Design and synthesis of a screening library using the natural product scaffold 3-chloro-4-hydroxyphenylacetic acid

The fungal metabolite 3-chloro-4-hydroxyphenylacetic acid (1) was utilized in the generation of a unique drug-like screening library using parallel solution-phase synthesis. A 20-membered amide library (3–22) was generated by first converting 1 to methyl (3-chloro-4-hydroxyphenyl)acetate (2), then reacting this scaffold with a diverse series of primary amines via a solvent-free aminolysis procedure. The structures of the synthetic analogues (3–22) were elucidated by spectroscopic data analysis. The structures of compounds 8, 12, and 22 were confirmed by single X-ray crystallographic analysis. All compounds were evaluated for cytotoxicity against a human prostate cancer cell line (LNCaP) and for antiparasitic activity toward Trypanosoma brucei brucei and Plasmodium falciparum and showed no significant activity at 10 μM. The library was also tested for effects on the lipid content of LNCaP and PC-3 prostate cancer cells, and it was demonstrated that the fluorobenzyl analogues (12–14) significantly reduced cellular phospholipid and neutral lipid levels.

Knowledge unlatched: A global library consortium model for funding open access scholarly books: Full report on the Proof of Concept Pilot 2014

This special issue of Cultural Science Journal is devoted to the report of a groundbreaking experiment in re-coordinating global markets for specialist scholarly books and enabling the knowledge commons: the Knowledge Unlatched proof-of-concept pilot. The pilot took place between January 2012 and September 2014. It involved libraries, publishers, authors, readers and research funders in the process of developing and testing a global library consortium model for supporting Open Access books. The experiment established that authors, librarians, publishers and research funding agencies can work together in powerful new ways to enable open access; that doing so is cost effective; and that a global library consortium model has the potential dramatically to widen access to the knowledge and ideas contained in book-length scholarly works.

Establishing a participatory library model: A Grounded Theory study

Purpose The purpose of this research is to explore the idea of the participatory library in higher education settings. This research aims to address the question, what is a participatory university library? Design/methodology/approach Grounded theory approach was adopted. In-depth individual interviews were conducted with two diverse groups of participants including ten library staff members and six library users. Data collection and analysis were carried out simultaneously and complied with Straussian grounded theory principles and techniques. Findings Three core categories representing the participatory library were found including “community”, “empowerment”, and “experience”. Each category was thoroughly delineated via sub-categories, properties, and dimensions that all together create a foundation for the participatory library. A participatory library model was also developed together with an explanation of model building blocks that provide a deeper understanding of the participatory library phenomenon. Research limitations The research focuses on a specific library system, i.e., academic libraries. Therefore, the research results may not be very applicable to public, special, and school library contexts. Originality/value This is the first empirical study developing a participatory library model. It provides librarians, library managers, researchers, library students, and the library community with a holistic picture of the contemporary library.

(Digital library) education or (digital) library education? An Australian perspective

Education for Library and Information professionals in the digital environment has been an important discussion point the world over. However, before designing and implementing a programme for digital library education, it is prudent that the skills and knowledge required to work in this environment are identified to enable informed decisions to be made. Hitherto, there has been very little research which has sought the opinion of both educators and practitioners on this topic, and none with a wide geographical coverage of Australia. This paper presents the key findings of research undertaken at Tallinn University in the first half of 2009.

Using a free online questionnaire to determine the skills, competencies and knowledge required to work in a digital library environment in Australia

This paper discusses the data collection technique used to determine the skills and knowledge required of academic librarians working in a digital library environment in Australia. The research was undertaken as part of the researcher’s master’s thesis conducted at Tallinn University. The data collection instrument used was a freely available online survey tool, and its advantages and disadvantages are discussed in terms of the desired outcomes and circumstances surrounding the thesis project. Decisions regarding the design of the questionnaire are also discussed.

The Library beyond (just) the book: Collaboration and co-working spaces for new technology and new technological practices

Libraries have often been first adopters of many new technological innovations, such as, punch cards, computers, barcodes, and e-book readers. It is thus not surprising that many libraries have embraced the advent of the internet as an opportunity to move away from just being repositories of books, towards becoming ideas stores and local network hubs for entrepreneurial thinking and new creative practices. This presentation will look at the case of “The Edge” – an initiative of the State Library of Queensland in Brisbane, Australia, to establish a digital culture centre and learning environment deliberately designed for the co-creation and co-construction of knowledge. This initiative illustrates the potential role of libraries as testing grounds for new technologies and technological practices, which is particularly relevant in the context of the NBN rollout across Australia. It also provides an example of new engagement strategies for innovative co-working spaces that are a vital element in a trend that sees professionals, creatives and designers leave their traditional places of work and embrace the city as their office.

