scholarly journals Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

2021 ◽  
Vol 14 (2) ◽  
pp. 76
Author(s):  
Qing Wang ◽  
Yu Zhou ◽  
Jianhui Huang ◽  
Niu Huang

Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in 5-HT2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, the gastrointestinal (GI) tract, and the nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas.

2013 ◽  
Vol 126 (7) ◽  
pp. 461-469 ◽  
Author(s):  
Carlos Maria Ferrario ◽  
Sarfaraz Ahmad ◽  
Sayaka Nagata ◽  
Stephen W. Simington ◽  
Jasmina Varagic ◽  
...  

Lessons learned from the characterization of the biological roles of Ang-(1–7) [angiotensin-(1–7)] in opposing the vasoconstrictor, proliferative and prothrombotic actions of AngII (angiotensin II) created an underpinning for a more comprehensive exploration of the multiple pathways by which the RAS (renin–angiotensin system) of blood and tissues regulates homoeostasis and its altered state in disease processes. The present review summarizes the progress that has been made in the novel exploration of intermediate shorter forms of angiotensinogen through the characterization of the expression and functions of the dodecapeptide Ang-(1–12) [angiotensin-(1–12)] in the cardiac production of AngII. The studies reveal significant differences in humans compared with rodents regarding the enzymatic pathway by which Ang-(1–12) undergoes metabolism. Highlights of the research include the demonstration of chymase-directed formation of AngII from Ang-(1–12) in human left atrial myocytes and left ventricular tissue, the presence of robust expression of Ang-(1–12) and chymase in the atrial appendage of subjects with resistant atrial fibrillation, and the preliminary observation of significantly higher Ang-(1–12) expression in human left atrial appendages.


Author(s):  
V. Serin ◽  
K. Hssein ◽  
G. Zanchi ◽  
J. Sévely

The present developments of electron energy analysis in the microscopes by E.E.L.S. allow an accurate recording of the spectra and of their different complex structures associated with the inner shell electron excitation by the incident electrons (1). Among these structures, the Extended Energy Loss Fine Structures (EXELFS) are of particular interest. They are equivalent to the well known EXAFS oscillations in X-ray absorption spectroscopy. Due to the EELS characteristic, the Fourier analysis of EXELFS oscillations appears as a promising technique for the characterization of composite materials, the major constituents of which are low Z elements. Using EXELFS, we have developed a microstructural study of carbon fibers. This analysis concerns the carbon K edge, which appears in the spectra at 285 eV. The purpose of the paper is to compare the local short range order, determined by this way in the case of Courtauld HTS and P100 ex-polyacrylonitrile carbon fibers, which are high tensile strength (HTS) and high modulus (HM) fibers respectively.


2020 ◽  
Vol 17 ◽  
Author(s):  
Biswajit Panda ◽  
Amal Kumar Gooyee

: Oceans can play a major role in supplying life-saving medicines in the world in future. Although considerable progress has been made in finding new medicines from marine sources, large efforts are still necessary to examine such molecules for clinical applications. Xyloketals are an important group of natural products with various powerful and prominent bioactivities such as inhibition of acetylcholine esterase, antioxidant activity, inhibition of L-calcium channels, radicalscavenging behavior, suppression of cell proliferation, reduction of neonatal hypoxic-ischemic brain injury, etc. This review describes the isolation and structural characterization of all xyloketal natural products giving major emphasis on their bioactivity.


Author(s):  
Bibian Bibeca Bumbila García ◽  
Hernán Andrés Cedeño Cedeño ◽  
Tatiana Moreira Chica ◽  
Yaritza Rossana Parrales Ríos

The objective of the work is to establish the characterization of the auditory disability and its relationship with resilience at the Technical University of Manabí. The article shows a conceptual analysis related to the inclusion and social integration of disabled students. Based on the fact that the person with disabilities grows and develops in the same way as that of people without disabilities and what usually happens is that disabled people are rejected and discriminated against based on a prefabricated and erroneous conceptualization of these people. The results associated with the application of the SV-RES test prepared by the researchers are shown (Saavedra & Villalta, 2008b). Characterization of the auditory deficit is made in the students, and the limitations that derive from it are pointed out. We analyze the particularities related to communication with students who have a hearing disability and resilience in this type of student, where some personal highlights that in this sense constitute an example of resilience. Finally, the results related to the study of the relationship between students' hearing disability and the level of resilience dimensions are shown.


HLA ◽  
2021 ◽  
Author(s):  
Maria Loginova ◽  
Olga Makhova ◽  
Daria Smirnova ◽  
Igor Paramonov ◽  
Maksim Zarubin

HLA ◽  
2020 ◽  
Author(s):  
Steve Genebrier ◽  
Vincent Elsermans ◽  
Emeric Texeraud ◽  
Gerald Bertrand ◽  
Virginie Renac

HLA ◽  
2021 ◽  
Author(s):  
Marine Cargou ◽  
Vincent Elsermans ◽  
Isabelle Top ◽  
Laura Blouin ◽  
Jonathan Visentin
Keyword(s):  

Viruses ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 27
Author(s):  
Jun Kwon ◽  
Sang Guen Kim ◽  
Hyoun Joong Kim ◽  
Sib Sankar Giri ◽  
Sang Wha Kim ◽  
...  

The increasing emergence of antimicrobial resistance has become a global issue. Therefore, many researchers have attempted to develop alternative antibiotics. One promising alternative is bacteriophage. In this study, we focused on a jumbo-phage infecting Salmonella isolated from exotic pet markets. Using a Salmonella strain isolated from reptiles as a host, we isolated and characterized the novel jumbo-bacteriophage pSal-SNUABM-04. This phage was investigated in terms of its morphology, host infectivity, growth and lysis kinetics, and genome. The phage was classified as Myoviridae based on its morphological traits and showed a comparatively wide host range. The lysis efficacy test showed that the phage can inhibit bacterial growth in the planktonic state. Genetic analysis revealed that the phage possesses a 239,626-base pair genome with 280 putative open reading frames, 76 of which have a predicted function and 195 of which have none. By genome comparison with other jumbo phages, the phage was designated as a novel member of Machinavirus composed of Erwnina phages.


HLA ◽  
2021 ◽  
Author(s):  
Steve Genebrier ◽  
Paul Rouzaire ◽  
Emeric Texeraud ◽  
Gerald Bertrand ◽  
Virginie Renac

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