Page last updated: 2024-10-24

RNA polymerase II complex binding

Definition

Target type: molecularfunction

Binding to an RNA polymerase II core enzyme, a multisubunit eukaryotic nuclear RNA polymerase typically composed of twelve subunits. [GOC:txnOH]

RNA polymerase II (RNAP II) complex binding is a fundamental molecular process that underpins gene expression in eukaryotic organisms. It involves the intricate interaction between RNAP II, a multi-subunit enzyme responsible for transcribing DNA into messenger RNA (mRNA), and a diverse array of proteins and regulatory elements. This binding event is crucial for initiating and regulating the transcription process.

The RNAP II complex itself comprises a core set of subunits essential for catalytic activity, including two large subunits (RPB1 and RPB2) that harbor the active site for RNA synthesis. The complex also incorporates smaller subunits that play crucial roles in DNA unwinding, template engagement, and transcript elongation.

Upon binding to DNA, RNAP II interacts with a variety of transcription factors (TFs). These TFs bind to specific DNA sequences upstream of the gene, known as promoters, and serve as molecular switches that recruit and activate RNAP II. Key TFs include general transcription factors (GTFs), which are required for basal transcription, and specific transcription factors that regulate gene expression in response to cellular signals and environmental cues.

The interaction of RNAP II with DNA and TFs initiates a complex series of events that ultimately lead to mRNA synthesis. The RNAP II complex, guided by TFs, unwinds the DNA double helix, exposing the template strand. The enzyme then proceeds to synthesize a complementary RNA molecule using the template strand as a blueprint. This process involves the sequential addition of ribonucleotides to the growing RNA chain, guided by the base-pairing rules between DNA and RNA.

During transcription elongation, RNAP II interacts with various regulatory proteins that influence the efficiency and fidelity of mRNA synthesis. These proteins can modify the enzyme's activity, alter its association with DNA, or affect its interaction with other factors.

In summary, the molecular function of RNA polymerase II complex binding is a complex and tightly regulated process involving the interaction of multiple proteins, DNA, and regulatory elements. This binding event is essential for initiating and regulating gene expression, thereby playing a central role in cellular function, development, and response to environmental cues.'
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Proteins (5)

ProteinDefinitionTaxonomy
Protein argonaute-2A protein argonaute-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UKV8]Homo sapiens (human)
N-lysine methyltransferase SMYD2An N-lysine methyltransferase SMYD2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NRG4]Homo sapiens (human)
Histone-lysine N-methyltransferase SMYD3A histone-lysine N-methyltransferase SMYD3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7B4]Homo sapiens (human)
DNA repair protein complementing XP-G cellsA DNA excision repair protein ERCC-5 that is encoded in the genome of human. [PRO:DNx]Homo sapiens (human)
Steroid hormone receptor ERR2A steroid hormone receptor ERR2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O95718]Homo sapiens (human)

Compounds (14)

CompoundDefinitionClassesRoles
sulfaguanidinesulfaguanidine : A sulfonamide incorporating a guanidine moiety used to block the synthesis of folic acid; mostly used in veterinary medicine

Sulfaguanidine: A sulfanilamide antimicrobial agent that is used to treat enteric infections.
sulfonamide antibioticantiinfective agent
sulfanilamidesubstituted aniline;
sulfonamide;
sulfonamide antibiotic
antibacterial agent;
drug allergen;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
sulfisomidinesulfisomidine : A sulfonamide consisting of pyrimidine having methyl substituents at the 2- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position.

Sulfisomidine: A sulfanilamide antibacterial agent.
pyrimidines;
sulfonamide;
sulfonamide antibiotic
antiinfective agent
uridine monophosphateuridine 5'-monophosphate : A pyrimidine ribonucleoside 5'-monophosphate having uracil as the nucleobase.

Uridine Monophosphate: 5'-Uridylic acid. A uracil nucleotide containing one phosphate group esterified to the sugar moiety in the 2', 3' or 5' position.
pyrimidine ribonucleoside 5'-monophosphate;
uridine 5'-phosphate
Escherichia coli metabolite;
human metabolite;
mouse metabolite
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenolstilbenoid
3-hydroxy-quinazoline-2,4-dione3-hydroxy-quinazoline-2,4-dione: structure in first source
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
4-phenyl-4-oxo-2-hydroxybuten-2-oic acid2,4-dioxo-4-phenylbutanoic acid: structure in first source
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
scutellareinscutellarein : Flavone substituted with hydroxy groups at C-4', -5, -6 and -7.

scutellarein: aglycone of scutellarin from Scutellaria baicalensis; carthamidin is 2S isomer of scutellarein; do not confuse with isoscutellarein and/or isocarthamidin which are respective regioisomers, or with the scutelarin protein
tetrahydroxyflavonemetabolite
gsk5182GSK5182: an estrogen-related receptor gamma inverse agonist
az 505AZ 505: an SMYD2 inhibitor; structure in first source
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
lly-507LLY-507 : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl}[biphenyl]-3-carboxylic acid with the amino group of 3-(pyrrolidin-1-yl)propan-1-amine. It is a potent and selective inhibitor of SMYD2 and inhibits the ability of SMYD2 to methylate p53. It serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.

LLY-507: inhibits methyltransferase SMYD2; structure in first source