Literature DB >> 16158972

Cytotoxicity of cortivazol in childhood acute lymphoblastic leukemia.

Jan Styczynski1, Andrzej Kurylak, Mariusz Wysocki.   

Abstract

BACKGROUND: Glucocorticoids are the most important group of drugs used in the treatment of childhood acute lymphoblastic leukemia (ALL), however, resistance to this group remains the main obstacle in curing the disease. One of the possibilities to circumvent glucocorticoid resistance is the use of new compounds, such as cortivazol (CVZ), which has two binding sites for the glucocorticoid receptor. AIM: Analysis of ex vivo sensitivity to cortivazol and other glucocorticoids in childhood acute lymphoblastic leukemia, as well as the relationship to anticancer therapy outcome. PATIENTS AND METHODS: Leukemic samples from 60 children with ALL were tested by the M7T assay for glucocorticoid resistance. Cell cycle before and after ex vivo glucocorticoid treatment was analyzed by flow cytometry.
RESULTS: Although all tested glucocorticoids presented significant cross-resistance, CVZ showed high antileukemic activity. The equivalent activity of CVZ was 165-fold higher than prednisolone, 7.ZS5-fold higher than dexamethasone and 2.8-fold higher than betamethasone. CVZ showed relatively better cytotoxicity than other glucocorticoids in prednisolone-poor-responders. CVZ, like other glucocorticoids, caused cell cycle arrest in the GI-phase, and increased the percentage of apoptotic cells to a greater extent than other glucocorticoids. The results of antileukemic therapy were strongly related to the ex vivo resistance to all tested glucocorticoids.
CONCLUSION: Cortivazol has potent antileukemic activity in childhood ALL. Its activity is related to cell cycle arrest and induction of apoptosis.

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Year:  2005        PMID: 16158972

Source DB:  PubMed          Journal:  Anticancer Res        ISSN: 0250-7005            Impact factor:   2.480


  5 in total

1.  Predictive value of multidrug resistance proteins and cellular drug resistance in childhood relapsed acute lymphoblastic leukemia.

Authors:  Jan Styczynski; Mariusz Wysocki; Robert Debski; Krzysztof Czyzewski; Beata Kolodziej; Beata Rafinska; Malgorzata Kubicka; Sylwia Koltan; Andrzej Koltan; Monika Pogorzala; Andrzej Kurylak; Dorota Olszewska-Slonina; Walentyna Balwierz; Edyta Juraszewska; Maria Wieczorek; Igor Olejnik; Maryna Krawczuk-Rybak; Marta Kuzmicz; Jerzy Kowalczyk; Jolanta Stefaniak; Wanda Badowska; Danuta Sonta-Jakimczyk; Tomasz Szczepanski; Michal Matysiak; Iwona Malinowska; Elzbieta Stanczak; Jacek Wachowiak; Benigna Konatkowska; Lidia Gil; Anna Balcerska; Lucyna Maciejka-Kapuscinska
Journal:  J Cancer Res Clin Oncol       Date:  2007-08-02       Impact factor: 4.553

Review 2.  Tissue-specific glucocorticoid action: a family affair.

Authors:  Katherine L Gross; John A Cidlowski
Journal:  Trends Endocrinol Metab       Date:  2008-09-19       Impact factor: 12.015

3.  Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazol.

Authors:  Kelly Suino-Powell; Yong Xu; Chenghai Zhang; Yong-Guang Tao; W David Tolbert; S Stoney Simons; H Eric Xu
Journal:  Mol Cell Biol       Date:  2007-12-26       Impact factor: 4.272

4.  The Role of Conformational Dynamics and Allostery in the Control of Distinct Efficacies of Agonists to the Glucocorticoid Receptor.

Authors:  Yuxin Shi; Shu Cao; Duan Ni; Jigang Fan; Shaoyong Lu; Mintao Xue
Journal:  Front Mol Biosci       Date:  2022-07-07

5.  Gene expression profiling of leukemic cells and primary thymocytes predicts a signature for apoptotic sensitivity to glucocorticoids.

Authors:  Aaron L Miller; Spogmai Komak; M Scott Webb; Edward H Leiter; E Brad Thompson
Journal:  Cancer Cell Int       Date:  2007-11-28       Impact factor: 5.722

  5 in total

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