- |||||||||| Alverix (amiloride hydrochloride) / Remedica, U0126 / Promega
Journal: Unilateral Nephrectomy Stimulates ERK and Is Associated With Enhanced Na Transport. (Pubmed Central) - Feb 27, 2021 In conclusion, pERK increases in whole kidney and, specifically, CCD cells after nephrectomy, but pERK was not associated with active proliferation at 1-month post-nephrectomy. In vitro studies suggest high tubular flow induces ERK dependent ENaC Na absorption and may play a critical role in Na balance post-nephrectomy.
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[VIRTUAL] REGULATION OF FGF2-INDUCED CELL PROLIFERATION BY INHIBITORY GPCR IN NORMAL PITUITARY CELL () - Feb 24, 2021 - Abstract #ICE2021ICE_462; These results show that the FGF2 and OCT combined treatment induced a decreased of prolactin and somatotroph population associated with G1-phase arrest, modulating key proteins in the early phases (transition from G0/G1 to the S-phase) of cell cycle progression and proteins involved in the cell proliferation. This regulatory effect, mediated for GPCR-Gαi, could participate in the homeostasis of lactotroph and somatotroph in phycological conditions
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Journal: A G-protein coupled receptor 39 agonist stimulates proliferation of keratinocytes via an ERK-dependent pathway. (Pubmed Central) - Feb 12, 2021 This effect was suppressed by co-treatment with wortmannin (PI3K inhibitor) and U0126 (MKK inhibitor)...Taken together, this study reveals novel insights into the role of GPR39 in regulating keratinocyte proliferation via a PI3K-MKK-ERK-dependent mechanism. GPR39 agonists may be used in enhancing keratinocyte proliferation, which may be beneficial for the cutaneous wound treatment.
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Journal: miR‑133b affects cell proliferation, invasion and chemosensitivity in renal cell carcinoma by inhibiting the ERK signaling pathway. (Pubmed Central) - Feb 11, 2021 The overexpression of miR‑133b significantly inhibited cell proliferation, migration and invasion, whilst inducing apoptosis and increasing the drug sensitivity of renal cell carcinoma cells to cisplatin, docetaxel and doxorubicin...However, the overexpression of miR‑133b combined with LM22B‑10 treatment weakened the anticancer effects of miR‑133b mimic transfection (P<0.05). In conclusion, miR‑133b overexpression was observed to inhibit the proliferation, migration and invasion of renal cell carcinoma cells and improve chemotherapeutic sensitivity; it was suggested that the mechanism maybe related to the inhibition of ERK1/2 phosphorylation and thus decreased ERK signaling pathway activity.
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Journal: Lactoferrin promotes osteogenesis of MC3T3-E1 cells induced by mechanical strain in an extracellular signal-regulated kinase 1/2-dependent manner. (Pubmed Central) - Feb 10, 2021 In conclusion, miR‑133b overexpression was observed to inhibit the proliferation, migration and invasion of renal cell carcinoma cells and improve chemotherapeutic sensitivity; it was suggested that the mechanism maybe related to the inhibition of ERK1/2 phosphorylation and thus decreased ERK signaling pathway activity. These findings demonstrate that LF promotes osteogenic activity by activating osteogenesis-related biomarkers, corroborating that the effects of mechanical strain depend on Erk1/2 signaling pathway.
- |||||||||| AG1478 / IDT Australia, U0126 / Promega, Vampex (carbenoxolone gel) / York Pharma
Journal: Betacellulin enhances ovarian cancer cell migration by up-regulating Connexin43 via MEK-ERK signaling. (Pubmed Central) - Feb 7, 2021 Most importantly, betacellulin-induced cell migration was attenuated by knockdown of Connexin43, and co-treatment with gap junction inhibitor carbenoxolone did not alter this effect. Our results suggest a bilateral role of Connexin43 in ovarian cancer migration, and also demonstrate a gap junction-independent mechanism of betacellulin.
- |||||||||| SB202190 / Amgen, U0126 / Promega
Journal: Nicotine inhibits MAPK signaling and spheroid invasion in ovarian cancer cells. (Pubmed Central) - Jan 27, 2021 Furthermore, SKOV3 spheroid invasion was blocked by p38 inhibition with SB202190, but not by MEK inhibition with U0126; whereas TOV112D spheroid invasion was reduced by MEK inhibition, but not by p38 inhibition. These results indicate that nicotine can suppress spheroid invasion and compaction as well as proliferation in SKOV3 and TOV112D OC cells; and p38 and ERK MAPK signaling pathways are important mediators of these responses.
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Clinical, Journal: Oxidative stress contributes to vascular calcification in patients with chronic kidney disease. (Pubmed Central) - Jan 23, 2021 Collectively, we provide a comprehensive set of evidence supporting an important role of OS in promoting VC development in CKD patients (particularly in those with ECKD); this was at least in part through induction of osteoblastic transition in VSMCs which may involve the Erk singling. Our research thus suggests that reductions in OS may prevent VC in CKD patients.
