Page last updated: 2024-10-24
MLL1 complex
Definition
Target type: cellularcomponent
A protein complex that can methylate lysine-4 of histone H3. MLL1/MLL is the catalytic methyltransferase subunit, and the complex also contains the core components ASH2L, HCFC1/HCF1 WDR5 and RBBP5. [GOC:sp, PMID:15960975]
The MLL1 complex is a multi-protein complex that plays a critical role in regulating gene expression during development. It is a large and dynamic complex, with different subunits associating and dissociating depending on the cellular context. The core components of the MLL1 complex include:
- **MLL1:** The catalytic subunit of the complex, responsible for histone H3 lysine 4 (H3K4) methylation. MLL1 is a large protein with multiple domains, including a SET domain that is required for its enzymatic activity.
- **WDR5, RbBP5, Ash2L, and DPY30:** These four proteins form a stable subcomplex that interacts with MLL1 and is essential for its activity. They help recruit MLL1 to specific target genes and enhance its catalytic activity.
- **Menin:** A protein that interacts with MLL1 and is required for its stability and activity. Menin is a tumor suppressor and mutations in the MEN1 gene, which encodes menin, are associated with multiple endocrine neoplasia type 1 (MEN1) syndrome.
- **LEDGF/p75:** A protein that interacts with MLL1 and is thought to play a role in targeting the complex to specific genomic regions. LEDGF/p75 is also a target for HIV-1 integration, and its interaction with MLL1 may contribute to the integration of the viral genome into the host cell's DNA.
- **Other associated proteins:** In addition to the core components, the MLL1 complex can also associate with a variety of other proteins, including transcription factors, chromatin remodeling enzymes, and histone chaperones. These additional proteins contribute to the diverse roles of the MLL1 complex in regulating gene expression.
The cellular component of the MLL1 complex is primarily located in the **nucleus**, where it interacts with chromatin and regulates gene expression. The complex is found associated with specific genomic regions, including promoters, enhancers, and transcribed regions. The MLL1 complex is highly dynamic and its composition can vary depending on the cellular context and the specific genes being regulated. Disruptions in the function of the MLL1 complex can lead to developmental abnormalities and cancer.
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Proteins (11)
| Protein | Definition | Taxonomy |
|---|---|---|
| RuvB-like 1 | A RuvB-like 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y265] | Homo sapiens (human) |
| RuvB-like 2 | A RuvB-like 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y230] | Homo sapiens (human) |
| Set1/Ash2 histone methyltransferase complex subunit ASH2 | A Set1/Ash2 histone methyltransferase complex subunit ASH2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBL3] | Homo sapiens (human) |
| Histone acetyltransferase KAT8 | A histone acetyltransferase KAT8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7Z6] | Homo sapiens (human) |
| Protein dpy-30 homolog | A protein dpy-30 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9C005] | Homo sapiens (human) |
| Retinoblastoma-binding protein 5 | A retinoblastoma-binding protein 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15291] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase 2A | A histone-lysine N-methyltransferase 2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q03164] | Homo sapiens (human) |
| WD repeat-containing protein 5 | A WD repeat-containing protein 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P61964] | Homo sapiens (human) |
| Protein max | A protein max that is encoded in the genome of human. [PRO:CNA] | Homo sapiens (human) |
| Transcription initiation factor TFIID subunit 1 | A transcription initiation factor TFIID subunit 1 that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
| Menin | A menin that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00255] | Homo sapiens (human) |
Compounds (31)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 4-aminophenol | 4-aminophenol : An amino phenol (one of the three possible isomers) which has the single amino substituent located para to the phenolic -OH group. 4-aminophenol: RN given refers to parent cpd | aminophenol | allergen; metabolite |
| lansoprazole | Lansoprazole: 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 |
| loperamide | loperamide : 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 |
| omeprazole | 5-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 | |
| rabeprazole | Rabeprazole: 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 |
| 1-nitronaphthalene | 1-nitronaphthalene : A mononitronaphthalene substituted by a nitro group at position 1. 1-nitronaphthalene: RN given refers to cpd with locant for nitro moiety in 1 position mononitronaphthalene : A nitronaphthalene carrying a single nitro group at unspecified position. nitronaphthalene : A nitroarene that is naphthalene substituted by at least one nitro group. | mononitronaphthalene | environmental contaminant; mouse metabolite |
| phenylhydrazine | phenylhydrazines | xenobiotic | |
| 4-chloroaniline | 4-chloroaniline : A chloroaniline in which the chloro atom is para to the aniline amino group. 4-chloroaniline: RN given refers to parent cpd; structure | chloroaniline; monochlorobenzenes | |
| framycetin | framycetin : 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) | aminoglycoside | allergen; antibacterial drug; Escherichia coli metabolite |
| 1-naphthylamine | 1-naphthylamine : A naphthylamine that is naphthalene substituted by an amino group at position 1. 1-Naphthylamine: A suspected industrial carcinogen (and listed as such by OSHA). Its N-hydroxy metabolite is strongly carcinogenic and mutagenic. naphthylamine : A primary arylamine that is naphthalene substituted by an amino group at unspecified position. | naphthylamine | human xenobiotic metabolite |
| 4-fluoroaniline | 4-fluoroaniline : A primary arylamine that is the derivative of aniline in which the hydrogen at position 4 has been substituted by fluorine. It is used as an intermediate in the manufacture of pharmaceuticals, herbicides and plant growth regulators. 4-fluoroaniline: chemical intermediate manufactured by the Halex process; RN given refers to parent cpd; structure given in first source | fluoroaniline; primary arylamine | |
| phenylhydrazine hydrochloride | phenylhydrazine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of phenylhydrazine and hydrogen chloride. | hydrochloride | |
| 4-fluorobenzylamine | |||
| 4-hydroxyquinoline | 4-quinolone : A quinolone that is 1,4-dihydroquinoline substituted by an oxo group at position 4. | monohydroxyquinoline; quinolone | |
| anacardic acid | anacardic acid : A hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities. anacardic acid: isolated from Anacardium occidentale; monophenol monooxygenase inhibitor | hydroxy monocarboxylic acid; hydroxybenzoic acid | anti-inflammatory agent; antibacterial agent; anticoronaviral agent; apoptosis inducer; EC 2.3.1.48 (histone acetyltransferase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; neuroprotective agent; plant metabolite |
| sorafenib | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor | |
| s-adenosylhomocysteine | S-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 |
| 10074-g5 | 10074-G5: structure in first source | ||
| scutellarein | scutellarein : 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 | tetrahydroxyflavone | metabolite |
| rottlerin | rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis. rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1); | aromatic ketone; benzenetriol; chromenol; enone; methyl ketone | anti-allergic agent; antihypertensive agent; antineoplastic agent; apoptosis inducer; K-ATP channel agonist; metabolite |
| dexlansoprazole | Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | benzimidazoles; sulfoxide | |
| 2-hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trien-1-yl]benzoic acid | hydroxybenzoic acid | ||
| bi 2536 | |||
| (3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine | indoles | ||
| i-bet726 | |||
| 4-[4-(5,5-dimethyl-4H-thiazol-2-yl)-1-piperazinyl]-6-propylthieno[2,3-d]pyrimidine | N-arylpiperazine; thienopyrimidine | ||
| gsk343 | GSK343 : 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-amine | 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source | ||
| kj-pyr-9 | KJ-Pyr-9: antineoplastic; structure in first source | ||
| oicr-9429 | OICR-9429: antineoplastic; structure in first source | ||
| akt-i-1,2 compound | Akt-I-1,2 compound: an aminopeptidase P inhibitor; structure in first source |