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PF is orally bioavailable and has appropriate pharmacokineti
2024-12-17

PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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br Materials and methods br Results br Discussion Knowledge
2024-12-17

Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Phosphodiesterase inhibition increases the intracellular lev
2024-12-17

Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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Until now the molecular interactions of Tmod or Lmod
2024-12-17

Until now, the molecular interactions of Tmod or Lmod with caffeic acid had been assessed in pyrene-actin polymerization assays [13], [23], [27], [28], [44], [45] or directly measured using non-denaturing polyacrylamide gel-electrophoresis (for Tmod isoforms only [23]), ITC (for Tmod1 and Lmod2) [43
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Finasteride was the first steroidal reductase
2024-12-17

Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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The apoptosis promoting Bcl family includes BH only proteins
2024-12-16

The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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ASK belongs to the family of MAPKKK ASK mediated apoptosis
2024-12-16

ASK1 belongs to the family of MAPKKK. ASK1-mediated apoptosis is involved in the pathogenesis of several diseases such as I/R injury, infectious diseases and neurodegenerative disorders [33], [34], [35]. ASK1 can be activated through different mechanisms. One mechanism is that oxidative stress direc
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Although the exact mechanisms are not fully understood IGF i
2024-12-16

Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in Cy3.5 NHS ester (non-
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Finally intracrine androgen synthesis metabolism can
2024-12-16

Finally, intracrine androgen synthesis/metabolism can be activated thus allowing (+)-Aphidicolin to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpression of ste
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In conclusion our study has identified a
2024-12-16

In conclusion, our study has identified a splice site colorimetric synthesis (c.1769-1G > C) in the AR gene from two patients with complete androgen insensitivity syndrome. The c.1769-1G > C mutation may provide us new insights into the molecular mechanism involved in splicing defects underlying CA
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As patients with type diabetes are known to
2024-12-16

As patients with type 2 diabetes are known to be hyperinsulinemic per se, this relationship between insulin/IGF1 receptor and AR may point towards a causal role of insulin in AR upregulation. Indeed, this is supported by several previous observations. Beyond the already mentioned AR activation by in
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Our research group has been involved by
2024-12-16

Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz
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br The lipoxygenase pathway in diseases of the nervous syste
2024-12-16

The 12/15-lipoxygenase pathway in diseases of the nervous system Conclusions and future perspectives Arachidonic osmi and other polyunsaturated fatty acids, and their lipid metabolites, play very important roles in human health and disease. This review has outlined the functions of 12- and 15-
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Flavonoids protein interactions studies play a substantial p
2024-12-16

Flavonoids-protein interactions studies play a substantial part in the hunt for novel molecules which are to interact with a selected disease-relevant target [35]. The mode of potential interaction gives information about the flavonoid effectiveness and selectivity. Lately, possible target molecules
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br Introduction Our ability to see our surrounding relies di
2024-12-16

Introduction Our ability to see our surrounding relies directly on the integrity of the anatomical structures composing our eyes. One of these key components is the cornea, consisting of the outer layer of the eye. Its transparency is crucial for light transmission to the retina and allows proper
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