• Lately using receptor TM peptides BiFC

  2019-10-01

  

  Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer

• br Introduction Addiction to opioids such as morphine is

  2019-10-01

  

  Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto

• Acknowledgments We are grateful to Dr Jean Marie Bernassau f

  2019-10-01

  

  Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C

• The serotonin transporter gene encodes

  2019-09-30

  

  The serotonin transporter gene () encodes an integral membrane protein that transports serotonin from the synaptic spaces into the presynaptic neurons. The encoded protein terminates the action of serotonin and recycles it in a sodium-dependent way. This protein is a target of psychomotor stimulants

• The COMT gene maps to chromosome q Grossman et

  2019-09-30

  

  The COMT gene maps to chromosome 22q11.2 (Grossman et al., 1992) and has two protein isoforms. The differences between S-COMT and longer MB-COMT are in the N-termini, which use alternative translation initiation sites and promoters. These two isoforms display different affinity and capacity for COMT

• In summary we demonstrated the high potency of fluxametamide

  2019-09-30

  

  In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited

• In addition to glutamatergic inputs the

  2019-09-30

  

  In addition to glutamatergic inputs, the RTn integrates cholinergic, serotonergic and noradrenergic synapses of fibers coming from nuclei located in the brainstem (Asanuma, 1992, Morrison and Foote, 1986, Pare et al., 1988) involved in the alternating firing mode and in the frequency changes of reti

• Although PQQ has nutritional importance and pharmacological

  2019-09-30

  

  Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov

• br Deregulation of CDK Many neurotoxic

  2019-09-30

  

  Deregulation of CDK5 Many neurotoxic or stress conditions like ischemic Ivachtin mass damage, oxidative stress, mitochondrial dysfunctions, excitotoxicity, Aβ exposure lead to disruption of the tight regulation of Cdk5 (De Strooper et al., 2010). Calpain-mediated cleavage of p35 to p25 is activa

• br Transparency document br Acknowledgments This work was

  2019-09-30

  

  Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0

• The physiological role of the

  2019-09-30

  

  The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown t

• Ceftazidime br O GlcNAcase Human OGA is a multidomain protei

  2019-09-29

  

  O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do

• The potential off target activity of against other

  2019-09-29

  

  The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d

• br Materials and methods br Results br

  2019-09-29

  

  Materials and methods Results Discussion Although autophagy is known to be implicated in the therapeutic effect of DNA alkylating agents such as MNNG [28], [29], [30], the molecular mechanisms underlying autophagy induced by MNNG remain largely elusive. In this study, we present evidence sh

• DDR plays a crucial role

  2019-09-29

  

  DDR2 plays a crucial role in regulating a wide variety of fundamental cellular processes, including cell proliferation, differentiation, and adhesion [17], [28], [29], [30]. The authors revealed compromised cell migration in DDR2-silenced fibroblasts exposed to Ang II, most likely due to the loss o

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