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What are the in situ effects of multi
2024-02-04

What are the in-situ effects of multi-site CaM associations with AT1R? Kai et al. showed that synthetic peptides corresponding to residues 125–137 (rat sequence) in SMD2, 217–227 in the N-terminal side of SMD3, and 304–316 in SMD4JM inhibit to various degrees AngII-induced GTPase activity of isolate
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Bay 11-7821 br Prostate cancer and resistance to AR targetin
2024-02-04

Prostate cancer and resistance to AR targeting treatment The AR plays a pivotal role in the development, differentiation, homeostasis and secretory function of the normal prostate (Wilson, 2011). The AR is also a key player in many phases of prostate carcinogenesis (Huggins et al., 1941, Scher an
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For all three fluorescent dyes used
2024-02-04

For all three fluorescent dyes used, the double-labeled UQ-bodies showed higher antigen responses. A plausible mechanism for the higher quenching observed for the double-labeled UQ-bodies is the dye-dye quenching due to H-dimer formation [19] between the two dyes introduced into the Fd and L chains.
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The AMP Activated Protein Kinase AMPK has
2024-02-04

The 5′AMP-Activated Protein Kinase (AMPK) has evolved as an important cellular sensor of reduced energy status that can subsequently phosphorylate its target proteins, slowing the rates of key biosynthetic processes and promoting energy producing pathways; for these reasons AMPK has been proposed as
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The excellent potencies selectivities and improved PK
2024-02-02

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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natriuretic peptide receptor In addition to the above mentio
2024-02-02

In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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DRiPs also contribute to formation of protein aggregates tha
2024-02-02

DRiPs also contribute to formation of protein GM6001 that result from dysregulation of proteostasis, during which the proteolytic machinery is unable to process and degrade defective proteins (Tyedmers et al., 2010). Aggregation of poly-ubiquitinated proteins has been observed in different cell typ
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br Materials and methods br Results br
2024-02-02

Materials and methods Results Discussion Numerous studies showed that Na+-K+-ATPase activity and membrane givinostat were decreased in cardiac tissue subjected to IR (Belliard et al., 2013; Lee et al., 2013). In return, treatment that alleviated the progress of IR-related myocardial injury
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Wound healing without blastema formation causes partial
2024-02-02

Wound healing without blastema formation causes partial restoration of lost tissue, and gives rise to fibrotic scars. Healing by fibrotic scarring rather than by regeneration leads to tissue dysfunction, and can place a huge burden for the health of the animal [4]. Therefore, understanding the molec
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br Results br Discussion br STAR
2024-02-02

Results Discussion STAR★Methods Author Contributions Acknowledgments We thank Angela Walker for assistance with the manuscript; Junlin Liu, Xiangxiang Gu, Na Chen, Lu Xue, and the BV Core Facility of iHuman Institute for their support; scientists and colleagues at Amgen Inc., Zhulun W
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Introduction Heterotrimeric G proteins mediate signal
2024-02-02

Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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Of the cardiovascular studies involving ARBs reported renal
2024-02-01

Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tria
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Cells have developed strategies aiming to enhance both the
2024-02-01

Cells have developed strategies aiming to enhance both the efficiency of proteins with chaperone activity as well as their overall antioxidant capacity to maintain proteostasis under oxidative stress conditions (Miyata et al., 2012). For instance, 2-Cys peroxiredoxin is an abundantly expressed, anti
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An important observation in our study is
2024-02-01

An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-arr
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AdipoR and AdipoR have been reported to be present in
2024-02-01

AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low ML-193 synthesis 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
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