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Molecular docking simulations were carried out for ligands
2024-04-29
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic ch
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Captopril The role of DHT in early teleost embryogenesis
2024-04-29
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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br Acknowledgements We would like to thank
2024-04-29
Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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apelin br Concluding remarks and future perspectives While
2024-04-28
Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered apelin with custom input and output parameters. Both in the context of molecular diagnostic
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br Implementation of sacubitril valsartan into clinical
2024-04-28
Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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AMP activated protein kinase AMPK is composed of
2024-04-28
AMP-activated protein kinase (AMPK) is composed of α-, β-, and γ-subunits [17,18]. Phosphorylation of α-subunit at Thr-172 residue is essential for AMPK activation [17,18]. The serine/threonine kinase coordinates metabolic pathways in response to energy supply and demand [17,18]. Studies have shown
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br Introduction It is well known that
2024-04-28
Introduction It is well known that when epithelial cells are deprived of anchorage, they undergo detachment-induced apoptosis, also known as anoikis. Cancer cells, by contrast, are able to suppress anoikis and survive under anchorage -independent conditions in the circulating system, which is tho
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br The lipoxygenase pathway and microvascular complications
2024-04-28
The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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Since HETEs and lipoxins the downstream products
2024-04-28
Since HETEs and lipoxins, the downstream products of 12/15-LOX from AA, may alter cellular proliferation and apoptosis,31, 32 and possibly explain the increase of tumour progression and metastasis. However, we here found that HETEs did not affect the proliferation of melanoma in vitro. This may part
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Unlike in humans hepatic expression of FGF increases in mice
2024-04-28
Unlike in humans, hepatic expression of FGF21 increases in mice consuming KD and is a necessary mediator of the physiologic adaptations to the diet. FGF21 knockout (KO) mice gain, rather than lose weight on the diet [6]. FGF21 also activates BAT in part by increasing SNS drive [3,7]. In addition, th
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In conclusion we have demonstrated that diaryl pyrazolo pyri
2024-04-28
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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To date the molecular responses of
2024-04-28
To date, the molecular responses of AChE have been partially analyzed in its mRNA level or protein activity in aquatic animals. To understand the correlation between transcriptional change and activity of AChE, we conducted both experiments in B. koreanus. Generally, the EPZ005687 patterns of the B
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In this study we make the first simultaneous
2024-04-28
In this study, we make the first simultaneous recordings of Schisandrol B synthesis release in multiple brain regions at a temporal resolution less than 1 s. One of the most striking findings is that acetylcholine release has a remarkably similar temporal profile in the mPFC and dHPC, suggesting a
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Although ACE genetic variance does not influence the level
2024-04-28
Although ACE genetic variance does not influence the level of bradykinin significantly, the bradykinin level tends to be affected by ACE inhibitor therapy used by patients. ACE inhibitor reduces the ACE activity that may lead to the accumulation of serum bradykinin. The level of bradykinin tends to
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br Future view and implications The selection and
2024-04-27
Future view and implications The selection and spread of multi(drug)-resistant microorganisms over the last decades has become a major and global public health concern [35]. Two growing threats originating from the fungal kingdom, i.e. Aspergillus fumigatus and Candida auris[36], [37], re-emphasi
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