gebhart/patrepeval huggingface dataset:
Abp1p and cortactin, new “hand-holds” for actin (2001)

Recently, two new ligands of the Arp2/3 complex have been described that may shed light on the way cells organize complex networks of actin in response to signals. Abp1p, a yeast protein involved in endocytosis, and cortactin, a mammalian src substrate, both enhance the ability of the Arp2/3 complex to assemble branched actin filament networks.
Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release (2010)

The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A(2) IIA and have potential in liposomal drug delivery targeting tumors. We have synthesized four different retinoid phospholipid prodrugs and shown that they form particles in the liposome size region with average diameters of 94-118 nm. Upon subjection to phospholipase A(2), the lipid prodrugs were hydrolyzed, releasing cytotoxic retinoids and lysolipids. The formulated lipid prodrugs displayed IC(50) values in the range of 3-19 microM toward HT-29 and Colo205 colon cancer cells in the presence of phospholipase A(2), while no significant cell death was observed in the absence of the enzyme.
A small‐scale open‐label study of the treatment of canine flea allergy dermatitis with fluralaner (2015)

A single administration of fluralaner alleviated or resolved signs associated with FAD in all treated dogs over the recommended 12-week treatment period.
4-bit rapid single-flux-quantum decoder (1995)

We describe the design of a fast single-flux-quantum decoder which can be used, e.g., in fast RAMs, general-purpose microprocessors, and communication channel switches. The core of the circuit is a tree of the single-bit SFQ demultiplexer with toggle (rather than the reset-set) control. Three new RSFQ cells: the demultiplexer, D flip-flop with complementary outputs, and serial XOR with large parameter tolerances (dc bias margins of /spl plusmn/25%, /spl plusmn/26%, and /spl plusmn/27%, respectively) have been developed for the decoder project. We have designed the first 16-bit prototype of the decoder for 1-kA/cm/sup 2/ niobium-trilayer technology and tested it at low frequencies. The circuit was completely operable except for 3 (of 16) output SFQ/DC converters. Simulations show that the circuit should allow data rate in excess of 60 Gbit/s and channel switching time below 20 ps.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Modification of Hematopoietic Stem/Progenitor Cells with CD19-Specific Chimeric Antigen Receptors as a Novel Approach for Cancer Immunotherapy (2013)

Chimeric antigen receptors (CARs) against CD19 have been shown to direct T-cells to specifically target B-lineage malignant cells in animal models and clinical trials, with efficient tumor cell lysis. However, in some cases, there has been insufficient persistence of effector cells, limiting clinical efficacy. We propose gene transfer to hematopoietic stem/progenitor cells (HSPC) as a novel approach to deliver the CD19-specific CAR, with potential for ensuring persistent production of effector cells of multiple lineages targeting B-lineage malignant cells. Assessments were performed using in vitro myeloid or natural killer (NK) cell differentiation of human HSPCs transduced with lentiviral vectors carrying first and second generations of CD19-specific CAR. Gene transfer did not impair hematopoietic differentiation and cell proliferation when transduced at 1-2 copies/cell. CAR-bearing myeloid and NK cells specifically lysed CD19-positive cells, with second-generation CAR including CD28 domains being more efficient in NK cells. Our results provide evidence for the feasibility and efficacy of the modification of HSPC with CAR as a strategy for generating multiple lineages of effector cells for immunotherapy against B-lineage malignancies to augment graft-versus-leukemia activity.
Smooth muscle cell-derived carbon monoxide is a regulator of vascular cGMP. (1995)

