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The inhibitory activities against HDAC and
2022-03-10
The inhibitory activities against HDAC1 and HDAC6 of title compounds were evaluated in a fluorescent assay using SAHA and ACY-1215 as positive control. The results were displayed in A. Compounds – with linker containing 5–7 carbons showed good inhibitory activities against HDAC6. They also displayed
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Interestingly in vivo infusion and uptake of Ang
2022-03-10
Interestingly, in vivo infusion and uptake of Ang II in intact mice indicated that multiligand endocytic receptor megalin has at least some role in the uptake of Ang II and the downstream signaling process in proximal tubule Cy3 carboxylic acid (non-sulfonated) (PTCs) in vivo [173]. Earlier in vivo
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Previous studies have shown that Cu
2022-03-10
Previous studies have shown that Cu(I) neurotoxicity includes induction of ROS with involvement of the NF-kB pathway and apoptosis (Butterworth, 2010) and that, in its Cu(I) state, Cu(I) alters microglia phenotype and inhibits nitric oxide release (Rossi-George et al., 2012). Cu(I) has a great affin
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We have previously established the pharmacokinetic profile a
2022-03-09
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in GSK621 synthesis and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The co
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Moreover we revealed that alanine and
2022-03-09
Moreover, we revealed that β-alanine and taurine, a structural analog of β-alanine, have different receptor affinity in the SG neurons of the spinal dorsal horn. Additionally, previous studies indicate that taurine regulates nociceptive information at the spinal cord level, and we have previously de
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The need for an inflammatory risk profile was recently discu
2022-03-09
The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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In this study our result suggests that exogenous GR agonist
2022-03-09
In this study, our result suggests that exogenous GR agonist DEX and GR inhibitor RU486 can affect dopaminergic neurotransmitters in the brain. Pituitary adenylate cyclase-activating polypeptide (PACAP), an endogenous neuropeptide, can regulate the synthesis and release of catecholamine. McArthur et
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How do myofibroblast sources compare between bone marrow and
2022-03-09
How do myofibroblast sources compare between bone marrow and other organs? Perivascular matrix metalloproteinases with MSC properties significantly contribute to fibrosis in muscle, fat, skin, heart, kidney, lung, and liver (reviewed in Iwayama et al., 2015) and activate Gli1 in many of these organ
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PHA-665752 Growth hormone secretagogue receptor GHSR is a
2022-03-09
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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FXR agonists represent an attractive
2022-03-09
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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The current gold standard for diagnosing BAM or BAD
2022-03-09
The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) EHop-016 mg (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid an
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We have isolated various bioactive peptides acting by bindin
2022-03-09
We have isolated various bioactive endothelin receptor antagonists acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin
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Acquiring resistance to the FGFR inhibitor may determine tre
2022-03-09
Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibit
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In our cohort each patient had
2022-03-09
In our cohort, each patient had a median of 2 Anti-FXa measurements performed daily and a median of 1 infusion rate change daily to maintain therapeutic unfractionated heparin levels. Previously, several studies have documented that APTT-based protocols lead to more fluctuations in comparison with A
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The IN gene of the HIV isolate
2022-03-09
The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN
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