3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and Related 2-Urea Derivatives Are Potent and Selective Inhibitors of the FGF Receptor-1 Tyrosine Kinase

2000 ◽  
Vol 43 (22) ◽  
pp. 4200-4211 ◽  
Author(s):  
Andrew M. Thompson ◽  
Cleo J. C. Connolly ◽  
James M. Hamby ◽  
Stacey Boushelle ◽  
Brian G. Hartl ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Selective Inhibitors ◽  
Urea Derivatives ◽  
Fgf Receptor

4-Thiophenoxy-N-(3,4,5-Trialkoxyphenyl)Pyrimidine-2-Amines as Potent and Selective Inhibitors of the T-Cell Tyrosine Kinase p56lck

2004 ◽  
Vol 11 (6) ◽  
pp. 747-753 ◽  
Author(s):  
D. F.C. Moffat ◽  
R. A. Allen ◽  
S. E. Rapecki ◽  
P. D. Davis ◽  
J. O'Connell ◽  
...  
Keyword(s):  
T Cell ◽  
Tyrosine Kinase ◽  
Selective Inhibitors

scholarly journals Structure of the FGF Receptor Tyrosine Kinase Domain Reveals a Novel Autoinhibitory Mechanism

Cell ◽  
1996 ◽  
Vol 86 (4) ◽  
pp. 577-587 ◽  
Author(s):  
Moosa Mohammadi ◽  
Joseph Schlessinger ◽  
Stevan R Hubbard
Keyword(s):  
Tyrosine Kinase ◽  
Receptor Tyrosine Kinase ◽  
Kinase Domain ◽  
Tyrosine Kinase Domain ◽  
Fgf Receptor

Expression of the CD117 Antigen on Multiple Myeloma and Its Significance.

Blood ◽  
2004 ◽  
Vol 104 (11) ◽  
pp. 4867-4867
Author(s):  
Juan Li ◽  
Shaokai Luo ◽  
Guocai Zhang ◽  
Wende Hong ◽  
Xiuzhen Tong
Keyword(s):  
Multiple Myeloma ◽  
Tyrosine Kinase ◽  
Selective Inhibitors ◽  
Differentiation Antigen ◽  
Color Flow ◽  
Myeloma Cells ◽  
Significant Difference ◽  
Theoretical Evidence ◽  
Highly Correlated

Abstract BACKGROUND & OBJECTIVE: Leukocyte differentiation antigen CD117 is one of the targets that tyrosine kinase selective inhibitors work on. CD117, whether the cell surface is expressed and the quality of its expression, is highly correlated with the tyrosine kinase selective inhibitors. And whether Multiple myeloma (MM) cells express CD117 and its expression quality is not reported domestic yet but only several reported overseas. In this study, CD117 expressed in MM cells is evaluated, which provide an theoretical evidence for tyrosine kinase selective inhibitors used in the MM, meanwhile, the value of the CD117 expressed in MM cells is estimated. METHODS:CD117,CD56,CD54 were measured by three -color flow cytometry with CD45/SSC gating strategy. RESULTS:Of 48 patients with MM, 17(35.5%) CD117 expression was positive in myeloma cells, and CD56, CD54 expression was positive in 39(81.2%), 48(100.0%), respectively. CD117 expression in myeloma cells was low compared with CD56, CD54 in 48 patients with MM; CD117 positive expression showed a positive correlation with myeloma cells in the bone marrow; CD117 positive in IgG type of MM was 64%, higher than other types such as light chain or IgA.CD117 positive showed no significant difference in different stage, untreated, relapsed and refractory patients (P>0.05, P>0.01); In untreated MM patient, chemotherapy of VAD in CD117 positive patient, the effectiveness was 71.4%, compared with the reaction rate 66.7% in CD117 negative, showed no significant difference (P>0.05). CONCLUSIONS:CD117 </SU

Analysis of tyrosine kinase mRNAs including four FGF receptor mRNAs expressed in MCF-7 breast-cancer cells

1992 ◽  
Vol 50 (4) ◽  
pp. 598-603 ◽  
Author(s):  
Laura Lehtola ◽  
Juha Partanen ◽  
Lea Sistonen ◽  
Jaana Korhonen ◽  
Anni Wärri ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Tyrosine Kinase ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Fgf Receptor ◽  
Receptor Mrnas ◽  
Mcf 7

scholarly journals Lacrimo-Auriculo-Dento-Digital Syndrome Is Caused by Reduced Activity of the Fibroblast Growth Factor 10 (FGF10)-FGF Receptor 2 Signaling Pathway

2007 ◽  
Vol 27 (19) ◽  
pp. 6903-6912 ◽  
Author(s):  
Imad Shams ◽  
Edyta Rohmann ◽  
Veraragavan P. Eswarakumar ◽  
Erin D. Lew ◽  
Satoru Yuzawa ◽  
...  
Keyword(s):  
Growth Factor ◽  
Tyrosine Kinase ◽  
Fibroblast Growth Factor ◽  
Signaling Pathway ◽  
Biological Activities ◽  
Fibroblast Growth ◽  
Loss Of Function ◽  
Fgf Receptor ◽  
Fibroblast Growth Factor 10 ◽  
Ladd Syndrome

ABSTRACT Lacrimo-auriculo-dento-digital (LADD) syndrome is characterized by abnormalities in lacrimal and salivary glands, in teeth, and in the distal limbs. Genetic studies have implicated heterozygous mutations in fibroblast growth factor 10 (FGF10) and in FGF receptor 2 (FGFR2) in LADD syndrome. However, it is not clear whether LADD syndrome mutations (LADD mutations) are gain- or loss-of-function mutations. In order to reveal the molecular mechanism underlying LADD syndrome, we have compared the biological properties of FGF10 LADD and FGFR2 LADD mutants to the activities of their normal counterparts. These experiments show that the biological activities of three different FGF10 LADD mutants are severely impaired by different mechanisms. Moreover, haploinsufficiency caused by defective FGF10 mutants leads to LADD syndrome. We also demonstrate that the tyrosine kinase activities of FGFR2 LADD mutants expressed in transfected cells are strongly compromised. Since tyrosine kinase activity is stimulated by ligand-induced receptor dimerization, FGFR2 LADD mutants may also exert a dominant inhibitory effect on signaling via wild-type FGFR2 expressed in the same cell. These experiments underscore the importance of signal strength in mediating biological responses and that relatively small changes in receptor signaling may influence the outcome of developmental processes in cells or organs that do not possess redundant signaling pathway.

Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases

MedChemComm ◽  
2012 ◽  
Vol 3 (7) ◽  
pp. 829 ◽  
Author(s):  
Thomas Beckers ◽  
Siavosh Mahboobi ◽  
Andreas Sellmer ◽  
Matthias Winkler ◽  
Emerich Eichhorn ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Histone Deacetylases ◽  
Kinase Inhibitors ◽  
Selective Inhibitors

The design and synthesis of selective inhibitors for the insulin tyrosine kinase receptor

1998 ◽  
Vol 50 (S9) ◽  
pp. 112-112
Author(s):  
P. W. Groundwater ◽  
S. P. Mackay ◽  
J. Mckiernan ◽  
P. S. Wilkie
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Receptor ◽  
Selective Inhibitors ◽  
Design And Synthesis
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