phosphatidylinositol-3,5-bisphosphate binding
Definition
Target type: molecularfunction
Binding to phosphatidylinositol-3,5-bisphosphate, a derivative of phosphatidylinositol in which the inositol ring is phosphorylated at the 3' and 5' positions. [GOC:bf, PMID:18397324]
Phosphatidylinositol-3,5-bisphosphate (PtdIns(3,5)P2) binding is a crucial molecular function that plays a significant role in various cellular processes. PtdIns(3,5)P2 is a rare but highly regulated phosphoinositide that acts as a signaling molecule and a membrane-associated scaffold. Its binding to specific proteins orchestrates a diverse array of cellular events, including:
1. **Regulation of membrane trafficking:** PtdIns(3,5)P2 is primarily localized to the endosomal compartments, where it participates in the regulation of vesicle formation, transport, and fusion. It interacts with proteins like Rab5, sorting nexins (SNXs), and EEA1, which are critical for endosome maturation and fusion.
2. **Control of ion channel activity:** PtdIns(3,5)P2 is involved in modulating the activity of specific ion channels, such as TRPML1, a cation channel located on the lysosomal membrane. This interaction contributes to the regulation of lysosomal ion homeostasis.
3. **Signal transduction:** PtdIns(3,5)P2 acts as a second messenger in several signaling pathways, including those activated by growth factors and stress stimuli. It interacts with signaling proteins like AKT and mTOR, regulating their downstream activities.
4. **Regulation of autophagy:** PtdIns(3,5)P2 plays a crucial role in the autophagic process, which involves the degradation of cellular components. It interacts with proteins like ATG18, a key regulator of autophagy, facilitating autophagosome formation and maturation.
5. **Regulation of cytoskeletal organization:** PtdIns(3,5)P2 is implicated in regulating the organization and dynamics of the actin cytoskeleton, influencing cellular morphology and migration.
6. **Cell growth and differentiation:** PtdIns(3,5)P2 contributes to cell growth and differentiation processes, regulating cell division and fate determination.
These diverse functions highlight the importance of PtdIns(3,5)P2 binding in maintaining cellular homeostasis and orchestrating various cellular processes.'
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Proteins (1)
| Protein | Definition | Taxonomy |
|---|---|---|
| Target of rapamycin complex 2 subunit MAPKAP1 | A target of rapamycin complex 2 subunit MAPKAP1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9BPZ7] | Homo sapiens (human) |
Compounds (10)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| pi103 | PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce | aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
| ku 0063794 | Ku 0063794: an mTOR inhibitor; structure in first source | benzyl alcohols; monomethoxybenzene; morpholines; pyridopyrimidine; tertiary amino compound | antineoplastic agent; mTOR inhibitor |
| gsk 2126458 | omipalisib : A member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors. omipalisib: inhibitor of mTOR protein | aromatic ether; difluorobenzene; pyridazines; pyridines; quinolines; sulfonamide | anticoronaviral agent; antineoplastic agent; autophagy inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor; radiosensitizing agent |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol: a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity; structure in first source | benzyl alcohols; morpholines; pyridopyrimidine; tertiary amino compound | antineoplastic agent; apoptosis inducer; mTOR inhibitor |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | WYE-354: an mTOR inhibitor; structure in first source | carbamate ester | |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | sapanisertib: an mTOR inhibitor | benzoxazole | |
| torin 1 | torin 1 : A member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | N-acylpiperazine; N-arylpiperazine; organofluorine compound; pyridoquinoline; quinolines | antineoplastic agent; mTOR inhibitor |
| torin 2 | torin 2 : A member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | aminopyridine; organofluorine compound; primary amino compound; pyridoquinoline | antineoplastic agent; mTOR inhibitor |
| cc214-2 | CC214-2: an mTOR kinase inhibitor; structure in first source | ||
| pp242 | torkinib : A member of the class of pyrazolopyrimidines that is 1H-pyrazolo[3,4-d]pyrimidine substituted by isopropyl, 5-hydroxyindol-2-yl and amino groups at positions 1, 3 and 4 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | aromatic amine; biaryl; hydroxyindoles; phenols; primary amino compound; pyrazolopyrimidine | antineoplastic agent; mTOR inhibitor |