当前位置： SCI文献检索 > LEUKEMIA RESEARCH期刊下所有文献 > Antineoplastic effect of a single oral dose of the novel Flt3 inhibitor KRN383 on xenografted human leukemic cells harboring Flt3-activating mutations.

Antineoplastic effect of a single oral dose of the novel Flt3 inhibitor KRN383 on xenografted human leukemic cells harboring Flt3-activating mutations.

Abstract：

:Activating mutations of Fms-like tyrosine kinase 3 (Flt3) are the most common genetic abnormalities found in acute myeloid leukemia (AML) and represent potential therapeutic targets. The novel Flt3 inhibitor KRN383 inhibited the autophosphorylation of Flt3 bearing internal tandem duplications (ITDs) and the Asp835Tyr (D835Y) point mutation with half-maximal inhibitory concentration (IC(50)) values of < or =5.9 and 43 nM, respectively. KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.

journal_name

Leuk Res

journal_title

Leukemia research

authors

Nishiyama U,Yoshino T,Ozai M,Yoshioka R,Fujisawa M,Ogasawara Y,Kitahori M,Yoshioka E,Kubo K,Komeno Y,Kurokawa M,Ogawa S,Chiba S,Osawa T,Kuwaki T,Hirai H,Miwa A

doi

10.1016/j.leukres.2006.02.028

subject

Has Abstract

pub_date

2006-12-01 00:00:00

pages

1541-6

issue

12

eissn

0145-2126

issn

1873-5835

pii

S0145-2126(06)00094-4

journal_volume

30

pub_type

杂志文章

相关文献

LEUKEMIA RESEARCH文献大全
  • Elevated argininosuccinate synthetase activity in adult T leukemia cell lines.

    abstract：:Argininosuccinate synthetase (ASS) is a ATP-dependent and rate-limiting enzyme of the urea cycle which catalyzes L-citrulline to L-arginine in combination with argininosuccinate lyase (ASL). We demonstrate here that (a) human normal T and B lymphocytes did not express ASS activity, (b) however, three adult T leukemia ...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(90)90184-b

    authors： Sugimura K,Kimura T,Arakawa H,Ohno T,Wada Y,Kimura Y,Saheki T,Azuma I

    更新日期：1990-01-01 00:00:00

  • In the absence of clinically significant graft vs. host disease, myeloablative conditioning may allow an effective graft vs. leukaemia effect.

    abstract：:In AML, prevention of GvHD leads to better tolerance of myeloablative therapy. 66 individuals with AML in CR underwent myeloablative conditioning and transplantation with allogeneic PBPC grafts. Median presentation age was 44.5 years. Karyotyping was intermediate in 48% and of unfavourable risk in 36%. For GvHD prophy...

    journal_title：Leukemia research

    pub_type： 临床试验,杂志文章

    doi：10.1016/j.leukres.2011.06.039

    authors： Novitzky N,Thomas V

    更新日期：2012-01-01 00:00:00

  • Functional alterations of Lin-CD34+CD38+ cells in chronic myelomonocytic leukemia and on progression to acute leukemia.

    abstract：:The functional behavior of hematopoietic stem cell (HSC) and progenitors in chronic myelomonocytic leukemia (CMML) and on disease progression is little known. We performed cell proliferation, apoptosis, hematopoietic colony forming/replating and differentiation potential studies in the purified subpopulations of Lin(-...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2008.02.011

    authors： Sun Q,So CC,Yip SF,Wan TS,Ma SK,Chan LC

    更新日期：2008-09-01 00:00:00

  • Dephosphorylation of specific proteins in HL-60 cells by 1 alpha, 25-dihydroxyvitamin D3: possible involvement of cAMP-dependent protein kinase.

    abstract：:Changes of phosphoprotein patterns in HL-60 cells were studied during short exposures to 1 alpha, 25-dihydroxyvitamin D3 [1,25(OH)2D3]. One hundred nanometers 1,25(OH)2D3 dephosphorylated at least three proteins in 6 h: phosphoproteins with molecular weights of 82 kD (pp82), 33 kD (pp33), and 31 kD (pp31). Phosphoryla...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(91)90169-t

    authors： Ueda T,Sawada H,Okuda T,Yumoto Y,Kato Y,Ogawa K,Tashima M,Yoshida Y,Okuma M

