gebhart/patrepeval huggingface dataset:
Development of Potent Pyrazolopyrimidinone‐Based WEE1 Inhibitors with Limited Single‐Agent Cytotoxicity for Cancer Therapy (2018)

WEE1 kinase regulates the G<sub>2</sub> /M cell-cycle checkpoint, a critical mechanism for DNA repair in cancer cells that can confer resistance to DNA-damaging agents. We previously reported a series of pyrazolopyrimidinones based on AZD1775, a known WEE1 inhibitor, as an initial investigation into the structural requirements for WEE1 inhibition. Our lead inhibitor demonstrated WEE1 inhibition in the same nanomolar range as AZD1775, and potentiated the effects of cisplatin in medulloblastoma cells, but had reduced single-agent cytotoxicity. These results prompted the development of a more comprehensive series of WEE1 inhibitors. Herein we report a series of pyrazolopyrimidinones and identify a more potent WEE1 inhibitor than AZD1775 and additional compounds that demonstrate that WEE1 inhibition can be achieved with reduced single-agent cytotoxicity. These studies support that WEE1 inhibition can be uncoupled from the potent cytotoxic effects observed with AZD1775, and this may have important ramifications in the clinical setting where WEE1 inhibitors are used as chemosensitizers for DNA-targeted chemotherapy.
스토리텔링을 활용한 네일아트 디자인 연구 - 작품제작을 중심으로 (2013)

본 연구에서는 우리나라 조선설화집 에 나오는 해와 달과 별의 스토리를 가지고 중심 어를 도출하여 색 채이미지와 단어 연상이미지를 바탕으로 스케치에서부터 디자인 도출과정을 디자인 프로세스의 형식으 로 스토리텔링을 활용한 네일아트 디자인 발상에 창의적인 작품제작 과정을 연구하였다. 그 결과는 다 음과 같다. 첫째, 거짓말에서 연상되는 단어로 새빨간 거짓말, 피노키오, 가면, 양치기 소년등과 같은 단어들 중 거 짓말의 두 얼굴을 가면으로 표현하였다. 베네치아 가면과 중국경극의 가면 등의 이미지를 디자인의 요소로 스케치하여 주제어에서 연상되는 거 짓말을 색채이미지 표에서 남을 속이려는 동적인 느낌의 화려함으로 선정하여 빨강, 파랑, 초록의 색의 보색과 반대색 관계의 화려함 속에 약간의 탁한 색채로 거짓말의 이면에 담긴 탁한 요소를 표현하였다. 둘째, 공포와 두려움의 연상단어로 흑조, 해골, 악마. 뭉크-절규의 이미지를 디자인의 요소로 공포에 동 공이 확대된, 손으로 눈을 가리고 싶은 마음을 스케치하여 색채이미지 표의 동적이고 경직된 딱딱함이 느껴지는 어두운 다크 톤과 다크 그레이 톤의 빨강, 파랑, 보라, 노란 색을 사용하여 두려움을 표현하였 다. 셋째, 탈출의 연상단어를 사다리, 비상구, 감옥, 쇠창살 의 디자인요소를 쇠창살을 붙잡고 있는 죄수의 이미지를 스케치하여 색채이미지 표에 동적임과 탈출의 의지를 기본 톤의 파란색을 주조 색으로 하고 하얀색을 써서 명도차를 크게 하여 탈출하고픈 강한 마음을 표현하였다. 넷째, 기도의 연상단어인 아맨, 십자가, 합장, 성경책을 디자인의 요소로 기도할 때 손을 모으는 합장의 이미지를 스케치 하여 색채이미지 표에서 기도의 느낌을 정적이고 간절함의 시간이 길게 느껴짐을 회색 으로 정하고 명도차를 두어 간절함을 표현 하였다. 다섯째, 영생, 구원의 연상단어로 천국, 무지개, 에덴동산, 성배(Holy Grail)의 디자인 요소로 천국으로 가 는 계단과 영원의 삶을 의미하는 성배를 함께 스케치에 표현하고 색채이미지 표 에서 동적인 느낌과 하 늘로 올라가는 가벼움의 채도를 사용하여 라이트 톤의 빨강 , 오렌지, 노랑, 초록, 연두, 파랑 색을 사용 하여 행복한 영원의 삶을 표현하고자 하였다. 이렇듯 스토리텔링의 구성 요소를 조선설화집 속 한편인 해와 달과 별의 이야기를 통해 주관적인 사고 의 디자인을 본 연구자는 아크릴 물감으로 평면아트 기법을 사용하였으나 다양한 기법을 활용하여 더욱 창의적이고 상상력의 예술적인 작품시도를 통한 연구가 필요하다고 사료된다.
Modeling Hydroxyl Radical Distribution and Trialkyl Phosphates Oxidation in UV−H<sub>2</sub>O<sub>2</sub> Photoreactors Using Computational Fluid Dynamics (2010)

