gebhart/patrepeval huggingface dataset:
Prothymosin-alpha mRNA expression correlates with that of c-myc in human colon cancer. (1993)

Prothymosin alpha (PT-alpha) is a nuclear protein involved in cell proliferation. Transcription of PT-alpha has been reported to be regulated by the c-myc gene in vitro. We identified PT-alpha as being overexpressed in a human colon cancer minus normal mucosa subtraction cDNA library. Northern blot (messenger RNA) analysis showed that both PT-alpha and c-myc genes were overexpressed in human colorectal cancers compared with adjacent normal tissues. Immunohistochemical studies for PT-alpha and c-myc supported these findings. There was no correlation between PT-alpha or c-myc messenger RNA expression and Dukes' stage of colorectal cancer; or between either of these two and actin messenger RNA expression. There was, however, a significant correlation between the PT-alpha expression and c-myc expression (P < 0.001). These findings support the hypothesis that PT-alpha gene transcription may be associated with, and possibly under the control of, the c-myc gene in human colorectal cancers.
Total Synthesis of Squamotacin (1999)

The first total synthesis of (+)-squamotacin, 1, which has shown cytotoxic selectivity for the human prostate tumor cell line, was achieved in 27 steps and 0.83% yield starting with (+)-muricatacin, 4. All asymmetric centers in the bistetrahydrofuran fragment of the molecules were produced by the Sharpless asymmetric dihydroxylation (AD) and the asymmetric epoxidation (AE) reactions.
A novel synthesis of 5‐chloro‐3‐methoxycarbonyl‐1‐arylpyrazoles from arylazomethylenetriphenylphosphoranes (1989)

Abstract The reaction of arylazomethoxycarbonylmethylenetriphenylphosphoranes 1 with chloroform and sodium hydroxide in the presence of benzyltriethylammonium chloride (TEBA) as phase transfer catalyst directly affords 5‐chloro‐3‐methoxycarbonyl‐1‐arylpyrazoles 3 .
Lymphatic Vessel Activation in Cancer (2002)

Metastasis of most cancers occurs primarily through the lymphatic system, and the extent of lymph node involvement is the most important prognostic indicator. While the importance of the lymphatic system as a pathway for metastasis has been well recognized, there is very little information available about the mechanisms by which tumor cells interact with the lymphatics. Recently, production of the lymphangiogenic factor VEGF-C has been detected in tumors, and the significance of VEGF-C-mediated lymphangiogenesis for tumor metastasis has been demonstrated. Increased lymphatic vessel density has been found associated with certain tumors. The mechanisms by which tumor cells gain access to and enter lymphatic vessels are critical issues that need to be addressed in the future. In contrast to the prevailing view that has assigned to the lymphatic system a passive role in the metastatic process, our results indicate the importance of lymphatic vessel activation in tumor dissemination.
Antitumor activity of a PKC-alpha antisense oligonucleotide in combination with standard chemotherapeutic agents against various human tumors transplanted into nude mice. (1998)

A 20-mer phosphorothioate oligodeoxynucleotide (ODN) directed against human protein kinase C-alpha (CGP 64128A = ISIS 3521) was analyzed for its antitumor activity either alone or in combination therapy. Combination studies with CGP 64128A and standard chemotherapeutic agents (cisplatin, mitomycin-C, vinblastine, estracyt and adriamycin) were performed in nude mice that had been transplanted s.c. with a variety of human tumors (breast, prostate, large cell lung and small cell lung carcinomas, and melanomas). Additive antitumor effects with CGP 64128A and the cytotoxins were found for half of the combinations studied. The combination of CGP 64128A with vinblastine or cisplatin showed superadditive antitumor activities against MCF-7 human breast carcinomas and PC3 prostate carcinomas with complete responses. CGP 64128A in combination with adriamycin resulted in superadditive antitumor effects against BT20 human breast carcinomas with complete tumor responses, and in combination with mitomycin-C superadditive antitumor effects with cures were observed against NCI-H460 human large cell carcinomas. The antitumor activity of CGP 64128A appeared to be due to a sequence-dependent mechanism of action as two 20-mer control ODNs were completely inactive as single agents against A549 and NCI-H69 human lung carcinomas. The antitumor activity of cisplatin against NCI-H69 human small cell lung carcinomas was slightly inhibited by one of the control ODNs, indicating that the superadditive antitumor activities of CGP 64128A in combination with cisplatin are the result of a sequence-dependent mechanism of action.
Early B cell development requires μ signaling (1993)

