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Toxicity is the main reason for the failure at
2024-02-18
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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Osteoblasts have been thought to be the
2024-02-18
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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BS-181 The role of DHT in early teleost embryogenesis is not
2024-02-18
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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For the TSH receptor signaling at the Golgi
2024-02-18
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as s3i depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued signaling b
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Molecular docking quantitative structure activity relationsh
2024-02-18
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Thus a majority of known chemical and physico
2024-02-18
Thus, a majority of known chemical and physico-chemical methods of metallic ions assay has a number of disadvantages, such as a low sensitivity and selectivity, high costs and complexity of the equipment. Therefore, the development of simple cost-effective sensitive methods of quantitative analysis
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NOS is classified into three
2024-02-18
NOS is classified into three isoforms: endothelial (eNOS), neuronal (nNOS), and inducible (iNOS), iNOS is expressed in macrophages (Eisenstein, Huang, Meissler Jr, & al-Ramadi, 1994) and osteoblast-like cells (Riancho et al., 1995) and is involved in the regulation of inflammatory reactions (Eisenst
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br Methods and materials br Results br Discussion
2024-02-18
Methods and materials Results Discussion GPCR regulation in response to agonist stimulation is common to nearly all GPCRs and is essential in physiological systems to limit persistent signalling. In this study we have investigated the [Pyr1]apelin-13-induced trafficking and desensitization
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Most human diseases e g cancer diabetes and
2024-02-18
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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br Experimental section br Acknowledgment S B
2024-02-18
Experimental section Acknowledgment S.B.T. is grateful to the Deutsche Forschungsgemeinschaft (DFG), the Wilhelm Sander-Stiftung and Interdisciplinary Center for Molecular Materials (ICMM) for generous research support. M.M. greatly acknowledges the experimental support and the scientific cont
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As regards feeding the ability to
2024-02-14
As regards feeding, the ability to dissipate surplus energy in the form of heat is beneficial for animals if the protein concentration in the food is low, since it allows them then to meet the adequate protein intake requirement without getting fat. Some of the major dietary activators of the AHR ar
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Heart failure is a chronic syndrome
2024-02-14
Heart failure is a chronic syndrome in which the heart is unable of pumping an adequate supply of blood to meet the metabolic requirements of the body or generating the required elevated ventricular filling pressures to maintain output [34]. Despite considerable advances in the treatment of heart fa
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AdipoR and AdipoR have been reported to be present in
2024-02-14
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low rsv levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN expression
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While the direct effects of ARI lead to a
2024-02-14
While the direct effects of 5-ARI lead to a dramatic Thonzonium Bromide in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laborat
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The mechanism by which Gas
2024-02-14
The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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