Literature DB >> 22875611

The N676D and G697R mutations in the kinase domain of FLT3 confer resistance to the inhibitor AC220.

Daphnie Pauwels, Bram Sweron, Jan Cools.   

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Year:  2012        PMID： 22875611      PMCID： PMC3487456          DOI： 10.3324/haematol.2012.069781

Source DB:  PubMed          Journal:  Haematologica        ISSN： 0390-6078            Impact factor:   9.941


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  12 in total

1.  Ponatinib may overcome resistance of FLT3-ITD harbouring additional point mutations, notably the previously refractory F691I mutation.

Authors:  Elisabeth Zirm; Bärbel Spies-Weisshart; Florian Heidel; Ulf Schnetzke; Frank-Dietmar Böhmer; Andreas Hochhaus; Thomas Fischer; Sebastian Scholl
Journal:  Br J Haematol       Date:  2012-03-13       Impact factor: 6.998

2.  Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain.

Authors:  Florian Heidel; Fian K Solem; Frank Breitenbuecher; Daniel B Lipka; Stefan Kasper; M H Thiede; Christian Brandts; Hubert Serve; Johannes Roesel; Francis Giles; Eric Feldman; Gerhard Ehninger; Gary J Schiller; Stephen Nimer; Richard M Stone; Yanfeng Wang; Thomas Kindler; Pamela S Cohen; Christoph Huber; Thomas Fischer
Journal:  Blood       Date:  2005-09-08       Impact factor: 22.113

3.  The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors.

Authors:  Els Lierman; Idoya Lahortiga; Helen Van Miegroet; Nicole Mentens; Peter Marynen; Jan Cools
Journal:  Haematologica       Date:  2007-01       Impact factor: 9.941

4.  FLT3 internal tandem duplication mutations associated with human acute myeloid leukemias induce myeloproliferative disease in a murine bone marrow transplant model.

Authors:  Louise M Kelly; Qing Liu; Jeffrey L Kutok; Ifor R Williams; Christina L Boulton; D Gary Gilliland
Journal:  Blood       Date:  2002-01-01       Impact factor: 22.113

5.  Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia.

Authors:  Catherine C Smith; Qi Wang; Chen-Shan Chin; Sara Salerno; Lauren E Damon; Mark J Levis; Alexander E Perl; Kevin J Travers; Susana Wang; Jeremy P Hunt; Patrick P Zarrinkar; Eric E Schadt; Andrew Kasarskis; John Kuriyan; Neil P Shah
Journal:  Nature       Date:  2012-04-15       Impact factor: 49.962

Review 6.  FLT3 as a therapeutic target in AML: still challenging after all these years.

Authors:  Thomas Kindler; Daniel B Lipka; Thomas Fischer
Journal:  Blood       Date:  2010-08-12       Impact factor: 22.113

7.  Prognostic relevance of integrated genetic profiling in acute myeloid leukemia.

Authors:  Jay P Patel; Mithat Gönen; Maria E Figueroa; Hugo Fernandez; Zhuoxin Sun; Janis Racevskis; Pieter Van Vlierberghe; Igor Dolgalev; Sabrena Thomas; Olga Aminova; Kety Huberman; Janice Cheng; Agnes Viale; Nicholas D Socci; Adriana Heguy; Athena Cherry; Gail Vance; Rodney R Higgins; Rhett P Ketterling; Robert E Gallagher; Mark Litzow; Marcel R M van den Brink; Hillard M Lazarus; Jacob M Rowe; Selina Luger; Adolfo Ferrando; Elisabeth Paietta; Martin S Tallman; Ari Melnick; Omar Abdel-Wahab; Ross L Levine
Journal:  N Engl J Med       Date:  2012-03-14       Impact factor: 91.245

8.  FLT3-internal tandem duplication and age are the major prognostic factors in patients with relapsed acute myeloid leukemia with normal karyotype.

Authors:  Katharina Wagner; Frederik Damm; Felicitas Thol; Gudrun Göhring; Kerstin Görlich; Michael Heuser; Irina Schäfer; Brigitte Schlegelberger; Gerhard Heil; Arnold Ganser; Jürgen Krauter
Journal:  Haematologica       Date:  2011-01-17       Impact factor: 9.941

9.  Insertion of FLT3 internal tandem duplication in the tyrosine kinase domain-1 is associated with resistance to chemotherapy and inferior outcome.