    更新日期：1991-01-01 00:00:00

  • The clonogenic potential of selected CD34+ cells from patients with MDS appear preserved when tested ex vivo.

    abstract：:Our aim was to examine in 17 patients with MDS the effects of PMA activated and non-activated autologous lymphocytes on selected bone marrow CD34+ progenitors, in dose response studies. We used a double layer culture technique. Compared with controls, there was no difference in the colony growth promoting capacity of ...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2011.03.017

    authors： Davison GM,Novitzky N,Abdulla R

    更新日期：2011-09-01 00:00:00

  • Dequalinium induces cell death in human leukemia cells by early mitochondrial alterations which enhance ROS production.

    abstract：:Dequalinium (DQA) has been proposed as a selective antitumoral agent due to its preferential accumulation in mitochondria of cancer cells. Our aim was a better understanding of DQA cytotoxicity. DQA-induced NB4 and K562 cell alterations are initiated within the first 30 min of treatment at a high DQA concentration wit...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2006.11.018

    authors： Sancho P,Galeano E,Nieto E,Delgado MD,García-Pérez AI

    更新日期：2007-07-01 00:00:00

  • Diagnostic criteria for hypocellular acute leukemia: a clinical entity distinct from overt acute leukemia and myelodysplastic syndrome.

    abstract：:In order to establish diagnostic criteria for hypocellular acute leukemia (HL), we have reviewed 32 cases selected on the basis of hypothetical 40% or less cellularity, by focusing on morphology, immunophenotype, karyotype and response to low dose Ara-C (LDAC) regimen and compared them with 40 cases of myelodysplastic...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(95)00136-0

    authors： Nagai K,Kohno T,Chen YX,Tsushima H,Mori H,Nakamura H,Jinnai I,Matsuo T,Kuriyama K,Tomonaga M,Bennett JM

    更新日期：1996-07-01 00:00:00

  • Bone and bone marrow interactions: hematological activity of osteoblastic growth peptide (OGP)-derived carboxy-terminal pentapeptide. II. Action on human hematopoietic stem cells.

    abstract：:Osteogenic growth peptide (OGP) is a peptide exerting regulatory effects on the bone and on bone marrow. The carboxy-terminal pentapeptide (OGP10-14) is the biologically active portion of OGP. We evaluated OGP10-14 hematopoietic activity performing colony-forming tests on human stem cells derived by bone marrow, perip...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/s0145-2126(02)00008-5

    authors： Fazzi R,Galimberti S,Testi R,Pacini S,Trasciatti S,Rosini S,Petrini M

    更新日期：2002-09-01 00:00:00

  • Distinct cellular origins of primary effusion lymphoma with and without EBV infection.

    abstract：:Kaposi's sarcoma-associated herpesvirus (KSHV) is associated with three distinct lymphoproliferative disorders: primary effusion lymphoma (PEL), multicentric Castleman's disease (MCD) and germinotropic lymphoproliferative disorder (GLD). KSHV positive lymphocytes in GLD and in most cases of PEL are co-infected by Epst...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2003.08.003

    authors： Hamoudi R,Diss TC,Oksenhendler E,Pan L,Carbone A,Ascoli V,Boshoff C,Isaacson P,Du MQ

    更新日期：2004-04-01 00:00:00

  • Response to therapy with interferon alpha-2b and prednisolone in aggressive systemic mastocytosis: report of five cases and review of the literature.

    abstract：:Aggressive systemic mastocytosis (ASM) is a hematopoietic neoplasm characterized by infiltration of visceral organs by neoplastic mast cells (MCs) with consecutive organopathy and respective clinical and laboratory findings (so called C-Findings). Whereas, it is generally appreciated that patients with ASM are candida...

    journal_title：Leukemia research

    pub_type： 杂志文章,评审

    doi：10.1016/s0145-2126(03)00259-5

    authors： Hauswirth AW,Simonitsch-Klupp I,Uffmann M,Koller E,Sperr WR,Lechner K,Valent P

    更新日期：2004-03-01 00:00:00

  • Effects of X-irradiation, ovariohysterectomy and estradiol-17 beta on incidence, benign/malignant ratio and multiplicity of rat mammary neoplasms--a preliminary report.

