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Structures ◽  
2021 ◽  
Vol 34 ◽  
pp. 2151-2163
Author(s):  
Saumitra Jain ◽  
Sumiran Pujari ◽  
Arghadeep Laskar

2021 ◽  
Vol 22 (23) ◽  
pp. 12893
Author(s):  
Xuetao Shi ◽  
Cheng Ye ◽  
Xiangfeng Qin ◽  
Lingling Zhou ◽  
Chuanhui Xia ◽  
...  

Tachykinin 4 (TAC4) is the latest member of the tachykinin family involved in several physiological functions in mammals. However, little information is available about TAC4 in teleost. In the present study, we firstly isolated TAC4 and six neurokinin receptors (NKRs) from grass carp brain and pituitary. Sequence analysis showed that grass carp TAC4 could encode two mature peptides (namely hemokinin 1 (HK1) and hemokinin 2 (HK2)), in which HK2 retained the typical FXGLM motif in C-terminal of tachyinin, while HK1 contained a mutant VFGLM motif. The ligand-receptor selectivity showed that HK2 could activate all 6 NKRs but with the highest activity for the neurokinin receptor 2 (NK2R). Interestingly, HK1 displayed a very weak activation for each NKR isoform. In grass carp pituitary cells, HK2 could induce prolactin (PRL), somatolactin α (SLα), urotensin 1 (UTS1), neuromedin-B 1 (NMB1), cocaine- and amphetamine-regulated transcript 2 (CART2) mRNA expression mediated by NK2R and neurokinin receptor 3 (NK3R) via activation cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA), phospholipase C (PLC)/inositol 1,4,5-triphosphate (IP3)/protein kinase C (PKC) and calcium2+ (Ca2+)/calmodulin (CaM)/calmodulin kinase-II (CaMK II) cascades. However, the corresponding stimulatory effects triggered by HK1 were found to be notably weaker. Furthermore, based on the structural base for HK1, our data suggested that a phenylalanine (F) to valine (V) substitution in the signature motif of HK1 might have contributed to its weak agonistic actions on NKRs and pituitary genes regulation.


2021 ◽  
Vol 6 ◽  
Author(s):  
Stefan Gurres ◽  
Klaus-Ulrich Dillmann ◽  
Wolfgang Reith ◽  
Christoph M. Krick

Many young people decide their professional direction during adolescence. This often coincides with vulnerable phases of puberty-related maturation that is usually accompanied by difficulties in assessing one’s personal inclinations and competences. Several psychological tests have been established among teachers and career advisers serving as a tool for professional coaching the teenagers’ competences and preferences. Many tools are based on the “Theory of Vocational Personalities in Work Environment” developed by John L. Holland since the 1950s, comprising the “RIASEC” model. Today, this theory provides the basis for tests which are used and refined all over the world. Professor Stangl’s online assessable “Situational Interest Test” (SIT) is based on Holland’s theory. By means of 30 short assessments the SIT questionnaire assesses the participant’s personality traits: Realistic (“Doers”), Investigative (“Thinkers”), Artistic (“Creators”), Social (“Helpers”), Enterprising (“Persuaders”), and Conventional (“Organizers”). Modern Magnetic Resonance Imaging (MRI) is able to discriminate between the brain’s compartments as Gray and White Matter using Voxel-Based Morphometry (VBM). This tool allows to reshape and to normalize human brains’ structure to statistically examining individual brains. Up to now findings from 20 years of functional MRI gave detailed insights in correlations between brain structures and mental functions. Hence, knowledge on structural base of cognitive or behavioral patterns is available as a brain’s map for assigning anatomical regions to their functions. The present study demonstrates that there are statistically relevant correlations between all dimensions of Holland’s RIASEC theory by assessing individual professional inclinations and the neuronal structures of the brain. Results show correspondence between the personality traits assigned by the RIASEC test and the functions of significant structural alterations in distinct brain areas well-known from literature.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 420
Author(s):  
Ana Matošević ◽  
Andreja Radman Kastelic ◽  
Ana Mikelić ◽  
Antonio Zandona ◽  
Maja Katalinić ◽  
...  

The treatment of central nervous system (CNS) diseases related to the decrease of neurotransmitter acetylcholine in neurons is based on compounds that prevent or disrupt the action of acetylcholinesterase and butyrylcholinesterase. A series of thirteen quinuclidine carbamates were designed using quinuclidine as the structural base and a carbamate group to ensure the covalent binding to the cholinesterase, which were synthesized and tested as potential human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors. The synthesized compounds differed in the substituents on the amino and carbamoyl parts of the molecule. All of the prepared carbamates displayed a time-dependent inhibition with overall inhibition rate constants in the 103 M−1 min−1 range. None of the compounds showed pronounced selectivity for any of the cholinesterases. The in silico determined ability of compounds to cross the blood–brain barrier (BBB) revealed that six compounds should be able to pass the BBB by passive transport. In addition, the compounds did not show toxicity toward cells that represented the main models of individual organs. By machine learning, the most optimal regression models for the prediction of bioactivity were established and validated. Models for AChE and BChE described 89 and 90% of the total variations among the data, respectively. These models facilitated the prediction and design of new and more potent inhibitors. Altogether, our study confirmed that quinuclidinium carbamates are promising candidates for further development as CNS-active drugs, particularly for Alzheimer’s disease treatment.


2021 ◽  
Vol 60 (5) ◽  
pp. 2101-2111
Author(s):  
Xu Liu ◽  
Guiqiang Zhangsun ◽  
Yong Zheng ◽  
Shijing Liang ◽  
Yanning Cao ◽  
...  