Advanced Oxidation Processes (AOPs) promoted by ultraviolet light are innovative and potentially cost-effective solutions for treating persistent pollutants recalcitrant to conventional water and wastewater treatment. While several studies have been performed during the past decade to improve the fundamental understanding of the UV-H(2)O(2) AOP and its kinetic modeling, Computational Fluid Dynamics (CFD) has only recently emerged as a powerful tool that allows a deeper understanding of complex photochemical processes in environmental and reactor engineering applications. In this paper, a comprehensive kinetic model of UV-H(2)O(2) AOP was coupled with the Reynolds averaged Navier-Stokes (RANS) equations using CFD to predict the oxidation of tributyl phosphate (TBP) and tri(2-chloroethtyl) phosphate (TCEP) in two different photoreactors: a parallel- and a cross-flow UV device employing a UV lamp emitting primarily 253.7 nm radiation. CFD simulations, obtained for both turbulent and laminar flow regimes and compared with experimental data over a wide range of UV doses, enabled the spatial visualization of hydrogen peroxide and hydroxyl radical distributions in the photoreactor. The annular photoreactor displayed consistently better oxidation performance than the cross-flow system due to the absence of recirculation zones, as confirmed by the hydroxyl radical dose distributions. Notably, such discrepancy was found to be strongly dependent on and directly correlated with the hydroxyl radical rate constant becoming relevant for conditions approaching diffusion-controlled reaction regimes (k(C,OH) > 10(9) M(-1) s(-1)).
Bacillary angiomatosis in patients with AIDS: multiorgan imaging findings. (1995)

Bacillary angiomatosis, a treatable infection, should be considered in patients with AIDS, particularly when Kaposi sarcoma is suspected clinically.
BrailleTouch (2011)

Texting is the essence of mobile communication and connectivity, as evidenced by today's teenagers, tomorrow's workforce. Fifty-four percent of American teens contact each other daily by texting, as compared to face-to-face (33%) and talking on the phone (30%) according to the Pew Research Center's Internet & American Life Project, 2010. Arguably, today's technologies support mobile text input poorly, primarily due to the size constraints of mobile devices. This is the case for everyone, but it is particularly relevant to the visually impaired. According to the World Health Organization, 284 million people are visually impaired worldwide. In order to connect these users to the global mobile community, we need to design effective and efficient methods for eyes-free text input on mobile devices. Furthermore, everyone would benefit from effective mobile texting for safety and speed. This design brief presents BrailleTouch, our working prototype solution for eyes-free mobile text input.
Erratum: “Vertical channel all-organic thin-film transistors” [Appl. Phys. Lett. <b>82</b>, 4579 (2003)] (2003)

First Page
Design and Synthesis of Novel Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors Bearing a Pyrrolo[3,2-<i>d</i>]pyrimidine Scaffold (2011)

Dual inhibitors of human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the receptors' ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
Binding of purified<i>Escherichia coli</i>O75X adhesin to frozen sections of human kidney (1986)

Binding characteristics of the purified Escherichia coli O75X adhesin in frozen sections of human kidney were determined, using antibodies raised against the purified antigen and rhodamine-conjugated second antibodies. To identify the adhesin-binding nephron domains, the same tissue sections were double stained with fluorescein isothiocynate-conjugated nephron site-specific lectins. The results revealed that, at the tubular pole, the O75X adhesin bound selectively to the basement membrane of proximal and distal tubules and, with a slightly lower efficiency, of collecting ducts. In the glomerulus, the O75X adhesin bound only to the parietal epithelial cells (Bowman's capsule). The purified O75X adhesin bound also to exfoliated epithelial cells in human urine. Our results suggest that the O75X adhesin may contribute to the uropathogenicity of E. coli by binding the bacteria to tissue structures in the human urinary tract.
Bandera: extracting finite-state models from Java source code (2002)

Finite-state verification techniques, such as model checking, have shown promise as a cost-effective means for finding defects in hardware designs. To date, the application of these techniques to software has been hindered by several obstacles. Chief among these is the problem of constructing a finite-state model that approximates the executable behavior of the software system of interest. Current best-practice involves hand-construction of models which is expensive (prohibitive for all but the smallest systems), prone to errors (which can result in misleading verification results), and difficult to optimize (which is necessary to combat the exponential complexity of verification algorithms).
Distance Dependent Scoring Function for Describing Protein−Ligand Intermolecular Interactions (2008)

