1,721,040 research outputs found
Carbonic anhydrase inhibitors for the treatment of epilepsy and obesity
No full textRecent advances in the management of epilepsy and obesity or obesity-related diseases have accounted for the carbonic anhydrase inhibitors becoming clinically used drugs. Although such diseases are not related to each other, they both share the human-expressed carbonic anhydrase (CA; EC 4.2.1.1) enzymes and some of their inhibitors, such as topiramate (TPM) and zonisamide (ZNS) as biologic targets and effective drugs, respectively. Herein we discuss the main features that have triggered appropriate medicinal chemistry-based experimental studies up to the validation of CAs for the management of such diseases. A combination therapy between TPM and phentermine (Qnexa/Qsymia) is currently marketed for the management of obesity and obesity-related diseases. Currently, the bupropion-ZNS slow-release compound, Empatic, is under FDA phase III clinical development for the same therapeutic application, confirming the great potential of CA as a drug target against obesity
Angiotensin-converting enzyme
No full textAngiotensin Converting Enzyme (ACE), is a zinc containing metallopeptidase, best known for its
role in the conversion of Ang I in the active peptide Ang II, which plays a pivotal role in the blood
pressure (BP) regulation trough the Renin Angiotensin System (RAS). In the last decades RAS has
been deeply studied in all its aspects and implications. It has been seen that ACE and its substrates
are involved in many other physiological and pathological processes in addition to pressure control,
such as: hematopoiesis, reproduction, renal development and immune response. Its homologous
protein ACE2, critical enzyme in counter-regulatory response to RAS, was studied and its
pharmacological modulation has been evaluated. According to ACE in vivo roles and its
implication in a great number of physiological pathways, several studies focused on the potential
role of classic ACE inhibitors (ACEIs) and new domain-selective compounds for the treatments of
several diseases. This chapter seeks to review the evolution of the physio/pathological roles of
ACEs and their pharmacological modulation, for the treatment of a wide range of pathologies
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
Bioorganometallic derivatives of 4-hydrazino-benzenesulfonamide as carbonic anhydrase inhibitors: Synthesis, characterization and biological evaluation
No full textVariations 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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