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ATP binding cassette transporters such as ABCA and
2019-12-02
ATP-binding cassette transporters such as ABCA1 and ABCG1 are expressed on cell membranes to transport cholesterol from 7867 to HDL. These transporters help to improve RCT and reduce atherosclerosis. ABCA1 and ABCG1 gene expression are primarily induced by the stimulation of liver X receptor/retino
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In order to evaluate the in vivo pharmacology associated wit
2019-12-02
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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In terms of its protease activity MME
2019-12-02
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other Thio-TEPA of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin r
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br Transparency document br Acknowledgements We thank Prof
2019-12-02
Transparency document Acknowledgements We thank Prof. Barbara Brodsky for valuable comments and discussion. We thank the support of the Tufts start-up fund and the Knez Family Faculty Investment Fund for Y.-S. L, and the Tufts Summer Scholar program for E.C. Introduction Discoidin domain r
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Recently a non proteolytic role of COP in
2019-12-02
Recently, a non-proteolytic role of COP1 in stabilizing PIF3 proteins in the dark has been revealed . Previous studies have shown that the endogenous levels of PIF3 protein in etiolated seedlings were nearly undetectable . Ling found that the GSK3-like kinase BRASSINOSTEROID-INSENSITIVE 2 (BIN2) p
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br Materials and methods br Results The i
2019-11-30
Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha
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Numerous small molecule CRF receptor
2019-11-30
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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It is noteworthy that epidemiological studies have demonstra
2019-11-30
It is noteworthy that epidemiological studies have demonstrated that some GAD patients have experienced anxiety symptoms in childhood and young adulthood, whereas others have developed their disorder at a later age (especially persons ≥ 50 years of age) (Hoehn-Saric et al., 1993; Le Roux et al., 200
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Although CK phosphorylated Msn as
2019-11-30
Although CK2 phosphorylated Msn4 as well as Msn2 (Fig. 1A), the two CK2-dependent phosphorylation sites in Msn2 are not conserved in Msn4. Thus, Msn2 and Msn4 might be differently regulated by CK2-dependent phosphorylation. Msn2 and Msn4, which have 41% identity and similarity in size and amino nisi
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br Materials and methods br Results br Discussion Human Chk
2019-11-30
Materials and methods Results Discussion Human Chk, a member of the Csk-family, was initially cloned from two different megakaryocytic cell lines [2], [3]. Structural comparison of human Chk with human Csk shows that human Chk has the additional N-terminal unique domain [2], [3], [25]. Chk
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br Substrate characterization of candidate peptide reporters
2019-11-30
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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The totality of evidence from randomized
2019-11-30
The totality of evidence from randomized clinical trials supports the premise that worsening isx receptor failure is a class effect of DPP-4 inhibitors. A meta-analysis by Verma et al. (54) of 100 randomized controlled clinical trials reported that the use of DPP-4 inhibitors was accompanied a signi
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To study the role of DNA PK
2019-11-30
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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Since the initial identification of DNA ligase inhibitors by
2019-11-30
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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Within the X CX PX RX motif of several prokaryotic
2019-11-29
Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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