gebhart/patrepeval huggingface dataset:
Hydrogen/Deuterium Exchange Kinetics of Apolipophorin-III in Lipid-free and Phospholipid-bound States (1996)

Attenuated total reflection Fourier transform infrared spectroscopy was used to probe the kinetics of hydrogen/deuterium exchange in Manduca sexta apolipophorin-III (apoLp-III). ApoLp-III is an exchangeable apolipoprotein that is made up of five elongated amphipathic alpha-helices in a helical bundle conformation in the monomeric lipid-free form. Upon interaction with phospholipids, it is postulated to undergo a large conformational change whereby the hydrophobic interior is exposed, facilitating binding to the lipid surfaces. We have used the lipid-free and dimyristoylphosphatidylcholine-bound apoLp-III to study the dynamically variable domains in the two forms. Three populations of amide protons varying in their hydrogen/deuterium exchange rates were found to exist: slow, intermediate, and fast exchanging, which could correspond to completely buried, partially buried, and solvent-exposed domains on the protein in both the states. In lipid-free apoLp-III, 36, 12, and 52% of the total residues contributed to the slow, intermediate, and fast exchanging populations, respectively. In the dimyristoylphosphatidylcholine-bound form, the corresponding distribution was 20, 16, and 64%, representing a 12% increase in the number of exposed residues. The results are discussed in terms of increased solvent accessibility due to gross tertiary structural reorganization.
Review of Poly (ADP-ribose) Polymerase (PARP) Mechanisms of Action and Rationale for Targeting in Cancer and Other Diseases (2013)

Poly (ADP-ribose) polymerases (PARPs) are a family of related enzymes that share the ability to catalyze the transfer of ADP-ribose to target proteins. PARPs play an important role in various cellular processes, including modulation of chromatin structure, transcription, replication, recombination, and DNA repair. The role of PARP proteins in DNA repair is of particular interest, in view of the finding that certain tumors defective in homologous recombination mechanisms, may rely on PARP-mediated DNA repair for survival, and are sensitive to its inhibition. PARP inhibitors may also increase tumor sensitivity to DNA-damaging agents. Clinical trials of PARP inhibitors are investigating the utility of these approaches in cancer. The hyperactivation of PARP has also been shown to result in a specific programmed cell death pathway involving NAD+/ATP depletion, mu-calpain activation, loss of mitochondrial membrane potential, and the release of apoptosis inducing factor. Hyperactivation of the PARP pathway may be exploited to selectively kill cancer cells. Other PARP forms, including tankyrase 1 (PARP 5a), which plays an important role in enhancing telomere elongation by telomerase, have been found to be potential targets in cancer therapy. The PARP pathway and its inhibition thus offers a number of opportunities for therapeutic intervention in both cancer and other disease states.
ChemInform Abstract: Chemical Shifts in Amino Acids, Peptides, and Proteins: From Quantum Chemistry to Drug Design (2002)

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.
Dose Response of Inhaled Dry-Powder Insulin and Dose Equivalence to Subcutaneous Insulin Lispro (2005)

While the time-action profile was longer for HIIP than for SC lispro, both treatments showed rapid initial absorption and similar overall PK exposure and GD effect. HIIP was as well tolerated as SC lispro, thereby offering a promising alternative to injectable insulin therapy.
Anchoring foreign substances on live cell surfaces using Sortase A specific binding peptide (2013)

A simple, rapid, and efficient live cell surface labeling method has been developed that uses a direct conjugation between Sortase A expressed transiently at the cell surface and Sortase A specific binding peptide.
Development of Large-Scale Syntheses of Ropinirole in the Pursuit of a Manufacturing Process1 (1998)