Funding the academic library: An ethnographic study

This thesis is an ethnographic study of social psychological theories of influence and persuasion in higher education decision making processes. It focuses on the academic library and the budget allocation process in one study site. The findings show that influence tactics such as liking, reciprocity and social proof are important elements in the interpersonal relationships which impact decisions. The researcher was able to determine and propose practical applications for academic library administrators and library and information science educators.

A happy compromise: Collaborative approaches to school library designing

Designing a school library is a complex, costly and demanding process with important educational and social implications for the whole school community. Drawing upon recent research, this paper presents contrasting snapshots of two school libraries to demonstrate the impacts of greater and lesser collaboration in the designing process. After a brief literature review, the paper outlines the research design (qualitative case study, involving collection and inductive thematic analysis of interview data and student drawings). The select findings highlight the varying experiences of each school’s teacher-librarian through the four designing phases of imagining, transitioning, experiencing and reimagining. Based on the study’s findings, the paper concludes that design outcomes are enhanced through collaboration between professional designers and key school stakeholders including teacher-librarians, teachers, principals and students. The findings and recommendations are of potential interest to teacher-librarians, school principals, education authorities, information professionals and library managers, to guide user-centred library planning and resourcing.

Characterization of novel microsatellite markers derived from Korean rose bitterling (Rhodeus uyekii) genomic library

Korean rose bitterling (Rhodeus uyekii) is a freshwater fish endemic to Korea. Natural populations of this species have experienced severe declines as a result of habitat fragmentation and water pollution. To conserve and restore R. uyekii, the genetic diversity of this species needs to be assessed at the population level. Eighteen novel polymorphic microsatellite loci for R. uyekii were developed using an enriched partial genomic library. Polymorphisms at these loci were studied in 150 individuals collected from three populations. The number of alleles at each locus ranged from 3 to 47 (mean = 17.1). Within the populations, the observed heterozygosity ranged from 0.032 to 1.000, expected heterozygosity from 0.082 to 0.967, and polymorphism information content from 0.078 to 0.950. Six loci showed significant deviation from Hardy-Weinberg equilibrium after Bonferroni’s correction, and no significant linkage disequilibrium was detected between most locus pairs, except in three cases. These highly informative microsatellite markers should be useful for genetic population structure analyses of R. uyekii.

Australian Library and Information Association (ALIA)

The Australian Library and Information Association (ALIA) is the professional association for the Australian library and information services sector. It seeks to empower the profession in the development, promotion and delivery of quality library and information services to the nation, through leadership, advocacy, and mutual support. The ALIA represents the interest of 6000 members, the profession and Australia's 12 million library users. The objects of the Association are listed in its constitution. They are To promote the free flow of information and ideas in the interest of all Australians and a thriving culture, economy, and democracy. To promote and improve the services provided by all kinds of library and information agencies. To ensure the high standard of personnel engaged in information provision and foster their professional interests and aspirations. To represent the interests of members to governments, other organizations, and the community. To encourage people to contribute to the improvement of library and information services through support and membership of the association.

Two monoclonal antibodies to precisely the same epitope of type ii collagen select non-crossreactive phage clones by phage display: Implications for autoimmunity and molecular mimicry

Two monoclonal antibodies (mAb) CB268 and CII-C1 to type II collagen (CII) react with precisely the same conformational epitope constituted by the residues ARGLT on the three chains of the CII triple helix. The antibodies share structural similarity, with most differences in the complementarity determining region 3 of the heavy chain (HCDR3). The fine reactivity of these mAbs was investigated by screening two nonameric phage-displayed random peptide libraries. For each mAb, there were phage clones (phagotopes) that reacted strongly by ELISA only with the selecting mAb, and inhibited binding to CII only for that mAb, not the alternate mAb. Nonetheless, a synthetic peptide RRLPFGSQM corresponding to an insert from a highly reactive CII-C1-selected phagotope, which was unreactive (and non-inhibitory) with CB268, inhibited the reactivity of CB268 with CII. Most phage-displayed peptides contained a motif in the first part of the molecule that consisted of two basic residues adjacent to at least one hydrophobic residue (e.g. RRL or LRR), but the second portion of the peptides differed for the two mAbs. We predict that conserved CDR sequences interact with the basic-basic-hydrophobic motif, whereas non-conserved amino acids in the binding sites (especially HCDR3) interact with unique peptide sequences and limit cross-reactivity. The observation that two mAbs can react identically with a single epitope on one antigen (CII), but show no cross-reactivity when tested against a second (phagotope) indicates that microorganisms could exhibit mimics capable of initiating autoimmunity without this being evident from conventional assays.