    abstract：:An overview is given of the effects of X-irradiation, ovariohysterectomy and estradiol-17 beta administration on mammary tumorigenesis in females of 3 rat strains, viz. the WAG/Rij, BN/BiRij and SD. The 3 rat strains differed significantly in their spontaneous mammary tumor incidence. Female SD rats had the highest in...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(86)90292-4

    authors： Solleveld HA,van Zwieten MJ,Broerse JJ,Hollander CF

    更新日期：1986-01-01 00:00:00

  • Cytotoxic effect of a lipophilic alkylating agent after incorporation into low density lipoprotein or emulsions: studies in human leukemic cells.

    abstract：:The use of low density lipoprotein (LDL) as drug carrier in acute myeloblastic leukemia chemotherapy is attractive due to high LDL uptake by leukemic cells. Lipid-based formulations, such as liposomes or microemulsions are promising alternatives. In the current study, we incorporated N-trifluoroacetyl-adriamycin-14-va...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2005.06.012

    authors： Masquelier M,Lundberg B,Peterson C,Vitols S

    更新日期：2006-02-01 00:00:00

  • Immunoglobulin G antibodies binding to a synthetic peptide deduced from the nucleotide sequence of the env gene of HTLV I in patients with leukemia and rheumatoid arthritis, HLA sensitized persons and blood donors.

    abstract：:A synthetic pentadecapeptide preparation, env 406-420, with an amino acid sequence deduced from the envelope glycoprotein gene of human T cell leukemia virus type I (HTLV I), was used as the antigen in an enzyme immunoassay for immunoglobulin G antibodies, exploring its usefulness for seroepidemiological purposes. The...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(85)90100-6

    authors： Blomberg J,Fölsch G,Nilsson I,Fäldt R

    更新日期：1985-01-01 00:00:00

  • Biochemical and immunological characteristics of ferritin from HL-60, U-937 and K-562 cell lines: implications for haemopoietic regulation.

    abstract：:It has been suggested that acidic isoferritins play a major role in the regulation of human granulocyte-macrophage (CFU-GM) proliferation. Such regulatory isoferritins are said to occur in some human tissues including both leukaemic and normal leucocytes, and certain established cell lines. They are glycosylated and b...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(84)90065-1

    authors： Wyllie F,Jacobs A,Waradanukul K,Worwood M,Wagstaff M

    更新日期：1984-01-01 00:00:00

  • Acid hydrolases in B-chronic lymphocytic leukemia (B-CLL): a comparison with normal peripheral B lymphocytes and normal B-cell subset with the phenotype of B-leukaemic cells.

    abstract：:The acid phosphatase (AP), beta-glucuronidase (BG), and alpha-naphthyl-acetate esterase (ANAE) distribution and the morphology of stage 0 B-CLL lymphocytes were studied. The results were compared with the same hydrolase equipment and morphology of normal B-cell populations showing the B-CLL-like phenotype, and thus re...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(87)90074-9

    authors： Palestro G,Novero D,Godio L,Micca FB,Resegotti L,Stramignon A

    更新日期：1987-01-01 00:00:00

  • Development of a mantle cell lymphoma in an ATM heterozygous woman after occupational exposure to ionising radiation and somatic mutation of the second allele.

    abstract：:Predisposition to lymphomagenesis is a well-known phenomenon of ataxia-telangiectasia, a recessive disorder caused by germline inactivation of ATM. ATM encodes a protein implicated in the repair of radiation induced double-strand breaks. Biallelic ATM inactivation was described also in sporadic lymphoid malignancies, ...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2005.11.010

    authors： Briani C,Schlotter M,Lichter P,Kalla C

    更新日期：2006-09-01 00:00:00

  • Production of a negative regulator of IL-3 by bone marrow cells in response to the supernatant of IL-3-producing STIL-3 leukemia cells.

    abstract：:When spleen cells of mice grafted with STIL-3 C5 cells, a leukemic T-cell line producing IL-3, are cultured in vitro, a high IL-3 activity is detectable in the culture supernatant. However, when bone marrow cells of the same grafted mice are cultured under similar conditions, hardly any IL-3 activity is detectable. To...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(92)90035-6

    authors： Sugimoto K,Taniguchi S,Ogata H,Ikehara S,Fujita J,Mori KJ

    更新日期：1992-09-01 00:00:00

  • Iron overload in myelodysplastic syndromes: Evidence based guidelines from the Canadian consortium on MDS.

