A novel class of bis-indole compounds capable of enhancing the cyto-differentiating effect of retinoids in acute promyelocytic leukemia cells.

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F01%3A00000614" target="_blank" >RIV/62157124:16370/01:00000614 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

A novel class of bis-indole compounds capable of enhancing the cyto-differentiating effect of retinoids in acute promyelocytic leukemia cells.

Popis výsledku v původním jazyce

All-trans retinoic acid (ATRA) is the only example of clinically useful cyto-differentiating agent, causing complete remission in acute promyelocytic leukemia (APL) patients. However, the clinical use of ATRA is limited by a number of problems, which include a narrow spectrum of activity , systemic and local toxicity, as well as induced resistance. Using the APL-derived and ATRA-sensitive NB4 cell line, we identified a novel class of retinoid sensitizers characterized by a bis-indole chemical structure.The prototypic molecule is ST1346. When NB4 cells are challenged with ST1346 (1-10 micromolar) alone for three days, no significant growth inhibition or cyto-differentiation is observed. By contrast, the induction of several granulocytic maturation markers triggered by ATRA is enhanced by the combination of ST1346+ATRA. The bis-indole shifts the cyto-differentiating activity of ATRA to lower concentrations without affecting the anti-proliferative activity of the retinoid. These potentia

Název v anglickém jazyce

A novel class of bis-indole compounds capable of enhancing the cyto-differentiating effect of retinoids in acute promyelocytic leukemia cells.

Popis výsledku anglicky

All-trans retinoic acid (ATRA) is the only example of clinically useful cyto-differentiating agent, causing complete remission in acute promyelocytic leukemia (APL) patients. However, the clinical use of ATRA is limited by a number of problems, which include a narrow spectrum of activity , systemic and local toxicity, as well as induced resistance. Using the APL-derived and ATRA-sensitive NB4 cell line, we identified a novel class of retinoid sensitizers characterized by a bis-indole chemical structure.The prototypic molecule is ST1346. When NB4 cells are challenged with ST1346 (1-10 micromolar) alone for three days, no significant growth inhibition or cyto-differentiation is observed. By contrast, the induction of several granulocytic maturation markers triggered by ATRA is enhanced by the combination of ST1346+ATRA. The bis-indole shifts the cyto-differentiating activity of ATRA to lower concentrations without affecting the anti-proliferative activity of the retinoid. These potentia

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2001

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Supplement to Clinical Cancer Research

ISSN

1078-0432

e-ISSN

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Svazek periodika

7

Číslo periodika v rámci svazku

11

Stát vydavatele periodika

CZ - Česká republika

Počet stran výsledku

1

Strana od-do

3653-3852

Kód UT WoS článku

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EID výsledku v databázi Scopus

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