A new empirical scoring function has been developed to estimate the binding affinity of a protein-ligand complex with known three-dimensional structure. The scoring function includes a small number of physicochemical descriptors and a large number of quasi-fragmental descriptors. The first group of descriptors is chosen from the following set: (1) the number of close nonbonded contacts, (2) a score for 'metal-atom' interactions, (3) the number of flexible bonds, (4) van der Waals interaction energy, and (5) electrostatic interaction energy. A training set of 288 'protein-ligand' complexes was used to develop the scoring function. The key benefit of this approach is that it reduces the computational complexity while maintaining similar predictive ability to existing methods (average for independent test sets is 2-2.2 kcal/mol). The quasi-fragmental descriptors provide a unique and novel way of accurately representing physical interactions, compared to using physicochemical ones alone.
Introduction (1984)

Conference Article| February 01 1984 Introduction BRIAN BURCHELL; BRIAN BURCHELL 1Departments of Biochemistry and Pharmacology, University of Dundee, Dundee DD1 4HN, Scotland, U.K. Search for other works by this author on: This Site PubMed Google Scholar IAN STEVENSON IAN STEVENSON 1Departments of Biochemistry and Pharmacology, University of Dundee, Dundee DD1 4HN, Scotland, U.K. Search for other works by this author on: This Site PubMed Google Scholar Biochem Soc Trans (1984) 12 (1): 1. https://doi.org/10.1042/bst0120001a Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Share Icon Share Twitter LinkedIn Cite Icon Cite Get Permissions Citation BRIAN BURCHELL, IAN STEVENSON; Introduction. Biochem Soc Trans 1 February 1984; 12 (1): 1. doi: https://doi.org/10.1042/bst0120001a Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search nav search search input Search input auto suggest search filter All ContentAll JournalsBiochemical Society Transactions Search Advanced Search This content is only available as a PDF. © 1984 Biochemical Society1984 Article PDF first page preview Close Modal You do not currently have access to this content.
172. o-Amino-ketones of the acetophenone and benzophenone types (1945)

J. C. E. Simpson, C. M. Atkinson, K. Schofield and O. Stephenson, J. Chem. Soc., 1945, 646 DOI: 10.1039/JR9450000646
Metal nanoparticle arrays for near-field optical lithography (2002)

We have recently proposed a new approach to optical lithography that could be used to replicate arrays of metal nanoparticles using broad beam illumination with visible light and standard photoresist. The method relies on resonant excitation of the surface plasmon oscillation in the nanoparticles. When excited at the surface plasmon frequency, a resonantly enhanced dipole field builds up around the nanoparticles. This dipole field is used to locally expose a thin layer of photoresist, generating a replica of the original pattern in the resist. Silver nanoparticles on photoresist can be resonantly excited at wavelengths ranging from 410 nm to 460 nm, allowing for resonantly enhanced exposure of standard g-line photoresist. Finite Difference Time Domain (FDTD) simulations of isolated silver particles on a thin resist layer show that broad beam illumination with p-polarized light at a wavelength of 439 nm can produce features as small as 30 nm, or λ/14. Depending on exposure time lateral spot sizes ranging from 30 to 80 nm with exposure depths ranging from 12 to 45 nm can be achieved. We discuss the effect of particle-particle interactions in the replica formation process. Experiments on low areal density Ag nanoparticle arrays are discussed. Resist layers (thickness 75 nm) in contact with 40 nm Ag nanoparticles were exposed using 410 nm light and were subsequently developed. Atomic Force Microscopy on these samples reveals nanoscale depressions in the resist, providing evidence for plasmon-enhanced resist exposure.
Conceptual design of a virtual library for personal use (1999)

This paper proposes a concept of the Yawara personalized virtual library and its prototype design. The main purpose of the library is to provide a user with a personalized information set accessible through a user-friendly interface. In order to attain machine and operating system independence, the library is constructed by VRML and its WWW browsers and, as information sources, HTML data widely distributed on the Internet. The virtual librarian agent helps to find and acquire the data sets based on user behavior. The virtual librarian keeps the user's personal characteristics, obtained from his/her reading history, and book characteristics. As the user working space, personal bookshelves are provided to work with the stored books. The system will be a powerful tool for intelligent work fully utilizing the Internet. © 1999 Scripta Technica, Syst Comp Jpn, 30(3): 43–51, 1999
Built-Up Films of Barium Stearate and Their Optical Properties (1937)