    abstract：:In 2008 the first evidence-based Canadian consensus guideline addressing the diagnosis, monitoring and management of transfusional iron overload in patients with myelodysplastic syndromes (MDS) was published. The Canadian Consortium on MDS, comprised of hematologists from across Canada with a clinical and academic int...

    journal_title：Leukemia research

    pub_type： 杂志文章,评审

    doi：10.1016/j.leukres.2018.09.005

    authors： Leitch HA,Buckstein R,Zhu N,Nevill TJ,Yee KWL,Leber B,Keating MM,St Hilaire E,Kumar R,Delage R,Geddes M,Storring JM,Shamy A,Elemary M,Wells RA

    更新日期：2018-11-01 00:00:00

  • Challenges in the use of NG2 antigen as a marker to predict MLL rearrangements in multi-center studies.

    abstract：:Rearrangements in MLL (MLL-r) are common within very young children with leukemia and affect the prognosis and treatment. Previous studies have suggested the use of the NG2 molecule as a marker for MLL-r but these studies were performed using a small number of infants. We analyzed 148 patients (all less than 24 months...

    journal_title：Leukemia research

    pub_type： 杂志文章,多中心研究

    doi：10.1016/j.leukres.2011.03.006

    authors： Emerenciano M,Renaud G,Sant'Ana M,Barbieri C,Passetti F,Pombo-de-Oliveira MS,Brazilian Collaborative Study Group of Infant Acute Leukemia.

    更新日期：2011-08-01 00:00:00

  • Stimulation of HTLV-I expression by subtoxic dose of 3-methylcholanthrene.

    abstract：:In vivo infection by HTLV-I is characterized by the lack of virus expression in the host's infected cells and in most cases it is clinically inapparent. The present study shows that exposure of HTLV-I-infected human T-cells to a maximal non-toxic dose of 3-MC remarkably enhances virus expression. This stimulatory effe...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(93)90098-6

    authors： Feldman G,Aboud M

    更新日期：1993-05-01 00:00:00

  • Central nervous system involvement in adult acute lymphoblastic leukemia at diagnosis and/or at first relapse: results from the GET-LALA group.

    abstract：:Outcome of adult acute lymphoblastic leukemia (ALL) with central nervous system (CNS) involvement is not clearly defined. We studied 104 patients presenting with CNS involvement at diagnosis among 1493 patients (7%) included into the LALA trials, and 109 patients presenting CNS disease at the time of first relapse amo...

    journal_title：Leukemia research

    pub_type： 杂志文章,多中心研究

    doi：10.1016/j.leukres.2008.04.011

    authors： Reman O,Pigneux A,Huguet F,Vey N,Delannoy A,Fegueux N,de Botton S,Stamatoullas A,Tournilhac O,Buzyn A,Charrin C,Boucheix C,Gabert J,Lhéritier V,Vernant JP,Fière D,Dombret H,Thomas X,GET-LALA group.

    更新日期：2008-11-01 00:00:00

  • Statins in the treatment of polycythaemia vera and allied disorders: an antithrombotic and cytoreductive potential?

    abstract：:Thrombohaemorrhagic complications are major clinical problems in the classical chronic Ph-negative myeloproliferative disorders (CMPDs), polycytaemia vera (PV), essential thrombocythaemia (ET) and idiopathic myelofibrosis (IMF), contributing significantly to morbidity and mortality. Pathophysiologically these disorder...

    journal_title：Leukemia research

    pub_type： 杂志文章,评审

    doi：10.1016/j.leukres.2005.12.018

    authors： Hasselbalch HC,Riley CH

    更新日期：2006-10-01 00:00:00

  • HL-R5 and HL-D4: two differentiation resistant HL-60 variants.

    abstract：:A wide range of different agents are capable of inducing the onset of HL-60 differentiation along the myeloid lineage. The diversity of these agents has made the analysis of the molecular mechanisms involved in the regulation of the onset and progress of terminal differentiation in these cells difficult. We have adapt...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(89)90081-7

    authors： Darling DC,Linskens MH,Farzaneh F

    更新日期：1989-01-01 00:00:00

  • Serum erythropoietin concentrations in patients with myelodysplastic syndromes.

    abstract：:Medullary dyserythropoiesis with reduced production of erythrocytes is an early and consistent feature of myelodysplastic syndromes (MDS). The mechanism underlying the disturbed red cell proliferation and maturation is presently unknown. In order to study the role of erythropoietic growth factors, we determined by rad...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(91)90025-o

    authors： Aul C,Arning M,Runde V,Schneider W

    更新日期：1991-01-01 00:00:00

  • Single-agent Smac-mimetic compounds induce apoptosis in B chronic lymphocytic leukaemia (B-CLL).

