• 7ACC1 An Ubl modification requires several steps

  2019-12-24

  

  An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo

• br Target enzyme attributes and

  2019-12-24

  

  Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma

• br Oxidoreductase like MEM for prodrug

  2019-12-24

  

  Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2

• ApoE is secreted from astrocytes glia

  2019-12-24

  

  ApoE is secreted from astrocytes/glia into the interstitial fluid and is important for metabolizing Aβ because of its propensity for binding Aβ as a cholesterol and phospholipid acceptor in reverse cholesterol transport [8]. Aβ oligomers show a direct toxicity to neurons, and ApoE inhibits oligomer

• A role for the E

  2019-12-24

  

  A role for the E2–E3 interface in governing mono- versus polyubiquitination is not mutually exclusive with that of the E2 backside, which has previously been shown to mediate polyubiquitination through its ability to bind to Ub [21], [25], [33]. Brzovic and colleagues first demonstrated the importan

• A great deal of research has focused on candidate

  2019-12-24

  

  A great deal of research has focused on candidate medications to modulate dopaminergic mechanisms through which psychomotor stimulants produce addictive effects, i.e., drugs that expressly target the DA transporter, D1-like receptor, or D2-like receptors., , However, effective dopaminergic-based pha

• br STAR Methods br Acknowledgments We thank Genevi

  2019-12-24

  

  STAR★Methods Acknowledgments We thank Geneviève Almouzni, Sophie Polo, Ralph Scully, Wael Mansour, and Jeremy Stark for providing cell lines and Wolf Heyer, Haico van Attikum, Martijn Luijsterburg, and Brendan Price for helpful discussions. We thank Ratna Weimer, Bettina Basso, Christel Braun,

• Itch also known as astrophin interacting

  2019-12-23

  

  Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane

• DNA replication checkpoint kinases in both yeast and human c

  2019-12-23

  

  DNA replication checkpoint kinases in both yeast and human Ezetimibe upregulate dNTP levels under replication stress to mediate their essential function at replication forks (Yeeles et al., 2013). It is possible that upregulation of dNTP levels under replication stress helps fork restart once repli

• We aim to apply the

  2019-12-23

  

  We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that

• These cytokines except for TGF can also

  2019-12-23

  

  These cytokines, except for TGF-β can also increase CysLT1R mRNA expression. We further demonstrated that TGF-β and IL-13 were able to increase the proliferation of human BSMC in response to LTD4. BSMC proliferation was CysLT1R-dependent, given that Montelukast ablated this effect. Taken together, o

• p Kip is a critical component of

  2019-12-23

  

  p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod

• This structure guided the variation of the compounds

  2019-12-23

  

  This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis

• The phenotypes of KD Ddr transgenic mice were less

  2019-12-20

  

  The phenotypes of KD-Ddr2 transgenic mice were less severe than expected from the results of miDdr2-transfected ATDC5 cells, which indicated that DDR2 might play important roles in endochondral ossification but neither critical nor essential roles in determining total body and skeleton size. The gr

• PD-1/PD-L1 inhibitor 2 As previously stated the most unexpec

  2019-12-19

  

  As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan

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