Bis-indols: a novel class of molecules enhancing the cytodifferentiating properties of retinoids in myeloid leukemia cells

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F02%3A00000626" target="_blank" >RIV/62157124:16370/02:00000626 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/62157124:16370/02:00000003

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Bis-indols: a novel class of molecules enhancing the cytodifferentiating properties of retinoids in myeloid leukemia cells

Popis výsledku v původním jazyce

Enhancing the pharmacological activity of all-trans retinoic acid (ATRA) is potentially useful in the management of acute promyelocytic leukemia (APL) and other types of myeloid leukemia. In this report, we identify a novel class of experimental agents selectively potentiating the cyto-differentiating activity of ATRA and synthetic RARa agonist in APL and other myelod leukemia cell lines. These agents have a bis-indolic structure and ST1346 is the prototypical compound of the series. Gene-profiling experiments and determination of the level of expression of myeloid associated markers indicate that ST1346 stimulates many aspects of the granulocytic maturation process set in motion by ATRA. Stimulation of the cyto-differentiating activity of ATRA by ST1346 enhances the efficacy of the retinoid in vivo, as demonstrated in the APL model of the SCID mouse transplanted with NB4 cells. Although the molecular mechanisms underlying the ATRA-potentiating action of ST1346 and congeners have not b

Název v anglickém jazyce

Bis-indols: a novel class of molecules enhancing the cytodifferentiating properties of retinoids in myeloid leukemia cells

Popis výsledku anglicky

Enhancing the pharmacological activity of all-trans retinoic acid (ATRA) is potentially useful in the management of acute promyelocytic leukemia (APL) and other types of myeloid leukemia. In this report, we identify a novel class of experimental agents selectively potentiating the cyto-differentiating activity of ATRA and synthetic RARa agonist in APL and other myelod leukemia cell lines. These agents have a bis-indolic structure and ST1346 is the prototypical compound of the series. Gene-profiling experiments and determination of the level of expression of myeloid associated markers indicate that ST1346 stimulates many aspects of the granulocytic maturation process set in motion by ATRA. Stimulation of the cyto-differentiating activity of ATRA by ST1346 enhances the efficacy of the retinoid in vivo, as demonstrated in the APL model of the SCID mouse transplanted with NB4 cells. Although the molecular mechanisms underlying the ATRA-potentiating action of ST1346 and congeners have not b

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

2002

Kód důvěrnosti údajů

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

Název periodika

Blood

ISSN

0006-4971

e-ISSN

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Svazek periodika

100

Číslo periodika v rámci svazku

10

Stát vydavatele periodika

CZ - Česká republika

Počet stran výsledku

12

Strana od-do

3719-3730

Kód UT WoS článku

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EID výsledku v databázi Scopus

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