In vitro studies with Abelson murine leukemia virus (AMuLV)-transformed murine pre-B cell lines demonstrated that wild-type mu but not mutant mu chains lacking the first constant domain (mu delta 1) can efficiently induce Ig light (L) chain gene rearrangement. Using antibodies against the cytoplasmic tail of the immunoglobulin co-receptor beta (Ig beta) chain we find mu, but not mu delta 1 chains associated with Ig beta. Since a heterodimer of surface-labeled proteins was co-precipitated with mu we conclude that only wild-type mu is associated with the Ig alpha/Ig beta co-receptor on the surface of pre-B cell lines. Mutant mu delta 1 chains achieve their surface expression by utilizing a glycophospholipid anchor. In vivo analysis of transgenic mice expressing either mu or mu delta 1 transgenes revealed the expected "normal" B cell development in the case of wild-type mu transgenic lymphocytes, but a block in differentiation of mu delta 1 transgenic lymphocytes. The maturation block occurs at the developmental transition of pre-B lymphocytes from the CD43/S7+, CD45R/B220low stage to the CD43/S7-, B220low/high stage in which the majority of L chain gene rearrangements occur. These results, together with the observed inability of the mu delta 1 chains to signal activation of L chain gene joining and to associate Ig alpha/Ig beta in pre-B cell lines suggests that signals mediated by the protein complex composed to mu/Ig alpha/Ig beta are crucial during differentiation of pre-B lymphocytes.
Increased sensitivity to oxanosine, a novel nucleoside antibiotic, of rat kidney cells upon expression of the integrated viral src gene. (1985)

The mechanism of antitumor action of oxanosine was studied using a strain of rat kidney cells infected with a mutant Rous sarcoma virus, the src gene of which was temperature sensitive. Oxanosine inhibited cell growth in vitro, as well as nucleic acid synthesis in these cells, 10 times more strongly at a permissive temperature (33 degrees C) than at a non-permissive temperature (39 degrees C). Protein synthesis was inhibited only slightly at either temperature. The inhibition of cell growth and nucleic acid synthesis was reversed by guanosine, GMP, and to a lesser extent by adenosine and inosine. Oxanosine inhibited the conversion of [14C]hypoxanthine to guanine nucleotides in cells and again in the same temperature-related fashion. The conversion to adenine nucleotides was not inhibited. Oxanosine-5'-monophosphate was found to be a potent nearly competitive inhibitor, with respect to IMP, of IMP dehydrogenase (EC 1.2.1.14; IMP:NAD+ oxidoreductase) isolated from cells grown either at 33 degrees C or at 39 degrees C; with the former and the latter enzyme preparations, KmS for IMP were 6.0 X 10(-6) M and 5.3 X 10(-6) M, respectively, while Kis for oxanosine-5'-monophosphate were 1-3 X 10(-6) M and 5.2 X 10(-6) M, as well.
Diethanolamine assisted secondary ion mass spectrometry of naturally occurring complex oligosaccharides (1982)

Abstract A remarkable technique for identifying the molecular weight of involatile and/or thermally unstable compounds by molecular secondary ion mass spectrometry is described. This technique uses diethanolamine as a matrix material instead of glycerol which is at present considered to be the best medium. When this amine is used, adduct ions [M+DEAH] + are formed from neutral saccharides, and these are very stable for reliable molecular weight determination.
FORMATION OF HIGHER ALCOHOLS FROM14C-LABELLED VALINE AND LEUCINE (1967)

The formation of isobutanol and 3-methylbutanol during alcoholic fermentation by brewer's yeast has been studied by adding uniformly 14C-labelled valine and leucine to the complex amino acid mixture which is used as nitrogen source. In the presence of 14C-leucine, only 3-methylbutanol becomes radioactive whereas, in the presence of 14C-valine, both isobutanol and 3-methylbutanol acquire label. The specific radioactivity of these compounds is, in all cases, inferior to that of the parent amino acids showing that a part of these higher alcohols is always formed by the synthetic functions of the yeast. The results suggest that the regulating effect of the valine and leucine level of the medium on the synthesis of these amino acids in yeast cells is rather limited. They furthermore indicate that intact assimilation of amino acids is not the only mode of their utilization, even in media with excessive levels of amino acids. An attempt is made to explain the dependence of the anabolic and catabolic modes of higher alcohol formation upon the nitrogenous nutrient level of the medium. The presence of radioactive isoleucine as impurity in the 14C-leucine used has allowed an approximative calculation of the formation of 2-methylbutanol from isoleucine which is very similar to the formation of isobutanol from valine.
Optical measurement of dental cast profile and application to analysis of three-dimensional tooth movement in orthodontics. (1989)