The technique of depositing successive single layers of molecules of various stearates on a solid surface is described. Films containing 3001 layers have been built of barium-copper stearate. A photograph shows films built in a series of steps having intervals of 2 molecular layers. The contrast of the steps is plainly visible when the slide is illuminated by polarized light at angles near grazing incidence. By measuring the angles at which films containing known numbers of layers reflect minimum intensity of monochromatic light for the first five interference fringes, the thickness per layer and refractive index can be calculated with great accuracy. The thickness per layer of barium stearate was found to be 24.40A. The presence of traces of foreign substances in the water affect the spacing by 1 to 3 percent. The films are uniaxial crystals, the optic axis being perpendicular to the surface on which the films are built. The refractive index of the ordinary ray, ${n}_{1}$, and of the extraordinary ray in a direction perpendicular to the axis, ${n}_{3}$, are ${n}_{1}=1.491$, ${n}_{3}=1.551$. Equations are given which describe the refraction of the extraordinary ray, the intensity of the rays reflected from the upper surface and from the film solid boundary, the phase change at the boundaries, Brewster's angle, and other special properties of birefringent films. The intensity of the light and dark fringes reflected by films built on a series of glasses of known refractive indices is used as a measure of ${n}_{1}$. Skeleton films. Barium stearate films built at $\mathrm{pH}<7.0$ are composed of a mixture of stearic acid and neutral stearate. The stearic acid can be dissolved by benzene leaving a skeleton of stearate which is birefringent and has refractive indices much lower than those of the normal film. Measurements are given of a skeleton for which ${n}_{1}=1.30$, others for which ${n}_{1}=1.32$, ${n}_{3}=1.39$. Skeletons have been built having ${n}_{1}=1.25$ and 1.22. The skeleton for which ${n}_{1}=1.30$ had 99.2 percent of the thickness of the original film, although only 63.7 percent of its density.
Virtual reality and computer-enhanced training devices equally improve laparoscopic surgical skill in novices. (2009)

Training on virtual reality and computer-enhanced devices had equivalent effects on skills improvement in novices. Despite the perception that haptic feedback is important in laparoscopic simulation training, its absence in the virtual reality device did not impede acquisition of skill.
Cell Yield, Proliferation, and Postexpansion Differentiation Capacity of Human Ear, Nasal, and Rib Chondrocytes (2004)

Human ear, nasal, and rib chondrocytes were compared with respect to their suitability to generate autologous cartilage grafts for nonarticular reconstructive surgery. Cells were expanded for two passages in medium containing 10% fetal bovine serum without (control) or with transforming growth factor beta(1) (TGF-beta(1)), fibroblast growth factor 2 (FGF-2), and platelet-derived growth factor bb (PDGF-bb) (TFP). Expanded cells were cultured as three-dimensional pellets in chondrogenic serum-free medium containing insulin, dexamethasone, and TGF-beta(1). Chondrocytes from all three sources were successfully isolated, increased their proliferation rate in response to TFP, and dedifferentiated during passaging. Redifferentiation by ear and nasal, but not rib, chondrocytes was enhanced after TFP expansion, as assessed by the significant increase in glycosaminoglycan (GAG)/DNA content and collagen type II mRNA expression in the resulting pellets. TFP-expanded ear and nasal chondrocytes generated pellets of better quality than rib chondrocytes, as assessed by the significantly higher GAG/DNA content and collagen type II mRNA expression, and by the relative stain intensities for GAG and collagen types I and II. In conclusion, postexpansion cell yields suggest that all three sources investigated could be used to generate autologous grafts of clinically relevant size. However, ear and nasal chondrocytes, if expanded with TFP, display superior postexpansion chondrogenic potential and may be a preferred cell source for cartilage tissue engineering.
Deep Learning for Unmanned Aerial Vehicle-Based Object Detection and Tracking: A survey (2021)

Owing to effective and flexible data acquisition, unmanned aerial vehicles (UAVs) have recently become a hotspot across the fields of computer vision (CV) and remote sensing (RS). Inspired by the recent success of deep learning (DL), many advanced object detection and tracking approaches have been widely applied to various UAV-related tasks, such as environmental monitoring, precision agriculture, and traffic management.
The pathogenesis of pulmonary hypertension in haemodialysis patients via arterio-venous access (2005)

