TY - JOUR

T1 - Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases

AU - Bulygin, Anatoliy A

AU - Davletgildeeva, Anastasiia T

AU - Kuznetsov, Nikita A

N1 - Bulygin, A.A.; Davletgildeeva, A.T.; Kuznetsov, N.A. Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases. Int. J. Mol. Sci. 2026, 27, 4560. https://doi.org/10.3390/ijms27104560 This work was supported by Russian Ministry of Science and Higher Education project No. 125012300658-9.

PY - 2026/5/19

Y1 - 2026/5/19

N2 - DNA methylation is one of the most important epigenetic mechanisms regulating gene expression. DNA methyltransferases (DNMTs) are key players in these processes, regulating dynamic DNA methylation patterns in embryonic and adult cells. Therefore, dysfunction of DNMTs can lead to serious diseases and cancer due to distortions in gene methylation, including that of tumor suppressor genes. Due to the reversibility of DNA methylation, DNMTs are considered an important epigenetic target for drug development. This narrative review summarizes knowledge about DNMTs, including structural features and biological functions, and describes the development of DNMT inhibitors as therapeutics, from the earliest developments to the most modern and promising ones.

AB - DNA methylation is one of the most important epigenetic mechanisms regulating gene expression. DNA methyltransferases (DNMTs) are key players in these processes, regulating dynamic DNA methylation patterns in embryonic and adult cells. Therefore, dysfunction of DNMTs can lead to serious diseases and cancer due to distortions in gene methylation, including that of tumor suppressor genes. Due to the reversibility of DNA methylation, DNMTs are considered an important epigenetic target for drug development. This narrative review summarizes knowledge about DNMTs, including structural features and biological functions, and describes the development of DNMT inhibitors as therapeutics, from the earliest developments to the most modern and promising ones.

KW - Humans

KW - Enzyme Inhibitors/pharmacology

KW - DNA Methylation/drug effects

KW - DNA (Cytosine-5-)-Methyltransferases/antagonists & inhibitors

KW - Epigenesis, Genetic/drug effects

KW - Animals

KW - Neoplasms/drug therapy

KW - ДНК-метилтрансферазы

KW - метилирование ДНК

KW - ингибиторы

KW - дизайн лекарственных средств

KW - CpG-динуклеотиды

UR - https://www.scopus.com/pages/publications/105040255091

U2 - 10.3390/ijms27104560

DO - 10.3390/ijms27104560

M3 - Review article

C2 - 42196535

VL - 27

JO - International Journal of Molecular Sciences

JF - International Journal of Molecular Sciences

SN - 1661-6596

IS - 10

M1 - 4560

ER -