bluuebunny/crossref_metadata_2025 huggingface dataset:
Should gambling be included in public health surveillance systems?
Authors: Gambino Blase
Published: August 2010

This paper examines the question of whether indicators of pathological or disordered gambling should be included in current public health surveillance systems. Such inclusion can be justified in terms of the emerging associations between disordered gambling and the leading indicators of the risk for premature morbidity and mortality. Additional justification can be seen in terms of the potential of Internet gambling to increase the incidence of gambling disorders, particularly among younger and older populations. The paper describes characteristics of public health surveillance systems and recommends including gambling in such systems, on at least a provisional basis.
A Qualitative Perspective on Physical, Social and Cognitive Accessibility to Gambling
Authors: Hing Nerilee , Nisbet Sharen
Published: August 2010

A possible relationship exists between heightened accessibility to gambling and the development and maintenance of gambling problems amongst employees at gambling venues. This paper takes an interpretive approach to exploring how working in a gambling venue influences accessibility to gambling. Semi-structured telephone interviews were conducted with 40 hotel and club employees in Victoria, Australia. Data were analysed along three key dimensions of accessibility to gambling. In terms of physical accessibility, respondents generally felt shiftwork and split shifts heavily influence the times staff are likely to access gambling facilities. Aspects of social accessibility, including familiarity and comfort of gambling in the workplace, encouragement by other staff, and workplace cultures that do not deter staff gambling, were considered encouraging influences. Cognitive accessibility (or knowledge and understanding about gambling) was heightened by enhanced knowledge of gambling products and processes, greater knowledge of jackpot levels, a desire to know what competing venues are offering, and cognitive distortions around winning.
Evaluation of various observing systems for the global monitoring of CO2 surface fluxes
Authors: Hungershoefer K. , Breon F.-M. , Peylin P. , Chevallier F. , Rayner P. , Klonecki A. , Houweling S.
Published: August 2010

Abstract. In the context of raising greenhouse gas concentrations, and the potential feedbacks between climate and the carbon cycle, there is an urgent need to monitor the exchanges of carbon between the atmosphere and both the ocean and the land surfaces. In the so-called top-down approach, the surface fluxes of CO2 are inverted from the observed spatial and temporal concentration gradients. The concentrations of CO2 are measured in-situ at a number of surface stations unevenly distributed over the Earth while several satellite missions may be used to provide a dense and better-distributed set of observations to complement this network. In this paper, we compare the ability of different CO2 concentration observing systems to constrain surface fluxes. The various systems are based on realistic scenarios of sampling and precision for satellite and in-situ measurements. It is shown that satellite measurements based on the differential absorption technique (such as those of SCIAMACHY, GOSAT or OCO) provide more information than the thermal infrared observations (such as those of AIRS or IASI). The OCO observations will provide significantly better information than those of GOSAT. A CO2 monitoring mission based on an active (lidar) technique could potentially provide an even better constraint. This constraint can also be realized with the very dense surface network that could be built with the same funding as that of the active satellite mission. Despite the large uncertainty reductions on the surface fluxes that may be expected from these various observing systems, these reductions are still insufficient to reach the highly demanding requirements for the monitoring of anthropogenic emissions of CO2 or the oceanic fluxes at a spatial scale smaller than that of oceanic basins. The scientific objective of these observing system should therefore focus on the fluxes linked to vegetation and land ecosystem dynamics.
Intermediate-m ULF waves generated by substorm injection: a case study
Authors: Yeoman T. K. , Klimushkin D. Yu. , Mager P. N.
Published: August 2010

Abstract. A case study of SuperDARN observations of Pc5 Alfvén ULF wave activity generated in the immediate aftermath of a modest-intensity substorm expansion phase onset is presented. Observations from the Hankasalmi radar reveal that the wave had a period of 580 s and was characterized by an intermediate azimuthal wave number (m=13), with an eastwards phase propagation. It had a significant poloidal component and a rapid equatorward phase propagation (~62° per degree of latitude). The total equatorward phase variation over the wave signatures visible in the radar field-of-view exceeded the 180° associated with field line resonances. The wave activity is interpreted as being stimulated by recently-injected energetic particles. Specifically the wave is thought to arise from an eastward drifting cloud of energetic electrons in a similar fashion to recent theoretical suggestions (Mager and Klimushkin, 2008; Zolotukhina et al., 2008; Mager et al., 2009). The azimuthal wave number m is determined by the wave eigenfrequency and the drift velocity of the source particle population. To create such an intermediate-m wave, the injected particles must have rather high energies for a given L-shell, in comparison to previous observations of wave events with equatorward polarization. The wave period is somewhat longer than previous observations of equatorward-propagating events. This may well be a consequence of the wave occurring very shortly after the substorm expansion, on stretched near-midnight field lines characterised by longer eigenfrequencies than those involved in previous observations.
Effect of ocean acidification on marine fish sperm (Baltic cod: Gadus morhua)
Authors: Frommel A. Y. , Stiebens V. , Clemmesen C. , Havenhand J.
Published: August 2010