Dental casts are frequently used for measuring the size, shape and position of a tooth. We have developed an optical apparatus for measuring a three-dimensional profile of a dental cast. The measurement is based on the triangular method which detects a laser spot on a cast by an image sensor. The apparatus is computer-controlled and designed to achieve a total measuring depth of 40 mm, a data acquisition time of 25 ms per point and a minimum scanning pitch of 0.1 mm. The depth and lateral resolutions are 0.05 and 0.1 mm, respectively, within a depth range of 25 mm. As a particular application of the apparatus, three-dimensional movement of teeth, including rotational movement, during orthodontic treatment, has been quantified by means of the superimposition of tooth profiles using a computer.
Characterization of an antibiotic produced by a strain of Pseudomonas fluorescens inhibitory to Gaeumannomyces graminis var. tritici and Pythium spp (1986)

The production, isolation, and characterization of an antibiotic substance from cultures of Pseudomonas fluorescens 2-79 (NRRL B-15132) is described. P. fluorescens 2-79 originally was isolated from the roots of wheat and is suppressive to the wheat root disease take-all caused by Gaeumannomyces graminis var. tritici. The antibiotic was isolated from potato glucose broth cultures of strain 2-79 by solvent extraction. It was purified by silica gel column chromatography and was a greenish yellow, needle-shaped crystal with a melting point of 242 degrees C (decomposition). It was soluble in methylene chloride, chloroform, acetone, 2 N sodium hydroxide, and 2 N hydrochloric acid and was insoluble in water, methanol, ethyl acetate, tetrahydrofuran, diethyl ether, carbon tetrachloride, hexane, and petroleum ether. On the basis of UV, infrared, 1H-nuclear magnetic resonance, 13C-nuclear magnetic resonance, mass spectral analysis, and elemental analysis, the structure of the antibiotic is proposed to be a dimer of phenazine carboxylic acid. Lithium aluminum hydride reduction of the antibiotic yielded hydroxymethyl phenazine as a major product which retained most of the biological characteristics of the parent molecule. There were no toxic symptoms when mice received this antibiotic by oral doses up to 464 mg/kg. The antibiotic showed excellent activity against several species of fungi, including the wheat pathogens Gaeumannomyces graminis var. tritici, Rhizoctonia solani, and Pythium aristosporum; and it may have a role in suppression of take-all in vivo by strain 2-79.
The 5'- and 3'-untranslated regions of ornithine decarboxylase mRNA affect the translational efficiency. (1990)

We have determined the roles of the 5'- and 3'-untranslated regions (UTR) of ornithine decarboxylase (ODC) mRNA in the post-transcriptional regulation of this enzyme. A series of expression vectors were constructed in which portions of the ODC 5' and/or 3' UTRs were placed flanking a reporter gene coding sequence, either firefly luciferase or chloramphenicol acetyltransferase, so as to generate a hybrid transcript. Translation of these chimeric genes in transient expression assays in wild type and ODC-deficient hamster cells was examined in the presence of normal or depleted polyamine pools. The ODC 5' UTR suppresses translation of the coding sequence it precedes irrespective of polyamine levels, and this effect is shown to be due to the GC-rich 5' segment of the UTR. The same effect is observed in vivo and in a rabbit reticulocyte in vitro translation system. The GC-rich region has the potential to form a very stable hairpin structure and inhibits translation in a position-dependent but orientation-independent manner. Insertion of the 3' UTR of ODC downstream of the translation termination codon of the reporter gene but prior to the polyadenylation signal partially relieves the suppression of translation imposed by the 5' UTR; the overall translatability of the message improves 30-50-fold.
Identification of novel oestrogen receptor target genes in human ZR75-1 breast cancer cells by expression profiling (2001)

