Target type: cellularcomponent
A phosphatidylinositol 3-kinase complex that contains a catalytic class III phosphoinositide 3-kinase (PI3K) subunit bound to a regulatory (adaptor) subunit. Additional adaptor proteins may be present. Class III PI3Ks have a substrate specificity restricted to phosphatidylinositol (PI). [GOC:bf, PMID:9255069]
The class III phosphatidylinositol 3-kinase (PI3K) complex is a multi-protein complex involved in various cellular processes, including autophagy, vesicular trafficking, and organelle biogenesis. Its cellular component is characterized by a unique set of proteins that contribute to its specific functions.
The core of the class III PI3K complex consists of the following proteins:
* **Vps34:** This is the catalytic subunit, responsible for the phosphorylation of phosphatidylinositol (PtdIns) to phosphatidylinositol-3-phosphate (PtdIns(3)P). It is a lipid kinase that is crucial for the formation of PtdIns(3)P, a key signaling molecule involved in autophagy and vesicular trafficking.
* **Vps15:** This protein acts as a regulatory subunit and is essential for the stability and activity of the complex. It interacts with Vps34 and contributes to the recruitment of other proteins to the complex.
* **Beclin 1:** This protein is a crucial autophagy regulator that interacts with Vps34 and Vps15. It plays a pivotal role in the initiation and progression of autophagy, a cellular process for degrading and recycling damaged or unnecessary cellular components.
In addition to these core components, the class III PI3K complex can also include a number of accessory proteins, depending on the specific cellular context and function. These accessory proteins can modulate the activity and localization of the complex, contributing to its diverse roles in various cellular processes.
Some of the common accessory proteins found in the class III PI3K complex include:
* **UVRAG:** This protein enhances the activity of the complex and promotes autophagy.
* **Atg14:** This protein is essential for the recruitment of the complex to the phagophore, a double-membrane structure that encapsulates cargo during autophagy.
* **Rubicon:** This protein acts as a negative regulator of autophagy, inhibiting the activity of the complex.
The specific composition and localization of the class III PI3K complex vary depending on the cellular context. These variations reflect the diverse functions of the complex in regulating various cellular processes, including autophagy, vesicular trafficking, and organelle biogenesis. The cellular localization and composition of the complex are dynamically regulated, allowing it to respond to various cellular signals and adapt its activity to specific cellular needs.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Phosphatidylinositol 3-kinase catalytic subunit type 3 | A phosphatidylinositol 3-kinase catalytic subunit type 3 that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| ML162 | ML162 : A monochlorobenzene that is benzene substituted by (chloroacetyl){2-oxo-2-[(2-phenylethyl)amino]-1-(thiophen-2-yl)ethyl}amino, chloro and methoxy groups at positions 1, 3 and 4, respectively. It is a covalent inhibitor of glutathione peroxidase 4 (GPX4) that induces ferroptosis in cells. | monochlorobenzenes; monomethoxybenzene; organochlorine compound; secondary carboxamide; tertiary carboxamide; thiophenes | EC 1.11.1.9 (glutathione peroxidase) inhibitor; ferroptosis inducer |
| PI3-Kinase alpha Inhibitor 2 | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
| idelalisib | idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia. idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source | aromatic amine; organofluorine compound; purines; quinazolines; secondary amino compound | antineoplastic agent; apoptosis inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| zstk474 | ZSTK-474 : A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase. | benzimidazoles; morpholines; organofluorine compound; triamino-1,3,5-triazine | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| dactolisib | dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
| ku 60019 | |||
| buparlisib | NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source | aminopyridine; aminopyrimidine; morpholines; organofluorine compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| gdc 0941 | pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | indazoles; morpholines; piperazines; sulfonamide; thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| gdc 0980 | |||
| azd2014 | vistusertib: potent and selective dual mTORC1 and mTORC2 inhibitor; structure in first source | ||
| pki 587 | gedatolisib: inhibits both phosphatidylinositol 3-kinase and mTOR; structure in first source | ||
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | sapanisertib: an mTOR inhibitor | benzoxazole | |
| ch 5132799 | CH 5132799: structure in first source | ||
| 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 |
| gdc-0032 | |||
| spautin-1 | |||
| 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 |
| cudc-907 | |||
| sar245408 | |||
| byl719 | proline derivative | ||
| amg 511 | AMG 511: structure in first source | ||
| cc-223 | |||
| sar405 | SAR405: a Vps34 inhibitor with antineoplastic activity; structure in first source |