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The role of the ER EK variant which is
2022-09-30
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of Prednisone levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect from the
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Natural Product Library In our reporter assay system C
2022-09-30
In our reporter assay system, C3H10T1/2-Gli1-Luc cells were incubated with Shh CM to induce Gli1-mediated luciferase activity (Fig. 1B). Z-Ajoene inhibited Shh CM-induced luciferase activity in a concentration-dependent manner as seen in Fig. 1C. Z-Ajoene also inhibited SAG (a Smo activator)-induced
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Recently unimolecular multi functional peptides that combine
2022-09-30
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with marbofloxacin and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and we
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GHSR A s have high levels
2022-09-30
GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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br Materials and methods br
2022-09-30
Materials and methods Transparency document Acknowledgments Introduction Hearing loss is the most common congenital sensory deficit. About 1–3 in 1000 children are affected at birth or during early childhood by severe hearing loss, which is defined as prelingual deafness, with at least h
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Cx mimetic peptides short synthetic peptides corresponding
2022-09-30
Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino 6 his tag sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concentr
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More polar substituents introduced on the position of the an
2022-09-30
More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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PBI is an agonist of GPR and acts as an
2022-09-30
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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The release of FBPase and aldolase from subcellular structur
2022-09-30
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle Helioxanthin derivative 5-4-2 was about 6–7 times
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Another important question for future studies will be
2022-09-29
Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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Lonidamine br Experimental br Acknowledgments We
2022-09-29
Experimental Acknowledgments We thank Mintek and Rhodes University for generous financial support and permission to publish these findings. T.O.O. gratefully acknowledges Obafemi Awolowo University, Ile-Ife, Nigeria for study leave. Introduction There are ∼35.3 million people living with H
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The coenzyme S adenosylmethionine SAM binding pocket of Set
2022-09-29
The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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In conclusion our results show that P C enhances
2022-09-29
In conclusion, our results show that P7C3 enhances endogenous neurogenesis by upregulating the generation of endogenous neuroblasts and neural stem/progenitor cells by increasing the expression of neuroprotective proteins (Bcl-2, ki67, DCX, adam11, adamts20, and β-tub3) by activation of the cAMP/PKA
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Rufinamide In vertebrates three cognate receptors or recepto
2022-09-28
In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino Rufinamid
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Tamoxifen is still the most frequently used
2022-09-28
Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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