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The transcription factor CREB has been extensively studied f
2020-11-10

The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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br Results br Discussion Adaptive drug resistance
2020-11-10

Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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Our previous high throughput screening
2020-11-10

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based 4-DAMP sale assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [
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The effect of transformation of the linker
2020-11-10

The effect of transformation of the linker Y between the carboxylic s6 kinase residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist activit
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br Conclusions Enzyme prodrug therapy mediated by
2020-11-10

Conclusions Enzyme prodrug therapy mediated by implantable biomaterials combines the benefits offered by the site specific drug delivery techniques and the systemic administration of drugs. From the former, SMEPT inherits the localized mode of drug delivery with lower systemic distribution of the
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br Conclusions Nanoparticles can be used to modulate
2020-11-10

Conclusions Nanoparticles can be used to modulate the catalytic activity of various industrially and clinically useful enzymes, as well as pH, temperature and storage stabilities, which will enable the process to occur more efficiently and less costly. The interaction between an enzyme and nanopa
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Endothelin appears to have direct effects on neoplastic
2020-11-10

Endothelin 1 appears to have direct effects on neoplastic Z-WEHD-FMK australia by inducing cellular proliferation, angiogenesis, migration, invasion, and inhibition of apoptosis [10]. Endothelin 1 mediates mitogenic effects in some epithelial tumors such as colorectal, ovarian, and prostate cancers
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The isomeric phenyloxazole not only exhibited
2020-11-10

The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand Bosutinib (as seen in compound pairs – and –) decreased ACE i
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PTEN is an evolutionarily conserved
2020-11-10

PTEN is an evolutionarily conserved protein and has been considered to be genetically unique without other isoforms. In this study, we identified an alternate translation initiation at a CUG site in the 5′ untranslated region (5′ UTR) of PTEN mRNA. This CUG start phenylephrine hydrochloride generat
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tak 242 br Ubiquitin ligases Ubiquitin ligases are categoriz
2020-11-10

Ubiquitin ligases Ubiquitin ligases are categorized into different tak 242 based on their specific structural configuration and the composition of subunits—HECT (homologous to E6-AP1 (E6-associated protein 1) carboxy-terminus)-type, RING (really interesting new gene)-finger-type, U-box-type, or
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PR619 The fibrillogenesis process of collagen is understood
2020-11-10

The fibrillogenesis process of collagen is understood to initiate in the extracellular space near the plasma membrane where secretory vesicles form regions of deep invagination. However, it is not clear how and when collagen-binding proteins interact with collagen molecules during fibrillogenesis or
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Studies carried out with LTRAs before the
2020-11-10

Studies carried out with LTRAs before the identification of the CysLT2R, showed a controversial picture, as results that suggest a role for cysteinyl-LTs in the expansion of ischemic damage and in cardiac dysfunction during reperfusion [5], [68], [69] were evenly balanced by others suggesting that t
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Among the CYP enzymes CYP D
2020-11-09

Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama
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On the basis of the published articles it
2020-11-09

On the basis of the published articles, it is known that chemokines are produced by leukocytes and tissue cells, constitutively or after induction. Chemokines are responsible for the recruitment of leukocytes to maintain proper functioning of the immune system [14]. They exist in the central nervous
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VE-822 Previous studies reported that NE and MHPG are deeply
2020-11-09

Previous studies reported that NE and MHPG are deeply involved in depression and that NE reuptake inhibitors are approved for use in patients with depression (for review, see [2]). We found increased hippocampal content of NE and MHPG in the CORT-treated CRTH2−/− mice (Fig. 3). In the hippocampus, a
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