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Small molecule therapeutics targeting F-box proteins in cancer.
- Source :
-
Seminars in cancer biology [Semin Cancer Biol] 2016 Feb; Vol. 36, pp. 105-19. Date of Electronic Publication: 2015 Sep 30. - Publication Year :
- 2016
-
Abstract
- The ubiquitin proteasome system (UPS) plays vital roles in maintaining protein equilibrium mainly through proteolytic degradation of targeted substrates. The archetypical SCF ubiquitin E3 ligase complex contains a substrate recognition subunit F-box protein that recruits substrates to the catalytic ligase core for its polyubiquitylation and subsequent proteasomal degradation. Several well-characterized F-box proteins have been demonstrated that are tightly linked to neoplasia. There is mounting information characterizing F-box protein-substrate interactions with the rationale to develop unique therapeutics for cancer treatment. Here we review that how F-box proteins function in cancer and summarize potential small molecule inhibitors for cancer therapy.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents pharmacology
Humans
Multiprotein Complexes metabolism
Proteasome Endopeptidase Complex metabolism
Protein Binding
Signal Transduction drug effects
Ubiquitins antagonists & inhibitors
Ubiquitins metabolism
Antineoplastic Agents therapeutic use
F-Box Proteins antagonists & inhibitors
F-Box Proteins metabolism
Molecular Targeted Therapy
Neoplasms drug therapy
Neoplasms metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1096-3650
- Volume :
- 36
- Database :
- MEDLINE
- Journal :
- Seminars in cancer biology
- Publication Type :
- Academic Journal
- Accession number :
- 26427329
- Full Text :
- https://doi.org/10.1016/j.semcancer.2015.09.014