PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 17169805-2 2006 This provided the rationale for a multicenter clinical trial in patients with refractory AML with SU5416, a small molecule kinase inhibitor which blocks phosphorylation of c-kit, FLT3, VEGFR-1, VEGFR-2 (KDR) and VEGFR-3. Semaxinib 98-104 fms related receptor tyrosine kinase 3 Homo sapiens 179-183 19411632-4 2009 Treatment of ITD-Flt3(+) human MV4-11 leukemia cells with the ITD-Flt3 inhibitor SU5416 reduced Survivin expression and inhibited cell proliferation. Semaxinib 81-87 fms related receptor tyrosine kinase 3 Homo sapiens 17-21 19411632-4 2009 Treatment of ITD-Flt3(+) human MV4-11 leukemia cells with the ITD-Flt3 inhibitor SU5416 reduced Survivin expression and inhibited cell proliferation. Semaxinib 81-87 fms related receptor tyrosine kinase 3 Homo sapiens 66-70 19411632-5 2009 ITD-Flt3 dramatically increased the number of primary mouse marrow c-kit(+), Sca-1(+), Lin(Neg) cells and colony-forming unit granulocyte-macrophages (CFU-GMs) able to proliferate in the absence of growth factors, whereas Survivin deletion significantly reduced growth factor-independent proliferation and increased apoptosis, which was further accentuated by SU5416. Semaxinib 360-366 fms related receptor tyrosine kinase 3 Homo sapiens 4-8 12843001-3 2003 This concept represented the rationale for the initiation of a multicenter phase 2 trial of SU5416, a small molecule inhibitor of phosphorylation of VEGF receptors 1 and 2, c-kit, the SCF receptor, and fms-like tyrosine kinase-3 (FLT3) in patients with advanced AML. Semaxinib 92-98 fms related receptor tyrosine kinase 3 Homo sapiens 202-228 17032739-3 2006 SU5416 is a potent inhibitor of vascular endothelial cell growth factor receptor, c-Kit, and FLT-3 receptor tyrosine kinases presently used in clinical trials. Semaxinib 0-6 fms related receptor tyrosine kinase 3 Homo sapiens 93-98 15158089-0 2004 Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia. Semaxinib 11-17 fms related receptor tyrosine kinase 3 Homo sapiens 75-79 15158089-2 2004 SU5416 is a small molecule inhibitor of VEGF receptors, c-kit and FLT3 and therefore provides a novel opportunity to target both angiogenesis and proliferation in AML. Semaxinib 0-6 fms related receptor tyrosine kinase 3 Homo sapiens 66-70 15158089-4 2004 Since AML provides a unique platform to evaluate mechanism of action of small molecule inhibitors, investigation of the effect of SU5416 on FLT3 expression and phosphorylation in blood and bone marrow was an additional focus of this trial. Semaxinib 130-136 fms related receptor tyrosine kinase 3 Homo sapiens 140-144 15158089-5 2004 Phosphorylated FLT3 was detected by immunoprecipitation/Western analysis in peripheral blood samples from 17 of 22 patients, and seven exhibited strong inhibition of phosphorylation immediately following a 1h SU5416 infusion, demonstrating that SU5416 can modulate RTK phosphorylation in humans. Semaxinib 209-215 fms related receptor tyrosine kinase 3 Homo sapiens 15-19 15158089-5 2004 Phosphorylated FLT3 was detected by immunoprecipitation/Western analysis in peripheral blood samples from 17 of 22 patients, and seven exhibited strong inhibition of phosphorylation immediately following a 1h SU5416 infusion, demonstrating that SU5416 can modulate RTK phosphorylation in humans. Semaxinib 245-251 fms related receptor tyrosine kinase 3 Homo sapiens 15-19 15158089-6 2004 Although no clear correlation with clinical response was observed, analysis of patient plasma drug levels suggested that a threshold SU5416 concentration of 15 microM was associated with FLT3 inhibition. Semaxinib 133-139 fms related receptor tyrosine kinase 3 Homo sapiens 187-191 12843001-3 2003 This concept represented the rationale for the initiation of a multicenter phase 2 trial of SU5416, a small molecule inhibitor of phosphorylation of VEGF receptors 1 and 2, c-kit, the SCF receptor, and fms-like tyrosine kinase-3 (FLT3) in patients with advanced AML. Semaxinib 92-98 fms related receptor tyrosine kinase 3 Homo sapiens 230-234 12649163-4 2003 SU5416 is a small molecule RTK inhibitor (RTKI) of VEGFR-2, c-kit, and both wild-type and mutant FLT3. Semaxinib 0-6 fms related receptor tyrosine kinase 3 Homo sapiens 97-101 12673719-3 2003 SU5416 is a small-molecule RTK inhibitor (RTKI) that targets VEGFR-2, c-kit, and fms-related tyrosine kinase Flk2. Semaxinib 0-6 fms related receptor tyrosine kinase 3 Homo sapiens 109-113 12351406-0 2002 SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase. Semaxinib 0-6 fms related receptor tyrosine kinase 3 Homo sapiens 66-70 12351406-6 2002 Both SU5416 and SU5614 were capable of inhibiting autophosphorylation of ITD and WT FLT3 (SU5416 concentration that inhibits 50% [IC(50)], 100 nM; and SU5614 IC(50) 10 nM). Semaxinib 5-11 fms related receptor tyrosine kinase 3 Homo sapiens 84-88 12351406-6 2002 Both SU5416 and SU5614 were capable of inhibiting autophosphorylation of ITD and WT FLT3 (SU5416 concentration that inhibits 50% [IC(50)], 100 nM; and SU5614 IC(50) 10 nM). Semaxinib 90-96 fms related receptor tyrosine kinase 3 Homo sapiens 84-88 12351406-8 2002 FLT3 inhibition by SU5416 and SU5614 resulted in reduced proliferation (IC(50), 250 nM and 100 nM, respectively) and induction of apoptosis of FLT3 ITD-positive leukemic cell lines. Semaxinib 19-25 fms related receptor tyrosine kinase 3 Homo sapiens 0-4 12351406-8 2002 FLT3 inhibition by SU5416 and SU5614 resulted in reduced proliferation (IC(50), 250 nM and 100 nM, respectively) and induction of apoptosis of FLT3 ITD-positive leukemic cell lines. Semaxinib 19-25 fms related receptor tyrosine kinase 3 Homo sapiens 143-147 12351406-10 2002 We conclude that SU5416 and SU5614 are potent inhibitors of FLT3. Semaxinib 17-23 fms related receptor tyrosine kinase 3 Homo sapiens 60-64