scholarly journals Molecular Modeling of Histamine Receptors—Recent Advances in Drug Discovery

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1778
Author(s):  
Pakhuri Mehta ◽  
Przemysław Miszta ◽  
Sławomir Filipek
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Molecular Modeling ◽  
Molecular Targets ◽  
Histamine Receptors ◽  
Experimental Characterization ◽  
Complex Disorders ◽  
Theoretical Investigations ◽  
Recent Developments

The recent developments of fast reliable docking, virtual screening and other algorithms gave rise to discovery of many novel ligands of histamine receptors that could be used for treatment of allergic inflammatory disorders, central nervous system pathologies, pain, cancer and obesity. Furthermore, the pharmacological profiles of ligands clearly indicate that these receptors may be considered as targets not only for selective but also for multi-target drugs that could be used for treatment of complex disorders such as Alzheimer’s disease. Therefore, analysis of protein-ligand recognition in the binding site of histamine receptors and also other molecular targets has become a valuable tool in drug design toolkit. This review covers the period 2014–2020 in the field of theoretical investigations of histamine receptors mostly based on molecular modeling as well as the experimental characterization of novel ligands of these receptors.

scholarly journals Immunological and Molecular Characterization of Goα-like Proteins in the Drosophila Central Nervous System

1989 ◽  
Vol 264 (31) ◽  
pp. 18552-18560 ◽  
Author(s):  
N C Thambi ◽  
F Quan ◽  
W J Wolfgang ◽  
A Spiegel ◽  
M Forte
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Molecular Characterization

scholarly journals Molecular cloning and analysis of l(1)ogre, a locus of Drosophila melanogaster with prominent effects on the postembryonic development of the central nervous system.

Genetics ◽  
1990 ◽  
Vol 126 (4) ◽  
pp. 1033-1044 ◽  
Author(s):  
T Watanabe ◽  
D R Kankel
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Postembryonic Development ◽  
P Element ◽  
Reading Frame ◽  
Isolation And Characterization ◽  
The Central Nervous System ◽  
Highly Hydrophobic ◽  
Conceptual Translation

Abstract Previous genetic studies have shown that wild-type function of the l(1)ogre (lethal (1) optic ganglion reduced) locus is essential for the generation and/or maintenance of the postembryonic neuroblasts including those from which the optic lobe is descended. In the present study molecular isolation and characterization of the l(1)ogre locus was carried out to study the structure and expression of this gene in order to gain information about the nature of l(1)ogre function and its relevance to the development of the central nervous system. About 70 kilobases (kb) of genomic DNA were isolated that spanned the region where l(1)ogre was known to reside. Southern analysis of a l(1)ogre mutation and subsequent P element-mediated DNA transformation mapped the l(1)ogre+ function within a genomic fragment of 12.5 kb. Northern analyses showed that a 2.9-kb message transcribed from this 12.5-kb region represented l(1)ogre. A 2.15-kb portion of a corresponding cDNA clone was sequenced. An open reading frame (ORF) of 1,086 base paris was found, and a protein sequence of 362 amino acids with one highly hydrophobic segment was deduced from conceptual translation of this ORF.

scholarly journals Detection and Characterization of Autoantibodies to Neuronal Cell-Surface Antigens in the Central Nervous System

2016 ◽  
Vol 9 ◽  
Author(s):  
Marleen H. van Coevorden-Hameete ◽  
Maarten J. Titulaer ◽  
Marco W. J. Schreurs ◽  
Esther de Graaff ◽  
Peter A. E. Sillevis Smitt ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Cell Surface ◽  
Neuronal Cell ◽  
Surface Antigens ◽  
Cell Surface Antigens ◽  
The Central Nervous System

Characterization of placental luteinizing hormone-relasing factor-like material

1981 ◽  
Vol 96 (3) ◽  
pp. 394-397 ◽  
Author(s):  
Jau-Nan Lee ◽  
Markku Seppälä ◽  
Tim Chard
Keyword(s):  
Central Nervous System ◽  
High Pressure ◽  
Nervous System ◽  
Acetic Acid ◽  
Liquid Chromatography ◽  
Luteinizing Hormone ◽  
Human Placenta ◽  
The Central Nervous System ◽  
Inhibition Curve

Abstract. High pressure liquid chromatography (HPLC) and radioimmunoassay were employed to characterize luteinizing hormone-releasing factor (LRF)-like material in the human placenta. Methanol extracts of the placenta were washed with acetic acid and chloroform, further purified on coarse octadecylsilane columns, fractionated on HPLC, and tested by radioimmunoassay. In HPLC, placental LRF had the same retention time as synthetic LRF, and such fractions gave an inhibition curve which was parallel to that of synthetic LRF in radioimmunoassav. It is concluded that human placental I.RF is similar or identical to LRF in the central nervous system.

