultrasonic backscatter from bovine tissues: Variation with pathology (1987)

This is the second in a series of two papers reporting results collected on ultrasonic propagation properties, namely, velocity, attenuation, and backscatter of various mammalian tissues. In the first paper [J. Acoust. Soc. Am 78, 871 (1985)], the experimental results of five different types of normal bovine tissues were given. In this paper, results obtained for the most common bovine disease in the liver, liver abscess, and in the heart, lymphosarcoma, will be presented. These data show that the ultrasonic properties of tissues with these two types of pathologies are significantly deviated from those of normal tissues, thus providing further evidence that ultrasonic properties may be used as quantitative indicators of a certain disease for diagnostic purposes.
Excision repair of UV-damaged plasmid DNA inXenopusoocytes is mediated by DNA polymerase α (and/or δ) (1990)

We studied DNA repair by injecting plasmids containing random pyrimidine dimers into Xenopus oocytes. We demonstrated excision repair by recovering plasmids and analyzing them with T4 UV endonuclease treatment and alkaline agarose gel electrophoresis. The mechanism for excision repair of these plasmids appears to be processive, rather than distributive, since repair occurs in 'all or none' fashion. At less than 4-5 dimers/plasmid, nearly all repair occurs within 4-6 hours (approximately 10(10) dimers repaired per oocyte); the oocyte, therefore, has abundant repair activity. Specific antibodies and inhibitors were used to determine enzymes involved in repair. We conclude that DNA polymerase alpha (and/or delta) is required because repair is inhibited by antibodies to human DNA polymerase alpha, as well as by aphidicolin, an inhibitor of polymerases alpha (and/or delta). Repair was not inhibited by hydroxyurea, cytosine beta-D-arabinofuranoside, or inhibitors of topoisomerase II (novobiocin). Oocyte repair does not activate semi-conservative DNA replication, nor is protein synthesis required. Photoreactivation cannot account for repair because dimer removal is independent of exogenous light.
Molecular cloning and characterization of ST7R (ST7-like, ST7L) on human chromosome 1p13, a novel gene homologous to tumor suppressor gene ST7 on human chromosome 7q31 (2002)

ST7 is a tumor suppressor gene, which is clustered with WNT2 gene in human chromosome 7q31 region. WNT2 gene is homologous to WNT2B gene. WNT2B gene encodes two isoforms due to alternative splicing of alternative promoter type. WNT2 and WNT2B isoform 2 (WNT2B2) are positive regulators of the WNT - beta-catenin - TCF signaling pathway. Here, a novel ST7-related gene ST7R (ST7-like, ST7L) was identified by using bioinformatics, and ST7R cDNAs were isolated by using cDNA-PCR. ST7R gene encoded 575-amino-acid polypeptide with leucine zipper domain and 3 tyrosine-phosphorylation sites. Human ST7R was homologous to human ST7 (72.1% total-amino-acid identity) and Drosophila CG3634 (56.8% total-amino-acid identity). Leucine zipper domain was unique to ST7R. Tyr 268 and Tyr 441 of ST7R were conserved in ST7 and CG3634. ST7R-homologous domains (S7H1, S7H2, and S7H3) were conserved among ST7R, ST7, and CG3634. ST7R gene consisted of at least 15 exons, and four ST7R isoforms were transcribed due to alternative splicing. ST7R and WNT2B genes, located in human chromosome 1p13 region, were clustered in tail-to-tail manner with an interval of less than 5.0-kb. ST7R-WNT2B and ST7-WNT2 gene clusters might be generated due to duplication of an ancestral gene cluster. Because allelic loss or rearrangements of human chromosome 1p13 region are reported in breast cancer, germ cell tumors, squamous cell carcinoma of head and neck, non-small cell lung cancer, gastrointestinal stromal/smooth muscle tumors (GIST), meningioma, melanoma, acute megakaryoblastic leukemia (M7), and Kaposi's sarcoma, ST7R might be a novel tumor suppressor gene on human chromosome 1p13.
SF/HGF is a mediator between limb patterning and muscle development (1999)

