Page last updated: 2024-10-24

MLL1/2 complex

Definition

Target type: cellularcomponent

A protein complex that can methylate lysine-4 of histone H3, and which contains either of the protein subunits MLL1 or MLL2 in human, or equivalent in other species. [GOC:sart, PMID:21875999]

The MLL1/2 complex is a multi-protein complex that plays a crucial role in regulating gene expression and development. Its cellular component is comprised of various proteins that assemble into a dynamic structure, contributing to its diverse functions. The core components of the MLL1/2 complex include:

1. **MLL1/2:** The catalytic subunit, a histone methyltransferase responsible for trimethylating histone H3 at lysine 4 (H3K4me3). This modification is associated with active transcription.

2. **MEN1:** A tumor suppressor protein that interacts with MLL1/2 and contributes to the complex's stability.

3. **WDR5:** A WD40 repeat protein that binds to the MLL1/2 catalytic domain and is crucial for the complex's enzymatic activity.

4. **RBBP5:** A retinoblastoma binding protein that interacts with the MLL1/2 complex and contributes to its recruitment to specific genomic regions.

5. **ASH2L:** A protein that associates with MLL1/2 and is important for the complex's stability and activity.

6. **Dpy-30:** A protein that interacts with ASH2L and is involved in the complex's assembly and localization.

7. **PAF1 complex:** This complex, consisting of PAF1, Cdc73, LEO1, and CTR9, interacts with MLL1/2 and contributes to the recruitment of the complex to transcribed genes.

8. **Other proteins:** The MLL1/2 complex also interacts with other proteins, including transcription factors, coactivators, and chromatin remodeling factors, depending on the specific context and cellular process involved.

The MLL1/2 complex is localized primarily in the nucleus and associates with chromatin, playing a key role in gene regulation. Its cellular component is dynamic, with different protein interactions and modifications occurring in response to various cellular signals and developmental stages. The assembly and disassembly of the complex are regulated by various mechanisms, contributing to the specificity of its function in different cellular contexts.'
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Proteins (6)

ProteinDefinitionTaxonomy
Histone-lysine N-methyltransferase 2BA histone-lysine N-methyltransferase 2B that is encoded in the genome of human. [PRO:DNx]Homo sapiens (human)
Set1/Ash2 histone methyltransferase complex subunit ASH2A Set1/Ash2 histone methyltransferase complex subunit ASH2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBL3]Homo sapiens (human)
Protein dpy-30 homologA protein dpy-30 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9C005]Homo sapiens (human)
Retinoblastoma-binding protein 5A retinoblastoma-binding protein 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15291]Homo sapiens (human)
WD repeat-containing protein 5A WD repeat-containing protein 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P61964]Homo sapiens (human)
MeninA menin that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00255]Homo sapiens (human)

Compounds (10)

CompoundDefinitionClassesRoles
lansoprazoleLansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.benzimidazoles;
pyridines;
sulfoxide
anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
loperamideloperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.

Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
omeprazole5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.

omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.

Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.
aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
rabeprazoleRabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.benzimidazoles;
pyridines;
sulfoxide
anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
framycetinframycetin : A tetracyclic antibacterial agent derived from neomycin, being a glycoside ester of neamine and neobiosamine B.

Framycetin: A component of NEOMYCIN that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed)
aminoglycosideallergen;
antibacterial drug;
Escherichia coli metabolite
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
dexlansoprazoleDexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE.benzimidazoles;
sulfoxide
4-[4-(5,5-dimethyl-4H-thiazol-2-yl)-1-piperazinyl]-6-propylthieno[2,3-d]pyrimidineN-arylpiperazine;
thienopyrimidine
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
oicr-9429OICR-9429: antineoplastic; structure in first source