Isolation and characterization of periaxolemmal and axolemmal enriched membrane fractions from the rat central nervous system

1992 ◽  
Vol 32 (4) ◽  
pp. 593-604 ◽  
Author(s):  
V. S. Sapirstein ◽  
R. Durrie ◽  
B. Cherksey ◽  
M. E. Beard ◽  
C. J. Flynn ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Isolation And Characterization

scholarly journals COVID-19 and anosmia: The story so far

2021 ◽  
pp. 014556132110489
Author(s):  
Xiangming Meng ◽  
Yuandan Pan
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Olfactory Epithelium ◽  
Underlying Disease ◽  
Predictive Tool ◽  
Olfactory Testing ◽  
High Prevalence ◽  
Smoking Behaviors ◽  
Recent Developments ◽  
Underlying Diseases

Objectives The pandemic has affected over 182 million coronavirus disease 2019 (COVID-19) cases worldwide. Accumulated evidence indicates that anosmia is one of the significant characteristics of COVID-19 with a high prevalence. However, many aspects of COVID-19-induced anosmia are still far from being fully understood. The purpose of this review is to summarize recent developments in COVID-19-induced anosmia to increase awareness of the condition. Methods A literature search was carried out using the PubMed, Embase, Web of Science, and Scopus. We reviewed the latest literature on COVID-19-induced anosmia, including mechanisms of pathogenesis, olfactory testing, anosmia as predictive tool, pathological examinations, imaging findings, affected factors, co-existing diseases, treatments, prognosis, hypothesis theories, and future directions. Results The possible pathogenesis of COVID-19-induced anosmia may involve inflammation of the olfactory clefts and damage to the olfactory epithelium or olfactory central nervous system by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The D614G spike variant may also play a role in the increased number of anosmia patients. Anosmia may also be an essential indicator of COVID-19 spread and an early indicator of the effectiveness of political decisions. The occurrence and development of COVID-19-induced anosmia may be influenced by smoking behaviors and underlying diseases such as type 2 diabetes, gastroesophageal disorders, and rhinitis. Most patients with COVID-19-induced anosmia can fully or partially recover their olfactory function for varying durations. COVID-19-induced anosmia can be treated with various approaches such as glucocorticoids and olfactory training. Conclusion Anosmia is one of the main features of COVID-19 and the underlying disease of the patient may also influence its occurrence and development. The possible pathogenesis of COVID-19-induced anosmia is very complicated, which may involve inflammation of the olfactory clefts and damage to the olfactory epithelium or olfactory central nervous system.

scholarly journals Fractal fluctuations in the cardiovascular dynamical system : from the autonomic control to the central nervous system influence

2021 ◽  
Author(s):  
Asif Hasan Sharif
Keyword(s):  
Central Nervous System ◽  
Heart Rate ◽  
Nervous System ◽  
Autonomic Nervous System ◽  
Dynamic Feature ◽  
Scale Free ◽  
Autonomic Nervous ◽  
Factorization Technique ◽  
The Central Nervous System

The fractal component in the complex fluctuations of the human heart rate represents a dynamic feature that is widely observed in diverse fields of natural and artificial systems. It is also of clinical significance as the diminishing of the fractal dynamics appears to correlate with heart disease processes and adverse cardiac events in old age. While the autonomic nervous system directly controls the pacemaker cells of the heart, it does not provide an immediate characterization of the complex heart rate variability (HRV). The central nervous system (CNS) is known to be an important modulator for various cardiac functions. However, its role in the fractal HRV is largely unclear. In this research, human experiments were conducted to study the influence of the central nervous system on fractal dynamics of healthy human HRV. The head up tilt (HUT) maneuver is used to provide a perturbation to the autonomic nervous system. The subsequent fractal effect in the simultaneously recorded electroencephalography and beat-to-beat heart rate data was examined. Using the recently developed multifractal factorization technique, the common multifractality in the data fluctuation was analyzed. An empirical relationship was uncovered which shows the increase (decrease) in HRV multifractality is associated with the increase (decrease) in multifractal correlation between scale-free HRV and the cortical expression of the brain dynamics in 8 out of 11 healthy subjects. This observation is further supported using surrogate analysis. The present findings imply that there is an integrated central-autonomic component underlying the cortical expression of the HRV fractal dynamics. It is proposed that the central element should be incorporated in the fractal HRV analysis to gain a more comprehensive and better characterization of the scale-free HRV dynamics. This study provides the first contribution to the HRV multifractal dynamics analysis in HUT. The multivariate fractal analysis using factorization technique is also new and can be applied in the more general context in complex dynamics research.

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