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On the basis of the above information we designed
2023-02-16

On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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On the basis of the above information we designed
2023-02-16

On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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Despite the growing knowledge surrounding the link between A
2023-02-14

Despite the growing knowledge surrounding the link between ATX and cholestatic pruritus in PBC, it remains unclear if the role of the ATX-LPA signaling axis includes lymphocytes homing in the liver of PBC, and if the resulting inflammation is associated with PBC pruritus (Fig. 3). PBC is characteriz
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Protein protein interaction networks are an important ingred
2023-02-13

Protein–protein interaction networks are an important ingredient for the system-level understanding of cellular processes. Such networks can be used for filtering and assessing functional genomics data and for providing an instinctive platform for annotating structural, functional and evolutionary p
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Recent studies have supported the existence of
2023-02-13

Recent studies have supported the existence of an inward RAS regulatory mechanism in which AT1 receptors downregulate angiotensin-converting enzyme 2 (ACE2) and subsequently impair angiotensin-(1-7) generation and MAS functionality (Jessup et al., 2006, Gallagher et al., 2008, Xia et al., 2009, Pern
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br Materials and methods br Results br Discussion Diabetic
2023-02-13

Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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Breast Cancer Although androgens have been considered to be
2023-02-13

Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast
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At the top of the S subsite cylinder are two
2023-02-13

At the top of the S1 subsite cylinder are two “cap” residues: E572 and M1034 [13]. Atomic structures of PfA-M1 have revealed important clues into potential roles for the cap residues in substrate selection. In the PfA-M1:bestatin co-crystal structure ([13]; Fig. 1), the P1 phenyl ring occupies the S
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In order to postulate its binding mode in
2023-02-13

In order to postulate its binding mode in APN, NCT-502 synthesis 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupie
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br Materials and methods br Results br Discussion
2023-02-13

Materials and methods Results Discussion We have in this study used semi-nested degenerative PCR to identify the lipoxygenases expressed in the lung tissue from M. fascicularis and report on the identification of 5- and 12/15-LO transcripts from this tissue. Although we did not find transcr
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Constitutive tyrosine kinase activity of
2023-02-13

Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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The activation of P Rs modulates
2023-02-13

The activation of P1Rs modulates the activity of many ion channels and receptors (Sebastião and Ribeiro, 2009) and the recent detection of P1Rs at the postsynaptic level of the adult NMJ (Garcia et al., 2014) makes potentially possible an adenosine-mediated modulation of the nicotinic silybin austra
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Toxicity is the main reason for the failure at
2023-02-13

Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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In summary we could identify and experimentally confirm
2023-02-13

In summary, we could identify and experimentally confirm two novel SBEs within the 5-LO promoter and we were able to demonstrate that TGFβ and SMADs stimulate 5-LO promoter activity. Moreover, an elevated 5-LO expression has been linked to different forms of leukaemia. Therefore, the influence of ML
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br Patients and Methods br Results br Discussion
2023-02-10

Patients and Methods Results Discussion Gjerdrum et al showed that Axl NE 100 hydrochloride is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also sh
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