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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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Finally we argue that the estimated penetrance of CI calcula
2024-07-02

Finally, we argue that the estimated penetrance of 0.45% (95% CI 0.02%, 9.35%) calculated by leveraging the gnomAD (Lek et al., 2016) population data indicate that T201S is at most a low-risk gene variant for CJD. If we arbitrarily consider a central estimate of 10% or higher as the clinically signi
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Immunohistochemistry in tissue samples showed the expression
2024-07-02

Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of SIS3 tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted in signif
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Consistent with the in vitro results memantine ameliorated
2024-07-02

Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its neu
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The proposed formulation is however
2024-07-01

The proposed formulation is, however, challenging to solve since the structured sparsity-inducing norms are non-smooth. In order to solve the new objective function, we consider two different approaches: proximal averaging, which takes the average the solutions from the proximal operator for the ind
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br Hypothesis The hypothesis is that AhR
2024-07-01

Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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