• Our finding that activating DDR variants are a cause of

  2019-09-10

  

  Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho

• Many studies have also demonstrated that CK inhibition

  2019-09-09

  

  Many studies have also demonstrated that CK2 inhibition profoundly affects the PI3K/AKT pathway in different cancer models; promising results have been obtained in hematological malignancies (Buontempo et al., 2014, Borgo et al., 2013, Piazza et al., 2012, Cheong et al., 2010, Gowda et al., 2016), a

• br Target enzyme attributes and substrate peptide selection

  2019-09-09

  

  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 Acknowledgement We acknowledge for funding support from M

  2019-09-09

  

  Acknowledgement We acknowledge for funding support from Maryada Foundation, a DoD/Army Contract No. W911NF-06-1-0095, and National Institutes of Health through the New England Center of Excellence for Biodefense (Grant AI057159-01). Introduction The Gram-negative bacterium Lysobacter sp. XL1

• br Materials and Methods br Results br Discussion ROS genera

  2019-09-09

  

  Materials and Methods Results Discussion ROS generated by SFN target many signaling pathways involved in initiating cancer cell death (Sestili and Fimognari, 2015). For example, ROS have been shown to activate both intrinsic and extrinsic caspase cascades in prostate cancer cells (Singh et

• HOIP s ability to build linear Ub chains arises from

  2019-09-09

  

  HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4

• Introduction Ubiquitylation is a post translational modifica

  2019-09-09

  

  Introduction Ubiquitylation is a post-translational modification which impacts almost every biological process in the cell. Dysregulation of the ubiquitylation pathway is associated with several diseases, including cancer, neurodegenerative disorders, and immunological dysfunctions. Single ubiquiti

• br Results and discussion br Conclusion In the current study

  2019-09-09

  

  Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I

• The differences between ground and transition state properti

  2019-09-09

  

  The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit

• 98014 and br Results br Discussion C is

  2019-09-09

  

  Results Discussion C4 is related to another VACV protein, C16, and the C-terminal domain of C16 also inhibits DNA-PK-mediated DNA sensing via the same mechanism and to a similar level as C4. Moreover, mutagenesis of C16 at the CYC residues equivalent to those in C4 abrogated the C16-Ku interac

• Preparation of the regioisomeric pyridooxazepinones

  2019-09-09

  

  Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and glucose transporter chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded

• In addition to an action

  2019-09-09

  

  In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se

• The mitogen activated protein kinase MAPK

  2019-09-09

  

  The mitogen-activated protein kinase (MAPK) family, which consists of extracellular signal-regulated protein kinase 1/2 (ERK1/2), p38 MAPK, and c-Jun N-terminal kinase (JNK), is involved in the development of NP (Hung et al., 2012, Ji et al., 2009). Recently, Zhuang et al. (2005) demonstrated that t

• Caspi et al first identified that the COMT polymorphism

  2019-09-07

  

  Caspi et al. (2005) first identified that the COMT polymorphism moderated the influence of adolescent cannabis use on developing adult psychosis (Caspi et al., 2005). In particular, compared to Met carriers, subjects with the Val/Val genotype were most likely to exhibit psychotic symptoms and to dev

• br Materials and methods br Results

  2019-09-07

  

  Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen

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