Scatter factor/hepatocyte growth factor (SF/HGF) is known to be involved in the detachment of myogenic precursor cells from the lateral dermomyotomes and their subsequent migration into the newly formed limb buds. As yet, however, nothing has been known about the role of the persistent expression of SF/HGF in the limb bud mesenchyme during later stages of limb bud development. To test for a potential role of SF/HGF in early limb muscle patterning, we examined the regulation of SF/HGF expression in the limb bud as well as the influence of SF/HGF on direction control of myogenic precursor cells in limb bud mesenchyme. We demonstrate that SF/HGF expression is controlled by signals involved in limb bud patterning. In the absence of an apical ectodermal ridge (AER), no expression of SF/HGF in the limb bud is observed. However, FGF-2 application can rescue SF/HGF expression. Excision of the zone of polarizing activity (ZPA) results in ectopic and enhanced SF/HGF expression in the posterior limb bud mesenchyme. We could identify BMP-2 as a potential inhibitor of SF/HGF expression in the posterior limb bud mesenchyme. We further demonstrate that ZPA excision results in a shift of Pax-3-positive cells towards the posterior limb bud mesenchyme, indicating a role of the ZPA in positioning of the premuscle masses. Moreover, we present evidence that, in the limb bud mesenchyme, SF/HGF increases the motility of myogenic precursor cells and has a role in maintaining their undifferentiated state during migration. We present a model for a crucial role of SF/HGF during migration and early patterning of muscle precursor cells in the vertebrate limb.
Synthesis and Biological Evaluation of Paclitaxel−C225 Conjugate as a Model for Targeted Drug Delivery1 (2003)

Tumor-targeted drug delivery is an attractive strategy in cancer treatment. We have previously reported a paclitaxel model conjugate using a bombesin receptor-recognizing peptide in which the drug cytotoxicity against H1299 human nonsmall cell lung cancer was enhanced compared to unconjugated taxol. In an effort to expand the development of tumor-recognizing taxanes, paclitaxel (PTX, taxol) was conjugated to the anti-epidermal growth factor receptor (anti-EGFR) monoclonal antibody (MAb) Erbitux (C225) to serve as a model MAb-mediated drug delivery compound. Thus, paclitaxel was derivatized at its 2'-hydroxy function by introduction of a succinate linker, and the carboxyl group of the latter was covalently attached to C225 through amide bond formation. The final product conjugate (PTXC225) was analyzed mass spectrometrically for assessment of the drug-to-antibody ratios. Cytotoxicity screening of the drug-antibody conjugate against A431, UM-SCC-1, and UM-SCC-6 cells indicated an enhancement in cytocidal effect of paclitaxel as compared to those of the free drug, the intact antibody, and a physical mixture of the two (the controls). In A431 cells, the conjugate showed 25.2% +/- 2.2% of apoptosis induction as compared to little or no apoptosis caused by the controls. Biodistribution analysis of the PTXC225 in tumor-implanted nude mice and a tyrosine-kinase assay showed that conjugation of the drug did not interfere with the immunoreactivity of the antibody. The 24-h tumor uptake of C225 and PTXC225 were 11.7% +/- 6.0% and 7.1% +/- 3.6% of the injected dose per gram of tissue (%ID/g), respectively, which were not significantly different. Also, in A431-implanted nude mice, the conjugate and C225 showed tumor growth inhibition effects of 57.2% and 41.2%, respectively, against a saline-treated control, which were not significantly different from each other. This lack of difference in the in vivo antitumor activity of the MAb-delivered drug and free PTX may be due to either a relatively low dose of the antibody-delivered drug (346 microg/kg), or an untimely release of it, or both. The tumor growth inhibition pattern of the conjugate, however, was identical to that of C225, indicating that the attachment of PTX did not affect the antigen-binding and growth inhibitory features of the MAb. These preliminary results demonstrate the potential of tumor-targeted delivery of taxol as a promising strategy in cancer treatment and warrant further work to develop more suitable drug-MAb linkers as well as improved dosage and treatment protocols.
In vitro neural injury model for optimization of tissue‐engineered constructs (2007)