Carbon monoxide (CO) is a product of the enzyme heme oxygenase (HO; EC 1.14.99.3). In vascular smooth muscle cells, exogenously administered CO increases cyclic guanosine 3',5'-monophosphate (cGMP), which is an important regulator of vessel tone. We report here that smooth muscle cells produce CO via HO and that it regulates cGMP levels in these cells. Hypoxia, which has profound effects on vessel tone, significantly increased the transcriptional rate of the HO-1 gene resulting in corresponding increases of its mRNA and HO enzymatic activity. In addition, under the same conditions, rat aortic and pulmonary artery smooth muscle cells accumulated high levels of cGMP following a similar time course to that of HO-1 production. The increased accumulation of cGMP in smooth muscle cells required the enzymatic activity of HO, since it was abolished by a specific HO inhibitor, tin protoporphyrin. In contrast, N omega-nitro-L-arginine, a potent inhibitor of nitric oxide (NO) synthesis, had no effect on cGMP produced by smooth muscle cells, indicating that NO is not responsible for the activation of guanylyl cyclase in this setting. Furthermore, conditioned medium from hypoxic smooth muscle cells stimulated cGMP production in recipient cells and this stimulation was completely inhibited by tin protoporphyrin or hemoglobin, an inhibitor of CO production and a scavenger of CO, respectively. This report shows that HO-1 is expressed by vascular smooth muscle cells and that its product, CO, may regulate vascular tone under physiologic and pathophysiologic (such as hypoxic) conditions.
Serum Thyrotropin (TSH) Levels after Thyroid Ablation Compared with TSH Levels after Exogenous Bovine TSH: Implications for131I Treatment of Thyroid Carcinoma (1972)

In a group of ten patients who had undergone thyroid ablation for thyroid carcinoma, serum endogenous TSH was measured after withdrawal of triiodothyronine treatment. Serum TSH levels rose progressively during the 10–20 days of observation. Only two patients reached a plateau in their TSH level 10 and 15 days after withdrawal. Another group of ten subjects (5 euthyroid, 5 hypothyroid) were given 10 U bovine thyrotropin im on 3 successive days. Bovine TSH levels in their serum measured in a specific radioimmunoassay reached a peak of approximately 100–120 μU/ml in 2–4 hr and declined about 50% at 8–10 hr. Successive injections did not have an additive effect on the level achieved. Assuming the units of human and bovine TSH have an equivalent effect in man, the sustained elevated levels reached 2–3 weeks after withdrawal of triiodothyronine probably cause as much stimulation of residual functional thyroid tissue as does administration of bovine thyrotropin.
Quinone Imides. XXXIX. Adducts of Quinone Monoimides and Conversion of Active Methylene Adducts to Benzofurans (1956)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTQuinone Imides. XXXIX. Adducts of Quinone Monoimides and Conversion of Active Methylene Adducts to BenzofuransRoger Adams and Leroy WhitakerCite this: J. Am. Chem. Soc. 1956, 78, 3, 658–663Publication Date (Print):February 1, 1956Publication History Published online1 May 2002Published inissue 1 February 1956https://pubs.acs.org/doi/10.1021/ja01584a037https://doi.org/10.1021/ja01584a037research-articleACS PublicationsRequest reuse permissionsArticle Views361Altmetric-Citations38LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Reassessing the Role of APOBEC3G in Human Immunodeficiency Virus Type 1 Infection of Quiescent CD4+ T-Cells (2009)

HIV-1 is restricted for infection of primary quiescent T-cells. After viral entry, reverse transcription is initiated but is not completed. Various hypotheses have been proposed for this cellular restriction including insufficient nucleotide pools and cellular factors, but none have been confirmed as the primary mechanism for restriction. A recent study by Chiu et al. implicates APOBEC3G, an anti-retroviral cytidine deaminase, as the cellular restriction factor. Here, we attempted to confirm these findings using the same strategy as reported by Chiu et al. of siRNA targeting knock-down of APOBEC3G expression. In contrast to the published study, our results do not support a role for APOBEC3G in restriction of HIV-1 in quiescent CD4+ T-cells. In our study, we tested the same siRNA as reported by Chiu et al. as well as two additional siRNAs targeting APOBEC3G, one of which showed 2-fold greater knock-down of APOBEC3G mRNA. However, none of the three siRNAs tested had a discernable effect on enhancing infection by HIV-1 in quiescent CD4+ T-cells. Therefore, we conclude that the primary mechanism of HIV-1 restriction in quiescent CD4+ T-cells remains to be elucidated.
Computer Assisted Interventionist Imaging: Application To The Vertebral Column Surgery (2005)

Included into a Computer Assisted Medical Interventionist program (6),(7), this paper presents a matching-based method that allows to reproduce in real conditions a positioning act previously simulated on a 3D modelling of medical images. A matching procedure is achieved by interactively comparing an on-line video image of the real world with a simulated video image, synthesized from the 3D modelling through the knowledge of geometrical camera parameters. The rigid coupling between the video camera and a physical guide performs by itself the desired positioning. The clinical application that we envisage is the vertebral column surgery.
Human telomeric sequence forms a hybrid-type intramolecular G-quadruplex structure with mixed parallel/antiparallel strands in potassium solution (2006)

Human telomeric DNA consists of tandem repeats of the sequence d(TTAGGG). The formation and stabilization of DNA G-quadruplexes in the human telomeric sequence have been shown to inhibit the activity of telomerase, thus the telomeric DNA G-quadruplex has been considered as an attractive target for cancer therapeutic intervention. However, knowledge of the intact human telomeric G-quadruplex structure(s) formed under physiological conditions is a prerequisite for structure-based rational drug design. Here we report the folding structure of the human telomeric sequence in K+ solution determined by NMR. Our results demonstrate a novel, unprecedented intramolecular G-quadruplex folding topology with hybrid-type mixed parallel/antiparallel G-strands. This telomeric G-quadruplex structure contains three G-tetrads with mixed G-arrangements, which are connected consecutively with a double-chain-reversal side loop and two lateral loops, each consisting of three nucleotides TTA. This intramolecular hybrid-type telomeric G-quadruplex structure formed in K+ solution is distinct from those reported on the 22 nt Tel22 in Na+ solution and in crystalline state in the presence of K+, and appears to be the predominant conformation for the extended 26 nt telomeric sequence Tel26 in the presence of K+, regardless of the presence or absence of Na+. Furthermore, the addition of K+ readily converts the Na+-form conformation to the K+-form hybrid-type G-quadruplex. Our results explain all the reported experimental data on the human telomeric G-quadruplexes formed in the presence of K+, and provide important insights for understanding the polymorphism and interconversion of various G-quadruplex structures formed within the human telomeric sequence, as well as the effects of sequence and cations. This hybrid-type G-quadruplex topology suggests a straightforward pathway for the secondary structure formation with effective packing within the extended human telomeric DNA. The hybrid-type telomeric G-quadruplex is most likely to be of pharmacological relevance, and the distinct folding topology of this G-quadruplex suggests that it can be specifically targeted by G-quadruplex interactive small molecule drugs.
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgesics (1991)

In an effort to discover a potent ultrashort-acting mu opioid analgetic that is capable of metabolizing to an inactive species independent of hepatic function, several classes of 4-anilidopiperidine analgetics were synthesized and evaluated. One series of compounds displayed potent mu opioid agonist activity with a high degree of analgesic efficacy and an ultrashort to long duration of action. These analgetics, 4-(methoxycarbonyl)-4-[(1-oxopropyl)phenylamino]-1-piperidinepropanoi c acid alkyl esters, were evaluated in vitro in the guinea pig ileum for mu opioid activity, in vivo in the rat tail withdrawal assay for analgesic efficacy and duration of action, and in vitro in human whole blood for their ability to be metabolized in blood. Compounds in this series were all shown to be potent mu agonists in vitro, but depending upon the alkyl ester substitution the potency and duration of action in vivo varied substantially. The discrepancies between the in vitro and in vivo activities and variations in duration of action are probably due to different rates of ester hydrolysis by blood esterase(s). The SAR with respect to analgesic activity and duration of action as a function of the various esters synthesized is discussed. It was also demonstrated that the duration of action for the ultrashort-acting analgetic, 8, does not change upon prolonged infusion or administration of multiple bolus injections.
Targeted Gene Silencing by Small Interfering RNA-Based Knock-Down Technology (2004)

