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br Special report Financial and personal benefits of early d
2024-12-12
Special report – Financial and personal benefits of early diagnosis Acknowledgments The Alzheimer’s Association acknowledges the contributions of Joseph Gaugler, Ph.D., Bryan James, Ph.D., Tricia Johnson, Ph.D., Allison Marin, Ph.D., and Jennifer Weuve, M.P.H., Sc.D., in the preparation of 201
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Aldose reductase ALR EC the first enzyme
2024-12-12
Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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Further evidence for action mechanism was provided by assays
2024-12-12
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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br Acknowledgements The authors would like to thank
2024-12-12
Acknowledgements The authors would like to thank Dr. Bradford B. Lowell for providing us with β-less and WT breeding pairs. Funding sources: This work was supported by NIH Grant DK028082 (to E.M.F) and by an Institutional Research Training Grant NRSA 5T32DK751627 (to N.D.). Introduction The e
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A clear link between ADR stimulation and decreased respirati
2024-12-12
A clear link between α2-ADR stimulation and decreased respiration in β-cells is established and consistent with proteomics data. Current discoveries in islets have identified physical interactions between ADR-coupled G proteins and cellular components such as insulin vesicles and ion channels (Zhao
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Previous work established interactions between CRF and KOR s
2024-12-12
Previous work established interactions between CRF and KOR systems in regulating attention (39). The CRF antagonist ANT attenuated, but did not completely reverse, the effects of PACAP (.5 µg) and did not have any effects on its own (Table 2). There were no significant differences in performance amo
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-12-12
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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PC is considered as a cancer of the epigenome
2024-12-12
PC is considered as a cancer of the epigenome (Grasso et al., 2012, Robinson et al., 2015). Our results demonstrate that the interaction of AR with ACK1 drives the positive feedback epigenetic circuitry that is ultimately conducive to promote AR transcription. Further, this circuitry subjugates AR t
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An alternative to the agonist or antagonist potential in dru
2024-12-12
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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ACE inhibition is often thought to play a central
2024-12-12
ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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br Conclusion The HT receptor
2024-12-12
Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless Nifuroxazide (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); molecular biol
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The apoptosis promoting Bcl family includes BH only proteins
2024-12-11
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 has been identified as an ASK
2024-12-11
ASK2 has been identified as an ASK1 binding protein (Wang et al., 1998). ASK1 supports the stability and active configuration of ASK2 in the heteromeric complex, while ASK2 has been found to activate ASK1 by direct phosphorylation (Takeda et al., 2007). Unlike ASK1, which is ubiquitously expressed i
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hsp90 inhibitor br Results br Discussion br Conclusions In s
2024-12-11
Results Discussion Conclusions In summary, this study provides novel report of pericardial adipose aromatase expression – in both human and rodent. We show that aromatase expression is remarkably upregulated with aging (Fig. 1C), and that total aromatase hsp90 inhibitor conversion capacity
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Although the exact mechanisms are not fully understood
2024-12-11
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 IC261 expressing bot
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