- |||||||||| quercetin (LY294002) / Eli Lilly, U0126 / Promega
Journal: AKT drives sustained motility following MEK inhibition via promoting SNAIL and AXL in MDA-MB-231 LM2. (Pubmed Central) - Jan 14, 2021 These results suggest that SNAIL and AXL are key factors mediating sustained motility of LM2 cells following MEK suppression. Because AKT mediates motile behavior under MEK suppression, our results suggest that AKT and AXL may be targeted to overcome resistance against drugs targeting the Ras/ERK pathway.
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Preclinical, Journal: An on-chip wound healing assay fabricated by xurography for evaluation of dermal fibroblast cell migration and wound closure. (Pubmed Central) - Jan 13, 2021 The pneumatically controlled system generates highly reproducible wound sizes compared to the conventional wound healing assay. As proof-of-principle study wound healing was investigated in the presence of several stimulatory and inhibitory substances and culture including bFGF, MMC, U0126 MEK1/2 inhibitor as well as serum starvation to demonstrate the broad applicability of the proposed miniaturized culture microsystem.
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Journal: P2X7 receptor activation aggravates NADPH oxidase 2-induced oxidative stress after intracerebral hemorrhage. (Pubmed Central) - Jan 13, 2021 Blocking ERK1/2 activation, using the ERK1/2 inhibitor U0126 (2 µg, intraventricular injection), reduced the level of NOX2-mediated oxidative stress induced by P2X7R activation after intracellular hemorrhage...The present study was approved by the Ethics Committee of Huazhong University of Science and Technology, China (approval No. TJ-A20160805) on August 26, 2016.
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Preclinical, Journal: Chronic real-time particulate matter exposure causes rat pulmonary arteriole hyperresponsiveness and remodeling: The role of ETR-ERK1/2 signaling. (Pubmed Central) - Jan 7, 2021 Rats were exposed to PM or filtered air for 2 to 4 months using a whole body exposure system, and intraperitoneally injected with the MEK1/2 inhibitor U0126...In conclusion, chronic real-time particulate matter exposure can activate the ERK1/2 signaling, thereby inducing the upregulation of contractile ETR in pulmonary arteriole, which may be involved in pulmonary arteriole hyperresponsiveness and remodeling in rats. These findings provide new mechanistic evidence of PM exposure-induced respiratory diseases, and a new possible target for treatment.
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Journal: Guanine nucleotide-binding protein subunit beta-4 promotes gastric cancer progression via activating Erk1/2. (Pubmed Central) - Jan 7, 2021 These tumor promoting effects were mediated by GNB4 which activates the Erk1/2 pathway through upregulating Erk1/2 phosphorylation, as U0126, an Erk1/2 phosphorylation inhibitor, could significantly inhibit GNB4-mediated cell proliferation, migration and invasion. In summary, GNB4 contributes to the proliferation and metastasis of GC cells by activating the Erk1/2 signaling pathway, and it may serve as a potential therapeutic target of GC.
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Journal: Fibroblast growth factor-2 and interleukin-4 synergistically induce eotaxin-1 expression in adipose tissue-derived stromal cells. (Pubmed Central) - Dec 18, 2020 Eotaxin-1 expression was inhibited in cells treated with the FGFR tyrosine kinase inhibitor and extracellular signal-regulated kinase (ERK) inhibitor U0126, even in the presence of FGF-2...Upregulation of eotaxin expression in adipose tissues could increase eosinophil migration, thereby inducing IL-4 secretion and activation of alternative macrophages and improving glucose homeostasis. These findings provide insights into the mechanisms through which eotaxin mediates metabolic homeostasis in adipose tissues and eosinophils.
- |||||||||| Desferal (deferoxamine) / Kermanshah University of Medical Sciences, Novartis, U0126 / Promega, SP600125 / BMS
Preclinical, Journal: Tert-Butyl Hydroperoxide Stimulated Apoptosis Independent of Prostaglandin E and IL-6 in the HTR-8/SVneo Human Placental Cell Line. (Pubmed Central) - Dec 18, 2020 TBHP-stimulated IL-6 release was blocked by PD169316 but unaltered by indomethacin. These data suggest that TBHP-stimulated IL-6 release and caspase 3/7 activation were independent of PGE yet were interrupted by treatments with known antioxidant properties, providing new insight into relationships between PGE, IL-6, and apoptosis under conditions of chemically induced cellular oxidation.
- |||||||||| Journal: Endothelin-1 stimulates preadipocyte growth via the PKC, STAT3, AMPK, c-JUN, ERK, sphingosine kinase, and sphingomyelinase pathways. (Pubmed Central) - Dec 18, 2020
However, neither p38 MAPK antagonist nor CerS inhibitor altered the effect of ET-1. The results indicate that ETR, JAK2/STAT3, ERK1/2, JNK/c-JUN, AMPK, PKC, SphK, and SMase2, but not ETR, p38 MAPK, or CerS, are necessary for the ET-1 stimulation of preadipocyte proliferation.
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