TY - JOUR
T1 - Phosphorylation of serine 230 promotes inducible transcriptional activity of heat shock factor 1
AU - Holmberg, C I
AU - Hietakangas, V
AU - Mikhailov, A
AU - Rantanen, J O
AU - Kallio, M
AU - Meinander, A
AU - Hellman, J
AU - Morrice, N
AU - MacKintosh, C
AU - Morimoto, R I
AU - Eriksson, J E
AU - Sistonen, L
PY - 2001/7/16
Y1 - 2001/7/16
N2 - Heat shock factor 1 (HSF1) is a serine-rich constitutively phosphorylated mediator of the stress response. Upon stress, HSF1 forms DNA-binding trimers, relocalizes to nuclear granules, undergoes inducible phosphorylation and acquires the properties of a transactivator. HSF1 is phosphorylated on multiple sites, but the sites and their function have remained an enigma. Here, we have analyzed sites of endogenous phosphorylation on human HSF1 and developed a phosphopeptide antibody to identify Ser230 as a novel in vivo phosphorylation site. Ser230 is located in the regulatory domain of HSF1, and promotes the magnitude of the inducible transcriptional activity. Ser230 lies within a consensus site for calcium/calmodulin-dependent protein kinase II (CaMKII), and CaMKII overexpression enhances both the level of in vivo Ser230 phosphorylation and transactivation of HSF1. The importance of Ser230 was further established by the S230A HSF1 mutant showing markedly reduced activity relative to wild-type HSF1 when expressed in hsf1(-/-) cells. Our study provides the first evidence that phosphorylation is essential for the transcriptional activity of HSF1, and hence for induction of the heat shock response.
AB - Heat shock factor 1 (HSF1) is a serine-rich constitutively phosphorylated mediator of the stress response. Upon stress, HSF1 forms DNA-binding trimers, relocalizes to nuclear granules, undergoes inducible phosphorylation and acquires the properties of a transactivator. HSF1 is phosphorylated on multiple sites, but the sites and their function have remained an enigma. Here, we have analyzed sites of endogenous phosphorylation on human HSF1 and developed a phosphopeptide antibody to identify Ser230 as a novel in vivo phosphorylation site. Ser230 is located in the regulatory domain of HSF1, and promotes the magnitude of the inducible transcriptional activity. Ser230 lies within a consensus site for calcium/calmodulin-dependent protein kinase II (CaMKII), and CaMKII overexpression enhances both the level of in vivo Ser230 phosphorylation and transactivation of HSF1. The importance of Ser230 was further established by the S230A HSF1 mutant showing markedly reduced activity relative to wild-type HSF1 when expressed in hsf1(-/-) cells. Our study provides the first evidence that phosphorylation is essential for the transcriptional activity of HSF1, and hence for induction of the heat shock response.
KW - Antibodies/immunology
KW - Calcium-Calmodulin-Dependent Protein Kinase Type 2
KW - Calcium-Calmodulin-Dependent Protein Kinases/metabolism
KW - DNA-Binding Proteins/chemistry
KW - Fluorescent Antibody Technique, Indirect
KW - Heat Shock Transcription Factors
KW - Hot Temperature
KW - Humans
KW - Mutagenesis, Site-Directed
KW - Phosphopeptides/immunology
KW - Phosphorylation
KW - Recombinant Proteins/metabolism
KW - Serine/metabolism
KW - Transcription Factors/chemistry
KW - Transcriptional Activation
KW - Tumor Cells, Cultured
U2 - 10.1093/emboj/20.14.3800
DO - 10.1093/emboj/20.14.3800
M3 - Article
C2 - 11447121
SN - 0261-4189
VL - 20
SP - 3800
EP - 3810
JO - EMBO Journal
JF - EMBO Journal
IS - 14
ER -