• The first example of a broadly acting antiviral drug

  2021-06-07

  

  The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth

• N,N-Dimethylsphingosine DGAT is specifically responsible for

  2021-06-07

  

  DGAT2 is specifically responsible for endogenous synthesis of TAGs which are then packed into cytosolic LDs in the cytosol for storage and luminal apolipoprotein B (apoB)-containing LDs in the ER lumen destined for VLDL secretion [122,127]. DGAT2 can also synthesize TAG using exogenous FAs and suppo

• Ultimately we decided to investigate the role of Cyp a

  2021-06-07

  

  Ultimately, we decided to investigate the role of Cyp3a in obesity because Hepatic P450 Reductase-null (HRN) mice with no P450 activity show hepatic steatosis with increased Cyp2b10 and Cyp3a11 expression, perturbations in liver size, lipid homeostasis, and increased liver polyunsaturated fatty acid

• A summary of the drug CDK hydrophobic hydrogen bonding

  2021-06-07

  

  A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different Darunavir Ethanolate the same value [77], which facilitates comparisons amo

• alisertib br Material and methods br Results br Discussion T

  2021-06-07

  

  Material and methods Results Discussion The present study shows that peripheral administration of the nonpeptidic corticotropin-releasing factor CRF1 receptor antagonist CP-154,526 before a social defeat inhibits the development of CPP induced with a subthreshold dose of cocaine and reverse

• By using the C elegans Matrisome Annotator tool we

  2021-06-07

  

  By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome amc 7 in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome for various b

• MdHCLB channels expressed in Xenopus oocytes produced curren

  2021-06-07

  

  MdHCLB channels expressed in Xenopus oocytes produced currents in response to HA and GABA (Fig. 1, Fig. 3). This is in agreement with the findings with Drosophila HCLB channels (Gisselmann et al., 2004). In the HA concentration-response curves, the effects of GABA were additive to those of HA only i

• br Allosteric inhibitors In general

  2021-06-07

  

  Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d

• br Acknowledgments br Introduction br Endothelin

  2021-06-05

  

  Acknowledgments Introduction Endothelin receptors Shortly after the discovery of ET‐1, two types of seven transmembrane G protein‐coupled receptors were cloned called endothelin receptor A (ETA) (Arai et al., 1990) and ETB (Sakurai et al., 1990). The affinity of the ETA receptor for ET-3 is

• The majority of serpins inhibit

  2021-06-05

  

  The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran

• br Materials and methods br Results

  2021-06-05

  

  Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th

• E is a classical initiator

  2021-06-05

  

  E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral Matrine known as the “origin of DNA replication”, or “ori” for short. For most PV types examined to date, the minimal

• The UPP broadly involves proteolysis in biochemical processe

  2021-06-05

  

  The UPP broadly involves proteolysis in biochemical processes and is a potential target for cancer therapy. The UPP degrades unfolding or damaged proteins by an ATP-dependent mechanism (Ciechanover, Elias, Heller, Ferber, & Hershko, 1980). It also plays an important role in ion channels regulation,

• Lately using receptor TM peptides BiFC and PLA experiments

  2021-06-05

  

  Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer

• In the gel shown in Figure at early time points

  2021-06-05

  

  In the gel shown in Figure 8, at early time-points, 14% of the input dsDNA is converted to these intermediate species. These persist in the gel to later times, with approximately 50% of these being unwound. This unwinding occurs at a considerably slower rate and is due to that fraction of the popula

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