TY - JOUR
T1 - Targeting the SAGA and ATAC transcriptional coactivator complexes in MYC-driven cancers
AU - Mustachio, Lisa Maria
AU - Roszik, Jason
AU - Farria, Aimee
AU - Dent, Sharon Y.R.
N1 - Publisher Copyright:
© 2020 American Association for Cancer Research.
PY - 2020/5
Y1 - 2020/5
N2 - Targeting epigenetic regulators, such as histone-modifying enzymes, provides novel strategies for cancer therapy. The GCN5 lysine acetyltransferase (KAT) functions together with MYC both during normal development and in oncogenesis. As transcription factors, MYC family members are difficult to target with small-molecule inhibitors, but the acetyltransferase domain and the bromodomain in GCN5 might provide alternative targets for disruption of MYC-driven functions. GCN5 is part of two distinct multiprotein histone-modifying complexes, SAGA and ATAC. This review summarizes key findings on the roles of SAGA and ATAC in embryo development and in cancer to better understand the functional relationships of these complexes with MYC family members, as well as their future potential as therapeutic targets.
AB - Targeting epigenetic regulators, such as histone-modifying enzymes, provides novel strategies for cancer therapy. The GCN5 lysine acetyltransferase (KAT) functions together with MYC both during normal development and in oncogenesis. As transcription factors, MYC family members are difficult to target with small-molecule inhibitors, but the acetyltransferase domain and the bromodomain in GCN5 might provide alternative targets for disruption of MYC-driven functions. GCN5 is part of two distinct multiprotein histone-modifying complexes, SAGA and ATAC. This review summarizes key findings on the roles of SAGA and ATAC in embryo development and in cancer to better understand the functional relationships of these complexes with MYC family members, as well as their future potential as therapeutic targets.
UR - http://www.scopus.com/inward/record.url?scp=85084935280&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85084935280&partnerID=8YFLogxK
U2 - 10.1158/0008-5472.CAN-19-3652
DO - 10.1158/0008-5472.CAN-19-3652
M3 - Review article
C2 - 32094302
AN - SCOPUS:85084935280
SN - 0008-5472
VL - 80
SP - 1905
EP - 1911
JO - Cancer Research
JF - Cancer Research
IS - 10
ER -