Two plant syntheses of ropinirole {4-[2-(di-n-propylamino)ethyl]-1,3-dihydro-2H-indolin-2-one hydrochloride, SK&F-101468-A} using the ferric chloride mediated cyclisation of β-nitrostyrenes to form 3-chlorooxindoles as the key step are described. The first synthesis suffered the severe limitation of the final-step chemistry being nonselective in the reaction between di-n-propylamine and the bromide precursor to ropinirole as both substitution and elimination pathways were promoted and by-product formation at a level of 40% resulted. This problem was rectified in the latter synthesis by the more selective reaction between di-n-propylamine and the sulfonate ester precursor promoting ropinirole formation to a level of 88%. This second synthesis is now used as the commercial route, and problems (and their solutions) identified during the development of this route are now described. The identification of novel by-products which enabled the Sommelet oxidation step to be optimised is also reported. A unimolecular decomposition mechanism during hydrolysis of the hexaminium salt to form the key benzaldehyde intermediate is proposed and substantiated with experimental data.
Selective Inhibition of ras -Dependent Transformation by a Farnesyltransferase Inhibitor (1993)

To acquire transforming potential, the precursor of the Ras oncoprotein must undergo farnesylation of the cysteine residue located in a carboxyl-terminal tetrapeptide. Inhibitors of the enzyme that catalyzes this modification, farnesyl protein transferase (FPTase), have therefore been suggested as anticancer agents for tumors in which Ras contributes to transformation. The tetrapeptide analog L-731,735 is a potent and selective inhibitor of FPTase in vitro. A prodrug of this compound, L-731,734, inhibited Ras processing in cells transformed with v-ras. L-731,734 decreased the ability of v-ras-transformed cells to form colonies in soft agar but had no effect on the efficiency of colony formation of cells transformed by either the v-raf or v-mos oncogenes. The results demonstrate selective inhibition of ras-dependent cell transformation with a synthetic organic inhibitor of FPTase.
Catalytic Asymmetric Dihydroxylation of Olefins Using a Recoverable and Reusable Polymer-Supported Osmium Catalyst (1999)

ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTCatalytic Asymmetric Dihydroxylation of Olefins Using a Recoverable and Reusable Polymer-Supported Osmium CatalystShū Kobayashi, Masahiro Endo, and Satoshi NagayamaView Author Information Graduate School of Pharmaceutical Sciences The University of Tokyo, Hongo, Bunkyo-ku Tokyo 113-0033, Japan Cite this: J. Am. Chem. Soc. 1999, 121, 48, 11229–11230Publication Date (Web):November 18, 1999Publication History Received26 August 1999Published online18 November 1999Published inissue 1 December 1999https://pubs.acs.org/doi/10.1021/ja993099mhttps://doi.org/10.1021/ja993099mrapid-communicationACS PublicationsCopyright © 1999 American Chemical SocietyRequest reuse permissionsArticle Views2610Altmetric-Citations139LEARN 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-AlertscloseSupporting Info (2)»Supporting Information Supporting Information SUBJECTS:Catalysts,Diols,Hydrocarbons,Osmium,Polymers Get e-Alerts
Model polypeptide of mussel adhesive protein. I. Synthesis and adhesive studies of sequential polypeptides (X-Tyr-Lys)n and (Y-Lys)n (2000)

The sequential polytripeptides and polydipeptides, (X-Tyr-Lys)n, (XGly, Ala, Pro, Ser, Leu, Ile, Phe), (Y-Lys)n, (YGly, Tyr), and (Gly-Tyr)n, which imitate a mussel adhesive protein, have been synthesized. The molecular weights of the polypeptides were estimated to be 7,200 ∼ 13,400 (19 ∼ 42 repeating units), and the polypeptides were found to have satisfactory amino acid sequences. The polypeptides were crosslinked by tyrosinase, and the optimal pH in the crosslinking reaction was 7.4 in the case of the polytripeptide, (Gly-Tyr-Lys)n. The optimal tyrosinase amount for the adhesive strength of (Gly-Tyr-Lys)n was 0.34 unit/mg (polypeptide) at pH 7.4. The shear adhesive strength of the polytripeptide increased with an increase in the polytripeptide concentration, and was not influenced by the third amino acid, X. The shear adhesive strengths of polytripeptides (X-Tyr-Lys)n were equal to one of the synthetic polydecapeptides, (Ala-Lys-Pro-Ser-Tyr-Pro-Pro-Thr-Tyr-Lys)n and (Gly-Pro-Lys-Thr-Tyr-Pro-Pro-Thr-Tyr-Lys)n which were the model polydecapeptides for blue mussel and Californian mussel, respectively. © 2000 John Wiley & Sons, Inc. J Appl Polym Sci 76: 929–937, 2000
Multi-frequency bioelectrical impedance: a comparison between the Cole-Cole modelling and Hanai equations with the classical impedance index approach (1996)