Oligonucleotide microarrays were used to analyse gene expression profiles in human ZR75-1 breast cancer cells in the presence of 17beta-oestradiol and oestrogen antagonists. Differential gene expression of a number of genes was confirmed by quantitative RNA analysis. In addition to known oestrogen-responsive genes, an appreciable number of novel targets were identified, including growth factors and components of the cell cycle, adhesion molecules, enzymes, signalling molecules and transcription factors. The most pronounced oestrogen-sensitive gene was that for the cytochrome P450-IIB enzyme, involved in metabolising steroids and xenobiotics, which was increased 100-fold over a 24 h period. It is a direct target gene for oestrogens, because its expression was increased in the presence of cyclohexamide. In contrast, expression of cytochrome P450-IIB was not detected in human MCF7 breast cancer cells. Expressions of the cationic amino acid transporter E16, gap junction protein and insulin-like growth factor binding protein 4 were also markedly increased by oestrogens, but the kinetics of induction varied according to the target gene. With the exception of the cationic amino acid transporter E16 and the insulin-like growth factor binding protein 4, the expression of the majority of the genes was unaffected by antioestrogen treatment. Further analysis of this set of markers will provide alternative approaches to the investigation of the mitogenicity of oestrogens in breast cancer cells.
Enantiopure drug synthesis: From methyldopa to imipenem to efavirenz (2005)

An historical retrospective is presented relative to the development of practical processes for the syntheses of three major drugs: methyldopa, imipenem, and efavirenz. Each highlights a major method for asymmetric synthesis. This work was initially presented as a lecture at the BLOCKBUSTER CHIRALITY section of the CHIRALITY 2004 meeting in New York City, and this paper is simply a written account of that presentation. The original literature that details the chemistry discussed herein is noted in the reference section.
Human epidermal growth factor receptor residue covalently cross-linked to epidermal growth factor. (1990)

An epidermal growth factor (EGF) receptor monoclonal antibody (mAb), mAb LA22, was used to analyze the covalent coupling of human EGF receptors to mouse EGF by the amine-reactive cross-linking agent disuccinimidyl suberate. A soluble Mr 105,000 truncated form of the receptor secreted by A-431 epidermoid carcinoma cells and consisting of the ligand-binding extracellular domain was cross-linked to 125I-labeled EGF. Digestion of this complex with an endoproteinase that specifically cleaves at the COOH side of glutamyl residue released a single radiolabeled glycosylated fragment of Mr 18,000 that reacted with mAb LA22. As the epitope for mAb LA22 resided between Ala-351 and Asp-364 of the mature receptor, this result localized the cross-linked receptor residue(s) to the 47-amino acid interval from Phe-321 to Glu-367. The receptor residue(s) involved in the covalent coupling of rat 125I-labeled transforming growth factor alpha was similarly localized to this region of the receptor. This receptor interval, which included two glycosylated asparaginyl residues at positions 328 and 337, contained but three amino acid residues that were potentially reactive with disuccinimidyl suberate: Lys-332, Lys-333, and Lys-336. Characterization of mAb LA22-reactive 125I-EGF-labeled receptor fragments generated by an endoproteinase specific for the COOH side of lysyl residue placed the NH2 termini of the two smallest fragments between the glycosylated residues Asn-328 and Asn-337. These results indicated that disuccinimidyl suberate cross-linked the NH2 group of EGF residue Asn-1 to the human EGF receptor residue Lys-336. Our results further suggest that EGF and transforming growth factor alpha, two members of the EGF family of peptide growth factors, interact with closely apposed or identical features of the receptor.
CC and CXC chemokine receptors mediate migration, proliferation, and matrix metalloproteinase production by fibroblast‐like synoviocytes from rheumatoid arthritis patients (2004)

These data suggest that through modulation of the migration, proliferation, and MMP production by FLS, the chemokine system may play a more direct role in the destructive phase of RA than is currently suspected, and thus emphasize the relevance of chemokines and their receptors as potential therapeutic targets in this disease.
Programming embedded systems in C and C (1999)

From the Publisher:
This book introduces embedded systems to C and C++ programmers. Topics include testing memory devices, writing and erasing flash memory, verifying nonvolatile memory contents, controlling on-chip peripherals, device driver design and implementation, optimizing embedded code for size and speed, and making the most of C++ without a performance penalty.
Conversion of Bcl-2 to a Bax-like Death Effector by Caspases (1997)

