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Because AM had limited efficacy on rodent GPR we used
2022-08-09
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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To further implicate the role of EAAT in morphine induced
2022-08-09
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 MLN8237 was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice at
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Boswellia papyrifera Del Hochst mostly grows in
2022-08-09
Boswellia papyrifera (Del.) Hochst., mostly grows in Sudanian and Sahelian regions and their oleo-gum resin is used medically in treatment of rheumatism, menorrhagia, amenorrhoea, vaginal infections, ulcers, sores, polyuria, syphilis, bronchitis, scrofulous affections, inflammations, asthma, diarrhe
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Z-FA-FMK The novel Ghsr IRES Cre
2022-08-09
The novel Ghsr-IRES-Cre knock-in mouse line allowed us to deconstruct the involvement of MBH GHSR-expressing neurons in mediating food intake responses using chemogenetic modulation of their neuronal activity. In our studies, hM4Di DREADD virus injections to inhibit GHSR neurons targeted several nuc
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Murine models of sickle disease have been valuable tools in
2022-08-09
Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot
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The active site of PS is located at the
2022-08-09
The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed
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cyp450 inhibitors Recently they reported an enyne
2022-08-08
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral cyp450 inhibitors (tmax=15min) and a decent pharmacokinetic prof
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With the nitrogen containing heterocycle components and the
2022-08-08
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic YO-01027 (, and ), followed by deprotection by TFA, smoothly provided the co
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In this study we intended
2022-08-08
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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The F P concentration reported
2022-08-08
The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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br Introduction Currently HIV infection
2022-08-08
Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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Interest in the non coding
2022-08-08
Interest in the non-coding genome has recently surfaced with accelerated emphasis in the past few years (Li et al., 2016). Transcription factors (TFs) bind to enhancers and mediate RNA initiation from distal transcriptional start sites (TSS) of genes. Epigenome sequencing of human and mouse during d
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br Main Text Metabolism drives diverse biological processes
2022-08-05
Main Text Metabolism drives diverse biological processes including differentiation, proliferation, and effector function in diverse cell types. In particular, the process of mounting an innate immune response to pathogens entails rapid sensing of a wide range of patterns displayed by invading mic
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Furthermore the absolute lack of E allele expression
2022-08-05
Furthermore, the absolute lack of E2 allele expression in both chronic and SVR cases, supports the protective role of the E2 allele against HCV infection at a time of exposure. However this hypothesis could not be entirely proved by this study due to lack of healthy individuals participation. Simila
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Mortality from breast cancer is almost always attributed
2022-08-05
Mortality from breast cancer is almost always attributed to metastatic spread of the disease to other organs, thus precluding resection as a treatment method. Unfortunately, conventional chemotherapy fails to eradicate most human cancers, including aggressive breast cancers. Studies over the past de
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