The chemical biology of apoptosis: Revisited after 17 years.
In: European journal of medicinal chemistry, Jg. 177 (2019-09-01), S. 63-75
academicJournal
Zugriff:
A balance of Bcl-2 family proteins dictates cell survival or death, as the interactions between these proteins regulate mitochondrial apoptotic signaling pathways. However, cancer cells frequently show upregulation of pro-survival Bcl-2 proteins and sequester activated pro-apoptotic BH3-only proteins driven by diverse cytotoxic stresses, resulting in tumor progression and chemoresistance. Synthetic molecules from either structure-based design or screening procedures to engage and inactivate pro-survival Bcl-2 proteins and restore apoptotic process represent a chemical biological means of selectively killing malignant cells. 17 years ago, one of us reviewed on the discovery of novel Bcl-2 targeted agents [1]. Here we revisit this area and examine the progress and current status of small molecule Bcl-2 inhibitor development, demonstrating the Bcl-2 family as a valid target for cancer therapy and providing successful examples for the discovery of inhibitors that target protein-protein interactions.
(Copyright © 2019. Published by Elsevier Masson SAS.)
Titel: |
The chemical biology of apoptosis: Revisited after 17 years.
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Autor/in / Beteiligte Person: | Yang, S ; Mao, Y ; Zhang, H ; Xu, Y ; An, J ; Huang, Z |
Zeitschrift: | European journal of medicinal chemistry, Jg. 177 (2019-09-01), S. 63-75 |
Veröffentlichung: | Paris : Editions Scientifiques Elsevier ; <i>Original Publication</i>: Paris, S.E.C.T. [etc.], 2019 |
Medientyp: | academicJournal |
ISSN: | 1768-3254 (electronic) |
DOI: | 10.1016/j.ejmech.2019.05.019 |
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