RNA interference (RNAi) has emerged as a powerful tool for the silencing of gene expression in animals and plants. RNAi is mediated by approximately 21-nt small interfering RNAs (siRNAs), which are originally produced from larger double stranded RNAs (dsRNAs) in vivo through the action of Dicer. Recently, many groups have reported systems designed to express siRNAs in mammalian cells through transfection of either oligonucleotides or plasmids encoding siRNAs. Although the use of siRNAs to silence genes in vertebrate cells was only reported three years ago, the emerging literature indicates that most vertebrate genes can be studied with this technology. This review summarizes some approaches to generate siRNAs, the delivery and application of siRNAs to target cells and the utility of siRNAs as analytical and potential therapeutic tools.
ChemInform Abstract: Inhibition of the EGF‐Stimulated Cellular Proliferation of ER 22 Cells by Hydroxybiphenyl Derivatives. (1996)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Transposon-Based Strategies for Microbial Functional Genomics and Proteomics (2003)

Transposons are mobile genetic elements that can relocate from one genomic location to another. As well as modulating gene expression and contributing to genome plasticity and evolution, transposons are remarkably diverse molecular tools for both whole-genome and single-gene studies in bacteria, yeast, and other microorganisms. Efficient but simple in vitro transposition reactions now allow the mutational analysis of previously recalcitrant microorganisms. Transposon-based signature-tagged mutagenesis and genetic footprinting strategies have pinpointed essential genes and genes that are crucial for the infectivity of a variety of human and other pathogens. Individual proteins and protein complexes can be dissected by transposon-mediated scanning linker mutagenesis. These and other transposon-based approaches have reaffirmed the usefulness of these elements as simple yet highly effective mutagens for both functional genomic and proteomic studies of microorganisms.
Prostheses for Primary Total Hip Replacement:A Critical Appraisal of the Literature (1995)

Eighty-one published papers on the performance of prostheses in total hip replacement were appraised. Sound methodology was demonstrated in 1 of 8 randomized controlled trials and 4 of 17 nonrandomized comparative studies. Of 56 case series without controls, 32 met the appraisal criteria, but these are intrinsically less useful. The published literature does not provide solid evidence for the superiority of cement-free or hybrid prostheses over modern cemented types.
Toxoid of Clostridium botulinum type F: purification and immunogenicity studies (1976)

Toxin from Clostridium botulinum type F was recovered from dialysis cultures and partially purifed by: (i) ammonium sulfate and ethanol precipitation; (ii) O-(diethylaminoethyl)-cellulose chromatography; or (iii) diethylaminoethyl-cellulose chromatography followed by O-(carboxymethyl)-cellulose chromatography. Toxin purities as reflected by specific activity were 1.83 X 10(6), 9.8 X 10(6), and 2.0 X 10(7) mouse 50% lethal doses (LD50)/mg of N, respectively, for toxins purified by the three methods. The toxins were converted to toxoids by incubation at 35 C in the presence of 0.3 to 0.45% formalin for 21 to 35 days. Toxoids were immunogenic in guinea pigs, as demonstrated by serum antitoxin response and the immunized animals' resistance to challenge by type F botulinal toxin. The immune response to type F toxoids was lower when toxoids of serotypes A, B, C, D, and E were combined with the type F toxoid than when the type F toxoid only was administered. The toxoid prepared from the most highly purified toxin (method [iii]) conferred the highest immunity in guinea pigs at a given dose level. A relation between serum antitoxin level and resistance to challenge was observed. At least 50% of the groups of guinea pigs with 0.015 antitoxin units or more per ml survived challenge by 10(5) mouse LD50 of type F botulinal toxin. A dose of 3.75 mug of N of the most highly purified type F toxoid in combination with the other five serotypes of botulinal toxoid invoked an immune response in guinea pigs comparable to that considered adequate for the other toxoids.
Biomarker discovery and development in pediatric critical care medicine* (2010)

