• APJ receptor expression is altered in

  2023-03-13

  

  APJ receptor expression is altered in various cardiovascular diseases, and both increases as well as decreases in APJ receptor expression have been reported. A decrease in mRNA and protein levels of APJ receptors was observed in patients with ischemic heart disease or idiopathic dilated cardiomyopat

• The protein kinase CK mediated

  2023-03-11

  

  The protein kinase CK2-mediated phosphorylation of HMGN1 was implicated to be involved in age-associated amnesia in rats [31]. It was shown that the decreased level of HMGN1 phosphorylation due to the down-regulation of CK2 activity could cause amnesia in aged rats, whereas the treatment with protei

• Based on the general structure function principle in biology

  2023-03-11

  

  Based on the general structure-function principle in biology [[19], [20], [21]], toxic oligomers are expected to have well-defined three-dimensional structures to carry out their pathological functions. A common amyloid toxicity mechanism also suggests that toxic oligomers of different amyloid prote

• br Acknowledgements This work was supported

  2023-03-11

  

  Acknowledgements This work was supported by Programme Grants from the MRC and the Wellcome Trust (SGC-C and MF). CB was in receipt of a Marie Curie Intra-European Fellowship during part of this work. We thank past and present members of our group for numerous valuable discussions throughout these

• br Results and discussion br Conclusion The

  2023-03-11

  

  Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte

• Adenosine is a ubiquitous homeostatic substance released

  2023-03-11

  

  Adenosine is a ubiquitous homeostatic substance released from most cells, including neurons and glias. Endogenous adenosine acts at four principal G-protein-associated receptor subtypes: A1, A2a, A2b and A3 (Ralevic and Burnstock, 1998). The stimulation of adenosine receptors by extracellular adenos

• As also found by Stolarski et al

  2023-03-11

  

  As also found by Stolarski et al. [14], inclusion of N2O in the model is successful in reducing the effect of dynamics [13] in the lower stratosphere in the Northern Hemisphere (30–60°N in our case). The inclusion of N2O also decreased the error bars on the trend values, but the trend values still c

• We have previously shown that the antinociceptive effect of

  2023-03-11

  

  We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific CA-074 Me blockade or activation (Rojas-Corrales et al., 2000). Moreover, it

• In order to increase the oral bioavailability abiraterone is

  2023-03-11

  

  In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral TAI-1 of abiraterone acetate (156), it is recommended that this drug should be taken on an empt

• A variety of quinazoline or fused pyrimidine substituted

  2023-03-11

  

  A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and

• ATX LPA signaling in cancer is also well known

  2023-03-11

  

  ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech

• br Autophagy inducers Macroautophagy is often

  2023-03-11

  

  Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of BINA mg and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sensitivity of can

• Nowadays more than kinases have been identified of

  2023-03-11

  

  Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme

• What can we learn about the anticancer

  2023-03-11

  

  What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito

• In bacteria H gler et al

  2023-03-11

  

  In bacteria (Hügler et al., 2007, Kanao et al., 2001), a glaucophyte alga (Ma et al., 2001), green algae/land plants (Fatland et al., 2002), and filamentous fungi (Nowrousian et al., 2000), ACL enzyme activity requires ACLA, and ACLB (referred to here as dual-subunit ACL, or dsACL) (Kanao et al., 20

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