Abstract. Ocean acidification, as a consequence of increasing marine pCO2, may have severe effects on the physiology of marine organisms. However, experimental studies remain scarce, in particular concerning fish. While adults will most likely remain relatively unaffected by changes in seawater pH, early life-history stages are potentially more sensitive – particularly the critical stage of fertilization, in which sperm motility plays a central role. In this study, the effects of ocean acidification (decrease of pH to 7.55) on sperm motility of Baltic cod, Gadus morhua, were assessed. We found no significant effect of decreased pH on sperm speed, rate of change of direction or percent motility for the population of cod analyzed. We predict that future ocean acidification will probably not pose a problem for sperm behavior, and hence fertilization success, of Baltic cod.
Adhesion and Mechanical Properties of PNIPAM Microgel Films and Their Potential Use as Switchable Cell Culture Substrates
Authors: Schmidt Stephan , Zeiser Michael , Hellweg Thomas , Duschl Claus , Fery Andreas , Möhwald Helmuth
Published: August 2010

Thermoresponsive poly(N‐isopropylacrylamide) (PNIPAM) microgel films are shown to allow controlled detachment of adsorbed cells via temperature stimuli. Cell response occurs on the timescale of several minutes, is reversible, and allows for harvesting of cells in a mild fashion. The fact that microgels are attached non‐covalently allows using them on a broad variety of (charged) surfaces and is a major advantage as compared to approaches relying on covalent attachment of active films. In the following, the microgels’ physico‐chemical parameters in the adsorbed state and their changes upon temperature variation are studied in order to gain a deeper understanding of the involved phenomena. By means of atomic force microscopy (AFM), the water content, mechanical properties, and adhesion forces of the microgel films are studied as a function of temperature. The analysis shows that these properties change drastically when crossing the critical temperature of the polymer film, which is the basis of the fast cell response upon temperature changes. Furthermore, nanoscale mechanical analysis shows that the films posses a nanoscopic gradient in mechanical properties.
Meningeal T cells associate with diffuse axonal loss in multiple sclerosis spinal cords
Authors: Androdias Géraldine , Reynolds Richard , Chanal Marie , Ritleng Cécile , Confavreux Christian , Nataf Serge
Published: August 2010

Objective

A link between diffuse axonal loss and diffuse inflammation has been established in the brain of patients with progressive multiple sclerosis (MS). In the present paper, we sought to determine whether such a link could be similarly demonstrated in the spinal cord of patients with progressive MS.

Methods

A neuropathological quantitative assessment of inflammation and axonal loss was performed in the cervical spinal cord of 18 patients with progressive MS and 5 control subjects.

Results

As previously reported, we found a mean 25% decrease of axonal density in the normal‐appearing white matter (NAWM) of MS versus control spinal cords. T‐cell perivascular infiltrates were rare, but a robust diffuse inflammation was observed in both the normal‐appearing parenchyma and the meninges. The extent of diffuse axonal loss in the NAWM correlated with both the density of major histocompatibility complex (MHC) class II+ microglia in the NAWM and, surprisingly, the density of CD3+ T cells in the meninges. Interestingly, close interactions between T cells and MHC class II+ macrophages were observed in the meninges of spinal cords from MS patients.

Interpretation

Recent studies assigned a major role to meningeal B‐cell follicles in the pathophysiology of secondary progressive MS. The present work also emphasizes the link between meningeal inflammation and parenchymal lesions and points to a specific role exerted by both meningeal T cells and activated microglia in diffuse axonal loss in the spinal cord. ANN NEUROL 2010
Synchrotron‐Based Micro‐CT Imaging of the Human Lung Acinus
Authors: Litzlbauer Horst Detlef , Korbel Kathrin , Kline Timothy L. , Jorgensen Steven M. , Eaker Diane R. , Bohle Rainer M. , Ritman Erik L. , Langheinrich Alexander C.
Published: August 2010

Structural data about the human lung fine structure are mainly based on stereological methods applied to serial sections. As these methods utilize 2D images, which are often not contiguous, they suffer from inaccuracies which are overcome by analysis of 3D micro‐CT images of the never‐sectioned specimen. The purpose of our study was to generate a complete data set of the intact three‐dimensional architecture of the human acinus using high‐resolution synchrotron‐based micro‐CT (synMCT). A human lung was inflation‐fixed by formaldehyde ventilation and then scanned in a 64‐slice CT over its apex to base extent. Lung samples (8‐mm diameter, 10‐mm height, N = 12) were punched out, stained with osmium tetroxide, and scanned using synMCT at (4 μm)3 voxel size. The lung functional unit (acinus, N = 8) was segmented from the 3D tomographic image using an automated tree‐analysis software program. Morphometric data of the lung were analyzed by ANOVA. Intra‐acinar airways branching occurred over 11 generations. The mean acinar volume was 131.3 ± 29.2 mm3 (range, 92.5–171.3 mm3) and the mean acinar surface was calculated with 1012 ± 26 cm2. The airway internal diameter (starting from the bronchiolus terminalis) decreases distally from 0.66 ± 0.04 mm to 0.34 ± 0.06 mm (P < 0.001) and remains constant after the seventh generation (P < 0.5). The length of each generation ranges between 0.52 and 0.93 mm and did not show significant differences between the second and eleventh generation. The branching angle between daughter branches varies between 113‐degree and 134‐degree without significant differences between the generations (P < 0.3). This study demonstrates the feasibility of quantitating the 3D structure of the human acinus at the spatial resolution readily achievable using synMCT. Anat Rec 293:1607–1614, 2010. © 2010 Wiley‐Liss, Inc.
Reproductive System of Female Scorpion: A Partial Review
Authors: Warburg M.R.
Published: August 2010

