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A rate limiting step in the generation
2023-10-09
A rate-limiting step in the generation of kynurenine and xanthurenic LJI308 receptor is the oxidation of N-formyl-kynurenine to l-kynurenine via indolamine 2,3-dioxygenase (IDO) or tryptophan dioxygenase (TDO). IDO and/or TDO knockdown decreases and ectopic over-expression increases production of e
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Growing evidence indicates that GRKs can exert
2023-10-09
Growing evidence indicates that GRKs can exert different effects within the cell depending on the stimulus, cell type, and localization [97], [121]. In this sense, we were the first to demonstrate a mitochondrial localization for GRK2 [122], later confirmed by other investigators [123], establishing
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Corticosterone induced inhibition of OCT mediated
2023-10-09
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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Altogether the situations described above
2023-10-08
Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have
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In summary the role of
2023-10-08
In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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Acknowledgments br P c is expressed
2023-10-08
Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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Our previous studies found that
2023-10-08
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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plk inhibitor LPA binds to six specific cell surface GPCR
2023-10-08
LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino plk inhibitor homology) An et al., 1997, An et a
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Aurora A overexpression is also related to the activation
2023-10-08
Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer SB505124 australia [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these gene products a
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In Rainey et al published the results
2023-10-08
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Inflammations lead to the perturbation
2023-10-08
Inflammations lead to the perturbation of aromatase enzyme [112], which normally is responsible for a broad array of critical functions. Chemotherapy targets this enzyme, so this treatment option is never side-effect-free and not fully-effective. Therefore, the mankind should be careful so as not to
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Several studies have explored the
2023-10-08
Several studies have explored the relationship between dental implants and MRONJ development. López-Cedrún JL et al. [13] reported that BRONJ developed after implant treatment in nine patients who were taking bisphosphonates orally. The mean interval between the initiation of treatment and the onset
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A phase I trial has
2023-10-08
A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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br Acknowledgement Work in the McEwan
2023-10-08
Acknowledgement Work in the McEwan Laboratory is funded by the Chief Scientist Office of Scottish Government: Grants ETM-258 and ETM-382. BE is supported by an Erasmus scholarship (D -JENA01). Introduction The equine placenta is a noninvasive transient organ, classified as diffuse and epithel
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It was reported that oral administration of CSZ to
2023-10-08
It was reported that oral administration of CSZ to C57BL/6J mice significantly improved spatial learning and memory, and prevented Aβ-induced immunoresponse in Aβ25-35-injected mice. However, post-treatment with CSZ after Aβ25-35 administration, when Aβ was already accumulated, did not prevent Aβ-in
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