• The first natural product described as LO inhibitor

  2024-12-12

  

  The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic Mevastatin from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time before mPGES-1

• Lower LDL C mediated by

  2024-12-12

  

  Lower LDL-C mediated by variants in the ACL gene is causally associated with the risk of cardiovascular events. Because, genetic variants that mimic the effect of an ACL inhibitor have the same effect on the risk of cardiovascular events per unit change in LDL-C as variants that mimic the effect of

• Among steroid saponins ginsenosides are the active

  2024-12-11

  

  Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid

• It remains unclear to what extent UCP and

  2024-12-11

  

  It remains unclear to what extent UCP2 and UCP3 are subject to the same acute molecular regulation as UCP1 (and the extent to which they share the same mechanism of uncoupling). Although they lack sequence homology in a matrix-localised region reportedly critical for fatty nos abbreviation activati

• Thus far a tight coupling has

  2024-12-11

  

  Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solub

• Kim et al found that hydroxydopamine OHDA

  2024-12-11

  

  Kim et al. (2013) found that 6-hydroxydopamine (6-OHDA) promoted the atrophy of dopaminergic neurons associated with the activation of poly (ADP-ribose) polymerase (PARP), the translocation of apoptosis inductor factor (AIF) and the depletion of ATP. An increase in p-AMPK and pS6K (upstream kinase o

• The fat body is one of the

  2024-12-11

  

  The fat body is one of the largest tissues of Bombyx mori, with components including fat, glycogen, protein and vitamins. The fat body exhibits important physiological functions, not only storing a large number of nutrients but also serving as an important site of biosynthesis and metabolism (Arrese

• The excellent potencies selectivities and improved PK associ

  2024-12-11

  

  The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This

• Based on the observation that antipsychotic drugs increase

  2024-12-11

  

  Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene

• The theoretical calculations of ADME parameters molecular we

  2024-12-10

  

  The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) co

• Introduction Microdialysis is an in

  2024-12-10

  

  Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the

• br Conclusion Growth survival and invasion of most PCs

  2024-12-10

  

  Conclusion Growth, survival, and invasion of most PCs have been shown to be androgen-dependent at the onset of castration therapy [31]. Thus, castration therapy has been central to systemic therapy and remains the standard approach to PC treatment. Even after progression to a castration-resistan

• Prostate cancer is the second leading

  2024-12-10

  

  Prostate cancer is the second leading cause of cancer-related death in men in the United States [25]. Similar to pancreatic cancer, prostate cancer has few diagnostic options available, particularly to differentiate indolent from aggressive disease. Axl is also overexpressed in ∼50% of prostate canc

• The authors thank Dr J Aoki University

  2024-12-10

  

  The authors thank Dr. J. Aoki, University of Tokyo, for kindly providing 5E5-ATX antibody. This work was supported by a grant from the Deutsche Forschungsgemeinschaft to A.E.K. (KR4391/1-1), research grants “Primary sclerosing cholangitis” from the Deutsche Crohn-Colitis-Vereinigung and the Norwegia

• Although several different membrane estrogen receptors have

  2024-12-10

  

  Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec

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