This study demonstrates a high prevalence of PHT among patients with ESRD on chronic HD via a surgical A-V fistula. In view of the vasodilatory and antimitogenic properties of NO, it is possible that the attenuated basal and HD-induced NO production in patients with PHT contributes to the increased pulmonary vascular tone. Furthermore, the partial restoration of normal PAP and CO in HD patients that underwent either temporal A-V shunt closure or successful transplantation indicates that excessive pulmonary blood flow is involved in the pathogenesis of the disease.
Fatty acid composition of the living layer and stratum corneum lipids of human sole skin epidermis (1970)

Abstract Lipids from the living layer and stratum corneum of human sole epidermis were extracted, saponified and the fatty acids analyzed. The proportion of fatty acids to unsaponifiables (mainly cholesterol), was higher in the living layer than in the stratum corneum. Fatty acids of the living layer and stratum corneum of human sole epidermis comprise saturates, monoenes, dienes, traces of polyenes and α‐hydroxy fatty acids. Homologs of monoenoic and dienoic fatty acids for both living layer and stratum corneum lipids have a similar distribution. C 16 and C 18 were major components for each type of acids. There appeared to be two clusters, especially for saturates of both living layer and stratum corneum acids. One of these clusters ranged from C 12 to C 20 with C 16 or C 18 as a maximum and the other ranged from C 21 to C 30 with C 24 as a maximum. The proportion of saturated acids with chain length C 20 and above was much higher in the stratum corneum than in the living layer. Position isomers of the monoenoic fatty acids for both the living layer and stratum corneum show a predominance of ω9 acids, due to the overwhelmingly large amount of oleic acid. Linoleic acid was by far the major component of the dienoic acids. Homolog distribution of α‐hydroxy fatty acids for the living layer was similar to that of the stratum corneum and again two clusters of acids below and above C 20 with maxima at C 16 and C 24 were noticeable. Comparison of epidermal acids with those of sebaceous glands showed that each tissue can synthesize the same kind of acids but in widely different amounts. Oxidation of palmitate and stearate could supply the necessary energy for the late stages of keratinization.
Stereocontrolled synthesis of withanolide D and related compounds (1984)

The synthesis of withanolide D, a withanolide having a hydroxy group at the C-20 position, has been accomplished from pregnenolone. The key reactions are based on successful stereochemical control at the C-22 position involving γ-coupling reaction of a lithium enolate with a protected 20-hydroxy-22-aldehyde, and allyl sulphoxide–sulphenate rearrangement of 2,4-dien-1 -one 6β-sulphoxide to introduce the 4β-hydroxy-2,5-dien-1-one system. The related natural withanolides, physalolactone B, deacetyl-physalolactone B, and 3α,20R-dihydroxy-1-oxowitha-5,24-dienolide were also synthesized via a common intermediate for withanolide D.
Band structures of Cu2ZnSnS4 and Cu2ZnSnSe4 from many-body methods (2011)

We calculate the band structures of kesterite and stannite Cu2ZnSnS4 and Cu2ZnSnSe4, using a state-of-the-art self-consistent GW approach. Our accurate quasiparticle states allow to discuss: the dependence of the gap on the anion displacement; the key-role of the nonlocality of the exchange-correlation potential to obtain good structural parameters; the reliability of less expensive hybrid functional and generalized gradient approximation+U approaches. In particular, we show that even if the band gap is correctly reproduced by hybrid functionals, the band-edge corrections are in disagreement with self-consistent GW results, which have decisive implications for the positioning of the defect levels in the band gap.
[Effect of a water-soluble derivative of silymarin on morphological and functional alterations of mouse hepatocytes induced by Frog Virus 3 (author's transl)]. (1979)

Pretreatment of mice with silymarin dihemisuccinate sodium salt (SHS-Na) 300 mg/kg 24 and 16 h before infection completely protected against the lethal effect of Frog Virus 3 (FV3). After the inoculation of 1 LD100 of virus it could be shown that: a) the same amount of radioactively labelled virus was found in the liver of control and SHS-Na treated animals, b) in SHS-Na pretreated animals the shut-off of macromolecular syntheses in the liver was considerably less extensive, c) the histological changes in the hepatocyte nuclei were attenuated in SHS-Na pretreated animals and the serum titer of the transaminases did no increase, d) in SHS-Na pretreated mice there were only limited functional alterations of the sinusoidal cells as studied by carbon phagocytosis and the serum titer of the lysosomal enzymes was only slightly modified, e) inhibition of protein synthesis during the period of pretreatment with SHS-Na did not decrease the level of protection. These results allow us to conclude that SHS-Na exerts its protective effect on the liver and that sinusoidal cells are most likely involved in this protection.