• Although little is known about the

  2023-12-25

  

  Although little is known about the etiopathogenesis of preeclampsia, this syndrome has a major impact on maternal and fetal health worldwide, since it is responsible for 10–15% of maternal deaths [16], [17], preterm births, intrauterine growth restriction (IUGR), and fetal deaths [2]. In developing

• Some of the earliest LOX inhibitors were redox inhibitors in

  2023-12-22

  

  Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic L-685,458 (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+) s

• To date LOX is the only LOX isoform

  2023-12-22

  

  To date, 12-LOX is the only LOX isoform that has been identified in the platelet [17]. Interestingly, while 12-LOX is highly expressed (∼14000 molecules/platelet) in the platelet, 12(R)-LOX expression is absent in the hematopoietic lineage and has therefore not been reported to be expressed in plate

• Adiponectin belongs to the CTRP C q

  2023-12-22

  

  Adiponectin belongs to the CTRP (C1q/TNF-related protein) superfamily. Except for adiponectin, 15 additional members have been identified (CTRP1-15) (Schaffler and Buechler, 2012). Of all the CTRPs, CTRP9 has the highest identity to adiponectin in globular domain (Wong et al., 2009). The structure o

• Regarding the HT B receptors

  2023-12-22

  

  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

• br Conclusions Several lines of

  2023-12-22

  

  Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute L-817,818 injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic adeno

• br AD and COX LOX pharmacology Early

  2023-12-22

  

  AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re

• Acknowledgements The work was supported by

  2023-12-22

  

  Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic

• Our previous work fails to show any maternal effect with

  2023-12-22

  

  Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef

• The knowledge on the structure of CYP including its

  2023-12-22

  

  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

• Several dehidropregnenolone derivatives functionalized at C

  2023-12-22

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• br Conclusion In summary screening a small

  2023-12-22

  

  Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b

• br Aurora A Aurora B

  2023-12-22

  

  Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig

• Whole body loss of ACLY is early embryonic

  2023-12-22

  

  Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv

• br Crystal structure ACLY protein is a homotetramer of

  2023-12-22

  

  Crystal structure ACLY protein is a homotetramer of four identical subunits [9]. Each polypeptide chain contains 1101 amino-acid residues [10]. The crystal structure of full-length ACLY protein is yet unresolved. However, Sun et al. recently succeeded in crystallizing chymotrypsin-truncated human

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