• The discoidin domain receptors DDR and DDR

  2021-04-25

  

  The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati

• br P Y receptor structure br

  2021-04-25

  

  P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar

• It has been shown that CK phosphorylates

  2021-04-25

  

  It has been shown that CK1δ phosphorylates α-, β- and γ-tubulin in vitro and that CK1δ specifically interacts with the trans Golgi network, COPI positive vesicles, and centrosomes in interphase cells [11], [12], [13], [14]. Moreover CK1δ is also associated with granular particles that are associated

• AON successfully alleviated the myotonic phenotype in DM mod

  2021-04-25

  

  AON successfully alleviated the myotonic phenotype in DM model mice [18], [23]. To screen for an optimal AON sequence, we used 25-mer phosphorothioate 2′ O-methyl RNA molecules that covered the exon 6B or exon 7A. Unexpectedly, AON 7A (+63−8) which covers the boundary of intron 7A and exon 7A enhanc

• An ideal CHK inhibitor would

  2021-04-25

  

  An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th

• br ANTITHROMBOTIC TREATMENTS br VOLUME OUTCOME RELATIONSHIP

  2021-04-25

  

  ANTITHROMBOTIC TREATMENTS VOLUME-OUTCOME RELATIONSHIP FOR REVASCULARIZATION PROCEDURES The guidelines also maintain the recommendations for training in PCI, both for ACS (≥ 75 procedures per operator in centers with at least 400 PCI procedures per year and a 24-hour on-call service) and for st

• Potential break through technology poised to overcome

  2021-04-25

  

  Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop

• Protein degradation via UPP involves

  2021-04-25

  

  Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a

• Many filarial species harbor an

  2021-04-23

  

  Many filarial species harbor an endosymbiotic bacterium of the genus Wolbachia. A recent investigation of Wolbachia distribution in 35 filarial species including 28 species and 7 genera and/or subgenera have shown that 37% of them harbor Wolbachia (Ferri et al., 2011). In filarial nematodes, Wolbach

• Ethyl naphthoates a h were successfully reduced to

  2021-04-23

  

  Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The

• Alternatively procedural factors may have contributed to the

  2021-04-23

  

  Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid

• br Acknowledgments This work was funded by

  2021-04-23

  

  Acknowledgments This work was funded by the EU ERDF and the Spanish Ministry of Economy and Competitiveness (MINECO) under Project TIN2013-41576-R, and the Spanish Ministry of Education, Culture and Sport (MECD) under a FPU grant (AP2010-3259), and the Andalusian Regional Government (Spain) under

• br Experimental Procedures br Acknowledgments br Introductio

  2021-04-23

  

  Experimental Procedures Acknowledgments Introduction Bisphenol A (BPA), 2,2-bis (4-hydroxyphenyl) propane, is widely used to manufacture consumer products including food and beverage containers (Vandenberg et al., 2007). It can be accumulated in human body via leaching from the polymers int

• In our former work our interest was in discovery

  2021-04-23

  

  In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b

• PD123319 EPAC induces SOCS gene expression in VECs

  2021-04-23

  

  EPAC1 induces SOCS3 gene expression in VECs, resulting in suppression of the JAK–STAT activation initiated by the sIL-6Rα/IL-6 trans-signalling complex [67]. EPAC1 regulates SOCS3 gene induction through the activation of C/EBP and c-Jun transcription factors, which interact directly with the SOCS3 p

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