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Hydantoin in region F bridging the phenoxybenzene and
2022-07-29

Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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The activation of GPR FFA signaling
2022-07-29

The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign
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ADAM has two alternative splicing forms a membrane
2022-07-29

ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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597 PKC does not however directly stimulate secretion by ini
2022-07-29

PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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Newly identified evidence has put immune checkpoint inhibito
2022-07-28

Newly identified evidence has put immune checkpoint inhibitors into the spotlight. However, even though they have been reported to achieve optimistic outcomes [67], there is still a provocative question about their limitations [68]. The solid evidence above has provided us with translational values
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Several studies have also suggested that
2022-07-28

Several studies have also suggested that Wnt signalling can in turn stimulate the transcriptional activity of Yap/Taz (Figure 2, Figure 3). In the Azzolin model, Yap/Taz not only block β-catenin signalling, but their association with Axin1 and/or β-catenin also maintains them in an inactivate state
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The RAS RAF MEK ERK pathway is
2022-07-28

The RAS/RAF/MEK/ERK pathway is a central controller of cell proliferation and survival and, consequently, alterations to some of its components lead to hyperactivation of the pathway, an event related to numerous types of cancer [172]. High rates of alterations to this pathway are found in leukemia,
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The HCV NS A protease
2022-07-28

The HCV NS3/4A protease consists of two subunits, NS3 and NS4A. NS3 comprises an N-terminal serine protease domain and a C-terminal RNA helicase domain [12]. NS4A acts as a cofactor, which ties the holoenzyme complex to an intracellular membrane compartment. The presence of the central region of NS4
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br Patients and methods br Results
2022-07-28

Patients and methods Results Discussion The positivity of serum anti-HBc is the most commonly used marker to confirm the history of HBV infection. Quantification of serum anti-HBc has been explored as a marker of HBV-induced hepatitis and the adaptive immune response against HBV infection a
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Decreasing GSK activity has therapeutic benefits in
2022-07-27

Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic Dexmedetomidine injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating
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While the specific set of challenges associated with deorpha
2022-07-27

While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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Introduction The onset of uterine labor
2022-07-27

Introduction The onset of uterine labor is the culmination of a gradual uterine activation wherein physiological inflammation induces a common prolabor pathway characterized by increased myometrial contractility, weakening of fetal membrane integrity, and cervical ripening. Pathological proinflamma
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5-Formyl-CTP A motivation for this study
2022-07-27

A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c
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GPR and TRPV co localized in
2022-07-27

GPR35 and TRPV1 co-localized in small- and medium-diameter DRG neurons. Nociceptive (Aδ- and C-fiber) neurons expressing TRPV1 mediate hyperalgesia, neurogenic inflammation, and neuropathic pain [12]. The cAMP-protein kinase A (PKA) dependent modifications of TRPV1 currents have been demonstrated in
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This definition of To assess the roles of GPR and GPR
2022-07-27

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) This definition of from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh1
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