Total body water and extracellular water were measured by deuterium oxide and bromide dilution respectively in 23 healthy males and 25 healthy females. In addition, total body impedance was measured at 17 frequencies, ranging from 1 kHz to 1350 kHz. Modelling programs were used to extrapolate impedance values to frequency zero (extracellular resistance) and frequency infinity (total body water resistance). Impedance indexes (height2/Zf) were computed at all 17 frequencies. The estimation errors of extracellular resistance and total body water resistance were 1% and 3%, respectively. Impedance and impedance index at low frequency were correlated with extracellular water, independent of the amount of total body water. Total body water showed the greatest correlation with impedance and impedance index at high frequencies. Extrapolated impedance values did not show a higher correlation compared to measured values. Prediction formulas from the literature applied to fixed frequencies showed the best mean and individual predictions for both extracellular water and total body water. It is concluded that, at least in healthy individuals with normal body water distribution, modelling impedance data has no advantage over impedance values measured at fixed frequencies, probably due to estimation errors in the modelled data.
Restless Legs Syndrome (2001)

Restless legs syndrome (RLS), although long ignored and still much underdiagnosed, disrupts the life and sleep considerably of those who have it. Recent clinical and basic research provides for better definition and pathophysiologic understanding of the disorder. The body of knowledge about this disorder has been expanding rapidly during the past decade and it has altered our concepts of this disorder. This review of RLS covers history, diagnosis, morbidity of sleep disturbance, relation to periodic limb movements in both sleep and waking, secondary causes, severity assessment methods, phenotypes for possible genetic patterns, epidemiology, pathophysiology, and medical treatment considerations. The emphasis on pathophysiology includes consideration of central nervous system localization, neurotransmitter and other systems involved, and the role of iron metabolism. Studies to date support the authors' recently advanced iron-dopamine model of RLS.
Multiple scattering lowtran and fascode models (1987)

This paper describes the implementation of an efficient and accurate multiple scattering parameterization within the LOWTRAN and FASCODE transmittance/radiance models. The parameterization is based on a stream approximation in which the local radiance field needed to evaluate the multiple scattering source function is estimated from the local radiation fluxes. The latter are calculated based on a parameterized two-flux for individual layers and an adding method for combining layers. Because of the line-by-line nature of FASCODE, it is straightforward to implement the multiple scattering treatment. For LOWTRAN, an interface scheme was developed using the k-distribution method to match the multiple scattering approach to the band model calculation of gas absorption. The interface scheme represents the LOWTRAN band model by a sum of pseudomonochromatic calculations. The approach is valid for any band model for which k-distribution parameters can be evaluated. The accuracy of the multiple scattering parameterization has been demonstrated by comparing it with more detailed calculations for a variety of atmospheric conditions. RMS errors in radiance considering all possible viewing angles are <20%. In addition, to insure consistency between models, overlapping LOWTRAN and FASCODE spectral regions are compared. Finally, it is demonstrated that the implemented multiple scattering parameterization corrects LOWTRAN's previous underestimation of path radiance for long horizon paths where multiple scattering is significant.
Interferon-alpha induces circulating tumor necrosis factor receptor p55 in humans (1995)

