Literature DB >> 28523099

Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.

Xiaochu Ma1,2,1, Jie Zhou1,1, Changhao Wang2, Brandon Carter-Cooper3, Fan Yang2, Elizabeth Larocque1,1, Jonathan Fine1,1, Genichiro Tsuji1,1, Gaurav Chopra1,1, Rena G Lapidus3, Herman O Sintim1,2,1,1.   

Abstract

Acute myeloid leukemia (AML) is an aggressive malignancy with only a handful of therapeutic options. About 30% of AML patients harbor mutated FLT3 kinase, and thus, this cancer-driver has become a hotly pursued AML target. Herein we report a new class of FLT3 inhibitors, which potently inhibit the proliferation of acute myeloid leukemia (AML) cells at nanomolar concentrations.

Entities:  

Keywords:  FMS-like tyrosine kinase 3 (FLT3); acute myeloid leukemia (AML); azo; click-it/staple-it; inhibitor

Year:  2017        PMID： 28523099      PMCID： PMC5430396          DOI： 10.1021/acsmedchemlett.6b00468

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  21 in total

1.  A receptor tyrosine kinase specific to hematopoietic stem and progenitor cell-enriched populations.

Authors:  W Matthews; C T Jordan; G W Wiegand; D Pardoll; I R Lemischka
Journal:  Cell       Date:  1991-06-28       Impact factor: 41.582

2.  Acute hemolytic anaemia due to phenazopyridine hydrochloride in G-6-PD deficient subject.

Authors:  J E Mercieca; M F Clarke; M E Phillips; J R Curtis
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Review 3.  Targeting FLT3 to treat leukemia.

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Journal:  Expert Opin Ther Targets       Date:  2014-09-18       Impact factor: 6.902

4.  Activation mechanisms of STAT5 by oncogenic Flt3-ITD.

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Journal:  Blood       Date:  2007-03-13       Impact factor: 22.113

5.  International expert panel on inflammatory breast cancer: consensus statement for standardized diagnosis and treatment.

Authors:  S Dawood; S D Merajver; P Viens; P B Vermeulen; S M Swain; T A Buchholz; L Y Dirix; P H Levine; A Lucci; S Krishnamurthy; F M Robertson; W A Woodward; W T Yang; N T Ueno; M Cristofanilli
Journal:  Ann Oncol       Date:  2010-07-05       Impact factor: 32.976

Review 6.  FLT3: ITDoes matter in leukemia.

Authors:  M Levis; D Small
Journal:  Leukemia       Date:  2003-09       Impact factor: 11.528

7.  Two distinct molecular mechanisms underlying cytarabine resistance in human leukemic cells.

Authors:  Jie Cai; Vijaya L Damaraju; Normand Groulx; Delores Mowles; Yunshan Peng; Morris J Robins; Carol E Cass; Philippe Gros
Journal:  Cancer Res       Date:  2008-04-01       Impact factor: 12.701

Review 8.  New drugs in acute myeloid leukemia.

Authors:  T M Kadia; F Ravandi; J Cortes; H Kantarjian
Journal:  Ann Oncol       Date:  2016-01-22       Impact factor: 32.976

Review 9.  The evolving role of FLT3 inhibitors in acute myeloid leukemia: quizartinib and beyond.

Authors:  Seth A Wander; Mark J Levis; Amir T Fathi
Journal:  Ther Adv Hematol       Date:  2014-06

10.  Triple negative breast cancer - prognostic factors and survival.

Authors:  Tanja Ovcaricek; Snjezana Grazio Frkovic; Erika Matos; Barbara Mozina; Simona Borstnar
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  7 in total

1.  Aminoisoquinoline benzamides, FLT3 and Src-family kinase inhibitors, potently inhibit proliferation of acute myeloid leukemia cell lines.

Authors:  Elizabeth Larocque; N Naganna; Xiaochu Ma; Clement Opoku-Temeng; Brandon Carter-Cooper; Gaurav Chopra; Rena G Lapidus; Herman O Sintim
Journal:  Future Med Chem       Date:  2017-05-11       Impact factor: 3.808

2.  Alkynylnicotinamide-Based Compounds as ABL1 Inhibitors with Potent Activities against Drug-Resistant CML Harboring ABL1(T315I) Mutant Kinase.

Authors:  Elizabeth A Larocque; N Naganna; Clement Opoku-Temeng; Alyssa M Lambrecht; Herman O Sintim
Journal:  ChemMedChem       Date:  2018-05-22       Impact factor: 3.466

3.  Computational chemoproteomics to understand the role of selected psychoactives in treating mental health indications.

Authors:  Jonathan Fine; Rachel Lackner; Ram Samudrala; Gaurav Chopra
Journal:  Sci Rep       Date:  2019-09-11       Impact factor: 4.379

4.  Isoquinoline Antimicrobial Agent: Activity against Intracellular Bacteria and Effect on Global Bacterial Proteome.

Authors:  Caroline W Karanja; Nimishetti Naganna; Nader S Abutaleb; Neetu Dayal; Kenneth I Onyedibe; Uma Aryal; Mohamed N Seleem; Herman O Sintim
Journal:  Molecules       Date:  2022-08-10       Impact factor: 4.927

5.  Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice.

Authors:  N Naganna; Clement Opoku-Temeng; Eun Yong Choi; Elizabeth Larocque; Elizabeth T Chang; Brandon A Carter-Cooper; Modi Wang; Sandra E Torregrosa-Allen; Bennett D Elzey; Rena G Lapidus; Herman O Sintim
Journal:  EBioMedicine       Date:  2019-01-25       Impact factor: 8.143

6.  Nicotinamide-Ponatinib Analogues as Potent Anti-CML and Anti-AML Compounds.

Authors:  Elizabeth Larocque; Elizabeth Fei Yin Chu; Nimmashetti Naganna; Herman O Sintim
Journal:  ACS Omega       Date:  2020-02-04

7.  Accurate Prediction of Inhibitor Binding to HIV-1 Protease Using CANDOCK.

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  7 in total

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