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br Drugs approved or in
2021-09-18
Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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Anti apoptotic Bcl proteins have
2021-09-18
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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HCV NS A inhibits induction of the type I interferon
2021-09-18
HCV NS3/4A inhibits induction of the type I interferon response by cleaving MAVS from the mitochondrial surface (Li et al., 2005b). MAVS is cleaved at cysteine 508, and citco of cysteine 508 to arginine (C508R) abrogates cleavage (Li et al., 2005b). GBV-B and the related canine hepatitis virus also
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JMJD C is another JmjC domain
2021-09-18
JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran
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br Acknowledgments br Introduction Histone deacetylases HDAC
2021-09-18
Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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br Results br Discussion To further evaluate the extent
2021-09-18
Results Discussion To further evaluate the extent of H3T3A and H3T3D roles in the segregation of sister chromatids enriched with different populations of H3 during mitosis (Figure 1B, step two), we modeled all possible segregation patterns in male GSCs and compared these estimates to our exper
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Selective pharmacological inhibition of tonic
2021-09-17
Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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Recent research reveals that human alkyladenine DNA glycosyl
2021-09-17
Recent research reveals that human alkyladenine DNA glycosylase (hAAG) is an important protein enzyme which can specifically recognize and excise a variety of alkylated purines and deoxyinosine from DNA [12]. hAAG plays pivotal roles in maintaining genomic integrity, and it is involved in Anisomycin
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br Conclusion In summary a series of novel GPR agonists
2021-09-17
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic l glycine motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent
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Transmembrane AMPA receptor regulatory proteins TARPs are a
2021-09-17
Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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br Acknowledgments The financial support from the
2021-09-17
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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Olanzapine has been reported to attenuate insulin
2021-09-17
Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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br Concluding remarks In this
2021-09-17
Concluding remarks In this small material of thirteen pituitary tumors of various kinds, we could not run statistical analysis. However, with a follow-up period of up to five years, we show that Disclosure Statement Acknowledgments Introduction Galanin is a 29/30-residue neuropeptide fo
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The effects of galanin on anxiety may depend on the
2021-09-17
The effects of galanin on anxiety may depend on the site of drug administration, on the galanin receptor subtypes activated and on the animal models of anxiety employed (Barrera et al., 2005, Holmes and Picciotto, 2006, Soares et al., 2016a, Soares et al., 2016b). For instance, administration of gal
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An advantage of photolabeling with tritiated
2021-09-17
An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled ionophores and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with other l
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