receptor structure
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Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5670
Author(s):  
Karolína Salvadori ◽  
Alena Krupková ◽  
Lucie Červenková Šťastná ◽  
Monika Müllerová ◽  
Václav Eigner ◽  
...  

The repetition of urea-based binding units within the receptor structure does not only lead to monomer properties multiplication. As confirmed by spectroscopic studies, UV-Vis and 1H-NMR in classical or competitive titration mode, the attachment to a carrier allocates the active moieties to mutual positions predetermining the function of the whole receptor molecule. Bivalent receptors form self-aggregates. Dendritic receptors with low dihydrogen phosphate loadings offer a cooperative complexation mode associated with a positive dendritic effect. In higher dihydrogen phosphate concentrations, the dendritic branches act independently and the binding mode changes to 1:1 anion: complexation site. Despite the anchoring, the dendritic receptors retain the superior efficiency and selectivity of a monomer, paving the way to recyclable receptors, desirable for economic and ecological reasons.


Author(s):  
Lucia Guzun ◽  
Pascal Fortier-Poisson ◽  
Jean-Sébastien Langlais ◽  
Allan M. Smith

AbstractSingle cutaneous fibers were recorded in the median nerve of the deeply anesthetized rat and the receptor morphology in the forelimb glabrous skin was analyzed to establish a probable correlation between receptor anatomy and physiology. Receptor complexes in the glabrous skin of the rat forelimb were stained immunologically with antibodies NF-200 and PGP-9.5, confirming the presence of Meissner corpuscles and Merkel complexes within the dermal papilla similar to other mammals including primates. Both the Meissner corpuscles and Merkel cell complexes were sparse and located in the pyramidal-shaped palmer pads and the apex of the digit extremities. They were almost totally absent elsewhere in the glabrous skin. No Ruffini receptors or Pacinian corpuscles were found in our samples. A total of 92 cutaneous fibers were retained long enough for analysis. Thirty-five (38%) were characterized as rapidly adapting fibers (RA) and 57 (62%) were slowly adapting afferents (SA). Despite the very limited number of receptors at the tip of the digit, RA receptors outnumbered SA fibers 3.2/1.0. In contrast, SA fibers on the thenar pad outnumbered RA receptors by a ratio of 3–1. Despite the very limited number of low threshold mechanoreceptors in the glabrous skin of the rat forelimb, the prevalence of SA afferents in the palm and more frequent occurrence of RA afferents in the digit extremity suggest differences in functionality both for locomotion and object manipulation.


2021 ◽  
Vol 64 (6) ◽  
pp. 3299-3319
Author(s):  
Jean-Olivier Zirimwabagabo ◽  
Ameera B. A. Jailani ◽  
Paris Avgoustou ◽  
Matthew J. Tozer ◽  
Karl R. Gibson ◽  
...  

2021 ◽  
Vol 11 (5) ◽  
pp. 13740-13753

An escalating pandemic by the novel SARS-CoV2 is spreading across the globe at a rate. An urgent need for therapy is needed. Initially, the virus appeared first in Wuhan, China, and later approximately in 187 countries worldwide. Coronaviruses are causative of respiratory as well as neurological diseases in humans. The novel zoonotic disease-causing coronaviruses are single-stranded RNA viruses. The coronavirus's outer structure consists of spike protein made up of glycoproteins, which binds to ACE (Angiotensin Converting Enzyme) protein when infected in humans. In the current study, 37 compounds that are already used in the biological field as anti-viral compounds are observed with bioinformatics tools. The repurposing drugs are docked against the spike receptor by molecular Docking. The ligand structure and the receptor structure are retrieved from Protein Data Bank. Patch dock server is an open freeware available for docking procedures. The results include acceleration and score of matched properties showing the feasibility of working the drug against SARS-nCoV. For the visualization of the final docked product, PyMOL and RasWin software’s are used. The scores of each ligand docked against the receptor show the compatibility working against the COVID-19 disease.


2021 ◽  
Author(s):  
Artur Kasprzak ◽  
Aleksandra Tobolska ◽  
Hidehiro Sakurai ◽  
Wojciech Wróblewski

Herein, we report for the first time the application of the sumanene derivative in potentiometric recognition of caesium cations. The structure of sumanene receptor was carefully tuned to obtain its...


Author(s):  
Yizhen Zhao ◽  
He Wang ◽  
Yongjian Zang ◽  
Xun Zhu ◽  
Shengli Zhang ◽  
...  

: The appropriate selection of initial receptor structure has been the "cornerstone" or foundation of successful structure-based virtual screening (SBVS), and plagued the structure-based design with a significantly practical problem to determine the major physiological states or important transition states of receptors (e.g. proteins with multiple low-energy conformations and ligand-dependent conformational dynamics). It is well known that current SBVS methods lack capacity to capture and characterize the intrinsic receptor flexibility with ideal cost-effectiveness. In recent years, cryoelectron microscopy (cryo-EM) has been routinely applied in the determination of biomolecular assemblies within physiological state. In this work, we review the roles of cryo-EM and ensemble docking methods to present the intrinsically dynamic behavior of biomacromolecules, as well as the ever-improving estimation of ligand binding affinities and receptor-ligand thermodynamics. Finally, we also provide an attitude for the further researches on the modeling receptor dynamics.


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