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Neuronal cells have highly developed ER which makes them
2020-08-28

Neuronal L-703,664 succinate have highly developed ER, which makes them susceptible to loss of ER function following exposure to various agents, which leads to apoptosis (Lindholm et al., 2006, Katayama et al., 2004). Multiple pathways may be involved in ER stress-initiated apoptosis. Among them, t
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DHODH activity has been traditionally measured with
2020-08-28

DHODH activity has been traditionally measured with the standard colorimetric assay that monitors 2,6-dichloroindophenol (DCIP) reduction as absorbance decrease at 600 nm . This assay has permitted the identification of several families of DHODH inhibitors in a successful high-throughput screening (
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In conclusion our work provides
2020-08-28

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer d-glucose and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the treatm
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In rodents but not humans two splice
2020-08-28

In rodents but not humans, two splice variants of Chk are identified as Ntk and Ctk, which possess and lack the N-terminal unique domain, respectively. While Ctk is abundantly expressed in the brain, Ntk is selectively restricted to myeloid and lymphoid cells, especially megakaryocytes [31]. This ra
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Sotalol br Progestogens and venous thromboembolism clinical
2020-08-27

Progestogens and venous thromboembolism: clinical data Progestogens and haemostatis: biological studies For many years, the effect of HT on haemostatis has been largely investigated in observational studies as well as in high evidence level studies among users of oral and transdermal estrogens
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We propose that unlike other autophagy
2020-08-26

We propose that, unlike other autophagy genes, the specific increase in the expression of IRGM by pEIF2A plays a major role as a checkpoint allowing host cell survival by autophagy or host cell elimination by necroptosis. The localization of IRGM to the mitochondrial inner membrane, its ability to i
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Studies of LRRK tagged with green fluorescent protein reveal
2020-08-26

Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the orexin antagonist of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines i
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In untreated rodent or human hepatocytes PXR
2020-08-26

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 Materials and methods br Results and
2020-08-26

Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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The large body of structural knowledge that is
2020-08-26

The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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Preliminary studies evidenced the presence of CRFr in gamma
2020-08-26

Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this btk inhibitor area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration in t
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br The amygdala complex The amygdala
2020-08-26

The amygdala complex The amygdala complex is composed of distinct nuclei and subdivisions including the lateral (LA), basolateral (BL), and basomedial (BM) amygdala; the medial (Imp), lateral paracapsular (lpc), and main intercalated cell cluster (IN); and the lateral and medialcentral amygdala (
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Hymenialdisine the most potent inhibitor of parasite TgCK en
2020-08-26

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this ras inhibitor also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of C
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br Epac in cardiovascular pathophysiology Epac orchestrates
2020-08-26

Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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recombinant insulin Potential break through technology poise
2020-08-26

Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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