av P Pettersson-Pablo · 2020 · Citerat av 1 — Leukaemia inhibitory factor enhances tissue factor expression in human monocyte-derived macrophages: a gp130-mediated mechanism.

2019-02-08 · Bazedoxifene, a third- generation selective estrogen modulator approved by the Food and Drug Administration (FDA), is a novel inhibitor of IL-11/GP130 signaling discovered by docking modeling.

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. cancer cells, and that the inhibition of GP130 expression significantly reduces cell viability, survival and migration. Downstream of GP130 is PI3K/AKT/mTOR signaling, which is inactivated by SC144, a GP130 inhibitor.

Gp130 inhibitor

by ROCK activity inhibition. Lindkvist, M. , Zegeye, M. M. , Sirsjö, A. , Grenegård, M. & Ljungberg, L. U. Comparative evaluation of gp130 signalling cytokines in Tumor necrosis factor inhibitor therapy and risk of serious postoperative · orthopedic STAT-mediated trefoil gene activation in gp130 mutant mice. Nat Med. Superantigen activates the gp130 receptor on adipocytes resulting in altered (the transcription factor nuclear factor of activated T-cells) inhibitor A-285222. Stavreus-Evers Leukaemia Inhibitory Factor Receptor and gp130 in Evers, Expression of LIF, its receptors LIFR and gp130, and its inhibitor Cytokine Receptor gp130 · Dipeptidyl Peptidase 4 · Endoglin · Epithelial Cell rho Guanine Nucleotide Dissociation Inhibitor beta · Thymidine Phosphorylase. the 130kDa (gp130) subunit that by itself does not bind LIF, but is required for Factor,D Factor,Melanoma-derived LPL Inhibitor,Leukemia Inhibitory Factor.

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. Although IL-6 has been associated with many epithelial cancers, IL-11 acts as a more potent driver of colorectal cancers [22].

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.

av A Krona · 2006 · Citerat av 1 — The function of OSM are unclear with conflicting reports of growth stimulatory or inhibitory effects in various cell types. OSM is known to signal through gp130 av R Karlsson · Citerat av 2 — transducing β-chain [98], and the family of cytokines signaling through the common receptor subunit gp130 comprises of IL-6, IL-11, leukemia inhibitory factor The diversity of IL-6 signaling mediated via gp130 explains its functional prostatic cancer cells, while inhibiting the proliferation of lung and breast cancer cells.

The first-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer (IC50 values 0.43-0.95 µM for a range of human ovarian cancer cell lines). SC144 binds gp130, induces gp130 phosphorylation and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.

Lindkvist, M. , Zegeye, M. M. , Sirsjö, A. , Grenegård, M. & Ljungberg, L. U. Comparative evaluation of gp130 signalling cytokines in Tumor necrosis factor inhibitor therapy and risk of serious postoperative · orthopedic STAT-mediated trefoil gene activation in gp130 mutant mice. Nat Med. Superantigen activates the gp130 receptor on adipocytes resulting in altered (the transcription factor nuclear factor of activated T-cells) inhibitor A-285222. Stavreus-Evers Leukaemia Inhibitory Factor Receptor and gp130 in Evers, Expression of LIF, its receptors LIFR and gp130, and its inhibitor Cytokine Receptor gp130 · Dipeptidyl Peptidase 4 · Endoglin · Epithelial Cell rho Guanine Nucleotide Dissociation Inhibitor beta · Thymidine Phosphorylase. the 130kDa (gp130) subunit that by itself does not bind LIF, but is required for Factor,D Factor,Melanoma-derived LPL Inhibitor,Leukemia Inhibitory Factor. We reveal mechanisms of NOD2-driven Crohn's disease, through enrichment of a pathogenic myeloid and stromal niche, and rescue by gp130 inhibition.

Nat Med. Superantigen activates the gp130 receptor on adipocytes resulting in altered (the transcription factor nuclear factor of activated T-cells) inhibitor A-285222. Stavreus-Evers Leukaemia Inhibitory Factor Receptor and gp130 in Evers, Expression of LIF, its receptors LIFR and gp130, and its inhibitor Cytokine Receptor gp130 · Dipeptidyl Peptidase 4 · Endoglin · Epithelial Cell rho Guanine Nucleotide Dissociation Inhibitor beta · Thymidine Phosphorylase. the 130kDa (gp130) subunit that by itself does not bind LIF, but is required for Factor,D Factor,Melanoma-derived LPL Inhibitor,Leukemia Inhibitory Factor. We reveal mechanisms of NOD2-driven Crohn's disease, through enrichment of a pathogenic myeloid and stromal niche, and rescue by gp130 inhibition.
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· IL-6 belongs to the family of Jan 23, 2014 We report here the discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 protein–protein interactions (PPIs) using multiple The IL-6 receptor blockers tocilizumab and sarilumab inhibit the low affinity IL-6 receptor to inhibit binding of IL-6 without interfering with binding to gp130 at TPX-0131 is a next-generation ALK inhibitor entering IND-enabling studies.
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Soluble gp130 is the natural inhibitor of soluble interleukin-6 receptor transsignaling responses. Signal transduction in response to interleukin-6 (IL-6) requires binding of the cytokine to its receptor (IL-6R) and subsequent homodimerization of the signal transducer gp130.

Chemical Therapeutics Discovery of a Novel Orally Active Small-Molecule gp130 Inhibitor for the Treatment of Ovarian Cancer Shili Xu1, Fedora Grande1,2, Antonio Garofalo2, and Nouri Neamati1 Abstract Interleukin (IL)-6 andStat3 play key roles in ovarian cancer progression. 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.

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2021-03-20

Effects of Dopamine Signaling on Recovery and Inflammation after Ischemic Stroke · Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 infection / Annelie Tjernlund. -. Stockholm, 2006. - 65 s. : ill.

The IL-6 receptor blockers tocilizumab and sarilumab inhibit the low affinity IL-6 receptor to inhibit binding of IL-6 without interfering with binding to gp130 at

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.

SC144 shows potent inhibition of gp130 ligand-triggered signaling. Inhibition of gp130 dependent proliferation of BAF/3 cells.