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FKBP12-rapamycin complex-associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1; rapamycin target protein; RAPT1; mammalian target of rapamycin; mTOR (FRAP1, FRAP, FRAP2)

Function: - role in cell cycle progression - interacts with the FKBP12-rapamycin complex - acts as the target for the cell-cycle arrest & immunosuppressive effects of the FKBP12-rapamycin complex - rapamycin inhibits mTOR pathway - component of the TORC1 complex - component of the TORC2 complex - role in actin cytoskeleton organization - binds directly to PRR5 & RICTOR within the TORC2 complex - forms complex with raptor - binds UBQLN1 - upstream regulator of HIF-1 in cancer cells - downstream targets include S6K1 & 4EBP1/eIF4E - inhibited by several natural products [4] - tuberin - hamartin - curcumin - resveratrol - epigallocatechin gallate - caffeine Structure: - belongs to the PI3/PI4-kinase family - contains 1 FAT domain - contains 1 FATC domain - contains 7 HEAT repeats - contains 1 PI3K/PI4K domain Expression: - expressed in numerous tissues, with highest levels in testis Notes: - inhibition of FRAPA1 & the TORC1 complex may account for some of the benefits of caloric restriction

General

HEAT repeat-containing protein (HEATR) protein kinase

Properties

SIZE: entity length = 2549 aa MW = 289 kD MOTIF: HEAT repeat {16-53} Ser phosphorylation site {S567} HEAT repeat {650-688} HEAT repeat {859-897} HEAT repeat {988-1025} HEAT repeat {1069-1106} HEAT repeat {1109-1148} HEAT repeat {1150-1186} MOTIF: Thr phosphorylation site {T1162} Ser phosphorylation site {S1261} FAT domain NAME: FAT domain SITE: 1382-1982 MOTIF: Tyr phosphorylation site binding site FOR-BINDING-OF: Paxillin PI3K/PI4K {2182-2516} MOTIF: Ser phosphorylation site {S2478} Ser phosphorylation site {S2481} FATC {2517-2549} STATE: active state

References

  1. UniProt :accession P42345
  2. Entrez Gene :accession 2475
  3. Atlas of Genetics & Cytogenetics in Oncology & Haematology http://atlasgeneticsoncology.org/genes/FRAP1ID40639ch1p36.html
  4. Hongyu Zhou,1 Yan Luo,1 and Shile Huang1, Updates of mTOR inhibitors Anticancer Agents Med Chem. 2010 September 1, 10(7):571-581 PMID: 20812900 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2980558/

Component-of

target of rapamycin 2 complex (TORC2 complex)

Databases & Figures

OMIM 601231 UniProt P42345 PFAM correlations Entrez Gene 2475 Kegg hsa:2475 RTK -> PI-3-kinase -> Akt -> ...