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PMID: 18068628 Published · ppublish English Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S.

Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles.

Cancer cell ·Vol. 12 ·No. 6 ·2007-12-00 ·Pages 501-13

Fröhling S, Scholl C, Levine RL, Loriaux M, Boggon TJ, Bernard OA, Berger R, Döhner H, Döhner K, Ebert BL, Teckie S, Golub TR, Jiang J, Schittenhelm MM, Lee BH, Griffin JD, Stone RM, Heinrich MC, Deininger MW, Druker BJ, Gilliland DG

Abstract

Mutations in the juxtamembrane and kinase domains of FLT3 are common in AML, but it is not known whether alterations outside these regions contribute to leukemogenesis. We used a high-throughput platform to interrogate the entire FLT3 coding sequence in AML patients without known FLT3 mutations and experimentally tested the consequences of each candidate leukemogenic allele. This approach identified gain-of-function mutations that activated downstream signaling and conferred sensitivity to FLT3 inhibition and alleles that were not associated with kinase activation, including mutations in the catalytic domain. These findings support the concept that acquired mutations in cancer may not contribute to malignant transformation and underscore the importance of functional studies to distinguish "driver" mutations underlying tumorigenesis from biologically neutral "passenger" alterations.

MeSH Terms
Adult Alleles Animals Cell Proliferation/drug effects DNA Mutational Analysis Enzyme Activation/drug effects Humans Leukemia, Monocytic, Acute/enzymology,genetics,pathology Mice Mutant Proteins/metabolism Mutation/genetics Phosphorylation/drug effects Protein Kinase Inhibitors/pharmacology Protein Structure, Secondary Signal Transduction/drug effects Staurosporine/analogs & derivatives,pharmacology fms-Like Tyrosine Kinase 3/chemistry,genetics
Chemicals
Mutant Proteins Protein Kinase Inhibitors fms-Like Tyrosine Kinase 3 Staurosporine midostaurin
Authors & Affiliations
21 authors, click to expand affiliations / ORCID
Fröhling Stefan
Division of Hematology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.
Scholl Claudia
Levine Ross L
Loriaux Marc
Boggon Titus J
Bernard Olivier A
Berger Roland
Döhner Hartmut
Döhner Konstanze
Ebert Benjamin L
Teckie Sewit
Golub Todd R
Jiang Jingrui
Schittenhelm Marcus M
Lee Benjamin H
Griffin James D
Stone Richard M
Heinrich Michael C
Deininger Michael W
Druker Brian J
Gilliland D Gary
Article Info
Journal
Cancer cell
Abbr.
Cancer Cell
ISSN
1535-6108
Published
2007-12-00
Pages
501-13
Language
English
Region
United States
NLM ID
101130617
Subset
IM
Grants
NCI NIH HHS · CA66996 · United States
NCI NIH HHS · CA113434 · United States
NCI NIH HHS · CA105423 · United States
NCI NIH HHS · T32 CA009172 · United States
NHLBI NIH HHS · HL082677 · United States
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