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br ABCA mRNA expression is elevated in Niemann
2024-04-28
ABCA2 mRNA expression is elevated in Niemann-Pick type C and familial hypercholesterolemia fibroblasts Niemann-Pick Type C disease is a neurological disorder of adolescents due to autosomal-recessive mutations in either one or both Niemann-Pick-2 (NPC2) and NPC1 genes, which, like ABCA2, are loca
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To our knowledge BAY has
2024-04-28
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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br Concluding remarks ROP is
2024-04-28
Concluding remarks ROP is a major cause of childhood blindness in the world. Current pharmacological therapy focus on anti-VEGF strategy, but this strategy is associated with the unintended effects on delayed eye growth and retinal vasculature development of preterm infants. Preclinical studies u
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SMI-4a An alternative to the agonist or
2024-04-28
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Considering the physicochemical stability results on Fig it
2024-04-28
Considering the physicochemical stability results on Fig. 5, it was observed that the particles are stable when they are stored at 4 °C for 30 days. After day 30, a significant increase was observed in particle size, but at the end of the 90 days the SLN particle size is still below 100 nm. Stabilit
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The role of DHT in early teleost embryogenesis
2024-04-28
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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However there are studies revealing the dark
2024-04-27
However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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br ACL A Metabolic Checkpoint for Sensing Excess Nutrients D
2024-04-27
ACL: A Metabolic Checkpoint for Sensing Excess Nutrients? During normal transitions between fasting and feeding, cells maintain energy homeostasis by integrating energy and nutrient status signals at key metabolic nodes, coordinating multiple processes. For example, the AMP-activated protein kina
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Ro 32-3555 exemplifies three of the compounds investigated
2024-04-27
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC Ro 32-3555 as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products.
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To evaluate the ability of
2024-04-27
To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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Hypoxia induced replication arrest has been
2024-04-27
Hypoxia-induced replication arrest has been demonstrated in a variety of organisms in addition to mammals; including Zebrafish , , and (brine shrimp) which have been shown to survive for 4 years and longer in anoxic conditions . Despite this breadth of study, little is known about the mechanism of h
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Neuropathic animals display increased sensitivity to the
2024-04-27
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB SB269970 HCl synthesis in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regulated
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To elucidate whether membrane fluidity changes could impact
2024-04-27
To elucidate whether membrane fluidity changes could impact on signaling pathways, we examined the effects of Rh2 on the activation of Akt, a lipid raft-associated protein kinase, which promotes cell survival and blocks the apoptotic pathways. Upon pretreatment with 5 mM MβCD and in the absence of R
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It is noticed that MDL only partly reversed
2024-04-27
It is noticed that MDL-28170 only partly reversed isoflurane-induced AIF release and nuclear translocation. In addition to calpain mechanism, activation of the DNA repair enzyme poly (ADP-ribose) polymerase-1 (PARP-1) is also essential for AIF release (Culmsee et al., 2005; Moubarak et al., 2007), a
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In summary these data show that agonist
2024-04-27
In summary, these data show that agonist exposure induces internalization and reduction in cell surface HA-mAPJ expression that occurs relatively rapidly during agonist exposure and recovers more slowly after agonist removal. Moreover the ppERK response of mAPJ-HEK293 cells to [Pyr1]apelin-13 desens
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