• Several studies have demonstrated that depletion of

  2025-01-04

  

  Several studies have demonstrated that depletion of functional ATR increases the sensitivity of cancer cells to oncogene-induced replication stress thereby hindering tumour growth and inducing extensive cell death (Gilad et al., 2010, Murga et al., 2011, Schoppy et al., 2012). Importantly, Schoppy e

• The canonical binding sites to which or contribute

  2025-01-04

  

  The canonical Polyphyllin VII sale to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effec

• br Materials and methods br Results br Discussion Because

  2025-01-04

  

  Materials and methods Results Discussion Because the Ser/Thr kinase domain of LRRK2 is homologous to that of other MLK family proteins belonging to the MAP3K superfamily, LRRK2 is suggested to be involved in MAPK signaling and activation of neuronal cell death by phosphorylating its downstr

• Although the role of apelin

  2025-01-04

  

  Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G

• Angiogenesis refers to the formation of new blood vessels fr

  2025-01-04

  

  Angiogenesis refers to the formation of new blood vessels from pre-existing vasculature [1]. Physiological angiogenesis is necessary for key processes such as wound healing, tissue regeneration and repair. In pathological conditions, including cardiovascular diseases, diabetes, cancer, and other pat

• Recent work has detailed the impact of genetic deletion

  2025-01-03

  

  Recent work has detailed the impact of genetic V-ATPase inhibitor of AMPK in the liver, revealing only minor phenotypes upon removal in mice (Boudaba et al., 2018). However, these studies very elegantly showed the potential for small molecule-mediated activation of AMPK to elicit large changes in l

• br Results The newly synthesized leucine ureido derivatives

  2025-01-03

  

  Results The newly synthesized leucine ureido derivatives were firstly evaluated for their enzymatic inhibition using porcine kidney APN (Microsomal, Biocol) with bestatin as the positive control (Table 1). One isoleucine ureido derivative 14 and phenylglycine ureido derivative 15 were also synthe

• br Conflicts of interest br

  2025-01-03

  

  Conflicts of interest Acknowledgements This work was sponsored by grants from Longyan University Scientific Research Fund for the Young Scholars (LQ2016010), Middle-aged and Young Teachers Education Research Projects of Fujian Province (JAT170569), Longyan University Scientific Research Fund f

• agonists simulate norepinephrine NE in binding to presynapti

  2025-01-03

  

  α2 agonists simulate norepinephrine (NE) in binding to presynaptic surface autoreceptors, which in turn mediates feedback inhibition of NE release. Another major control mechanism for noradrenergic neurotransmission is termination of signaling by presynaptic NE transporter (NET)-mediated NE reuptake

• br ABCA is a sterol responsive gene The first

  2025-01-03

  

  ABCA2 is a sterol-responsive gene The first evidence to demonstrate that ABCA2 expression responded to sterol loading was provided in an experiment involving monocyte to macrophage differentiation in vitro. Upon sterol loading with enzymatically degraded LDL (eLDL), ABCA2 expression increased onl

• br Funding This work was supported by Arena Pharmaceuticals

  2025-01-03

  

  Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo

• The fact that the BPloopAsn regains

  2025-01-03

  

  The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li

• The nAChR has been considered an interesting potential targe

  2025-01-03

  

  The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none

• Of the many different types of DNA lesions DNA double

  2025-01-02

  

  Of the many different types of DNA lesions, DNA double strand breaks (DSBs) are amongst the most deleterious. It has been suggested that a single unrepaired DSB may be sufficient to induce cell death (Bennett et al., 1993), whereas misrepaired DSBs can result in loss of genetic information, potentia

• In addition to calpain I activity

  2025-01-02

  

  In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep

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