Stem cell transplantation is a promising approach for the treatment of traumatic brain injury, although the therapeutic benefits are limited by a high degree of donor cell death. Tissue engineering is a strategy to improve donor cell survival by providing structural and adhesive support. However, optimization prior to clinical implementation requires expensive and time-consuming in vivo studies. Accordingly, we have developed a three-dimensional (3-D) in vitro model of the injured host-transplant interface that can be used as a test bed for high-throughput evaluation of tissue-engineered strategies. The neuronal-astrocytic cocultures in 3-D were subjected to mechanical loading (inducing cell death and specific astrogliotic alterations) or to treatment with transforming growth factor-beta1 (TGF-beta1), inducing astrogliosis without affecting viability. Neural stem cells (NSCs) were then delivered to the cocultures. A sharp increase in the number of TUNEL(+) donor cells was observed in the injured cocultures compared to that in the TGF-beta1-treated and control cocultures, suggesting that factors related to mechanical injury, but not strictly astrogliosis, were detrimental to donor cell survival. We then utilized the mechanically injured cocultures to evaluate a methylcellulose-laminin (MC-LN) scaffold designed to reduce apoptosis. When NSCs were co-delivered with MC alone or MC-LN to the injured cocultures, the number of caspase(+) donor cells significantly decreased compared to that with vehicle delivery (medium). Collectively, these results demonstrate the utility of an in vitro model as a pre-animal test bed and support further investigation of a tissue-engineering approach for chaperoned NSC delivery targeted to improve donor cell survival in neural transplantation.
Induction of TNBS Colitis in Mice (2002)

The animal model described in this unit is one of several that have been used to study the immunopathogenesis of inflammatory bowel disease. The model employs the use of 2,4,6-trinitrobenzenesulfonic acid (TNBS), which induces severe colonic inflammation when administered intrarectally in SJL/J mice. The colitis which results from this procedure presents clinical and histopathological findings that resemble those seen in Crohn's disease. The unit describes the critical parameters needed for successful induction of TNBS-colitis as well methods for monitoring and grading disease levels. A support protocol for isolating lamina propria mononuclear cells from mouse colons is also included.
Femtosecond laser for black silicon and photovoltaic cells (2008)

We have prepared absorbing structures for photovoltaic cells with different nano-texturization, obtained by means of a femtosecond laser, without the use of corrosive gas (i.e. under vacuum). To take in account the 3D structured front surface, the emitter doping has been realized by using Plasma Immersion Ion Implantation (so-called PULSION). The results show a photocurrent increase up to 60 % in the laser texturized zones.
Compartmentalization of Cardiac β-Adrenergic Inotropy Modulation by Phosphodiesterase Type 5 (2007)

Regulation of cardiac beta-adrenergic response by cGMP is specifically linked to a nitric oxide-synthesis/PDE-5-hydrolyzed pool signaling via protein kinase G. Natriuretic peptide stimulation achieves greater detectable increases in cGMP but not protein kinase G activity and does not modulate beta-adrenergic response. Such disparities likely contribute to differential cardiac regulation by drugs that modulate cGMP synthesis and hydrolysis.
Cell biology of arterial proteoglycans. (1989)

Although proteoglycans constitute a minor component of vascular tissue, these molecules have been shown to influence a number of arterial properties such as viscoelasticity, permeability, lipid metabolism, hemostasis, and thrombosis. A hallmark of early and late atherosclerosis is the accumulation of proteoglycans in the intimal lesions. Yet, it is not clear why this accumulation occurs. This article reviews the classes of proteoglycans synthesized by the two major cell types of the arterial wall--the endothelial and smooth muscle cell. Detailed consideration is then given to the modulation of proteoglycan metabolism and the role that proteoglycans play in a number of cellular events such as adhesion, migration, and proliferation--important processes in both the development and the pathogenesis of blood vessels. Last, the involvement of proteoglycans in two critical vascular wall processes--hemostasis and lipid metabolism--is reviewed, because these events pertain to atherogenesis. This review emphasizes the importance of proteoglycans in regulating several key events in normal and pathophysiological processes in the vascular tissue.
Transcription by T7 RNA polymerase using benzo[a]pyrene-modified templates (1991)

Synthesis of T7 RNA polymerase is inhibited by the presence of bulky adducts in the DNA template. Of the types of adducts tested, those formed by the potent carcinogen benzo[a]pyrene (B[a]P) caused the greatest inhibition. M13 DNA molecules containing a single late T7 RNA polymerase promoter have been prepared containing B[a]P adducts in either the displaced or template strand and these have been used as templates for in vitro RNA transcription by the T7 RNA polymerase. We find that the level of inhibition of RNA synthesis is substantially greater (≥10-fold) when adducts are positioned specifically in the template strand. Polyacrylamide gel analysis of the products synthesized off these strand-specifically modified templates showed that adducts situated in the template strand gave rise to discrete bands which presumably represent the termination of synthesis at the adduct site while the product derived from a template containing adducts in the displaced resembled that obtained using a native template.