Caspases are a family of cysteine proteases implicated in the biochemical and morphological changes that occur during apoptosis (programmed cell death). The loop domain of Bcl-2 is cleaved at Asp34 by caspase-3 (CPP32) in vitro, in cells overexpressing caspase-3, and after induction of apoptosis by Fas ligation and interleukin-3 withdrawal. The carboxyl-terminal Bcl-2 cleavage product triggered cell death and accelerated Sindbis virus-induced apoptosis, which was dependent on the BH3 homology and transmembrane domains of Bcl-2. Inhibitor studies indicated that cleavage of Bcl-2 may further activate downstream caspases and contribute to amplification of the caspase cascade. Cleavage-resistant mutants of Bcl-2 had increased protection from interleukin-3 withdrawal and Sindbis virus-induced apoptosis. Thus, cleavage of Bcl-2 by caspases may ensure the inevitability of cell death.
Dispersion-managed soliton in optical fibers with zero average dispersion (2000)

A dispersion-managed optical system with stepwise periodic variation of dispersion is studied in the framework of a path-averaged Gabitov-Turitsyn equation. The soliton solution is obtained by means of iterating the path-averaged equation. The dependence of soliton parameters on dispersion map strength is investigated, together with the oscillating tails of the soliton.
Role of Factor XII in hemostasis and thrombosis: clinical implications (2007)

The plasma coagulation system reacts quickly to limit blood loss from injury sites but also contributes to vascular thrombosis. In current models of hemostatic balance, normal coagulation and thrombosis represent two sides of the same coin, however, recent data from gene-deleted murine models have challenged this dogma. Deficiency of coagulation Factor XII (Hageman factor), a serine protease that initiates the intrinsic pathway of coagulation, severely impairs arterial thrombus formation but is not associated with excessive bleeding. These findings suggest that fibrin-generating mechanisms that operate during pathologic thrombus formation involve pathways distinct from those that are active during normal hemostasis. As Factor XII selectively contributes to thrombus formation in occlusive disease, but not to normal hemostasis, inhibition of this protease may offer a novel treatment strategy for prevention of arterial thrombosis with minimal or no risk of bleeding.
Research and Development of the Intelligently-Controlled Prosthetic Ankle Joint (2006)

The purpose of this study is to develop a prosthetic ankle joint intelligently controlled by specially designed linear MR (magneto-rheological) brake. MR fluid changes its rheology depending on the intension of an applied magnetic field. The brake using MR fluid (we call it MR brake) has a simple structure and can control its braking force with a low voltage. Prosthesis users often tumble because they don't have dorsiflexor, so that we propose putting MR brake taking the place of dorsiflexion. We hope that prosthesis users can walk more naturally and smoothly by use of developed intelligent prosthetic ankle joint with MR brake. We developed a prototype of it and evaluated it with walking experiments before. But there were some problems with the prototype in terms of hardware and experimental environments. Therefore we have developed a 2nd prototype of the intelligent prosthetic ankle joint with the MR brake, which was improved considering previous problems, and then we have carried out the walking experimental evaluation of it
PDX1 homeobox protein expression in pseudopyloric glands and gastric carcinomas (2004)

Our study suggests that PDX1 plays an important role in the development of pseudopyloric glands, and that pseudopyloric glands may reflect a condition associated with gastric carcinogenesis.
Synthesis and Evaluation ofS-Acyl-2-thioethyl Esters of Modified Nucleoside 5‘-Monophosphates as Inhibitors of Hepatitis C Virus RNA Replication (2005)

Several triphosphates of modified nucleosides (1-6) were identified as inhibitors (IC(50) = 0.08-3.8 microM) of hepatitis C virus RNA-dependent RNA polymerase (RdRp). Although the initial SAR developed by determining the ability of the triphosphates to inhibit the in vitro activity of the HCV RdRp identified several potent inhibitors, none of the corresponding nucleosides exhibited significant inhibitory potency in a cell-based replicon assay. To improve upon the activity, bis(tBu-S-acyl-2-thioethyl) nucleoside 5'-monophosphate esters (7-12) were synthesized, and these derivatives exhibited improved potency compared to the corresponding nucleosides in the cell-based assay. Analysis of the intracellular metabolism demonstrated that the S-acyl-2-thioethyl (SATE) prodrug is metabolized to the 5'-triphosphate 40- to 155-fold more efficiently compared to the corresponding nucleoside. The prodrug approach involving bis(tBuSATE)cytidine 5'-monophosphate ester significantly reduced the deamination of cytidine derivatives by cellular deaminases. Additionally, chromosomal aberration studies with the SATE prodrug in cells showed no statistically relevant increase in aberrations compared to the concurrent controls.