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br Materials and methods br Results and discussion In
2021-03-03
Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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mexiletine hcl The use of inhibitors clearly has its caveats
2021-03-03
The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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Leukotrienes themselves are implicated in the development of
2021-03-03
Leukotrienes themselves are implicated in the development of gastrointestinal ulcers, asthmas, and different inflammatory processes [18], [19]. It is noteworthy that COX isozymes and LOX share the same substrate arachidonic acid; therefore, inhibition of prostaglandins production by cyclooxygenase p
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We have previously reported that
2021-03-03
We have previously reported that CK2 is downregulated in senescent human lung fibroblast IMR-90 cells, aged rat tissues, and aging nematodes [17,18]. CK2 downregulation induces cellular senescence via the PI3K-AKT-mTOR-reactive oxygen species-p53-p21Cip1/WAF1 pathway in human cells [[19], [20], [21]
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Epac proteins consist of a carboxyl terminal catalytic
2021-03-03
Epac proteins consist of a carboxyl-terminal catalytic region and an amino-terminal regulatory region, which harbors one cAMP-binding domain in Epac1 and two in Epac2 [22], [32], [51]. In the absence of cAMP, the regulatory region covers the CDC25-homology domain and autoinhibits Epac's enzymatic ac
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The interaction of EPAC with Rim
2021-03-03
The interaction of EPAC2 with Rim1 has an important role in regulating neurotransmitter release. In addition, a recent EPAC2 knockout mice model study provides evidence that EPAC2 promotes transmitter release by maintaining the readily releasable pool (RRP) at mossy fiber (MF) synapses in the hippo
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br Halogenases Enzymatic C H activation leading
2021-03-03
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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LVDP values of at the end of reperfusion L NAME
2021-03-03
LVDP values of ~80% at the end of reperfusion. L-NAME treatment did not modify the contractility detected in ischemic control hearts but annulled the actions of BZ acquiring LVDP values up to 40% (Fig. 4 A). A similar pattern was observed when +dP/dtmax was analysed (Fig. 4 B). LVEDP, as an index o
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Next we elucidated that the Mtb
2021-03-03
Next, we elucidated that the Mtb enolase binds to host plasminogen with a high affinity. The KD value of 360nM for this interaction suggested an avid binding between the two proteins in vivo. This observation is also in conciliation with the observed KD values for enolase-plasminogen interactions in
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Upon Edn ligand binding endothelin receptors can induce a
2021-03-03
Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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br Materials and methods F philippinensis plants were collec
2021-03-03
Materials and methods F. philippinensis plants were collected in August 2014 at a farm in Ninning, Guangxi province, China and identified by Dr. Yimmin Zhao. Voucher specimens (No. 530) were deposited in the Herbarium of Gaunxi Botanical Garden, China. Human recombinant neutrophil elastase (EC 3.
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An important role for the
2021-03-03
An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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One of the most fundamental
2021-03-03
One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it PYR-41 only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most examples of mono
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The physiological role of the UCNs in the regulation of
2021-03-03
The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown to
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Recently we have observed that pharmacological PPAR and PPAR
2021-03-03
Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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