The female scorpion ovariuterus was examined in 10 scorpion species belonging to five families: Buthidae, Vaejovidae, Scorpionidae, Urodacidae, and Diplocentridae. Two main patterns of development are known in scorpions: (1) The apoikogenic type with an ovariuterus containing yolk‐rich eggs housed in follicles. This type is found in many scorpion taxa (largely buthids). A peculiar case of apoikogenic ovariuterus is a “beaded” ovariuterus where most of the ova's embryogenesis takes place inside the ovariuterus rather than on pedicels situated on the external wall of the ovariuterus as in most buthids. This type is found in a few scorpion species. (2) The katoikogenic type with an ovariuterus where the embryo develops in a diverticulum composed of four parts: a stalk (pedicel), a thickened collar, a conical portion containing the ovum, and an appendix containing the oral feeding apparatus where the embryos' chelicerae grip a “teat”‐like structure, described in four families: Hemiscorpiidae, Scorpionidae, Urodacidae, and Diplocentridae. There are three kinds of diverticulae: small rudimentary finger‐like diverticulae, embryonic (ED) large projections, and postpartum diverticulae (PPD) empty diverticulae, which are remnants after parturition. The subject is reviewed and its bearing on reproduction in scorpions are discussed. Anat Rec 293:1738–1754, 2010. © 2010 Wiley‐Liss, Inc.
Dynamic style analysis of Spanish balanced pension plans: A Bayesian approach
Authors: Andreu L. , Gargallo P. , Salvador M. , Sarto J. L.
Published: August 2010

This paper is focused on the dynamic allocations of Spanish balanced pension plans that invest predominantly in Euro‐zone equities. Applying a Bayesian method to a return‐based style analysis that includes the constraints of the strong version and time‐varying exposures, we provide evidence for no statistically significant changes over time in the main strategic asset allocations, namely, equity assets, long‐term debt and cash allocations. However, we find time‐varying selection abilities, indicating that the value added by managers is not the same over time.

Although the investment style tends to be constant in each pension plan, these allocations are variable across plans which allow us to find different subsets of portfolios that present different mean returns and volatilities. Some pension plan features, such as size and type of financial institution that manages the portfolio, have been considered in trying to find concurrent characteristics in each subset. Copyright © 2010 John Wiley & Sons, Ltd.
Total chemical synthesis of human T‐cell leukemia virus type 1 protease via native chemical ligation
Authors: Li Changqing , Li Xiangqun , Lu Wuyuan
Published: August 2010

Human T‐cell leukemia virus 1 (HTLV‐1) protease, a member of the aspartic acid protease family, plays critical roles in the pathogenesis of the virus and is an attractive viral target for therapeutic intervention. HTLV‐1 protease consists of 125 amino acid residues and functions as a homodimer stabilized in part by a four‐stranded β‐sheet comprising the N‐ and C‐termini. Compared with many other viral proteases such as HIV‐1 protease, HTLV‐1 protease is elongated by an extra 10 amino acid residue “tail” at the C‐terminus. The structural and functional role of the extra C‐terminal residues in the catalysis of HTLV‐1 protease has been a subject of debate for years. Using the native chemical ligation technique pioneered by Kent and coworkers, we chemically synthesized a full‐length HTLV protease and a C‐terminally truncated form encompassing residues 1‐116. Enzyme kinetic analysis using three different peptide substrates indicated that truncation of the C‐terminal tail lowered the turnover number of the viral enzyme by a factor of 2 and its catalytic efficiency by roughly 10‐fold. Our findings differ from the two extreme views that the C‐terminal tail of HTLV‐1 protease is either fully dispensable or totally required for enzyme dimerization and/or catalysis. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 487–494, 2010.
Protecting group variations of δ‐mercaptolysine useful in chemical ubiquitylation
Authors: Haj‐Yahya Mahmood , Ajish Kumar K. S. , Erlich Lesly A. , Brik Ashraf
Published: August 2010

