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Recently multiple receptor agonists have been
2022-01-25
Recently, multiple receptor agonists have been developed to treat type II diabetes (Finan et al., 2013, Finan et al., 2015). We have tested novel dual GLP-1/GIP receptor agonists that showed good neuroprotective effects that are superior to single GLP-1 analogues (Cao et al., 2016, Jalewa et al., 20
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CORM-3 Various strategies have been pursued in the search fo
2022-01-25
Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino CORM-3 substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro3(
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RO4987655 GHRL effect on appetite is influenced by its dose
2022-01-25
GHRL effect on appetite is influenced by its dose and route of administration, where central or peripheral administration of GHRL at low doses increases feed intake, via acting on orexigenic hypothalamic neurons, and decreases appetite at high doses in chickens (Jonaidi et al., 2012), quails (Shoush
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To obviate the mitogenic FGF activity several engineered
2022-01-25
To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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It is considered that activations
2022-01-25
It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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ddhGTP what A few previous studies have
2022-01-25
A few previous studies have examined Factor Xa inhibitors for VTE prophylaxis in hip fracture patients. In a 2001 paper, Eriksson et al. studied 1250 patients with hip fractures that had been randomized to either postoperative Factor Xa inhibitor or enoxaparin [13]. Each patient received bilateral v
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br Experimental procedures br Results Hdc KO mice show basal
2022-01-25
Experimental procedures Results Hdc-KO mice show basal activation of the MAPK and AKT/GSK3β pathways in the dorsal striatum (Rapanelli et al., 2014). These signaling pathways are differentially regulated by the H3 receptor in dMSNs and iMSNs in wild-type mice (Rapanelli et al., 2016). To bette
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br Funding br Conflict of interest statement br References a
2022-01-25
Funding Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Recent papers have shown that Interferon-free hepatitis C virus (HCV) therapies with
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An interesting question is why RhoF has
2022-01-25
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino Necrostatin 1 mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF, rather
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We have previously established the pharmacokinetic profile a
2022-01-25
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in Cy5 NHS ester (non-sulfonated) and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cel
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The mechanisms of action of
2022-01-25
The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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In addition to vertebrate species GnRH has
2022-01-24
In addition to vertebrate species, GnRH has been identified in invertebrates, such as in the Protochordate Ciona intestinalis (Powell et al., 1996; Adams et al., 2003), the decapods mollusk Octopus vulgaris (Iwakoshi et al., 2002), the gastropod mollusk, the sea hare Aplysia californica (Zhang et al
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We first investigated the influence of the acyl
2022-01-24
We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents
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SGLT inhibitors have been accepted as a
2022-01-24
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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A-803467 br Hedgehog HH signaling plays an important role bo
2022-01-24
Hedgehog (HH) signaling plays an important role both during embryonic development and adult life. It is involved in the regulation of cell differentiation, cell proliferation and tissue polarity, as well as in the maintenance of stem cells, tissue repair, and regeneration (, ). Three ligands, Indi
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