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hexokinase inhibition Suspecting that ACL might regulate the
2024-01-16
Suspecting that ACL might regulate the expression or activity of myogenic transcription factors, Das knocked down MyoD and found that such intervention abolished the effect of ACL on fast MyHC expression and that, conversely, MyoD overexpression partially rescued reduced fast MyHC expression caused
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Although the LB domains of mGlu receptors have not
2024-01-16
Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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br ASK in multiple sclerosis and optic neuritis Multiple
2024-01-16
ASK1 in multiple sclerosis and optic neuritis Multiple sclerosis (MS), a chronic inflammatory demyelinating disease of the central nervous system (CNS), is the most common neurological disease among young adults in the United States and Europe (Dutta and Trapp, 2011). Although MS primarily affect
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As the experimental procedure used could reflect agonist sti
2024-01-16
As the experimental procedure used could reflect agonist-stimulation of both anterograde and retrograde APJ trafficking, as has been described for the δ-opioid peptide receptor (Zhang et al., 2006b, Zhang et al., 2006a), receptor internalization was more directly monitored by loading cell surface HA
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br Acknowledgments br Introduction Angiotensin II AngII is a
2024-01-16
Acknowledgments Introduction Angiotensin II (AngII) is among the most potent vasoactive substances produced in humans. Its effects are numerous, from vasoconstriction to control of fluid and electrolytes balances. Many of the physiological and pathological effects of AngII are mediated by the
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The clinical impact of our findings is
2024-01-16
The clinical impact of our findings is also supported by our earlier report that the level of 12-LOX expression was correlated with the tumor stage and grade [17], [52] and that overall, 38% of patients demonstrated elevated levels of 12-LOX in prostate cancer tissue compared with their matching nor
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The excellent potencies selectivities and
2024-01-15
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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Human testicular peritubular cells HTPCs are also the only
2024-01-15
Human testicular peritubular NVP-LCQ195 (HTPCs) are also the only human testicular cell type that can be isolated, cultured and studied in vitro (Albrecht et al., 2006, Mayerhofer, 2013). Results from recent studies indicate that their roles go beyond sperm transport and include immunological funct
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Regenerative mechanisms often require reemployment
2024-01-15
Regenerative mechanisms often require reemployment of pathways used during development in the embryonic and postnatal periods (Waschek, 2002). PACAP has diverse neurodevelopmental and growth factor-like effects (Botia et al., 2007; Vaudry et al., 2009; Waschek, 2002; Watanabe et al., 2016) and it is
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Optimization of the B ring specifically targeted
2024-01-15
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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Young disease transitioning B Sle mice show partial loss of
2024-01-15
Young disease-transitioning B6·Sle1 mice show partial loss of leukocyte Axl versus B6 controls (data not shown). Further, BMDM from diseased B6·Sle1.Yaa mice do not express detectable levels of ADAM10 and TACE (ADAM17) but do express basal levels of Axl similar to wild type B6-derived BMDM (Suppleme
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Autotaxin has been linked to chemoresistance through its abi
2024-01-15
Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer EDTA [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in patients
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In pancreatic islets we found an
2024-01-15
In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta
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LX7101 HCL br Regulatory mechanisms of ASK activity
2024-01-15
Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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br Experimental Procedures Additional information can be fou
2024-01-15
Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from
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