The high efficiency and chemoselectivity of peptide ubiquitylation that is achieved using the δ‐mercaptolysine prompted us to expand the scope of this residue in various ligation schemes. In this report, we demonstrate the synthesis of five analogues of this important amino acid bearing a variety of protecting groups, which is essential in sequential peptide ligation and ubiquitylation. The key‐step in the synthesis is the nucleophilic 1,4‐addition of a variety of thiols on a nitro olefin scaffold. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 504–510, 2010.
Synthesis and characterization of ester‐based prodrugs of glucagon‐like peptide 1
Authors: De Arnab , DiMarchi Richard D.
Published: August 2010

Peptides represent a rich natural source of potential medicines with one notable pharmaceutical limitation being their relatively short duration of action. A particularly good example of this phenomenon is glucagon‐like peptide 1 (GLP), a hormone of appreciable interest for the treatment of type II diabetes. In the native form, GLP demonstrates an extremely short half‐life in plasma and a relatively narrow therapeutic index with gastrointestinal adverse pharmacology. We envisioned a prodrug of GLP as a means to extend the duration of action and broaden the therapeutic index of this peptide hormone. We designed, synthesized, and characterized ester‐based prodrugs of GLP that differentially convert to the parent drug under physiological conditions driven by their inherent chemical instability. In a set of dipeptide extended GLP‐analogs we explored the rate of diketopiperazine (DKP) and diketomorpholine (DMP) formation, and the release of the active peptide. The rate of cleavage was observed to be a function of the conformation of the dipeptide promoiety and the strength of the cyclization nucleophile. Through the careful selection of chemical functionality, a set of GLP ester prodrugs of variable half‐lives has been identified. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 448–456, 2010.
Biological activity of laminin peptide‐conjugated alginate and chitosan matrices
Authors: Yamada Yuji , Hozumi Kentaro , Katagiri Fumihiko , Kikkawa Yamato , Nomizu Motoyoshi
Published: August 2010

Laminin active peptide‐conjugated chitosan mambranes have been previously demonstrated as a useful biomaterial for tissue engineering. Here, three laminin active peptides, A99 (AGTFALRGDNPQG), AG73 (RKRLQVQLSIRT), and EF1zz (ATLQLQEGRLHFXFDLGKGR, X: Nle), which interact with integrin αvβ3, syndecans, and integrin α2β1, respectively, were conjugated to alginate and evaluated the biological activities. A99‐alginate (3–3000 ng/mm2) promoted cell attachment depending on the amount of alginate. More than 300 ng/mm2 of the A99‐alginate matrices effectively promoted cell attachment, cell spreading with well‐organized actin stress fibers, and neurite outgrowth. AG73‐ and EF1zz‐alginates promoted strong cell attachment at the all amounts (3–3000 ng/mm2). A99‐alginate (30–3000 ng/mm2) promoted strong neurite outgrowth but lower amounts of A99‐alginate (3 ng/mm2) showed weak activity. In contrast, AG73‐alginates (3–30 ng/mm2) showed strong neurite outgrowth activity but higher amounts of AG73‐alginate (300–3000 ng/mm2) decreased the activity. These data indicate that neurite outgrowth activity of peptide‐alginate matrices is peptide specific and the activity is dependent on the amount of alginate. Further, biological activities of the peptides on alginate and chitosan matrices were different, suggesting that the integrin‐ and syndecan‐mediated cellular functions on the peptide‐matrices are highly influenced by the scaffold structure including polysaccharide types and amounts. The laminin active peptide‐conjugated alginate and chitosan matrices can control receptor type specific functions and are useful for tissue engineering. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 711–720, 2010.

This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
Tryptophan residues: Scarce in proteins but strong stabilizers of β‐hairpin peptides
Authors: Santiveri Clara M. , Jiménez M. Angeles
Published: August 2010

Tryptophan plays important roles in protein stability and recognition despite its scarcity in proteins. Except as fluorescent groups, they have been used rarely in peptide design. Nevertheless, Trp residues were crucial for the stability of some designed minimal proteins. In 2000, Trp–Trp pairs were shown to contribute more than any other hydrophobic interaction to the stability of β‐hairpin peptides. Since then, Trp–Trp pairs have emerged as a paradigm for the design of stable β‐hairpins, such as the Trpzip peptides. Here, we analyze the nature of the stabilizing capacity of Trp–Trp pairs by reviewing the β‐hairpin peptides containing Trp–Trp pairs described up to now, the spectroscopic features and geometry of the Trp–Trp pairs, and their use as binding sites in β‐hairpin peptides. To complete the overview, we briefly go through the other relevant β‐hairpin stabilizing Trp–non‐Trp interactions and illustrate the use of Trp in the design of short peptides adopting α‐helical and mixed α/β motifs. This review is of interest in the field of rational design of proteins, peptides, peptidomimetics, and biomaterials. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 779–790, 2010.

