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It has been reported that
2022-04-15

It has been reported that the pathway upstream of YAP phosphorylation is operative in a tissue or context-specific manner. LPA or S1P bound to their corresponding membrane GPCRs and act through Rho GTPases to activate YAP/TAZ [11]. Consistently, another report showed that activation of PAR1 (a GPCR)
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Sumoylation of transcription factors has
2022-04-15

Sumoylation of transcription factors has been generally linked to transcriptional repression and, in a few cases, to transcriptional activation [60] Accumulating evidence implies that corepressor complex subunits, including CoREST, CtBP, Daxx, NCoR1, SMRT and histone deacetylase complexes (HDACs), p
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The exact mechanism by which N BPs
2022-04-15

The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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EZH interaction with HADC and HDAC through the
2022-04-15

EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic daunoru
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PKC s effect on quantal size may involve
2022-04-15

PKC’s effect on quantal size may involve regulation of endocytotic protein components responsible for mediating kiss-and-run exocytosis. There is a growing body of evidence to suggest that canonical endocytotic proteins—dynamin, amphiphysin, syndapin, and others—may play a role in modulating fusion
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Given the major differences between the molecular regulation
2022-04-15

Given the major differences between the molecular regulation of the genes encoding HO-1 (HMOX1) in mice and humans, it is not appropriate to utilize mouse models for mechanistic analyses of human HMOX1[35]. In addition, it has been reported that drugs, such as statins, as well as stressors and the r
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Interestingly interactions between Smad and
2022-04-14

Interestingly, interactions between Smad3 and RhoA, the other small GTPase which is highly homologous to RhoB [9], could not be observed suggesting that the Smad3/RhoB interactions require amino thymidine phosphorylase inhibitor residues that are unique to RhoB. Combined with our previous observati
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We observed that the Toc G domain
2022-04-14

We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate
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Historically pharmacological investigations have been
2022-04-14

Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery
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br Experimental br Results and discussion br Conclusion In t
2022-04-14

Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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Nemonapride Depressed survival rate body weight and colon
2022-04-14

Depressed survival rate, body weight, and colon length along with elevated clinical score comprise the essential characteristics of IBD (Hung et al., 2014; Shen et al., 2011; Sun et al., 2010). In the present study, we found that SB improved the survival rate, body weight, and colon length and decre
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A number of synthetic GPR agonists have been reported
2022-04-14

A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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In three independent groups identified GPR A HM
2022-04-14

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niacin
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The differential tissue and ligand
2022-04-14

The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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TGR is a class A GPCR transducing
2022-04-14

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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