Proteins > DNA (cytosine-5)-methyltransferase 1
Page last updated: 2024-08-07 18:32:55
DNA (cytosine-5)-methyltransferase 1
A DNA (cytosine-5)-methyltransferase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P26358]
Synonyms
Dnmt1;
EC 2.1.1.37;
CXXC-type zinc finger protein 9;
DNA methyltransferase HsaI;
DNA MTase HsaI;
M.HsaI;
MCMT
Research
Bioassay Publications (25)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 4 (16.00) | 29.6817 |
2010's | 17 (68.00) | 24.3611 |
2020's | 4 (16.00) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
sgi-1027 | Homo sapiens (human) | EC50 | 10.2000 | 1 | 1 |
Drugs with Other Measurements
Synthesis of NSC 106084 and NSC 14778 and evaluation of their DNMT inhibitory activity.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 29, Issue:6, 2019
Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Synthesis and Characterization of Transition-State Analogue Inhibitors against Human DNA Methyltransferase 1.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Synthesis of NSC 106084 and NSC 14778 and evaluation of their DNMT inhibitory activity.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 29, Issue:6, 2019
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
Development of rationally designed DNA N6 adenine methyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.Bioorganic & medicinal chemistry, , 09-01, Volume: 45, 2021
Targeting DNA methylation with small molecules: what's next?Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan (RG108) as inhibitors of DNA methyltransferase 1.Journal of medicinal chemistry, , Jan-23, Volume: 57, Issue:2, 2014
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Targeting DNA methylation with small molecules: what's next?Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Design and synthesis of new non nucleoside inhibitors of DNMT3A.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1.The Journal of biological chemistry, , Aug-16, Volume: 288, Issue:33, 2013
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Enables
This protein enables 8 target(s):
Target | Category | Definition |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
DNA (cytosine-5-)-methyltransferase activity | molecular function | Catalysis of the reaction: S-adenosyl-L-methionine + DNA containing cytosine = S-adenosyl-L-homocysteine + DNA containing 5-methylcytosine. [EC:2.1.1.37] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
methyl-CpG binding | molecular function | Binding to a methylated cytosine/guanine dinucleotide. [GOC:jl, PMID:11746232] |
DNA-methyltransferase activity | molecular function | Catalysis of the transfer of a methyl group to a DNA molecule. [GOC:jl, ISBN:0198506732, PMID:7862522] |
promoter-specific chromatin binding | molecular function | Binding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
female germ cell nucleus | cellular component | The nucleus of the female germ cell, a reproductive cell in females. [CL:0000021, GOC:hjd] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
replication fork | cellular component | The Y-shaped region of a replicating DNA molecule, resulting from the separation of the DNA strands and in which the synthesis of new strands takes place. Also includes associated protein complexes. [GOC:mah, ISBN:0198547684] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
pericentric heterochromatin | cellular component | Heterochromatin that is located adjacent to the CENP-A rich centromere 'central core' and characterized by methylated H3 histone at lysine 9 (H3K9me2/H3K9me3). [PMID:12019236, PMID:20206496, PMID:21437270, PMID:22729156, PMID:9413993] |
Involved In
This protein is involved in 14 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
DNA methylation-dependent heterochromatin formation | biological process | Repression of transcription by methylation of DNA, leading to the formation of heterochromatin. [GOC:mah] |
DNA-templated transcription | biological process | The synthesis of an RNA transcript from a DNA template. [GOC:jl, GOC:txnOH] |
positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
methylation | biological process | The process in which a methyl group is covalently attached to a molecule. [GOC:mah] |
epigenetic programming of gene expression | biological process | A epigenetic process that happens during embryonic development that modulates gene expression potential at later stages of development of the organism, including the adult. Epigenetic regulation takes place via chromatin remodeling either by modifying higher order chromatin fiber structure, nucleosomal histones, or cytosine DNA methylation. [GOC:go_curators, PMID:12138111, PMID:22868271] |
negative regulation of gene expression via chromosomal CpG island methylation | biological process | An epigenetic gene regulation mechanism that negatively regulates gene expression by methylation of cytosine residues in chromosomal CpG islands. CpG islands are genomic regions that contain a high frequency of the CG dinucleotide associated with the transcription start site of genes. [PMID:11898023, Wikipedia:Cpg_island] |
cellular response to amino acid stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amino acid stimulus. An amino acid is a carboxylic acids containing one or more amino groups. [GOC:mah] |
chromosomal DNA methylation maintenance following DNA replication | biological process | The process that maintains methylated cytosine in newly synthesized DNA following DNA replication. After the establishment of novel DNA methylation marks, the newly created patterns must be faithfully transmitted by maintenance DNA methyltransferases during cell division. [PMID:11005794, PMID:20142834, PMID:26077819, PMID:34968368] |
cellular response to bisphenol A | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a bisphenol A stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:22957036] |
positive regulation of vascular associated smooth muscle cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467] |
negative regulation of vascular associated smooth muscle cell apoptotic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular associated smooth muscle cell apoptotic process. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:26493107] |
negative regulation of vascular associated smooth muscle cell differentiation involved in phenotypic switching | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular smooth muscle cell differentiation involved in phenotypic switching. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:25089138] |