A novel grass pollen allergen mimotope identified by phage display peptide library inhibits allergen-human IgE antibody interaction

The aim of this study was to investigate the molecular basis of human IgE-allergen interaction by screening a phage-displayed peptide library with an allergen-specific human IgE-mimicking monoclonal antibody (mAb). A mAb that reacted with major grass pollen allergens was successfully identified and shown to inhibit human IgE-allergen interaction. Biopanning of a phage-displayed random peptide library with this mAb yielded a 12 amino acid long mimotope. A synthetic peptide based on this 12-mer mimotope inhibited mAb and human IgE binding to grass pollen extracts. Our results indicate that such synthetic peptide mimotopes of allergens have potential as novel therapeutic agents. © 2001 Published by Elsevier Science B.V. on behalf of the Federation of European Biochemical Societies.

Monoclonal antibody screening of a phage-displayed random peptide library reveals mimotopes of chemokine receptor CCR5: Implications for the tertiary structure of the receptor and for an n-terminal binding site for HIV-1 gp120

The chemokine receptor CCR5 contains seven transmembrane-spanning domains. It binds chemokines and acts as co-receptor for macrophage (m)-tropic (or R5) strains of HIV-1. Monoclonal antibodies (mAb) to CCR5, 3A9 and 5C7, were used for biopanning a nonapeptide cysteine (C)-constrained phage-displayed random peptide library to ascertain contact residues and define tertiary structures of possible epitopes on CCR5. Reactivity of antibodies with phagotopes was established by enzyme-linked immunosorbent assay (ELISA). mAb 3A9 identified a phagotope C-HASIYDFGS-C (3A9/1), and 5C7 most frequently identified C-PHWLRDLRV-C (5C7/1). Corresponding peptides were synthesized. Phagotopes and synthetic peptides reacted in ELISA with corresponding antibodies and synthetic peptides inhibited antibody binding to the phagotopes. Reactivity by immunofluorescence of 3A9 with CCR5 was strongly inhibited by the corresponding peptide. Both mAb 3A9 and 5C7 reacted similarly with phagotopes and the corresponding peptide selected by the alternative mAb. The sequences of peptide inserts of phagotopes could be aligned as mimotopes of the sequence of CCR5. For phage 3A9/1, the motif SIYD aligned to residues at the N terminus and FG to residues on the first extracellular loop; for 5C7/1, residues at the N terminus, first extracellular loop, and possibly the third extracellular loop could be aligned and so would contribute to the mimotope. The synthetic peptides corresponding to the isolated phagotopes showed a CD4-dependent reactivity with gp120 of a primary, m-tropic HIV-1 isolate. Thus reactivity of antibodies raised to CCR5 against phage-displayed peptides defined mimotopes that reflect binding sites for these antibodies and reveal a part of the gp120 binding sites on CCR5.

Use of phage display technology to investigate allergen-antibody interactions

Phage display is an advanced technology that can be used to characterize the interactions of antibody with antigen at the molecular level. It provides valuable data when applied to the investigation of IgE interaction with allergens. The aim of this rostrum article is to provide an explanation of the potential of phage display for increasing the understanding of allergen- IgE interaction, the discovery of diagnostic reagents, and the development of novel therapeutics for the treatment of allergic disease. The significance of initial studies that have applied phage display technology in allergy research will be highlighted. Phage display has been used to clone human IgE to timothy grass pollen allergen Phl p 5, to characterize the epitopes for murine and human antibodies to a birch pollen allergen Bet v 1, and to elucidate the epitopes of a murine mAb to the house dust mite allergen Der p 1. The technology has identified peptides that functionally mimic sites of human IgE constant domains and that were used to raise antiserum for blocking binding of IgE to the FcεRI on basophils and subsequent release of histamine. Phage display has also been used to characterize novel peanut and fungal allergens. The method has been used to increase our understanding of the molecular basis of allergen-IgE interactions and to develop clinically relevant reagents with the pharmacologic potential to block the effector phase of allergic reactions. Many advances from these early studies are likely as phage display technology evolves and allergists gain expertise in its research applications.

Indonesian library and information science professionals’ understanding of Library 2.0: A pilot study

The literature around Library 2.0 remains largely theoretical with few empirical studies and is particularly limited in developing countries such as Indonesia. This study addresses this gap and aims to provide information about the current state of knowledge on Indonesian LIS professionals’ understanding of Library 2.0. The researchers used qualitative and quantitative approaches for this study, asking thirteen closed- and open-ended questions in an online survey. The researchers used descriptive and in vivo coding to analyze the responses. Through their analysis, they identified three themes: technology, interactivity, and awareness of Library 2.0. Respondents demonstrated awareness of Library 2.0 and a basic understanding of the roles of interactivity and technology in libraries. However, overreliance on technology used in libraries to conceptualize Library 2.0 without an emphasis on its core characteristics and principles could lead to the misalignment of limited resources. The study results will potentially strengthen the research base for Library 2.0 practice as well as inform LIS curriculum in Indonesia so as to develop practitioners who are able to adapt to users’ changing needs and expectations. It is expected that the preliminary data from this study could be used to design a much larger and more complex future research project in this area.