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The objective of this study
2022-06-21

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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Although pharmacological studies from the end of
2022-06-21

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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alizarin Introduction Thrombotic disorders including ischemi
2022-06-21

Introduction Thrombotic disorders including ischemic heart disease, deep venous thrombosis, and ischemic stroke represent one of the most common causes of death in the world [1]. All these conditions relate to states accompanied by a shift of hemostasis balance into a coagulation side because of va
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Paroxysmal or sustained atrial fibrillations
2022-06-21

Paroxysmal or sustained atrial fibrillations profoundly activate platelets and induce coagulation factors in the heart (Choudhury and Lip, 2003). Accumulating factor Xa and downstream thrombin in the fibrillating left atrium activate PAR1 and/or PAR2 signaling to modulate electrical characteristics
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In addition to Rabs several
2022-06-20

In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori
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The mechanism study demonstrated that
2022-06-20

The mechanism study demonstrated that BDNF is one of the fundamental mechanisms underlying JMJD2A effects during neuropathic pain. BDNF is a neurotrophin with essential functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels un
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microRNAs miRNAs of approximately nucleotides play vital rol
2022-06-20

microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme
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In conclusion while class I
2022-06-20

In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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A series of P P ureas
2022-06-20

A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen 43 7 of the urea yielded , a molecule which retained intrinsic potency against t
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HBV is an enveloped double
2022-06-20

HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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Hydroxyurea mg br Discussion The aminoglycoside antibiotic g
2022-06-20

Discussion The aminoglycoside antibiotic gentamicin continues to be an important agent against life threatening infections. However, nephrotoxicity is a major complication of the gentamicin administration. Thus amelioration of nephrotoxicity would enhance its clinical use. Several approaches invo
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Reduction of the hydrolysis of ATP is an
2022-06-20

Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct
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Fibronectin protein level was not affected by DIF
2022-06-20

Fibronectin protein level was not affected by DIF-1, although fibronectin has also been considered a canonical Wnt signaling pathway target gene product [39]. Thus, the canonical Wnt signaling pathway may not be critical for the regulation of the expression of fibronectin in malignant melanoma cells
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br Ketone body metabolism and neuronal
2022-06-20

Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona
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Recently an increasing number of
2022-06-20

Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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