Toxic Mechanisms of α-Amanitin and Its Potential to Fight Cancer

Xueke Bai, Peixi Jiang, Yuyou Wu

2022

Abstract

In fighting one of the major health problems in the world, the common approach to cancer treatment is the combination of chemotherapy and radiation therapy yet from which the cytotoxic effects on normal tissues and the drug tolerance gained through remain a huge obstacle ahead; thus, new approaches are in immediate demand. In the past decades, toxins such as a-Amanitin have been studied in treating colorectal cancer, breast cancer and pancreatic tumor as a therapeutic agent mostly by conjugating to moieties with targeting property and reduced toxicity. The Amanitin toxin blocks RNA polymerase II activity and is the most specific and most potent inhibitor of the eukaryotic transcription, hepatotoxicity being the main syndrome. For the selective inhibition of RNAPII and induced RNPII activity in cancer cells, using this transcriptional arrest to fight cancer cells appears to be a novel approach with broad applications. Considering the liver toxicity of aAmanitin, conjugation of a-Amanitin to antibodies or small molecules minimizes its toxicity and increases the efficacy of treatment with relatively accurate targeting properties. In addition, further enhancements such as photocaged a-Amanitin analog, conjugation with pH low insert peptide (pHLIP) and Fc Domain provide access to more controlled drug release and ideal pharmacokinetics.

Paper Citation

in Harvard Style

Bai X., Jiang P. and Wu Y. (2022). Toxic Mechanisms of α-Amanitin and Its Potential to Fight Cancer. In Proceedings of the 4th International Conference on Biomedical Engineering and Bioinformatics - Volume 1: ICBEB, ISBN 978-989-758-595-1, pages 1095-1103. DOI: 10.5220/0011378000003443

in Bibtex Style

@conference{icbeb22,
author={Xueke Bai and Peixi Jiang and Yuyou Wu},
title={Toxic Mechanisms of α-Amanitin and Its Potential to Fight Cancer},
booktitle={Proceedings of the 4th International Conference on Biomedical Engineering and Bioinformatics - Volume 1: ICBEB,},
year={2022},
pages={1095-1103},
publisher={SciTePress},
organization={INSTICC},
doi={10.5220/0011378000003443},
isbn={978-989-758-595-1},
}

in EndNote Style

TY - CONF

JO - Proceedings of the 4th International Conference on Biomedical Engineering and Bioinformatics - Volume 1: ICBEB,
TI - Toxic Mechanisms of α-Amanitin and Its Potential to Fight Cancer
SN - 978-989-758-595-1
AU - Bai X.
AU - Jiang P.
AU - Wu Y.
PY - 2022
SP - 1095
EP - 1103
DO - 10.5220/0011378000003443