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In this study we have
2023-07-12

In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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The first identified auxiliary subunit stargazin
2023-07-12

The first identified auxiliary subunit, stargazin, is essential for AMPAR function in cerebellar granule neurons (Hashimoto et al., 1999). Subsequently, a family of six transmembrane AMPAR regulatory proteins (TARPs) were defined that modify channel trafficking, gating, and pharmacology (Kato and Br
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Cell surface metalloproteases coordinate signaling
2023-07-12

Cell surface metalloproteases coordinate signaling during development, tissue homeostasis, and disease. A disintegrin and metalloprotease 17 (ADAM17) is a well-characterized member among ADAM family, which mediates the cleavage of various cell surface proteins (Black, 2002, Black et al., 1997, Dello
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In this study we designed and synthesized two
2023-07-12

In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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Blocking the action of CREB
2023-07-12

Blocking the action of CREB with the C646 inhibitor together with increasing Akt activation with the SC79 agonist is particularly interesting as it significantly reduced wound closure time from 7 days (which is required for complete closure of control hTECs exposed to DMSO) to only 4 days (when hTEC
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br Materials and methods br Results
2023-07-12

Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic Poziotin
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To examine whether the interaction between
2023-07-12

To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes
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br Thymic expression of AChR
2023-07-06

Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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Because LTs are proved to mediate
2023-07-06

Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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The mechanism by which Gas prevents inflammation has been re
2023-07-06

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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Two major categories of arginase inhibitors
2023-07-05

Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt
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Recent studies revealed that certain plant derived compounds
2023-07-05

Recent studies revealed that certain plant-derived compounds can also interfere with AR function. One way of such an interference is by modulating its expression levels. This is the case for the two flavonoids quercetin and luteolin that have been reported to repress the function of AR by inhibiting
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In mice the Tfm mutation increased
2023-07-05

In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th
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Based on structure activity relationship of several SARM tem
2023-07-05

Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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br Results and discussion In order to investigate
2023-07-05

Results and discussion In order to investigate the assembly dynamics and aggregate structures of Aβ16-22, twelve molecular systems with the number of peptides varying from 1 to 12 were studied. In all simulations, the same peptide concentration (~15 mM) was maintained by adjusting the dimensions
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