• The lactam emerged as lead candidate due to

  2024-10-26

  

  The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok

• br Discussion AhR is a receptor

  2024-10-26

  

  Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds

• br Conflicts of interest br Newly Identified Mechanisms of

  2024-10-26

  

  Conflicts of interest Newly Identified Mechanisms of APN Resistance Hold Therapeutic Potential APN, APN Receptors, and APN Cardiovascular Protection APN Resistance in Cardiovascular Disease The Molecular Mechanisms of APN Resistance Concluding Remarks and Future Directions Finally,

• br Perspectives and challenges Previously the main focus

  2024-10-26

  

  Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular

• br Conflicts of interest br Acknowledgments br Significance

  2024-10-26

  

  Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A

• Although effects of low concentrations of

  2024-10-26

  

  Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major Tie2 kinase inhibitor α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-estera

• The hippocampus is the primary brain structure involved in

  2024-10-26

  

  The hippocampus is the primary brain structure involved in learning and memory. The role of hippocampal synaptic plasticity in neurological processes in cognition and depression has been extensively demonstrated. Synaptophysin is a critical substance in synaptogenesis, which is necessary for learnin

• br Experimental procedure br Introduction Migraine is a

  2024-10-26

  

  Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of

• A positive correlation between nasopharyngeal CCL and CCL co

  2024-10-25

  

  A positive correlation between nasopharyngeal CCL3 and CCL5 [16] concentrations and illness severity was shown in evaluating patients with RSV bronchiolitis [17]. CCL5 and CCL3 are important for monocyte and lymphocyte recruitment to the lung during RSV infection [7], [16], [18]. Despite the signifi

• Previous studies have demonstrated ATR inhibition is effecti

  2024-10-25

  

  Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Pyronaridine Tetraphosphate mg to enhance chemotherapy sensitivity [[16], [17], [18]

• Etoposide receptor Recent studies have demonstrated signific

  2024-10-25

  

  Recent studies have demonstrated significant cross-talk between XRCC1 (a key player in Etoposide receptor excision repair (BER) and single strand break repair) and DDR [30], [31], [32]. ATM and DNA-PKcs are known to be involved in the phosphorylation of XRCC1 to promote BER [30], [31]. We have rece

• Angiogenesis is a process of formation

  2024-10-25

  

  Angiogenesis is a process of formation of new vessels from arterial vascularization created by endothelial cells. It is essential for the continuous growth of the tumor because it supplies the tumor with nutrients and oxygen, and eliminates cellular waste, which can be toxic to cancer cells [8]. Inf

• Inhibition of autophagy has been shown to alleviate

  2024-10-25

  

  Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention

• LAP locations in the parasite tissues

  2024-10-25

  

  LAP locations in the parasite tissues would provide clues for the potential physiological roles of it inside the parasite body. To date, tissue localization of LAPs has been carried out in many helminth parasites; however, information regarding LAPs in tapeworm is scarce. It was shown that LAPs were

• In large biopsies series from ALK NSCLC treated patients the

  2024-10-25

  

  In large biopsies series from ALK+ NSCLC treated patients, the number of detected mutations increased after second generation ALKi (Gainor et al., 2016) and in one study were present in 56% of the entire cohort (Shaw et al., 2013b). For example, the rate of G1202R mutations increases from 2% in post

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