• In large biopsies series from ALK NSCLC treated patients the

  2023-10-12

  

  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

• Nutritional factors affecting ASD have also recently

  2023-10-12

  

  Nutritional factors affecting ASD have also recently received attention. An increase in postsynaptic zinc (Zn) level induced by clioquinol (a Zn chelator and ionophore), and the subsequent activation of NMDA receptors through the tyrosine kinase Src, rescued social interaction in Shank2−/− mice (Lee

• Subsequently Palvimaki et al corroborated Ni and Miledi

  2023-10-12

  

  Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a

• The surprising finding of our study

  2023-10-11

  

  The surprising finding of our study is that human M1 macrophages stimulated by LPS express ALOX15B to high levels. So far 12/15-lipoxygenase activity was only reported for IL-4 stimulated anti-phlogistic M2 macrophages [9] but not for the classically activated M1 macrophages. Our data suggest that s

• br Aromatase the key enzyme for

  2023-10-11

  

  Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma

• Earlier studies with SERMs identified that

  2023-10-11

  

  Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes

• Most intriguingly however there was no change

  2023-10-11

  

  Most intriguingly, however, there was no change in basal glutamatergic neurotransmission despite a loss of about half of the neuronal AMPAR population. Highest levels of ammonia did neither affect the amplitude nor the frequency of AMPAR mediated mEPSCs. As revealed by our recordings from somatic ou

• Our previous study revealed expression of

  2023-10-11

  

  Our previous study revealed expression of AhR in human parotid gland in cytoplasm of striated duct 360A (Drozdzik, Kowalczyk, Urasińska, & Kurzawski, 2013). In a further study we observed regulation of AhR expression and function by its specific inducer, i.e. 2,3,7,8-tetrachlorodibenzo-p-dioxin (TC

• br Conflicts of interest br Newly Identified Mechanisms of

  2023-10-11

  

  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,

• Subsequently Palvimaki et al corroborated Ni and Miledi

  2023-10-11

  

  Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a

• Although the role of mossy fiber sprouting in epileptogenesi

  2023-10-11

  

  Although the role of mossy fiber sprouting in epileptogenesis has been challenged (Elmer et al., 1997, Nissinen et al., 2001), in addition to astrogliosis, mossy fiber sprouting is one of the characteristic histopathological findings in TLE (Kharatishvili et al., 2006, Pitkanen et al., 2007, Represa

• Nicotine The difficulty of characterizing nAChRs in the cent

  2023-10-10

  

  The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neur

• Finasteride has been shown to be a mechanism based inhibitor

  2023-10-10

  

  Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a

• We demonstrate a role for low oxygen to

  2023-10-10

  

  We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 ddhUTP and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a positive association between elevated ATX mRNA levels i

• Having established the structural requirements for potency

  2023-10-10

  

  Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr

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