• br Transparency document br Main Text The centrosome

  2020-03-07

  

  Transparency document Main Text The centrosome is a non-membrane-bound organelle found in most animal cells. It has several important functions, including control of cilia formation, microtubule organization and nucleation, spindle assembly and transport of organelles and vesicles. Centrosomes

• For the SAR optimization of the

  2020-03-07

  

  For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic Venlafaxine moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by condens

• Our results suggest that formation of DDR

  2020-03-07

  

  Our results suggest that formation of DDR1b clusters may be important for and precede receptor phosphorylation. Indeed, while DDR1b clustering was readily detected (by YFP signal) 30 min after collagen administration, phosphorylated DDR1 species at Y513 (present in the IJXM) were evident after 4 h o

• In conclusion our data demonstrated that montelukast

  2020-03-07

  

  In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va

• Collagen compaction and alignment are generated by cell medi

  2020-03-06

  

  Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano

• Determination of relative potency EC by dose response

  2020-03-06

  

  Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an

• Williamson et al interrogated the fusion gene

  2020-03-06

  

  Williamson et al. [30] interrogated the fusion gene status of 210 appropriately reviewed and annotated RMS specimens divided into three groups: ERMS (n=77); fusion gene-positive ARMS (n=94); and fusion gene-negative ARMS (n=39), the latter comprising a group of tumor samples that appeared histologic

• br Materials and methods br Results br Discussion PKA and

  2020-03-06

  

  Materials and methods Results Discussion PKA and Epac are two principal effector proteins involved in cAMP signaling; they are expressed in a wide range of tissues and control diverse biological functions [10]. The existence of two cAMP effectors provides more precise regulation of cAMP sig

• br Multi subunit RINGs There

  2020-03-06

  

  Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,

• Ubiquitin activating enzyme activates ubiquitin by

  2020-03-06

  

  Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP producti

• br The related catalytic regions of the human DNA ligases

  2020-03-06

  

  The related catalytic regions of the human DNA ligases contain three domains, a DNA binding domain (DBD), a nucleotidyl transferase domain (NTase) and an oligonucleotide/oligosaccharide-fold binding domain (OBD) (Ellenberger and Tomkinson, 2008). Similar to DNA ligase I, the DNA ligase III polypep

• Herein we explored by docking studies

  2020-03-06

  

  Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the

• One of the therapeutic proteins used in cancer therapy

  2020-03-06

  

  One of the therapeutic proteins used in cancer therapy is glucarpidase, also known as Carboxypeptidase G2, CPG2, which originates from the bacterium Variovorax paradoxus (old name, Pseudomonas sp. strain RS-16). It has no mammalian equivalent (Thompson et al., 1994; Kamlage, 1994) and is a zinc-depe

• The action of pt PGE

  2020-03-06

  

  The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in

• br The ubiquitin proteasome system The ubiquitin

  2020-03-05

  

  The ubiquitin proteasome system The ubiquitin proteasome system (UPS) plays a significant role in the regulation of cell growth and survival, in addition to maintaining cellular homeostasis. By means of the UPS, Cinchonidine receptor can precisely and temporally degrade approximately 80% of the e

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