Authors:  Sabine Kayser; Richard F Schlenk; Martina Correa Londono; Frank Breitenbuecher; Kerstin Wittke; Juan Du; Silja Groner; Daniela Späth; Jürgen Krauter; Arnold Ganser; Hartmut Döhner; Thomas Fischer; Konstanze Döhner
Journal:  Blood       Date:  2009-07-14       Impact factor: 22.113

10.  AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Authors:  Patrick P Zarrinkar; Ruwanthi N Gunawardane; Merryl D Cramer; Michael F Gardner; Daniel Brigham; Barbara Belli; Mazen W Karaman; Keith W Pratz; Gabriel Pallares; Qi Chao; Kelly G Sprankle; Hitesh K Patel; Mark Levis; Robert C Armstrong; Joyce James; Shripad S Bhagwat
Journal:  Blood       Date:  2009-08-04       Impact factor: 22.113
View more
  10 in total

1.  The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.

Authors:  Trevor J Mathias; Karthika Natarajan; Suneet Shukla; Kshama A Doshi; Zeba N Singh; Suresh V Ambudkar; Maria R Baer
Journal:  Invest New Drugs       Date:  2015-01-20       Impact factor: 3.850

Review 2.  Predicting Chemotherapy Resistance in AML.

Authors:  Cecilia C S Yeung; Jerald Radich
Journal:  Curr Hematol Malig Rep       Date:  2017-12       Impact factor: 3.952

3.  G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia.

Authors:  Hee Kyu Lee; Hong Woo Kim; In Yong Lee; Jungmi Lee; Jaekyoo Lee; Dong Sik Jung; Sang Yeop Lee; Sung Ho Park; Haejun Hwang; Jang-Sik Choi; Jung-Ho Kim; Se Won Kim; Jung Keun Kim; Jan Cools; Jong Sung Koh; Ho-Juhn Song
Journal:  Blood       Date:  2014-02-14       Impact factor: 22.113

4.  Targeting oncoprotein stability overcomes drug resistance caused by FLT3 kinase domain mutations.

Authors:  Chuanjiang Yu; Rama Krishna Kancha; Justus Duyster
Journal:  PLoS One       Date:  2014-05-21       Impact factor: 3.240

5.  Prospective identification of resistance mechanisms to HSP90 inhibition in KRAS mutant cancer cells.

Authors:  Arefeh Rouhi; Christina Miller; Sarah Grasedieck; Stefanie Reinhart; Britta Stolze; Hartmut Döhner; Florian Kuchenbauer; Lars Bullinger; Stefan Fröhling; Claudia Scholl
Journal:  Oncotarget       Date:  2017-01-31

Review 6.  Potential targeting of FLT3 acute myeloid leukemia.

Authors:  Alexander J Ambinder; Mark Levis
Journal:  Haematologica       Date:  2021-03-01       Impact factor: 9.941

7.  LT-171-861, a novel FLT3 inhibitor, shows excellent preclinical efficacy for the treatment of FLT3 mutant acute myeloid leukemia.

Authors:  Zhou Yu; Jiaying Du; Hui Hui; Shaoxin Kan; Tongxin Huo; Kai Zhao; Tao Wu; Qinglong Guo; Na Lu
Journal:  Theranostics       Date:  2021-01-01       Impact factor: 11.600

Review 8.  An overview of kinase downregulators and recent advances in discovery approaches.

Authors:  Beilei Wang; Hong Wu; Chen Hu; Haizhen Wang; Jing Liu; Wenchao Wang; Qingsong Liu
Journal:  Signal Transduct Target Ther       Date:  2021-12-20

Review 9.  Kinase-targeted cancer therapies: progress, challenges and future directions.

Authors:  Khushwant S Bhullar; Naiara Orrego Lagarón; Eileen M McGowan; Indu Parmar; Amitabh Jha; Basil P Hubbard; H P Vasantha Rupasinghe
Journal:  Mol Cancer       Date:  2018-02-19       Impact factor: 27.401

10.  DOT1L: a key target in normal chromatin remodelling and in mixed-lineage leukaemia treatment.

Authors:  Federica Sarno; Angela Nebbioso; Lucia Altucci
Journal:  Epigenetics       Date:  2019-12-28       Impact factor: 4.528
  10 in total

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