In the present studies we investigated the effect of interferon-alpha (IFN alpha) on the release of the soluble (extracellular) form of the tumor necrosis factor p55 receptor (TNFsRp55), because TNFsRp55 is a natural antagonist of tumor necrosis factor (TNF)-induced inflammation and also might be part of the antiinflammatory properties of IFN alpha. Plasma levels of TNFsRp55 were measured by a specific radioimmunoassay in five healthy volunteers and in five patients with chronic hepatitis C treated with IFN alpha. Levels showed a significant increase after a single injection of 5.0 million U IFN alpha in both healthy and hepatitis patient groups. Peak values (3.5 to 4.5 ng/mL) were observed within 12 hours of beginning treatment. Thereafter, levels promptly declined, reaching baseline values within 24 hours. TNF alpha and C-reactive protein (CRP) levels were below the detection limit in the same plasma samples. In addition, IFN alpha suppressed significantly interleukin (IL)-1 alpha-induced TNF alpha protein synthesis by human peripheral blood mononuclear cells. These results suggest that the antiinflammatory properties of IFN alpha may be, in part, also due to the induction and/or release of TNF soluble receptors and the suppression of TNF alpha synthesis.
Patterns of calcium‐binding proteins support parallel and hierarchical organization of human auditory areas (2003)

The human primary auditory cortex (AI) is surrounded by several other auditory areas, which can be identified by cyto-, myelo- and chemoarchitectonic criteria. We report here on the pattern of calcium-binding protein immunoreactivity within these areas. The supratemporal regions of four normal human brains (eight hemispheres) were processed histologically, and serial sections were stained for parvalbumin, calretinin or calbindin. Each calcium-binding protein yielded a specific pattern of labelling, which differed between auditory areas. In AI, defined as area TC [see C. von Economo and L. Horn (1930) Z. Ges. Neurol. Psychiatr.,130, 678-757], parvalbumin labelling was dark in layer IV; several parvalbumin-positive multipolar neurons were distributed in layers III and IV. Calbindin yielded dark labelling in layers I-III and V; it revealed numerous multipolar and pyramidal neurons in layers II and III. Calretinin labelling was lighter than that of parvalbumin or calbindin in AI; calretinin-positive bipolar and bitufted neurons were present in supragranular layers. In non-primary auditory areas, the intensity of labelling tended to become progressively lighter while moving away from AI, with qualitative differences between the cytoarchitectonically defined areas. In analogy to non-human primates, our results suggest differences in intrinsic organization between auditory areas that are compatible with parallel and hierarchical processing of auditory information.
Events in the Natural History of Prostate Cancer: Using Salvage Curves, Mean Age Distributions and Contingency Coefficients (1968)

No AccessJournal of Urology1 Jan 1968Events in the Natural History of Prostate Cancer: Using Salvage Curves, Mean Age Distributions and Contingency Coefficients Galen B. Cook, and Francis R. Watson Galen B. CookGalen B. Cook More articles by this author , and Francis R. WatsonFrancis R. Watson More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(17)62647-8AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail © 1968 by The American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetailsCited ByGleave M, Hsieh J, Von Eschenbach A and Chung L (2018) Prostate and Bone Fibroblasts Induce Human Prostate Cancer Growth in Vivo: Implications for Bidirectional Tumor-Stromal Cell Interaction in Prostate Carcinoma Growth and MetastasisJournal of Urology, VOL. 147, NO. 4, (1151-1159), Online publication date: 1-Apr-1992.Silber I and Mcgavran M (2018) Adenocarcinoma of the Prostate in Men Less than 56 Years Old: A Study of 65 CasesJournal of Urology, VOL. 105, NO. 2, (283-285), Online publication date: 1-Feb-1971.Cook G and Watson F (2018) A Comparison by Age of Death Rates due to Prostate Cancer AloneJournal of Urology, VOL. 100, NO. 5, (669-671), Online publication date: 1-Nov-1968.Cook G and Watson F (2018) Twenty Single Nodules of Prostate Cancer Not Treated by Total ProstatectomyJournal of Urology, VOL. 100, NO. 5, (672-674), Online publication date: 1-Nov-1968. Volume 99Issue 1January 1968Page: 87-96 Advertisement Copyright & Permissions© 1968 by The American Urological Association Education and Research, Inc.MetricsAuthor Information Galen B. Cook More articles by this author Francis R. Watson More articles by this author Expand All Advertisement PDF DownloadLoading ...
Emergence of permanently differentiated cell clones in a human colonic cancer cell line in culture after treatment with sodium butyrate. (1984)

