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CD 2665 Our study demonstrated that the sequential events
2021-08-20
Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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br Allosteric inhibitors In general candidate drugs
2021-08-20
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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br Menopausal hormone therapy from the beginning
2021-08-20
Menopausal hormone therapy, from the beginning to WHI Estrogen products have been used since the 1940s, with increasing prescription through the 1960s. First concerns appeared in the 1970s when oral treatment was linked to uterine cancer. Oral estrogens have traditionally been coupled with proges
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br Conflict of interest br Acknowledgments
2021-08-20
Conflict of interest Acknowledgments This work was supported in part by grants from the , Spain (INCITE08PXIB203092PR). VGM was supported by a FPU pre-doctoral scholarship from the , Spain. MLR was supported in part by a crowdfunding campaign (PRECIPITA), coordinated by the Spanish Foundation
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The interaction of EPAC with Rim has
2021-08-20
The interaction of EPAC2 with Rim1 has an important role in regulating neurotransmitter release. In addition, a recent EPAC2 knockout mice model study provides evidence that EPAC2 promotes transmitter release by maintaining the readily releasable pool (RRP) at mossy fiber (MF) synapses in the hippo
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As a co factor CIITA lacks the ability to
2021-08-19
As a co-factor, CIITA lacks the ability to recognize and directly bind to specific DNA elements to regulate transcription; instead, it relies on interaction with sequence-specific transcription factors (TFs) to be recruited to the chromatin. Therefore, the observation that CIITA binds to a specific
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It has previously been established that DDRs
2021-08-19
It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) rosavin s
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the later elementary years br Acknowledgements br Introducti
2021-08-19
Acknowledgements Introduction Supramolecular collagen assemblies are crucial for the mechanical stability of animal bodies (Myllyharju and Kivirikko, 2004). The basic collagen structure is a triple helix of three chains containing multiple Gly-X-X' repeats; X and X' are often proline and 4-hyd
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We examined the function of immobilised THPs by seeding cell
2021-08-19
We examined the function of immobilised THPs by seeding cells transfected with DDR2-Flag on derivatised crosslinked collagen films, then detecting the phosphorylation of tyrosine 740 (Y740) on the intracellular domain of DDR2 [50]. This regulatory residue is a target for the intracellular tyrosine k
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Introduction Quassinoids are natural products formed through
2021-08-19
Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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We did not observe inhibition
2021-08-18
We did not observe inhibition of vCPH by any of the TCA cycle intermediates (apart from the metal chelators citrate and isocitrate), nor by the factor inhibiting HIF (FIH; a 2OG-dependent asparaginyl hydroxylase) inhibitor N-oxalyl d-phenylalanine (NOF) or the γ-butyrobetaine dioxygenase inhibitor m
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Fluorescein RNA Furthermore in silico physicochemical charac
2021-08-18
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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Another important consideration with respect to drug conditi
2021-08-18
Another important consideration with respect to drug conditioning suggested by the present findings is the observation of an attenuated ras gtpase on the second extinction trial. Seemingly, if ERK measurements were made following a partial reduction in the conditioned response the ERK response woul
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As for the molecular mechanism Ferguson BD
2021-08-18
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of PF-573228 with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression level
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Another milestone in the field is the de
2021-08-18
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of nos inhibitor , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and
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