1,721,031 research outputs found
A Role for Metal-Based Drugs in Fighting COVID-19 Infection? The Case of Auranofin
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Looking beyond dna as the target of inorganic chemotherapy agents: The key role of protein metalation and metal homeostasis
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The Effects on Angiogenesis of Relevant Inorganic Chemotherapeutics
No full textAngiogenesis is a key process allowing the formation of blood vessels. It is crucial for all the tissues and organs, ensuring their function and growth. Angiogenesis is finely controlled by several mechanisms involving complex interactions between pro- or antiangiogenic factors, and an imbalance in this control chain may result in pathological conditions. Metals as copper, zinc and iron cover an essential role in regulating angiogenesis, thus therapies having physiological metals as target have been proposed. In addition, some complexes of heavier metal ions (e.g., Pt, Au, Ru) are currently used as established or experimental anticancer agents targeting genomic or non-genomic targets. These molecules may affect the angiogenic mechanisms determining different effects that have been only poorly and non-systematically investigated so far. Accordingly, in this review article, we aim to recapitulate the impact on the angiogenic process of some reference anticancer drugs, and how it is connected to the overall pharmacological effects. In addition, we highlight how the activity of these drugs can be related to the role of biological essential metal ions. Overall, this may allow a deeper description and understanding of the antineoplastic activity of both approved or experimental metal complexes, providing important insights for the synthesis of new inorganic drugs able to overcome resistance and recurrence phenomena
AS101: An overview on a leading tellurium-based prodrug
Full text linkInorganic chemistry holds a central role in the management of several diseases both from the diagnostic as well as from the therapeutic point of view. Various platinum drugs are approved at the global or local level for cancer treatment while other transition metals are used for different therapeutic applications or diagnosis. However, even semimetals i.e., the elements which lie on the diagonal connecting boron to polonium are being used in medicine where some compounds with therapeutic properties have been approved by the Food and drugs Administration (FDA) and the European Medicinal Agency (EMA). In the last decades growing attention has been devoted towards tellurium for the preparation of pharmacologically active agents. In this context, Ammonium trichloro(dioxoethylene-O,O′)tellurate (AS101) emerged as a reference tellurium-based compound. This Te(IV) compound is well tolerated in animal models and its peculiar reactivity towards thiol residues of enzymes such as cysteine proteases is at the heart of its pharmacological effects. Actually, AS101 entered several clinical trials due to its good tolerability. In this mini-review the main chemical and biological aspects of this promising metalloid-based drug are briefly summarized and the outcomes as well as future perspectives for the design of improved Te-based compounds are discussed
An unprecedented palladium-arsenic catalytic cycle for nitriles hydration
Full text linkAn unprecedented palladium/arsenic-based catalytic cycle for the hydration of nitriles to the corresponding amides is here described. It occurs in exceptionally mild conditions such as neutral pH and moderate temperature (60°C). The versatility of this new catalytic cycle was tested on various nitriles from aliphatic to aromatic. Also, the effect of ring substitution with electron withdrawing and electron donating groups was investigated in the cases of aromatic nitriles, as well as the effect of potentially interferent functional groups such as hydroxy group or pyridinic nitrogen. Furthermore, a pilot study on the potential suitability of this approach for its scale-up is presented, revealing that the catalytic cycle could be potentially and quickly scaled up
Strike a Balance: Between Metals and Non-Metals, Metalloids as a Source of Anti-Infective Agents
Full text linkMost of the commercially available anti-infective agents are organic molecules. In fact, though, during the pioneering times of modern medicine, at the beginning of the 20th century, several inorganic compounds of transition metals were used for medicinal application, to date, only a small number of inorganic drugs are used in clinical practice. Beyond the transition metals, metalloids—or semimetals—offer a rich chemistry in between that of metallic and non-metallic elements, and accordingly, peculiar features for their exploitation in medicinal chemistry. A few important examples of metalloid-based drugs currently used for the treatment of various diseases do exist. However, the use of this group of elements could be further expanded on the basis of their current applications and the clinical trials they entered. Considering that metalloids offer the opportunity to expand the “chemical-space” for developing novel anti-infective drugs and protocols, in this paper, we briefly recapitulate and discuss the current applications of B-, Si-, As-, Sb- and Te-based anti-infective drugs
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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