    abstract：:Defective apoptosis is a hallmark of the progression of B chronic lymphocytic leukaemia (B-CLL). Smac-mimetics have been shown to induce apoptosis in several tumours. We describe the in vitro pro-apoptotic activity and regulation of the molecular pathway induced by new Smac-mimetics in B-CLL. The cytotoxic effect was ...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2013.03.016

    authors： Scavullo C,Servida F,Lecis D,Onida F,Drago C,Ferrante L,Seneci P,Barcellini W,Lionetti M,Todoerti K,Neri A,Delia D,Deliliers GL

    更新日期：2013-07-01 00:00:00

  • Analysis of the novel cyclin-dependent kinase 4 and 6 inhibitor gene p18 in lymphoma and leukemia cell lines.

    abstract：:The genes for the CDK4/6-inhibitors p16INK4A/MTS1 and p15INK4B/MTS2 are frequently deleted in hematological malignancies. A new member of this family of CDK4/6 inhibitors is p18. In order to assess p18 growth-suppressor gene alterations in hematological neoplasms, we investigated 31 lymphoma and leukemia cell lines by...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/0145-2126(95)00137-9

    authors： Siebert R,Willers CP,Fosså A,Kloke O,Nowrousian MR,Seeber S,Opalka B

    更新日期：1996-02-01 00:00:00

  • Long-term follow-up of intensive ara-C-based chemotherapy followed by bone marrow transplantation for adult acute lymphoblastic leukemia: impact of induction Ara-C dose and post-remission therapy.

    abstract：:We report single institution outcome of brief, intensive ara-C-based chemotherapy using bone marrow transplantation as primary intensification for untreated adult patients with acute lymphoblastic leukemia (ALL). Overall disease-free and overall survival were inferior to those reported with prolonged chemotherapy mode...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/s0145-2126(01)00175-8

    authors： Sotomayor EM,Piantadosi S,Miller CB,Karp JE,Jones RJ,Rowley SD,Kaufmann SH,Braine H,Burke PJ,Gore SD

    更新日期：2002-05-01 00:00:00

  • XIAP downregulation promotes caspase-dependent inhibition of proteasome activity in AML cells.

    abstract：:To further understand the role of XIAP in acute myeloid leukemia (AML), we suppressed XIAP expression by antisense oligonucleotides and determined the effect on gene expression profiles and biological pathways. XIAP inhibition upregulated expression of proteasome genes in a manner similar to the proteasome inhibitor b...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2013.04.018

    authors： Carter BZ,Mak DH,Wang Z,Ma W,Mak PY,Andreeff M,Davis RE

    更新日期：2013-08-01 00:00:00

  • Characterization of a 4 lncRNAs-based prognostic risk scoring system in adults with acute myeloid leukemia.

    abstract：PURPOSE:The study aims to develop a prognostic scoring system based on prognostic lncRNAs for acute myeloid leukemia (AML). METHODS:Based on lncRNA expression profiles downloaded from The Cancer Genome Atlas (TCGA), differentially expressed long noncoding RNAs (DELs) between good prognosis and bad prognosis samples we...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2019.106261

    authors： Zeng H,Wu H,Yan M,Tang L,Guo X,Zhao X

    更新日期：2020-01-01 00:00:00

  • Expression pattern of the septin gene family in acute myeloid leukemias with and without MLL-SEPT fusion genes.

    abstract：:Septins are proteins associated with crucial steps in cell division and cellular integrity. In humans, 14 septin genes have been identified, of which five (SEPT2, SEPT5, SEPT6, SEPT9, and SEPT11) are known to participate in reciprocal translocations with the MLL gene in myeloid neoplasias. We have recently shown a sig...

    journal_title：Leukemia research

    pub_type： 杂志文章

    doi：10.1016/j.leukres.2009.08.018

    authors： Santos J,Cerveira N,Bizarro S,Ribeiro FR,Correia C,Torres L,Lisboa S,Vieira J,Mariz JM,Norton L,Snijder S,Mellink CH,Buijs A,Shih LY,Strehl S,Micci F,Heim S,Teixeira MR

    更新日期：2010-05-01 00:00:00