This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
Building a bridge between peptide chemistry and organic chemistry: Intramolecular macrocyclization reactions and supramolecular chemistry with helical peptide substrates
Authors: Moretto Alessandro , Crisma Marco , Formaggio Fernando , Toniolo Claudio
Published: August 2010

In our ongoing efforts to build a bridge between peptide chemistry and organic chemistry, we are currently investigating: (1) two types of intramolecular macrocyclization reactions in 310‐helical peptides, and (2) a peptido[2]rotaxane molecular machine as a supramolecular tool using a 310‐helical peptide as the axle. More specifically, we studied the following two reactions: (a) the intramolecular ring‐closing olefin metathesis between two amino acid residues with side chains bearing an allyl group, and (b) the intramolecular Paternò‐Yang photoreaction, using a benzophenone‐based amino acid as a photoaffinity reagent for a Met residue. Both reactions involve formation of a new CC bond. As for the supramolecular system examined, we were able to identify the two stations of a new peptido[2]rotaxane characterized by an ‐(Aib)6‐ axle and to reversibly switch the aromatic tetramide macrocyclic wheel from one station to the next. This article summarizes the information available in the literature from other groups and the published/unpublished data originated from our laboratory on these research areas. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 721–732, 2010.

This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
Synthetic diastereomeric‐antimicrobial peptide: Antibacterial activity against multiple drug resistant clinical isolates
Authors: Park Seong‐Cheol , Kim Jin‐Young , Lee Jong‐Kook , Yoo Suyeon , Kim Hyunjoong , Seo Chang Ho , Nah Jae‐Woon , Hahm Kyung‐Soo , Park Yoonkyung
Published: August 2010

Increasing resistance of pathogenic bacteria to antibiotics is a serious problem in health care system and has intensified the search for potent novel drugs. Cationic antibacterial peptides are the most abundant antibiotics in nature and have been frequently proposed as new anti‐infective agents. In this study, a set of diastereomeric peptides is researched about their antibiotic activity against multiple drug resistant clinical isolates and their modes of action against gram‐positive cocci. MIC was suggested by the NCCLS against ten clinically isolated antibiotic‐resistant strains. Mode of action studies included killing kinetics and a series of experiments designed to characterize the impact of the diastereomeric peptides on bacterial membranes. The tested diastereomers displayed high antimicrobial and broad spectrum activity with D‐P5‐18mer. The antimicrobial activity of diastereomeric‐P5‐18mer was two times stronger against gram‐negative bacteria than either CA‐MA‐20mer or P5‐18mer. When tested against ten clinically isolated antibiotic‐resistant strains in the presence of 0, 150, or 300 mM NaCl, diastereomeric‐P5‐18mer retained strong activity against all bacteria, yet showed little or no cytotoxicity against the HaCaT human keratinocyte cell line. Finally, D‐P5‐18mer showed resistance against trypsin digestion unlike other analogues. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 96: 130–136, 2011.
Native chemical ligation with Nα acyl transfer auxiliaries
Authors: Offer John
Published: August 2010

Native chemical ligation (NCL) is a simple procedure that enables synthetic access to many proteins and is increasingly harnessed to study protein structure and function. However, the generality of this method is limited by the requirement for cysteine residues suitably positioned throughout the target protein. Auxiliary approaches have been developed to overcome this limitation, wherein a removable group is introduced at the amino terminus of a peptide conveying ligation properties comparable to cysteine. Present auxiliary approaches combine the thioester exchange concept applied first in NCL with a number of acyl transfer reactions first systematically explored by Kemp and coworkers. The current methods for auxiliary mediated ligation appear promising for the synthesis of proteins and in particular post‐translational modified proteins. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 530–541, 2010.
Posttranslationally modified peptides efficiently mimicking neoantigens: A challenge for theragnostics of autoimmune diseases
Authors: Nuti Francesca , Peroni Elisa , Real‐Fernández Feliciana , Bonache M. Angeles , Le Chevalier‐Isaad Alexandra , Chelli Mario , Lubin‐Germain Nadège , Uziel Jacques , Rovero Paolo , Lolli Francesco , Papini Anna Maria
Published: August 2010

We report the design, synthesis, and immunological evaluation of a series of glycopeptide analogues of the previously described antigenic probe CSF114(Glc), with the aim of understanding the importance of N‐glycosylation on Asn residue in multiple sclerosis antibody recognition. The glucopeptide, characterized by a β‐turn conformation which is fundamental for a correct presentation of the epitope, has been modified by introducing various natural glycoamino acids in position 7. The new glycopeptides were evaluated by measuring the IgG and IgM antibody titer in multiple sclerosis patients' and normal blood donors' sera. Moreover, we achieved the efficient synthetic strategy of new Asn derivative bearing N‐acetylneuraminic acid (Neu5Ac), linked by an N‐glycosidic bond, on the side chain of the Asn residue orthogonally protected for Fmoc/tBu SPPS. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 791–799, 2010.

