TPX-0131 is a next-generation ALK inhibitor entering IND-enabling studies. has shown preclinical potent inhibition of wildtype and numerous ALK mutations,
Sep 23, 2008 PubMed Abstract: gp130 is a shared receptor for at least nine cytokines and can signal either as a homodimer or as a heterodimer with Leukemia
Author: Tjernlund, Annelie. Date: 2006-12-14. 2021-03-20 · Figure 2. SC144 induces gp130 phosphorylation and deglycosylation.
The focus of my research has been to investigate and understand if and how LIF exerts HIV-1 suppressing activity. 2009-04-30 SC144 is an inhibitor of gp130 with IC50 values of 0.43 μmol/L and 0.88 μmol/L in NCI/ADR-RES and HEY cell lines, respectively [1]. SC144 is a first-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer. It can substantially SC-144 is an orally active small-molecule gp130 inhibitor. Products are for laboratory research use only. Not for human use.
To determine whether the deficiency in N-glycosylation has any effects on the activity of the gp130-associated IL-6/JAK/STAT3 signaling [], we carried out the following investigations.First, we studied IL-6 binding to DU145 cells in the presence and absence of glucosamine. Repositioning Bazedoxifene as a novel IL-6/GP130 inhibitor for sarcoma therapy Lin, Jiayuh Nationwide Children's Hospital, Columbus, OH, United States Search 24 grants from Jiayuh Lin Search grants from Nationwide Children's Hospital.
Comparative evaluation of gp130 signalling cytokines in human endothelial cells: evidence for both specific and overlapping molecular responsesManuskript
The binding of IL-6 to IL-6Rα induces trimer formation via recruitment of gp130 followed by formation of hexamer through homodimerization. Then gp130 cytoplasmic domain is phosphorylated by JAKs (JAK1, JAK2, JAK3 or Tyk2), which leads to the activation of STAT3.
Interestingly, the soluble form of gp130 (sgp130) acts as a natural inhibitor of IL-6 signaling . The complex of (IL-6/sIL-6R)/sgp130 also inhibits IL-6 activity and limits systemic responses to IL-6, suggesting its importance in regulating IL-6 signaling and as a potential therapeutic agent in RA (10, 13).
2011-09-01 · To mechanistically link the control of disease processes with IL-6/STAT3 signaling, an increasing number of studies have used a gp130 knockin mouse model in which an amino acid substitution prevents feedback inhibition of the receptor, resulting in exaggerated STAT3 signaling (79, 98, 99). small-molecule inhibitor of GP130 [24]. Our previous work has repositioned this drug as a potent GP130 in-hibitor in pancreatic cancer therapy [25], but its effects on colon cancer have not been investigated.
Interestingly, the soluble form of gp130 (sgp130) acts as a natural inhibitor of IL-6 signaling . The complex of (IL-6/sIL-6R)/sgp130 also inhibits IL-6 activity and limits systemic responses to IL-6, suggesting its importance in regulating IL-6 signaling and as a potential therapeutic agent in RA (10, 13). Leukemia inhibitor factor (LIF) is a polyfunctional cytokine that belongs to the IL-6 family which mainly signals through the Jak/Stat pathway via the gp130/LIFR-α heterodimer. The focus of my research has been to investigate and understand if and how LIF exerts HIV-1 suppressing activity. We correlate post-treatment induction of this pathway in anti-TNF non-responders and demonstrate in vivo amelioration of the activated myeloid-stromal niche, using a specific gp130 inhibitor
SC144 is an inhibitor of gp130 with IC50 values of 0.43 μmol/L and 0.88 μmol/L in NCI/ADR-RES and HEY cell lines, respectively [1].
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Combined bazedoxifene and oxaliplatin therapy may be a viable therapeutic approach for human colon cancer.
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Currently, there are no small-molecule inhibitors of gp130 under clinical development. In this study, we show that gp130 is an attractive drug target in ovarian cancer due to its role in promoting cancer progression via the activation of its downstream Stat3 signaling.
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For the stimulant drug, see G-130. Glycoprotein 130 (also known as gp130, IL6ST, IL6-beta or CD130) is a transmembrane protein which is the founding member of the class of all cytokine receptors. It forms one subunit of the type I cytokine receptor within the IL-6 receptor family.
Downstream of GP130 is PI3K/AKT/mTOR signaling, which is inactivated by SC144, a GP130 inhibitor. However, Raf/MEK/ERK signaling, which also is downstream of … 2019-02-08 2013-06-01 2019-11-01 2021-03-02 SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling.