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Receptors containing an x y subunit interface where x
2024-01-11
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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br Concluding remarks It is clear that a disordered
2024-01-11
Concluding remarks It is clear that a disordered l-arginine homeostasis by changes in arginase, NOS and ADMA activity and expression, is not only vital in the chronic airway diseases, smad pathway and COPD, but also seems to play an important role in many co-morbidities. Unknown, however, is whe
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As an internal control this
2024-01-11
As an internal control, this study validated many of the known associations between GATA3 and predictive markers. GATA3 was shown to be associated with ER and PR, which are both well-known correlations. GATA3 was also negatively correlated with nuclear grade, which is consistent with our knowledge o
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Immunohistochemistry in tissue samples showed the expression
2024-01-11
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of apiii tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted in signif
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In pancreatic islets we found an increase in protein
2024-01-11
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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Recently two distinct small molecule inhibitors of PHGDH
2024-01-11
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Fmoc-Hyp-OH with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the gro
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The correlation in the increase of BADH mRNA protein levels
2024-01-11
The correlation in the increase of BADH mRNA, protein levels, and enzyme activity, demonstrate that oxidation of betaine aldehyde by BADH is primordial to regulate the GB accumulation during physiological cardiac hypertrophy induced by pregnancy, this implies a major role because GB levels enhance c
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The excellent potencies selectivities and improved PK associ
2024-01-11
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
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We have previously shown that the antinociceptive effect of
2024-01-11
We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific EPZ015666 blockade or activation (Rojas-Corrales et al., 2000). Moreover, i
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Serum soluble sCD is a
2024-01-11
Serum soluble sCD21 is a shedding product from the ectodomain of membrane CD21 after B cell activation (Masilamani et al., 2003, Masilamani et al., 2004a, Masilamani et al., 2004b, Grottenthaler et al., 2006, Hoefer et al., 2008), which resembles the ligand-binding capacity of intact CD21 (Wu et al.
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Finasteride has been shown to be a mechanism
2024-01-10
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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It has been reported that HT R involves in type
2024-01-10
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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Taniyama et al reported a female
2024-01-10
Taniyama et al. reported a female with infertility who had a homozygous T-to-A transversion at nucleotide position g.2472 in exon 3 of the CYP17A1 gene (mutation Y201N) and decreased 17-hydroxylase and 17,20-lyase activities of GSK2334470 mg was initiated using dexamethasone to control adrenal P pr
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Our sample is representative of
2024-01-10
Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to
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br Conflict of interest br Acknowledgements We thank Ann
2024-01-10
Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota
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