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Table 1 Phosphorylation of histone methyltransferases and demethylases, and its effect on the enzymatic activity

From: The phosphorylation to acetylation/methylation cascade in transcriptional regulation: how kinases regulate transcriptional activities of DNA/histone-modifying enzymes

Isoforms of KMTs

Synonyms

Target residues

Kinases

Functional regulation upon phosphorylation

Involved in diseases and signaling pathways

References

KMT1A

SUV39H1

Tyr297

ERBB4

Activation of enzymatic activity; Chromatin remodeling

NRG-1/ErbB4 signaling

[61]

Ser391

CDK2

KMT1C

G9a/

EHMT2

Ser211

CK2

Suppression of its binding affinity for RPA70

DNA damage repair

[63]

Ser591

ATM

Inhibition of enzymatic activity; Suppression of the recruitment of DNA repair factors

DNA damage repair

[80]

KMT2A

MLL1

Ser136

CK2

Increase of the affinity of IBMs for the LEDGF/p75 IBD

MLL-rearranged leukemia

[64]

Ser142

Thr2724

CK2

Degradation

MLL-rearranged leukemia

[65]

Ser2726

KMT2B

MLL2

Thr542

CDK2

Chromatin remodeling

Cell cycle

[69]

KMT2D

MLL4

Ser1331

AKT

Inhibition of enzymatic activity

PI3K pathway

[59]

KMT2E

MLL5

Thr912

CDC2

Activation of enzymatic activity

Cell cycle

[81]

KMT4

DOT1L

Ser1105(Mouse)

CDK1

Inhibition of enzymatic activity

Embryonic stem cell (ESC) differentiation

[73]

KMT6A

EZH2

Ser21

AKT

Inhibition of enzymatic activity

Oncogenesis

[77]

Ser220

MELK

Degradation

Natural killer/T-cell lymphoma (NKTL)

[82]

Tyr244

JAK3

Promotion of the dissociation of the PRC2 complex

Natural killer/T-cell lymphoma (NKTL)

[83]

Thr261

CDK5

Degradation

Pancreatic cancer cell migration and invasion

[84]

Thr311

AMPK

Disruption of the interaction with SUZ12

Tumor growth

[85]

Thr350

CDK4/6

Activation of enzymatic activity

Psoriasis

[76]

S363

GSK3β

Inhibition of enzymatic activity

Human breast cancers

[86]

T416

CDK2

Chromatin remodeling

Triple-negative breast cancer; Cell cycle

[87]

T492

CDK1

Degradation

Lung cancer cell migration and invasion

[88]

Y646

JAK2

Degradation

Lymphoma pathogenesis

[89]

KMT6B

EZH1

Ser560(Mouse)

Unknown

Degradation

Adaptive stress response pathway

[75]

PRMT1

 

Tyr291

Unknown

Inhibition of enzymatic activity

Mitosis; Tumorigenicity; Radiation response of glioblastoma stem cells

[79]

Ser297

Unknown

Activation of enzymatic activity

Inflammation

[78]

PRMT6

 

Ser11

CK2

Stabilization

Mitosis; Tumorigenicity; Radiation response of glioblastoma stem cells

[79]

Thr21

KDM2A

CXXC8

FBL7

FBXL11

JHDM1A

KIAA1004

Thr632

ATM

Disruption of its binding to chromatin

DNA damage repair

[90]

KDM2B

CXXC2

FBL10

FBLX10

JHDM1B

PCCX2

Ser265

PKA

Chromatin remodeling

Cell cycle

[91]

KDM4B

JMJD2B

JHDM3B

Ser666

PKA

Enhance of its binding to SF3B3

Androgen deprivation

[92]

Thr305

ERK

Stabilization

Colon cancer

[93]

Ser352

Ser566

Thr1065

KDM4C

JMJD2C

JHDM3C

Ser918

PKR

Degradation

Glioblastoma Tumorigenesis; Wnt/β-catenin signaling

[94]

KDM5B

JARID1B

Ser1456

CDK1

Disruption of its binding to chromatin

Triple negative breast cancer

[95]