• An important observation in our study

  2024-07-18

  

  An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-arr

• In summary we suggest that both cofilin and

  2024-07-18

  

  In summary, we suggest that both cofilin and gelsolin are essential factors that regulate sperm capacitation and the acrosomal exocytosis by modulating actin. The relationships between activation/inactivation of cofilin and gelsolin suggest that inhibition of cofilin is important for allowing F-acti

• Taken together our results indicated that

  2024-07-17

  

  Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 pak1 induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new therapeutic

• Direct inhibition of LO activity by BRP

  2024-07-17

  

  Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de

• The knowledge on the structure of CYP including its active

  2024-07-17

  

  The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig

• In conclusion AXL overexpression preexisted in a subgroup of

  2024-07-17

  

  In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi

• What can we learn about the anticancer therapeutic

  2024-07-17

  

  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

• Loss of virulence in ACL mutants may be

  2024-07-17

  

  Loss of virulence in ACL mutants may be caused by defect in vegetative growth and conidial germination, and reduced trichothecene production. However, supplement of potassium acetate restored the defects in germination rate and vegetative growth, but not virulence in wheat heads (Table 2, Fig. 2B),

• We next sought to determine the kinase

  2024-07-17

  

  We next sought to determine the kinase responsible for IR-induced phosphorylation of 53BP1. Because the sites under investigation all lie in a consensus sequence for ATM, ATR and DNA-PK, that are all activated by IR, the involvement of each of these kinases was investigated. Preincubation of Pleurom

• As the effects of baclofen on primary afferent

  2024-07-17

  

  As the effects of baclofen on primary afferent activity are not reproduced by GABAA receptor agonists like muscimol and isoguvacine, this ionotropic receptor may play minimal role in the modulation of primary afferent activity. However, it is important to note that post-synaptic GABAA receptors rema

• Songbirds are outstanding models in the study

  2024-07-17

  

  Songbirds are outstanding models in the study of vocal communication (Maney and Pinaud, 2011). Following the pioneering studies of William H. Thorpe and Peter Marler on the development of song in chaffinches (Fringilla coelebs) and white-crowned sparrows (Zonotrichia leucophrys) (Marler, 2004; Thorp

• br Experimental procedures br Results br Discussion Major de

  2024-07-17

  

  Experimental procedures Results Discussion Major depressive disorder is among the leading causes of disability worldwide (Vos et al., 2015). One of the major causal or exacerbating factors of depression is long term stress or psychological trauma (Liu and Alloy, 2010). Dysregulation of the

• br Conclusion P gingivalis expresses various exopeptidases i

  2024-07-17

  

  Conclusion P. gingivalis expresses various exopeptidases, i.e., DPP4, DPP5, DPP7, DPP11, PtpA, and AOP, in periplasmic space, which produce di- and tri-peptides from most oligopeptides. This oligopeptide processing step is important as an extracellular event in the triphos of asaccharolytic P. g

• In young animals the HT A receptor antagonist ketanserin at

  2024-07-16

  

  In young animals, the 5-HT2A hepititis b antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for the anta

• The zebrafish Danio rerio is

  2024-07-16

  

  The zebrafish (Danio rerio) is a popular model organism for virtually any biological function of vertebrates, and has, therefore, received a wide distribution in particular in developmental biology and toxicology (Strähle et al., 2012). With respect to AChE, the zebrafish has, e.g., been identified

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