Page last updated: 2024-10-24

regulation of transcription regulatory region DNA binding

Definition

Target type: biologicalprocess

Any process that modulates the frequency, rate or extent of transcription regulatory region DNA binding. [GOC:obol]

Regulation of transcription regulatory region DNA binding is a multifaceted process that governs the expression of genes. It involves a complex interplay of proteins and other molecules that bind to specific DNA sequences called regulatory elements. These elements can be located upstream, downstream, or even within the gene they regulate.

Transcription factors (TFs) play a pivotal role in this process. TFs are proteins that can bind to specific DNA sequences in regulatory elements. They act as molecular switches, either activating or repressing gene expression. Binding of a TF to a regulatory element can influence the recruitment of RNA polymerase, the enzyme responsible for transcribing DNA into RNA.

The process begins with the recognition of a specific DNA sequence by a TF. This interaction is typically highly specific, determined by the shape and chemical properties of the TF and the DNA sequence. Once bound, the TF can influence transcription in several ways:

- **Recruitment of other proteins**: TFs can act as scaffolding proteins, recruiting other proteins to the regulatory element. These proteins may include co-activators, which enhance the activity of RNA polymerase, or co-repressors, which inhibit its activity.
- **Alteration of chromatin structure**: Chromatin, the complex of DNA and proteins that makes up chromosomes, can be remodeled to make DNA more or less accessible to TFs. TFs can recruit enzymes that modify histone proteins, the core components of chromatin, leading to changes in chromatin structure and gene expression.
- **Direct interaction with RNA polymerase**: Some TFs directly interact with RNA polymerase, influencing its activity.
- **Competition with other TFs**: Multiple TFs can bind to the same regulatory element, leading to competition for binding sites. This competition can influence the overall transcriptional output.

The regulation of transcription regulatory region DNA binding is a dynamic process that is influenced by a wide range of factors, including:

- **Signaling pathways**: Extracellular signals can trigger intracellular pathways that activate or repress TFs.
- **Developmental stage**: The expression of specific TFs can vary depending on the developmental stage of an organism.
- **Environmental factors**: Environmental factors, such as temperature or nutrient availability, can influence the activity of TFs.
- **Genetic factors**: Genetic variations can affect the binding affinity of TFs to their target sequences.

The regulation of transcription regulatory region DNA binding is essential for proper gene expression and cellular function. Dysregulation of this process can lead to various diseases, including cancer, developmental disorders, and metabolic diseases. Therefore, understanding the molecular mechanisms underlying this process is crucial for developing new therapeutic strategies.'
"

Proteins (1)

ProteinDefinitionTaxonomy
Histone-lysine N-methyltransferase, H3 lysine-79 specificA histone-lysine N-methyltransferase, H3 lysine-79 specific that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8TEK3]Homo sapiens (human)

Compounds (11)

CompoundDefinitionClassesRoles
toyocamycintoyocamycin : An N-glycosylpyrrolopyrimidine that is tubercidin in which the hydrogen at position 5 of the pyrrolopyrimidine moiety has been replaced by a cyano group.

Toyocamycin: 4-Amino-5-cyano-7-(D-ribofuranosyl)-7H- pyrrolo(2,3-d)pyrimidine. Antibiotic antimetabolite isolated from Streptomyces toyocaensis cultures. It is an analog of adenosine, blocks RNA synthesis and ribosome function, and is used mainly as a tool in biochemistry.
antibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
nitrile;
ribonucleoside
antimetabolite;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite
nsc 65346sangivamycin : A nucleoside analogue that is adenosine in which the nitrogen at position 7 is replaced by a carbamoyl-substituted carbon. It is a potent inhibitor of protein kinase C.

sangivamycin: RN given refers to parent cpd
nucleoside analogueprotein kinase inhibitor
adenosinequinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlitadenosines;
purines D-ribonucleoside
analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
sinefunginadenosines;
non-proteinogenic alpha-amino acid
antifungal agent;
antimicrobial agent
5-iodotubercidin7-iodotubercidin: inhibits Toxoplasma gondii adenosine kinaseorganoiodine compound
s-adenosyl-3-thiopropylamineS-adenosyl-3-thiopropylamine : A thioadenosine that is adenosine in which the hydroxy group at C-5' is replaced by a 3-aminopropyl group.

S-adenosyl-3-thiopropylamine: decarboxylated S-adenosylhomocysteine; RN given refers to parent cpd
organic sulfide;
primary amino compound;
thioadenosine
s-adenosylhomocysteineS-adenosyl-L-homocysteine : An organic sulfide that is the S-adenosyl derivative of L-homocysteine.

S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.
adenosines;
amino acid zwitterion;
homocysteine derivative;
homocysteines;
organic sulfide
cofactor;
EC 2.1.1.72 [site-specific DNA-methyltransferase (adenine-specific)] inhibitor;
EC 2.1.1.79 (cyclopropane-fatty-acyl-phospholipid synthase) inhibitor;
epitope;
fundamental metabolite
epz004777N-glycosyl compound
epz-56765'-deoxyribonucleoside
gsk343GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM).

GSK343: an EZH2 methyltransferase inhibitor
aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source