Targeting BCL2-Proteins for the Treatment of Solid Tumours
Due to their central role in the regulation of apoptosis, the antiapoptotic BCL2-proteins are highly promising targets for the development of novel anticancer treatments. To this end, several strategies have been developed to inhibit BCL2, BCL-XL, BCL-w, and MCL1. While early clinical trials in haem...
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doaj-442333a4bc154895a8c296d9e7103c0c2020-11-24T22:59:32ZengHindawi LimitedAdvances in Medicine2356-67522314-758X2014-01-01201410.1155/2014/943648943648Targeting BCL2-Proteins for the Treatment of Solid TumoursMeike Vogler0Department of Biochemistry, University of Leicester, Henry-Wellcome Building, Lancaster Road, Leicester LE19HN, UKDue to their central role in the regulation of apoptosis, the antiapoptotic BCL2-proteins are highly promising targets for the development of novel anticancer treatments. To this end, several strategies have been developed to inhibit BCL2, BCL-XL, BCL-w, and MCL1. While early clinical trials in haematological malignancies demonstrated exciting single-agent activity of BCL2-inhibitors, the response in solid tumours was limited, indicating that, in solid tumours, different strategies have to be developed in order to successfully treat patients with BCL2-inhibitors. In this review, the function of the different antiapoptotic BCL2-proteins and their role in solid tumours will be discussed. In addition, a comprehensive analysis of current small molecules targeting these antiapoptotic BCL2-proteins (e.g., ABT-737, ABT-263, ABT-199, TW-37, sabutoclax, obatoclax, and MIM1) will be provided including a discussion of the results of any clinical trials. This analysis will summarise the potential of BCL2-inhibitors for the treatment of solid tumours and will unravel novel approaches to utilise these inhibitors in clinical applications.http://dx.doi.org/10.1155/2014/943648 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Meike Vogler |
spellingShingle |
Meike Vogler Targeting BCL2-Proteins for the Treatment of Solid Tumours Advances in Medicine |
author_facet |
Meike Vogler |
author_sort |
Meike Vogler |
title |
Targeting BCL2-Proteins for the Treatment of Solid Tumours |
title_short |
Targeting BCL2-Proteins for the Treatment of Solid Tumours |
title_full |
Targeting BCL2-Proteins for the Treatment of Solid Tumours |
title_fullStr |
Targeting BCL2-Proteins for the Treatment of Solid Tumours |
title_full_unstemmed |
Targeting BCL2-Proteins for the Treatment of Solid Tumours |
title_sort |
targeting bcl2-proteins for the treatment of solid tumours |
publisher |
Hindawi Limited |
series |
Advances in Medicine |
issn |
2356-6752 2314-758X |
publishDate |
2014-01-01 |
description |
Due to their central role in the regulation of apoptosis, the antiapoptotic BCL2-proteins are highly promising targets for the development of novel anticancer treatments. To this end, several strategies have been developed to inhibit BCL2, BCL-XL, BCL-w, and MCL1. While early clinical trials in haematological malignancies demonstrated exciting single-agent activity of BCL2-inhibitors, the response in solid tumours was limited, indicating that, in solid tumours, different strategies have to be developed in order to successfully treat patients with BCL2-inhibitors. In this review, the function of the different antiapoptotic BCL2-proteins and their role in solid tumours will be discussed. In addition, a comprehensive analysis of current small molecules targeting these antiapoptotic BCL2-proteins (e.g., ABT-737, ABT-263, ABT-199, TW-37, sabutoclax, obatoclax, and MIM1) will be provided including a discussion of the results of any clinical trials. This analysis will summarise the potential of BCL2-inhibitors for the treatment of solid tumours and will unravel novel approaches to utilise these inhibitors in clinical applications. |
url |
http://dx.doi.org/10.1155/2014/943648 |
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