Biomarker discovery and development are an important portion of the pediatric critical care medicine translational research agenda. This effort will require collaboration across multiple institutions and investigators. Rigorous conduct of biomarker-focused research holds the promise of transforming our ability to care for individual patients and our ability to conduct clinical trials in a more effective manner.
The Surface Area of the Adult Human Mouth and Thickness of the Salivary Film Covering the Teeth and Oral Mucosa (1987)

The surface area of the mouth was measured to calculate the average thickness of the salivary film which separates the opposing layers of the oral mucosa and which also overlies the dental plaque. The subjects were 10 adults of each sex, all of whom had essentially a full complement of teeth. Impressions were taken of the upper and lower jaws, the buccal and labial vestibular mucosa, and the ventral surface of the tongue, and stone models were cast. The dorsum of the tongue was assumed to have the same area as the palate plus that of the palatal surfaces of the upper teeth. The six separate areas considered were the teeth, the palate, the buccal and lingual gingival and alveolar mucosa, the buccal and labial vestibular mucosa, the ventral surface of the tongue, including the floor of the mouth, and the dorsum of the tongue. Aluminum foil, of known weight per unit area, was adapted to the models of the different regions of the mouth, and the surface areas were calculated from the weights of the foil. The mean total surface area of the mouth was 214.7 +/- 12.9 cm2, and there was no significant difference due to gender. The teeth, keratinized epithelium, and non-keratinized epithelium occupied about 20%, 50%, and 30% of the total surface area, respectively. Given that the average volumes of saliva present in the mouth before and after swallowing have been estimated to be 0.77 and 1.07 mL, respectively, it can be calculated that the average thickness of the salivary film in the mouth varies between 0.07 and 0.10 mm.(ABSTRACT TRUNCATED AT 250 WORDS)
InAs self-assembled nanostructures grown on InP(001) (2000)

The 6-period stacked layers of self-assembled InAs quasi-quantum wires(qQWRs) and quantum dots(QDs) embedded into InAlAs on InP(001) substrates have been prepared by solid molecular beam epitaxy. The structures are characterized by atomic force microscopy(AFM) and transmission electron microscopy(TEM). From AFM we have observed for the first time that InAs qQWRs and QDs coexist, and we explained this phenomenon from the view of the energy related to the islands. Cross-sectional TEM shows that InAs qQWRs are vertically aligned every other layer along the growth direction [001], which disagrees with conventional vertical self-alignment of InAs QDs on GaAs substrate.
6-Alkylamino- and 2,3-Dihydro-3‘-methoxy-2-phenyl-4-quinazolinones and Related Compounds:  Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization (2000)

As part of our continuing search for potential anticancer candidates among 2-phenyl-4-quinolones and 2-phenyl-4-quinazolinones, two series of 6,7,2',3',4',5'-substituted 2-phenyl-4-quinazolinones and 6,2',3',4',5'-substituted 2,3-dihydro-2-phenyl-4-quinazolinones were synthesized and evaluated for cytotoxicity and as inhibitors of tubulin polymerization. In general, a good correlation was found between the two activities. Five of the 6-substituted heterocyclic 2-phenyl-4-quinozolinones (37-51) showed significant cytotoxicity against a panel of human tumor cell lines with EC(50) values in the low micromolar to nanomolar concentration ranges. Compound 38 was the most potent of these compounds, as well as the most potent inhibitor of tubulin polymerization in this series. The activity of 38 was in the same range as those of the antimitotic natural products, colchicine, podophyllotoxin, and combretastatin A-4. Substituted 2-phenyl-4-quinazolinones and 2, 3-dihydro-2-phenyl-4-quinazolinones also displayed highly selective cytotoxicity against the ovarian cancer 1A9 and P-gp resistant KB-VIN cell lines.