Chromatin proteins and modifications as drug targets

TY - JOUR

T1 - Chromatin proteins and modifications as drug targets

AU - Helin, Kristian

AU - Dhanak, Dashyant

PY - 2013/10/24

Y1 - 2013/10/24

N2 - A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.

AB - A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.

KW - Animals

KW - Chromatin

KW - Histone Demethylases

KW - Histone-Lysine N-Methyltransferase

KW - Humans

KW - Molecular Targeted Therapy

KW - Neoplasms

KW - Protein Structure, Tertiary

U2 - 10.1038/nature12751

DO - 10.1038/nature12751

M3 - Review

C2 - 24153301

SN - 0028-0836

VL - 502

SP - 480

EP - 488

JO - Nature

JF - Nature

IS - 7472

ER -