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br Regulation of GCK by intrinsic conformational dynamics GC
2021-10-06

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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Based upon the present findings it is
2021-10-06

Based upon the present findings, it is tempting to imagine that selective, and especially stable blood–brain barrier (BBB) penetrating GalR1 antagonists might be useful as drugs for acute suppression of appetite. While this may be possible, previous studies using nonspecific galanin antagonists yiel
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br Acknowledgement This work was supported by National Scien
2021-10-06

Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H
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br Conclusions GPCRs are versatile signaling molecules regul
2021-10-04

Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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To investigate an involvement of GPR and
2021-10-04

To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) 6-Chloromelatonin were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, w
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In a preliminary communication we showed that AT
2021-10-03

In a preliminary communication, we showed that AT and ETB receptors colocalize and coimmunoprecipitate in renal proximal tubule cells, and stimulation of the AT receptor increases ETB receptor expression in Wistar-Kyoto (WKY) rats [abstract; Zeng C,, 26:80A, 2003]. We hypothesize that the ETB recept
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The IN gene of the HIV
2021-10-03

The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN
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br Materials and methods br
2021-10-02

Materials and methods Results Discussion Previously, it is well known that methionine and choline deficient (MCDD) or choline-deficient, L-amino acid-defined (CDAA) models are widely accepted in NASH research. MCDD or CDAA dietary model has been mimic human NASH in rodents by sequentially p
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In addition to their functional activation of GPR
2021-10-02

In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic E-64-d to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlabel
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There is sufficient evidence to indicate that kisspeptin pla
2021-10-02

There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH igf ir and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region of GnRH was cloned,
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br Acknowledgments This work was supported by the
2021-10-02

Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200
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Post translational ubiquitination has been shown to regulate
2021-10-02

Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra
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Erlotinib It is becoming increasingly apparent that membrane
2021-10-02

It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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br Acknowledgments br Free fatty acids FFAs are not
2021-10-02

Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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Expression and translocation of GLUT
2021-10-02

Expression and translocation of GLUT4 are regulated by various mechanisms including protein kinase C isoforms (PKCs) and mitogen-activated protein kinase (MAPK) signals [22], [23], but the real mechanism that statins alter expression and function of GLUT4 has not been fully identified. It is general
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