This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
The influence of incorporating lipids or liposaccharides on the particle size of peptide therapeutics
Authors: Coles Daniel J. , Simerska Pavla , Fujita Yoshio , Toth Istvan
Published: August 2010

The characterization of peptide‐based drugs is essential to obtain information about their potential suitability. In this study, a therapeutic peptide epitope alone or in combination with a lipid or liposaccharide moiety were assessed to determine their particle sizes by diffusion ordered NMR spectroscopy, dynamic light scattering, and mathematical expressions. These methods were compared and their suitability for different types of peptides is discussed herein. When compared with the mathematical expressions, we found that the NMR method resulted in a particle size that was consistent with the radius of the peptide monomer. The dynamic light scattering method showed that when lipids were conjugated to the peptide epitope, the resulting particles had a larger sized distribution compared with the peptide alone. These experiments provided information which can be applied when formulating these peptides as drugs. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 96: 172–176, 2011.
Design and conformational analysis of natively folded β‐hairpin peptides stabilized by nucleobase interactions
Authors: Uozumi Ryuichi , Takahashi Tsuyoshi , Yamazaki Toshimasa , Granholm Viktor , Mihara Hisakazu
Published: August 2010

To examine stabilizing effects of the base pair interaction on a protein scaffold, various peptides with L‐α‐amino acids bearing a nucleobase in the side chain (nucleobase amino acids; NBAs) were designed based on a G‐peptide β‐hairpin structure, and their conformational properties were investigated by circular dichroism and NMR spectroscopy. Thermodynamic analyses based on the chemical shifts showed that adenine‐thymine pairing in a diagonal fashion at positions 4 and 15 (2AT) enhanced thermal stability of the peptide conformation by more than 30 K as compared with the wild‐type G‐peptide. In NOESY spectrum, not only numerous nonadjacent crosspeaks but also long‐range crosspeaks between the nucleobases were observed in some peptides with the base pairing. NMR structure calculations of the 2AT peptide confirmed that cross‐strand pairing of the nucleobases occurs on the well‐defined β‐hairpin structure as designed. Taken together, the base pairing in an appropriate position and orientation facilitates folding and stabilization of a native‐like β‐hairpin structure. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 830–842, 2010.

This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com
Design and development of analogues of dimers of insulin‐like peptide 3 B‐chain as high‐affinity antagonists of the RXFP2 receptor
Authors: Shabanpoor Fazel , Zhang Suode , Hughes Richard A. , Hossain Mohammed Akhter , Layfield Sharon , Ferraro Tania , Bathgate Ross A. D. , Separovic Frances , Wade John D.
Published: August 2010

Insulin‐like peptide 3 (INSL3) is one of 10 members of the human relaxin–insulin superfamily of peptides. It is a peptide hormone that is expressed by fetal and postnatal testicular Leydig cells and postnatal ovarian thecal cells. It mediates testicular descent during fetal life and suppresses sperm apoptosis in adult males, whereas, in females, it causes oocyte maturation. INSL3 has also been shown to promote thyroid tumor growth and angiogenesis in human. These actions of INSL3 are mediated through its G protein‐coupled receptor, RXFP2. INSL3, a two‐chained peptide, binds to its receptor primarily via its B‐chain, whereas elements of the A‐chain are essential for receptor activation. In an attempt to design a high‐affinity antagonist with potential clinical application as an anticancer agent as well as a contraceptive, we have previously prepared a synthetic parallel dimer of INSL3 B‐chain and demonstrated that it binds to RXFP2 with high affinity. In this work, we undertook full pharmacological characterization of this peptide and show that it can antaogonize INSL3‐mediated cAMP signaling through RXFP2. Further refinement by truncation of 18 residues yielded a minimized analogue that retained full binding affinity and INSL3 antagonism. It is an attractive lead peptide for in vivo evaluation as an inhibitor of male and female fertility and of INSL3‐mediated carcinogenesis. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 96: 81–87, 2011.
Deletion of Ac‐NMePhe1 from [NMePhe1]arodyn under acidic conditions, part 2: Effects of cleavage conditions and N‐terminal functionality
Authors: Fang Wei‐Jie , Bennett Marco A. , Aldrich Jane V.
Published: August 2010

Peptides containing N‐methylamino acids can exhibit improved pharmacodynamic and pharmacokinetic profiles compared to nonmethylated peptides, and therefore interest in these N‐methylated peptides has been increasing in recent years. Arodyn (Ac[Phe1,2,3,Arg4,D‐Ala8]Dyn A(1–11)NH2) is an acetylated dynorphin A (Dyn A) analog that is a potent and selective κ opioid receptor antagonist (Bennett et al., J Med Chem 2002, 45, 5617), and its analog [NMePhe1]arodyn shows even higher affinity and selectivity for κ opioid receptors (Bennett et al., J Pept Res 2005, 65, 322). During the synthesis of [NMePhe1]arodyn analogs, the arodyn‐(2–11) derivatives were obtained as major products. Analysis indicated that Ac‐NMePhe was lost from the completed peptide sequence during acidic cleavage of the peptides from the resin and that the acetyl group played an important role in this side reaction. Different cleavage conditions were evaluated to minimize this side reaction and maximize the yield of pure [NMePhe1]arodyn analogs. Modifications to the N‐terminus of the peptides to prevent the side reaction were also explored. The incorporation of a heteroatom‐containing group such as methoxycarbonyl as the N‐terminal functionality prevented this side reaction, while the incorporation of a bulky acyl group could not. Substituting NMePhe with the conformationally constrained analog Tic (1,2,3,4‐tetrahydroisoquinoline‐3‐carboxylic acid) also prevented the side reaction. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 96: 97–102, 2011.
p‐Nitrobenzyl protection for cysteine and selenocysteine: A more stable alternative to the acetamidomethyl group
Authors: Muttenthaler Markus , Ramos Yesica Garcia , Feytens Debby , de Araujo Aline D. , Alewood Paul F.
Published: August 2010

