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The GPR receptor is also
2022-02-21

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Als
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The synthesized methoxyamide derivatives were evaluated for
2022-02-21

The synthesized -methoxyamide derivatives were evaluated for in vitro as GPR119 agonists (, , ) whereas GSK1292263 (II in ) was used as the reference standard. To identify novel sulfone or tetrazole surrogates, diverse functional groups including amide, -sulfonyl amide, hydrazide, -methoxy--methyla
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GW was also the starting point for
2022-02-21

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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Introduction Cancer is known as a
2022-02-21

Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous Ac-IETD-pNA synthesis have the ability to bypass the normal apoptosis mechanism
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We also demonstrated that inhibition of NAAG hydrolysis to
2022-02-18

We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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This GluR A independent mechanism by which the associative s
2022-02-18

This GluR-A-independent mechanism, by which the associative strength of spatial locations can be increased (and/or decreased) gradually over many trials, and which presumably underlies spatial reference memory acquisition during tasks such as the Morris watermaze or the radial maze (Zamanillo et al.
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The dorsal horn of the spinal cord shows
2022-02-18

The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,
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L Family Leguminosae widely distributed in tropical and
2022-02-18

L. (Family Leguminosae) widely distributed in tropical and subtropical regions of the world. As a medicinal and edible plant, it is widely used in Asia, especially in China, Korea, Japan and India. It was first recorded in Shen Nong Ben Cao Jing (神农本草经), and was described having the effect of cleari
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br Conclusions Temporally controlled disruption of
2022-02-18

Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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nrf2 inhibitor In Solloway and colleagues reported that mice
2022-02-18

In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino nrf2 inhibitor dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin
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RVX-208 The molecular nature of these
2022-02-18

The molecular nature of these putative Ca2+ RVX-208 is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which were characterized as B-channels, seem to have very lon
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br Materials and methods br Results br Discussion
2022-02-18

Materials and methods Results Discussion The current study validates a key role for GAL3 receptors in consummatory drive for sucrose, saccharin, and most notably ethanol intake in mice. We show that alcohol preferring mice drink less ethanol compared to wildtype mice when treated with the G
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Having shown that some of substitutions Cl CF at the
2022-02-18

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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Accordingly and in animal models a high fat diet
2022-02-18

Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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Recently the classical view of the compartmentalization of t
2022-02-18

Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic ap-1 (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, the last two enz
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