Targeting FLT3 kinase in acute myelogenous leukemia: Progress, perils, and prospects

被引:12
作者
Heinrich, MC
机构
[1] Oregon Hlth & Sci Univ, Div Hematol & Med Oncol, Portland, OR 97201 USA
[2] Portland VA Med Ctr, Portland, OR 97201 USA
关键词
FLT3; tyrosine kinase; kinase inhibitor; AML; KIT; PDGFR;
D O I
10.2174/1389557043487394
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Activating mutations of the FLT3 receptor tyrosine kinase are the most common recurring genetic abnormality in acute myelogenous leukemia (AM). Inhibition of FLT3 kinase activity by small molecule inhibitors has been proposed as a novel therapeutic approach AML. The pre-clinical and clinical development of candidate FLT3 inhibitors will be reviewed.
引用
收藏
页码:255 / 271
页数:17
相关论文
共 152 条
[51]   LIGAND FOR FLT3 FLK2 RECEPTOR TYROSINE KINASE REGULATES GROWTH OF HEMATOPOIETIC STEM-CELLS AND IS ENCODED BY VARIANT RNAS [J].
HANNUM, C ;
CULPEPPER, J ;
CAMPBELL, D ;
MCCLANAHAN, T ;
ZURAWSKI, S ;
BAZAN, JF ;
KASTELEIN, R ;
HUDAK, S ;
WAGNER, J ;
MATTSON, J ;
LUH, J ;
DUDA, G ;
MARTINA, N ;
PETERSON, D ;
MENON, S ;
SHANAFELT, A ;
MUENCH, M ;
KELNER, G ;
NAMIKAWA, R ;
RENNICK, D ;
RONCAROLO, MG ;
ZLOTNIK, A ;
ROSNET, O ;
DUBREUIL, P ;
BIRNBAUM, D ;
LEE, F .
NATURE, 1994, 368 (6472) :643-648
[52]  
Haylock DN, 1997, BLOOD, V90, P2260
[53]   Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor [J].
Heinrich, MC ;
Griffith, DJ ;
Druker, BJ ;
Wait, CL ;
Ott, KA ;
Zigler, AJ .
BLOOD, 2000, 96 (03) :925-932
[54]  
Heinrich MC, 2002, BLOOD, V100, p336A
[55]   PDGFRA activating mutations in gastrointestinal stromal tumors [J].
Heinrich, MC ;
Corless, CL ;
Duensing, A ;
McGreevey, L ;
Chen, CJ ;
Joseph, N ;
Singer, S ;
Griffith, DJ ;
Haley, A ;
Town, A ;
Demetri, GD ;
Fletcher, CDM ;
Fletcher, JA .
SCIENCE, 2003, 299 (5607) :708-710
[56]  
Heinrich Michael C., 1994, P22
[57]   Expression of a conditional AML1-ETO oncogene bypasses embryonic lethality and establishes a murine model of human t(8;21) acute myeloid leukemia [J].
Higuchi, M ;
O'Brien, D ;
Kumaravelu, P ;
Lenny, N ;
Yeoh, EJ ;
Downing, JR .
CANCER CELL, 2002, 1 (01) :63-74
[58]   THE FLT3 LIGAND SUPPORTS PROLIFERATION OF LYMPHOHEMATOPOIETIC PROGENITORS AND EARLY B-LYMPHOID PROGENITORS [J].
HIRAYAMA, F ;
LYMAN, SD ;
CLARK, SC ;
OGAWA, M .
BLOOD, 1995, 85 (07) :1762-1768
[59]   Tandem duplications of the FLT3 receptor gene are associated with leukemic transformation of myelodysplasia [J].
Horiike, S ;
Yokota, S ;
Nakao, M ;
Iwai, T ;
Sasai, Y ;
Kaneko, H ;
Taniwaki, M ;
Kashima, K ;
Fujii, H ;
Abe, T ;
Misawa, S .
LEUKEMIA, 1997, 11 (09) :1442-1446
[60]   Protein tyrosine kinase structure and function [J].
Hubbard, SR ;
Till, JH .
ANNUAL REVIEW OF BIOCHEMISTRY, 2000, 69 :373-398