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The ambiguity surrounding the role played by the
2023-04-18

The ambiguity surrounding the role played by the 15-LOXs in malignant biological processes stems also from the limitations of current animal models, and especially the usage of its 12/15-LOX murine homolog, which can also catalyze the production of 12-HETE. Indeed, the proinflammatory effect of 12-H
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In this review we will present the traditional and actual
2023-04-18

In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Fourth non canonical sites may
2023-04-18

Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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br Acknowledgement br Introduction Estrogens play an importa
2023-04-18

Acknowledgement Introduction Estrogens play an important role in the development and progression of breast cancer (McGuire et al., 1976; Clemons and Goss, 2001). 17β-Estradiol (E2), the most biologically active estrogen in breast tissue, functions via its nuclear receptors, estrogen receptor (
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As patients with type diabetes are
2023-04-17

As patients with type 2 diabetes are known to be hyperinsulinemic per se, this relationship between insulin/IGF1 receptor and AR may point towards a causal role of insulin in AR upregulation. Indeed, this is supported by several previous observations. Beyond the already mentioned AR activation by in
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Recent studies revealed that certain plant derived compounds
2023-04-17

Recent studies revealed that certain plant-derived compounds can also interfere with AR function. One way of such an interference is by modulating its expression levels. This is the case for the two flavonoids quercetin and luteolin that have been reported to repress the function of AR by inhibiting
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The present study determined the effect
2023-04-17

The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that PF-573228 non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcifica
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BIX 01294 synthesis The direction of glutamate transport by
2023-04-17

The direction of glutamate transport by the cell membrane transporter is reversible. As mentioned above, glutamate transport is an electrogenic process associated with a transmembrane ion gradient established by the Na+-K+ pump through hydrolysis of adenosine triphosphate. Under conditions of energy
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The excellent potencies selectivities and improved PK associ
2023-04-17

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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It is worth mentioning that
2023-04-17

It is worth mentioning that cordycepin, as an adenosine analogue, is structurally similar to adenosine. A previous study has shown that the anti-apoptotic effects of cordycepin are partially dependent on the activation of A1R [16], and cordycepin increases theta waves power density via nonspecific a
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The following are the supplementary data related to this art
2023-04-17

The following are the supplementary data related to this article. Conflict of interest Acknowledgements Disclosure of interest Introduction Since the introduction of platinum-based chemotherapy, metastatic testicular cancer has become a curable disease and most testicular cancer patient
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br Funding br Introduction The interest
2023-04-17

Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely a
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The downstream targets of ATR involved
2023-04-17

The downstream targets of ATR involved in mediating human telomerase recruitment have not yet been identified. Under stalled fork conditions, activated ATR is able to phosphorylate and activate ATM (Stiff et al., 2006, and Figures 4C and 4D); whether this Avasimibe of ATM participates in a positive
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br COPD As in asthma also
2023-04-17

COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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br Prostate cancer and resistance to
2023-04-17

Prostate cancer and resistance to AR targeting treatment The AR plays a pivotal role in the development, differentiation, homeostasis and secretory function of the normal prostate (Wilson, 2011). The AR is also a key player in many phases of prostate carcinogenesis (Huggins et al., 1941, Scher an
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