Pharmacological targeting of PI3K isoforms as a therapeutic strategy in chronic lymphocytic leukaemia
Pharmacological targeting of PI3K isoforms as a therapeutic strategy in chronic lymphocytic leukaemia
PI3K? inhibitors such as idelalisib are providing improved therapeutic options for the treatment of chronic lymphocytic leukaemia (CLL). However under certain conditions, inhibition of a single PI3K isoform can be compensated by the other PI3K isoforms, therefore PI3K inhibitors which target multiple PI3K isoforms may provide greater efficacy. The development of compounds targeting multiple PI3K isoforms (?,?,?,?) in CLL cells, in vitro, resulted in sustained inhibition of BCR signalling but with enhanced cytotoxicity and the potential for improve clinical responses. This review summarises the progress of PI3K inhibitor development and describes the rationale and potential for targeting multiple PI3K isoforms.
60-63
Blunt, Matthew D.
b1109de3-6045-4bc3-bd77-6cf26504697d
Steele, Andrew J.
4349f6aa-2e3a-49a8-be73-7716056ae089
2015
Blunt, Matthew D.
b1109de3-6045-4bc3-bd77-6cf26504697d
Steele, Andrew J.
4349f6aa-2e3a-49a8-be73-7716056ae089
Blunt, Matthew D. and Steele, Andrew J.
(2015)
Pharmacological targeting of PI3K isoforms as a therapeutic strategy in chronic lymphocytic leukaemia.
Leukemia Research Reports, 4 (2), .
(doi:10.1016/j.lrr.2015.09.001).
Abstract
PI3K? inhibitors such as idelalisib are providing improved therapeutic options for the treatment of chronic lymphocytic leukaemia (CLL). However under certain conditions, inhibition of a single PI3K isoform can be compensated by the other PI3K isoforms, therefore PI3K inhibitors which target multiple PI3K isoforms may provide greater efficacy. The development of compounds targeting multiple PI3K isoforms (?,?,?,?) in CLL cells, in vitro, resulted in sustained inhibition of BCR signalling but with enhanced cytotoxicity and the potential for improve clinical responses. This review summarises the progress of PI3K inhibitor development and describes the rationale and potential for targeting multiple PI3K isoforms.
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Accepted/In Press date: 11 September 2015
e-pub ahead of print date: 18 September 2015
Published date: 2015
Additional Information:
CLL, PI3K, idelalisib, duvelisib
Organisations:
Cancer Sciences
Identifiers
Local EPrints ID: 381796
URI: http://eprints.soton.ac.uk/id/eprint/381796
ISSN: 2213-0489
PURE UUID: 876d929f-7bd4-429d-910f-dca160923b66
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Date deposited: 22 Sep 2015 16:06
Last modified: 15 Mar 2024 03:46
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