• br Halogenases Enzymatic C H activation leading to halogenat

  2020-06-08

  

  Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical

• br Iterative design approach overview An iterative design st

  2020-06-08

  

  Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti

• br Activity based probes br

  2020-06-08

  

  Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f

• br Conclusion From the series of synthesized N methylated

  2020-06-08

  

  Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration

• br Discussion Although DNA has a limited chemical stability

  2020-06-08

  

  Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap

• A An optimized BEI SEIscore based

  2020-06-08

  

  (A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare

• High throughput screening HTS of the

  2020-06-08

  

  High throughput screening (HTS) of the AstraZeneca gpr120 agonist collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) an

• Our previous studies have demonstrated that

  2020-06-08

  

  Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma

• In astrocytes mitogen activated protein kinases MAPKs are

  2020-06-08

  

  In astrocytes, mitogen-activated protein kinases (MAPKs) are activated after OGD-induced ischemic injury (Yung and Tolkovsky, 2003, Niu et al., 2009) and they regulate induction of AQP expression (Arima et al., 2003, McCoy and Sontheimer, 2010). It is well known that MAPKs, including extracellular s

• The X ray crystal structure of palbociclib bound

  2020-06-08

  

  The X-ray crystal structure of palbociclib bound to CDK6 without a Phosphate Colorimetric Assay Kit (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK

• We have previously characterized the leucine rich NESs locat

  2020-06-08

  

  We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma

• VEGF inhibition causes vascular regression and tissue hypoxi

  2020-06-08

  

  VEGF inhibition causes vascular regression and tissue hypoxia in tumor tissues and their surrounding healthy adipose tissues. In this regard, tumors in steatotic livers and adjacent to adipose tissues would experience more hypoxia than non-adipose tumors. Indeed, our present experimental results sup

• Michel et al calculated the mutual solubilities of water

  2020-06-08

  

  Michel et al. [34] calculated the mutual solubilities of water and hydrocarbons by a cubic equation of state. They asserted that conventional mixing rules can not satisfactorily describe the hydrogen bonding compounds. Kabadi and Danner [35] applied a modified form of Soave-Redlich-Kwong equation of

• Two major mechanisms including apoptosis and

  2020-06-05

  

  Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,

• SPR was used to measure biomolecular kinetic interactions be

  2020-06-05

  

  SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp

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