Journal: Blood

Article Title: An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia

doi: 10.1182/blood-2014-08-595934

Figure Lengend Snippet: Entospletinib shows greater selectivity for Syk than for R406. The blue circle represents Syk. Kinase activity for entospletinib is illustrated on the left, and kinase activity for R406 is illustrated on the right. Entospletinib is Syk-selective (Syk Kd = 7.6 nM, with only 1 other kinase with a Kd < 100 nM). R406 is nonselective (Syk Kd = 15 nM, with 25 kinases with Kd < 15 nM and 54 additional kinases with Kd < 100 nM).

Article Snippet: 12 Dissociation constant ( K d ) determinations of the strongest hits from the broad panel KINOME scan (DiscoveRx Corporation, San Diego, CA) showed that aside from Syk itself, only 1 kinase, TNK1, had a K d < 100 nM for entospletinib, whereas 79 kinases had K d < 100 nM for R406 ( ).

Techniques: Activity Assay

Journal: Molecular Medicine Reports

Article Title: In vitro and in vivo study of the expression of the Syk/Ras/c-Fos pathway in chronic glomerulonephritis

doi: 10.3892/mmr.2018.9355

Figure Lengend Snippet: mRNA levels of (A) Syk, (B) Ras, (C) MEK1/2, (D) ERK1/2 and (E) c-Fos in HBZY-1 cells were determined by reverse transcription-quantitative polymerase chain reaction. Syk, Ras, MEK1/2, ERK1/2 and c-Fos mRNA levels significantly increased in the LPS model group. The inhibitor R406 inhibited the LPS-induced activation of the Syk/Ras/c-Fos signaling pathway. Data are presented as the mean ± standard deviation of at least three independent experiments. **P<0.01 vs. normal group; ## P<0.01 vs. LPS group. Syk, spleen associated tyrosine kinase; MEK, mitogen activated protein kinase kinase; ERK, extracellular signal regulated kinase; p-, phosphorylated; LPS, lipopolysaccharide.

Article Snippet: The Syk/Ras/c-Fos pathway inhibitor R406 (inhibitor of Syk) was purchased from AbMole BioScience, (Shanghai, China).

Techniques: Reverse Transcription, Real-time Polymerase Chain Reaction, Activation Assay, Standard Deviation

Journal: Molecular Medicine Reports

Article Title: In vitro and in vivo study of the expression of the Syk/Ras/c-Fos pathway in chronic glomerulonephritis

doi: 10.3892/mmr.2018.9355

Figure Lengend Snippet: Protein levels of (A) p-Syk, (B) Ras, (C) p-MEK1/2, (D) p-ERK1/2 and (E) c-Fos in HBZY-1 cells were determined by western blotting. p-Syk, Ras, p-MEK1/2, p-ERK1/2 and c-Fos protein levels significantly increased in the LPS model group. The inhibitor R406 inhibited the LPS-induced activation of the Syk/Ras/c-Fos signaling pathway. Data are presented as the mean ± standard deviation of at least three independent experiments. **P<0.01 vs. normal group; ## P<0.01 vs. LPS group. Syk, spleen associated tyrosine kinase; MEK, mitogen activated protein kinase kinase; ERK, extracellular signal regulated kinase; p-, phosphorylated; LPS, lipopolysaccharide.

Article Snippet: The Syk/Ras/c-Fos pathway inhibitor R406 (inhibitor of Syk) was purchased from AbMole BioScience, (Shanghai, China).

Techniques: Western Blot, Activation Assay, Standard Deviation