2020 ◽  
Vol 1 (2) ◽  
pp. 87-92
Author(s):  
Vishnu Dev R. S. ◽  
S. Harikumar

Abstract: Livestock markets perform major exchange function of animals in India. These markets play a considerable share in the economic gain of farmers and act as a social and cultural migration hub for the domestic and foreign tourists also. But they are largely unorganized and dominated by informal traders. The structural base of livestock markets determines the sales pattern and the major price value of animals is bagged by middlemen. These markets are functioning under the jurisdiction of the state governments and supervision is under the control of the local bodies. The different marketing strategies in the markets and pricing are affected by qualitative and quantitative factors of animals. The major constraints regarding the livestock markets are the lack of facilities and unawareness of knowledge among the sellers and buyers. The role of livestock markets in disease transmission is also a matter of concern. Details regarding animal movement will facilitate epidemiological studies to prevent contagious diseases from outside the country. In the present COVID-19 pandemic, conventional livestock markets are closed and virtual markets based on online platforms such as Facebook, WhatsApp and E-commerce sites are coming up and these transformations are absolutely inevitable. Keywords: Livestock markets, Marketing strategies, India


2020 ◽  
Vol 14 (4) ◽  
pp. 132-137
Author(s):  
I. S. Dydykina ◽  
E. V. Arutyunova ◽  
P. S. Kovalenko ◽  
E. G. Zotkin

The paper gives the current definition of osteoarthritis (OA), which reflects the pathogenetic and clinical characteristics of this disease, as well as general principles for choosing an OA treatment. It describes the effect of glucosamine and chondroitin on the key pathogenetic mechanisms of OA. It is noted that one of the promising areas of therapy for OA is the intra-articular administration of biopolymer-based hydrogels that provide not only an anti-inflammatory, but also regenerative effect that has been experimentally confirmed during their injection into the tendon sheaths. There are data on the efficacy and safety of the Russian drug Sphero®gel, a biopolymer-based microheterogeneous collagen-containing hydrogel that belongs to a class of multicomponent biopolymer-based extracellular matrix mimetics. It consists of the cross-linked farm animal tissue-derived collagen microparticles placed in the gel base. The gel is not only a structural base for collagen microparticles; it also has its own therapeutic potential, since it is structurally similar to the natural extracellular matrix. The drug contains collagen, biologically active components of the extracellular matrix, such as proteoglycans, glycoproteins, uronic acids, growth factors, monosaccharides, and chondroitin sulfate. Extended-release symptomatic agents, Sphero®gel among them, are currently recommended for the treatment of OA. Application of Sphero®gel contributes to increased joint mobility and reduced pain, which allows the limited use of nonsteroidal anti-inflammatory drugs that cause adverse reactions, especially in the presence of comorbid diseases.


2020 ◽  
Vol 28 (11) ◽  
pp. 2525-2536
Author(s):  
Kai Yuan ◽  
Xin Wang ◽  
Cheng Chen ◽  
Cathy Choi-Yin Lau ◽  
Winnie Chiu-Wing Chu ◽  
...  

Science ◽  
2020 ◽  
Vol 369 (6509) ◽  
pp. 1351-1354 ◽  
Author(s):  
Douglas B. Rasher ◽  
Robert S. Steneck ◽  
Jochen Halfar ◽  
Kristy J. Kroeker ◽  
Justin B. Ries ◽  
...  

Predator loss and climate change are hallmarks of the Anthropocene yet their interactive effects are largely unknown. Here, we show that massive calcareous reefs, built slowly by the alga Clathromorphum nereostratum over centuries to millennia, are now declining because of the emerging interplay between these two processes. Such reefs, the structural base of Aleutian kelp forests, are rapidly eroding because of overgrazing by herbivores. Historical reconstructions and experiments reveal that overgrazing was initiated by the loss of sea otters, Enhydra lutris (which gave rise to herbivores capable of causing bioerosion), and then accelerated with ocean warming and acidification (which increased per capita lethal grazing by 34 to 60% compared with preindustrial times). Thus, keystone predators can mediate the ways in which climate effects emerge in nature and the pace with which they alter ecosystems.


Crystals ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 464 ◽  
Author(s):  
Sergey N. Britvin ◽  
Maria G. Krzhizhanovskaya ◽  
Vladimir N. Bocharov ◽  
Edita V. Obolonskaya

Stanfieldite, natural Ca-Mg-phosphate, is a typical constituent of phosphate-phosphide assemblages in pallasite and mesosiderite meteorites. The synthetic analogue of stanfieldite is used as a crystal matrix of luminophores and frequently encountered in phosphate bioceramics. However, the crystal structure of natural stanfieldite has never been reported in detail, and the data available so far relate to its synthetic counterpart. We herein provide the results of a study of stanfieldite from the Brahin meteorite (main group pallasite). The empirical formula of the mineral is Ca8.04Mg9.25Fe0.72Mn0.07P11.97O48. Its crystal structure has been solved and refined to R1 = 0.034. Stanfieldite from Brahin is monoclinic, C2/c, a 22.7973(4), b 9.9833(2), c 17.0522(3) Å, β 99.954(2)°, V 3822.5(1)Å3. The general formula of the mineral can be expressed as Ca7M2Mg7(PO4)12 (Z = 4), where the M = Ca, Mg, Fe2+. Stanfieldite from Brahin and a majority of other meteorites correspond to a composition with an intermediate Ca≈Mg occupancy of the M5A site, leading to the overall formula ~Ca7(CaMg)Mg9(PO4)12 ≡ Ca4Mg5(PO4)6. The mineral from the Lunar sample “rusty rock” 66095 approaches the M = Mg end member, Ca7Mg2Mg9(PO4)12. In lieu of any supporting analytical data, there is no evidence that the phosphor base with the formula Ca3Mg3(PO4)4 does exist.


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