The human colonic cancer cell line HT29 is undifferentiated in standard culture conditions (Dulbecco's medium:10% fetal bovine serum). These cells were cultured in 5 mM sodium butyrate for 9 days; then they were trypsinized and subcultured in sodium butyrate for an additional 14 days. Multinucleation occurred during this second phase of the treatment. The cells were then transferred to standard medium and multinucleation disappeared. Morphological changes appeared 10 to 12 days after return to standard culture conditions; some cells flattened and became more adherent to the bottom of the flasks. These altered cells divided actively and formed "flat foci" interspersed among the densely packed undifferentiated HT29 cells. This altered phenotype persists after more than 24 months of culture in standard medium. Clonal cell lines were established from these flat foci-forming cells and characterized. These clonal lines exhibited morphological cell polarity defined by an apical cell surface separated by junctional complexes from the basolateral cell surface. Functional differentiation did also occur since some clonal lines formed domes representing active transepithelial transport, and others exhibited massive mucus secretion. In conclusion, our findings indicate that permanently differentiated cell populations emerged in a colonic cancer cell line after sodium butyrate treatment. These new clonal lines will be useful in future models for the study of differentiation programs of both normal and cancerous colonic cells.
Comprehensive evaluation of NT5E/CD73 expression and its prognostic significance in distinct types of cancers (2018)

High CD73 expression was significantly associated with lymph node metastases and a promising prognostic factor in different types of cancers.
Cell-derived unesterified cholesterol cycles between different HDLs and LDL for its effective esterification in plasma. (1993)

Pulse-chase incubations of human plasma with [3H]cholesterol-laden skin fibroblasts or low density lipoproteins (LDL) and nondenaturing two-dimensional electrophoresis were used to study the transfer and esterification of cell-derived unesterified cholesterol (UC) in human plasma lipoproteins. Specific radioactivities ([3H]UC per microgram of UC) were calculated, and net cholesterol mass transfer was quantified using a fluoro-enzymatic assay to validate productive transfers of UC between high density lipoprotein (HDL) and LDL. Cellular UC was initially taken up by pre-beta 1-HDL and subsequently transferred in the sequence pre-beta 2-HDL-->pre-beta 3-HDL-->alpha-HDL-->LDL. During the first 5 minutes of this process, only 5% of cellular cholesterol was esterified in pre-beta 3-HDL and alpha-HDL; the remainder reached LDL as UC. Cellular UC accumulating in LDL was then redistributed to various HDL particles via two pathways: 1) the partially LDL receptor-mediated uptake and re-secretion of UC by cells and 2) the direct transfer of UC to HDL, mostly to alpha-HDL and a small amount to pre-beta-HDL. UC was not transferred from LDL to HDL after inhibition of lecithin:cholesterol acyltransferase (LCAT). The esterification of cellular [3H]cholesterol in plasma was competitively inhibited by the addition of excess unlabeled LDL but not of excess HDL. However, both excess LDL and excess HDL prevented the esterification of cell-derived cholesterol in apolipoprotein B-free plasma. This demonstrated that LDL is the major source of UC to the LCAT reaction and that the transfer of UC from LDL to HDL is LCAT dependent. In conclusion, the effective esterification of cell-derived cholesterol in plasma involves a rapid transfer of UC via HDL particles to LDL, from which it is distributed to pre-beta-HDL and alpha-HDL. Furthermore, we hypothesize that the transfer per se of cellular UC to LDL forms a cholesterol concentration gradient between cell membranes and HDL and thus a second, reverse cholesterol transport mechanism in addition to the esterification of cholesterol by LCAT.