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Through activation of the CD GOPC pathway attenuated vaccina
2024-07-03
Through activation of the CD46–GOPC pathway, attenuated/vaccinal MeVs rapidly induce a transient phase of autophagy which then diminishes with no signs of negative regulation and precedes a second autophagy phase related to viral protein synthesis [115]. In sharp contrast, virulent MeVs do not inter
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Therefore the rational design of target compounds is based o
2024-07-03
Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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Sixth significant progress has been made during the last
2024-07-03
Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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Further validation for a role in LOX pathway
2024-07-03
Further validation for a role in 12/15-LOX pathway in mediating adipocyte function comes from studies revealing a regulatory role of lipocalin-2 on 12/15-LOX activity. Lipocalin-2, a glycoprotein member of the lipocalin superfamily, is a novel abundant adipokine implicated in obesity-mediated inflam
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The literature suggests that adiponectin has
2024-07-03
The literature suggests that adiponectin has a steroidogenic effect on ovarian function. In pigs, in vitro studies have shown that adiponectin reduced basal testosterone secretion in internal theca cells; in granulosa cells, it increased secretion of estradiol and, in combination with insulin, incre
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The CK catalyzes the reversible
2024-07-02
The CK catalyzes the reversible conversion of creatine into creatine phosphate using ATP and thereby releasing ADP. The CK isoenzymes, specifically localized in places where there is a demand and production of energy, are linked to a creatine/creatine phosphate shuttle (Wallimann et al., 1998). This
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As an alternative to chronic receptor blockade we have been
2024-07-02
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Imiloxan hydrochloride adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK
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sVRPs were more sensitive to ABT than MSRs
2024-07-02
sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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Encouraged by this observation a systematic SAR
2024-07-02
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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br Introduction Myasthenia gravis MG is an
2024-07-02
Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic ceramide sale receptor (AChR; (Lindstrom et al., 1976). Many
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Later the same group designed
2024-07-02
Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18
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It has also been reported that defects
2024-07-02
It has also been reported that defects in ATM or ATR signalling are synthetically lethal with PARP inhibition (Turner et al., 2008, Peasland et al., 2011, Yap et al., 2011, Michels et al., 2014), suggesting that combined inhibition of PARP and ATM or ATR may be an effective therapeutic strategy. In
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Bioavailability has been defined as the amount of
2024-07-02
Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the
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br Introduction Active oxygen radicals in the
2024-07-02
Introduction Active oxygen radicals in the human body have a strong effect of inducing lipid peroxidation, which in turn induces oxidative imbalance and causes various diseases. Natural polysaccharides are substances with certain antioxidant activity. They are used as antioxidants and have advant
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Weak and transient interactions of HMGB proteins in such hit
2024-07-02
Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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