Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin

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Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin. / Vashist, Yogesh-K; Tiffon, Celine; Stoupis, Christoforos; Redaelli, Claudio-A.

in: WORLD J GASTROENTERO, Jahrgang 12, Nr. 42, 14.11.2006, S. 6771-8.

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@article{76425efd92414f9aa50d7cb5594692ef,
title = "Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin",
abstract = "AIM: To investigate the inhibitory effects of taltobulin (HTI-286), a synthetic analogue of natural hemiasterlin derived from marine sponges, on hepatic tumor growth in vitro and in vivo.METHODS: The potential anti-proliferative effects of HTI-286 on different hepatic tumor cell lines in vitro and in vivo were examined.RESULTS: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure. Moreover, intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model).CONCLUSION: HTI-286 might be considered a potent promising drug in treatment of liver malignancies. HTI-286 is currently undergoing clinical evaluation in cancer patients.",
keywords = "Animals, Carcinoma, Hepatocellular, Cell Cycle, Cell Line, Tumor, Cell Proliferation, Dose-Response Relationship, Drug, Female, Humans, Liver Neoplasms, Microtubules, Oligopeptides, Rats, Tubulin Modulators, Xenograft Model Antitumor Assays",
author = "Yogesh-K Vashist and Celine Tiffon and Christoforos Stoupis and Claudio-A Redaelli",
year = "2006",
month = nov,
day = "14",
language = "English",
volume = "12",
pages = "6771--8",
journal = "WORLD J GASTROENTERO",
issn = "1007-9327",
publisher = "WJG Press",
number = "42",

}

RIS

TY - JOUR

T1 - Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin

AU - Vashist, Yogesh-K

AU - Tiffon, Celine

AU - Stoupis, Christoforos

AU - Redaelli, Claudio-A

PY - 2006/11/14

Y1 - 2006/11/14

N2 - AIM: To investigate the inhibitory effects of taltobulin (HTI-286), a synthetic analogue of natural hemiasterlin derived from marine sponges, on hepatic tumor growth in vitro and in vivo.METHODS: The potential anti-proliferative effects of HTI-286 on different hepatic tumor cell lines in vitro and in vivo were examined.RESULTS: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure. Moreover, intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model).CONCLUSION: HTI-286 might be considered a potent promising drug in treatment of liver malignancies. HTI-286 is currently undergoing clinical evaluation in cancer patients.

AB - AIM: To investigate the inhibitory effects of taltobulin (HTI-286), a synthetic analogue of natural hemiasterlin derived from marine sponges, on hepatic tumor growth in vitro and in vivo.METHODS: The potential anti-proliferative effects of HTI-286 on different hepatic tumor cell lines in vitro and in vivo were examined.RESULTS: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure. Moreover, intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model).CONCLUSION: HTI-286 might be considered a potent promising drug in treatment of liver malignancies. HTI-286 is currently undergoing clinical evaluation in cancer patients.

KW - Animals

KW - Carcinoma, Hepatocellular

KW - Cell Cycle

KW - Cell Line, Tumor

KW - Cell Proliferation

KW - Dose-Response Relationship, Drug

KW - Female

KW - Humans

KW - Liver Neoplasms

KW - Microtubules

KW - Oligopeptides

KW - Rats

KW - Tubulin Modulators

KW - Xenograft Model Antitumor Assays

M3 - SCORING: Journal article

C2 - 17106924

VL - 12

SP - 6771

EP - 6778

JO - WORLD J GASTROENTERO

JF - WORLD J GASTROENTERO

SN - 1007-9327

IS - 42

ER -