This study evaluated the acidic lability of the acetamidomethyl (Acm), trimethylacetamidomethyl (Tacm), and thep‐nitrobenzyl (pNB) as protecting groups for cysteine and selenocysteine (Sec) during thetert‐butyloxycarbonyl (Boc)‐chemistry solid‐phase peptide synthesis of oxytocin (OT). Two novel Sec building blocks (Nα‐tert‐butyloxycarbonyl‐Se(acetamidomethyl)‐L‐selenocysteine (Boc‐L‐Sec(Acm)‐OH) andNα‐tert‐butyloxycarbonyl‐S(4‐nitrobenzyl)‐L‐selenocysteine (Boc‐L‐Sec(pNB)‐OH)) were developed for this study. Six partially protected thio‐ and seleno‐OT analogues were synthesized, purified, and exposed to neat trifluoroacetic acid (TFA) at temperatures of 25, 40, 50, and 60°C for 1 h, and HF treatment at 0°C for 1 h. Significant losses were observed for the Acm and Tacm group in TFA at temperatures greater than 25°C and during HF treatment at 0°C, whereas thepNB group remained intact. Removal of thepNB was achieved via reduction to thep‐aminobenzyl group either with zinc in acetic acid in solution or via tin chloride in hydrochloric acid on solid support, followed by oxidative cleavage with iodine yielding the corresponding disulfide or diselenide bond. No major side reactions were observed. This study confirms the occasionally described Acm instability and underpins the development of thepNB group as an alternative for cysteine and Sec protection. © 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 423–432, 2010.
Water Stable Zr–Benzenedicarboxylate Metal–Organic Frameworks as Photocatalysts for Hydrogen Generation
Authors: Gomes Silva Cláudia , Luz Ignacio , Llabrés i Xamena Francesc X. , Corma Avelino , García Hermenegildo
Published: August 2010

The Zr‐containing metal–organic frameworks (MOFs) formed by terephthalate (UiO‐66) and 2‐aminoterephthalate ligands [UiO‐66(NH2)] are two notably water‐resistant MOFs that exhibit photocatalytic activity for hydrogen generation in methanol or water/methanol upon irradiation at wavelength longer than 300 nm. The apparent quantum yield for H2 generation using monochromatic light at 370 nm in water/methanol 3:1 was of 3.5 % for UiO‐66(NH2). Laser‐flash photolysis has allowed detecting for UiO‐66 and UiO‐66(NH2) the photochemical generation of a long lived charge separated state whose decay is not complete 300 μs after the laser flash. Our finding and particularly the influence of the amino group producing a bathochromic shift in the optical spectrum without altering the photochemistry shows promises for the development of more efficient MOFs for water splitting.
Synthesis and Conformational Characterisation of Hexameric β‐Peptide Foldamers by Using Double POAC Spin Labelling and cw‐EPR
Authors: Wright Karen , Wakselman Michel , Mazaleyrat Jean‐Paul , Franco Lorenzo , Toffoletti Antonio , Formaggio Fernando , Toniolo Claudio
Published: August 2010

A selected set of terminally protected β‐hexapeptides, each containing two nitroxide‐based (3R,4R)‐4‐amino‐1‐oxyl‐2,2,5,5‐tetramethylpyrrolidine‐3‐carboxylic acid (POAC) residues combined with four (1S,2S)‐2‐aminocyclopentane‐1‐carboxylic acid (ACPC) residues, was synthesised by using solution methods and was fully characterised. The two POAC residues are separated in the sequences by different numbers of intervening ACPC residues. The conformational features of the doubly spin‐labelled β‐hexapeptides were examined in chloroform by FTIR absorption and continuous‐wave electron paramagnetic resonance spectroscopic techniques. In particular, the biradical exchange coupling (J) between two POAC residues within each peptide indicates unambiguously that the secondary structure overwhelmingly adopted is the 12‐helix. Taken together, these results support the view that POAC is an excellent β‐amino acid for exploring this type of helical conformation in doubly labelled β‐peptides.
ChemInform Abstract: Na8Au11In6: A Gold Indium Polyhedra Framework with Pentagonal Bipyramidal AuAu5In Building Units.
Authors: ZACHWIEJA U.
Published: August 2010

