• Because of its role in tumor growth proliferation and

  2023-10-24

  

  Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t

• In this scenario the receptor tyrosine kinase inhibitors TKI

  2023-10-24

  

  In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; PIberin in a

• br The complementary role of chaperone mediated autophagy

  2023-10-24

  

  The complementary role of chaperone mediated autophagy Chaperone-mediated autophagy (CMA) mediates the degradation of specific cellular proteins and participates in the regulation of lipid metabolism, DNA repair, or the response to stress (Kaushik and Cuervo, 2018). CMA provides an alternative pa

• The resolution cocrystal structure of ACL in complex with ci

  2023-10-24

  

  The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of

• ion channels Several mechanisms have been suggested to

  2023-10-24

  

  Several mechanisms have been suggested to account for the causal association of ICAM-1 induction and leukocyte adhesion with DR, including oxidative stress [16], NF-κB [17], PKC [18], and bioactive lipids [19]. Our previous studies highlighted the role of bioactive lipid metabolites derived from 12/

• Oocytes from the African clawed frog Xenopus laevis have bee

  2023-10-24

  

  Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data

• Thirdly and finally multiple studies have analyzed the activ

  2023-10-24

  

  Thirdly and finally, multiple studies have analyzed the activation of neurons in the auditory telencephalic areas of songbirds in response to various auditory stimuli. Neuronal activation was identified by the increased expression of immediate early genes such as fos or ZENK (also know as zif-268, e

• In a study highlighted the usefulness of arginase

  2023-10-24

  

  In 2010, a study highlighted the usefulness of arginase-1 as a sensitive and specific marker of hepatocytic differentiation for diagnostic pathology [9]. Subsequent studies have validated the high sensitivity and specificity of arginase-1, in particular its added value in evaluating poorly different

• br LO synaptic integrity and memory Interestingly several gr

  2023-10-24

  

  12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt

• For the first series we decided to

  2023-10-24

  

  For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives

• Regarding the HT B receptors they

  2023-10-24

  

  Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur

• In the presence of detrimental

  2023-10-24

  

  In the presence of detrimental conditions, such as inflammation, hypoxia, ischemia trauma or neoplastic milieu, the extracellular levels of adenosine increase massively, reaching micromolar range [51,52]. In these pathological contexts, adenosine accumulation stems from increased extracellular depho

• br Conclusions br Conflicts of interest br Acknowledgements

  2023-10-23

  

  Conclusions Conflicts of interest Acknowledgements This work was supported by Ege University Research Fund [BAP, 14-ECZ-030, 2016]. Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, sp

• The introduction of a pyrazole moiety

  2023-10-23

  

  The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,

• Steroidal CYP inhibitors can further

  2023-10-23

  

  Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a

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