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Sodium Picosulfate During the course of our research on mGlu
2020-01-29
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Phylogenetically three related CXC chemokines
2020-01-29
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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Introduction Angiotensin II Ang II
2020-01-29
Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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Angiomatoid fibrous histiocytoma originally described
2020-01-29
Angiomatoid fibrous histiocytoma (originally described as angiomatoid malignant fibrous histiocytoma) is a soft tissue tumor of intermediate biologic potential. AFH typically arises within extremity deep dermis and subcutis in children and young adults,157, 158, 159 but can arise in older adults and
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In untreated rodent or human hepatocytes PXR
2020-01-25
In untreated rodent or human hepatocytes, PXR or CAR is stabilized by cytoplasmic co-chaperone partners like heat shock protein 90 (HSP90, Fig. 1). Upon ligand binding, the nuclear receptors are freed and translocated into the nucleus, identified as a pivotal step in PXR- or CAR-mediated transactiva
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br Acknowledgements This work was
2020-01-25
Acknowledgements This work was supported by the National Institute of Neurologic Disorders and Stroke (U54 HD061222, 1K23 NS107646-01, and 1K12NS089417-01), Rocky Mountain Rett Association, International Foundation for CDKL5 Research, the Ponzio Family Chair in Neurology Research, and NHMRC Senio
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N methyl d aspartate NMDA
2020-01-25
N-methyl-d-aspartate (NMDA) receptor antagonists, such as MK-801 and phencyclidine, induce cognitive dysfunction in both mice and humans [18]. In addition, antipsychotic drugs ameliorate MK-801-induced cognitive dysfunction; therefore, the acute application of MK-801 can be used as an animal model o
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It is important to note that
2020-01-25
It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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Unlike many forms of SNHL cCMV
2020-01-25
Unlike many forms of SNHL, cCMV may be treatable. The antiviral drug valganciclovir (VGCV) has been proposed to improve hearing, speech, and language outcomes associated with this infection [6]. A recent publication from the CASG (Collaborative Antiviral Study Group) reported that a six-month course
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ClC is not only a chloride ion
2020-01-25
ClC-3 is not only a chloride ion channel but also a regulatory protein involved in the regulation of multiple signaling pathways. The PI3K/AKT/mTOR signaling pathway plays a crucial role in regulating cell growth, migration, invasion, and distant metastasis [13,14]. Although abnormal PI3K/AKT/mTOR a
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br Dienogest DNG Dienogest is a nortestosterone
2020-01-25
Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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Prostanoids typically act in an autocrine and paracrine
2020-01-25
Prostanoids typically act in an autocrine and paracrine fashion by binding to specific receptors in target cell adhesion molecules and there is evidence that both PGE2 and prostacyclin may be required for the optimal activation of angiogenesis (Hata and Breyer, 2004). PGE2 and prostacyclin bind to
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Introduction Neuropathic pain occurs in approximately one th
2020-01-25
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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The DDRs have also been shown
2020-01-25
The DDRs have also been shown to be regulators of certain immunological functions. DDR1 is expressed in stimulated peripheral blood mononuclear ret pathway (Kamohara et al., 2001) and on activated T cells (Chetoui et al., 2011, Hachehouche et al., 2010, Kamohara et al., 2001). DDR1 can mediate cell
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br Results br Discussion The ubiquitin
2020-01-25
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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