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.
ChemInform Abstract: A New Layer‐Structured Nitride Superconductor. Lithium‐Intercalated β‐Zirconium Nitride Chloride, LixZrNCl.
Authors: YAMANAKA S. , KAWAJI H. , HOTEHAMA K. , OHASHI M.
Published: August 2010

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.
ChemInform Abstract: Nickel Catalysts for Internal Reforming in Molten Carbonate Fuel Cells
Authors: BERGER R. J. , DOESBURG E. B. M. , VAN OMMEN J. G. , ROSS J. R. H.
Published: August 2010

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.
ChemInform Abstract: Synthesis and Structure of Cyclic Selenium Oxide SeVISeIV2O7.
Authors: TOUZIN J. , KILIAN P. , ZAK Z.
Published: August 2010

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.
ChemInform Abstract: Ground‐State Stereoelectronic Effects Involving Silicon and Germanium: A Comparison of the Effects of Germanium and Silicon Substituents on C‐ O Bond Lengths at the β‐Position.
Authors: CHAN V. Y. , CLARK C. I. , GIORDANO J. , GREEN A. J. , KARALIS A. , WHITE J. M.
Published: August 2010

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.
ChemInform Abstract: Soluble Polymer‐Bound Ligand‐Accelerated Catalysis: Asymmetric Dihydroxylation.
Authors: HAN H. , JANDA K. D.
Published: August 2010

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.
ChemInform Abstract: Intramolecular (2 + 2) Photocycloaddition of N‐Alkenoyl‐β‐ enaminones.
Authors: AMOUGAY A. , PETE J.‐P. , PIVA O.
Published: August 2010

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.
ChemInform Abstract: Synthesis of a Water‐Soluble Conjugated (3)Rotaxane.
Authors: ANDERSON S. , ANDERSON H. L.
Published: August 2010

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.
ChemInform Abstract: Synthesis of (.+‐.)‐trans‐Cyclopropane‐1,2‐N,N′‐dinitroamine and Its Derivatives
Authors: IVSHIN V. P. , KOMELIN M. S.
Published: August 2010

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.
ChemInform Abstract: A General and Convenient Synthetic Method of Geometrically Pure (Z)‐1‐ Bromo‐1‐alkenes.
Authors: UENISHI J. , KAWAHAMA R. , SHIGA Y. , YONEMITSU O. , TSUJI J.
Published: August 2010

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.
ChemInform Abstract: Synthesis of Phenolic Biaryls and p‐Terphenyls and Their Heteroaromatic Analogues via a Cycloaddition Route Using 4‐Aryl‐2‐ silyloxybuta‐1,3‐dienes and Electron‐Deficient Alkynes.
Authors: YAMAMOTO Y. , NUNOKAWA K. , OHNO M. , EGUCHI S.
Published: August 2010

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.
ChemInform Abstract: The First Optically Active and Sterically Regular Poly(1,1′‐bi‐2‐ naphthol)s: Precursors to a New Generation of Polymeric Catalysts.
Authors: HU Q. S. , ZHENG X.‐F. , PU L.
Published: August 2010

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.
ChemInform Abstract: Intramolecular 1,6‐Conjugate Addition Approach for Construction of the Hydrindan Framework: Total Synthesis of (.+‐.)‐Coronafacic Acid.
Authors: NARA S. , TOSHIMA H. , ICHIHARA A.
Published: August 2010

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.
ChemInform Abstract: Novel Enantioselective Approach to γ‐Lactams from Chiral Enol Ethers: Synthesis of (‐)‐Statine.
Authors: NEBOIS P. , GREENE A. E.
Published: August 2010

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.
ChemInform Abstract: The Thermal Rearrangement of N‐Alkyl‐N‐vinylpropargylamines into 2‐ Methylpyrroles. A New Synthesis of Annulated(b)pyrroles.
Authors: COSSY J. , POITEVIN C. , SALLE L. , GOMEZ PARDO D.
Published: August 2010

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.
ChemInform Abstract: Formation of Benzofuran and 2H‐Chromene Structures During One Reaction. A New Synthesis of 2H‐Chromene Derivatives.
Authors: UKHIN L. YU. , ORLOVA ZH. I. , SHISHKIN O. V. , STRUCHKOV YU. T.
Published: August 2010

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.
ChemInform Abstract: A Convenient Synthesis of Diastereomeric Synthons: Ethyl 3‐Methyl‐1,2, 3,4‐tetrahydroisoquinoline‐1‐acetates by Direct and Reverse Substituent Introductions.
Authors: FUELOEP F. , TARI J. , BERNATH G. , SOHAR P.
Published: August 2010

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.
ChemInform Abstract: A Convenient Way to Dibenzo(c,h)‐1,5‐naphthyridines (11‐Aza‐benzo(c) phenanthridines).
Authors: BISAGNI E. , LANDRAS C. , THIROT S. , HUEL C.
Published: August 2010

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.
ChemInform Abstract: Synthesis of Homohydantoin‐Thiazolidine Bicyclic Compounds.
Authors: HATAM M. , KOEPPER S. , MARTENS J.
Published: August 2010

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.