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Introduction Nicotinic acid niacin NA
2021-09-17

Introduction Nicotinic m-Chlorophenylbiguanide hydrochloride (niacin, NA) has been used in the treatment of dislipidemia and cardiovascular disease for almost 60years (Offermanns, 2006). Large clinical studies showed that niacin alone or in combination with LDL-lowering drugs improved cardiovascula
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The typical pharmacophore for GPR agonists contains four
2021-09-17

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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br Presenilins in protein trafficking proteolysis
2021-09-17

Presenilins in protein trafficking, proteolysis and degradation An obvious explanation for the role of presenilins and γ-secretase in protein trafficking and degradation is that many reported γ-secretase substrates are functionally involved in protein transport. For example, members of the mammal
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OCA has recently been approved for the treatment of
2021-09-17

OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep
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Introduction Since the development of the
2021-09-17

Introduction Since the development of the first radioimmunoassay (RIA) to measure hormone levels in the late 1950s, for which Rosalyn Sussman Yalow was awarded the Nobel Prize for Medicine in 1977 (the second woman ever receiving it), the use of ml7 mg in molecular research has increased tremendou
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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 NP118809 and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with other liga
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Although pharmacological studies from the end of
2021-09-17

Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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Although pharmacological studies from the end of
2021-09-17

Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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In addition JMJ proteins respond to
2021-09-16

In addition, JMJ proteins respond to biotic stress and abiotic stress in plants. Rice genes OsJMJ704 and OsJMJ705, which have demethylase activities of H3K27me2/3 and H3K4me2/3, respectively, regulate defense-related genes and affect the defense ability of rice against bacterial pathogen Xoo (Li et
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br Prostaglandins meet Hippo The prostaglandins lie
2021-09-16

Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic ITD 1 by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced colitis,
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In the adult normal spinal cord the resident cells mainly
2021-09-16

In the adult normal spinal cord, the resident cells mainly include neurons, astrocytes, oligodendroglia and microglia (Lecca et al., 2012, Miyagi et al., 2012). After SCI, the lesion microenvironment is complex, which includes the functional changes of CNS resident cells and the infiltration of leuk
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Notably we observed that GPR activation
2021-09-16

Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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To facilitate the development of
2021-09-16

To facilitate the development of novel diagnostic and therapeutic interventions in NASH, a plethora of animal models have been used to identify molecular targets that are involved in the onset and progression of NASH. In view of recent advances in the understanding of the pathogenesis of NASH and pr
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In summary activated A AR exacerbated the reverse
2021-09-16

In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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To get a broader view of
2021-09-16

To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat GW 6471 and confirm the inhibition of this interaction
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