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Home > Curated Information Page > PubMed Id: 16585200
Zeng Z, et al. (2006) Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Res 66, 3737-46 16585200
This page summarizes selected information from the record referenced above and curated into PhosphoSitePlus®, a comprehensive online resource for the study of protein post-translational modifications (NAR, 2015, 43:D512-20). To learn more about the scope of PhosphoSitePlus®, click here.
Information from this record has been curated, but not yet edited in PhosphoSitePlus® and may be incomplete.
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T308-p - Akt1 (human)
Modsite: kDGAtMKtFCGtPEy SwissProt Entrez-Gene
Orthologous residues
Akt1 (human): T308‑p, Akt1 iso2 (human): T246‑p, Akt1 (mouse): T308‑p, Akt1 (rat): T308‑p, Akt1 (fruit fly): T423‑p, Akt1 (cow): T308‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease

S473-p - Akt1 (human)
Modsite: RPHFPQFsysAsGtA SwissProt Entrez-Gene
Orthologous residues
Akt1 (human): S473‑p, Akt1 iso2 (human): S411‑p, Akt1 (mouse): S473‑p, Akt1 (rat): S473‑p, Akt1 (fruit fly): S586‑p, Akt1 (cow): S473‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease
siRNA increase p70S6K siRNA
KP-372-1 decrease
siRNA KP-372-1 inhibit treatment-induced decrease p70S6K siRNA
LY294002 decrease

S99-p - BAD (human)
Modsite: PFrGrsRsAPPNLWA SwissProt Entrez-Gene
Orthologous residues
BAD (human): S99‑p, BAD (mouse): S136‑p, BAD (rat): S137‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease Very slight decrease

T202-p - ERK1 (human)
Modsite: HDHtGFLtEyVAtRW SwissProt Entrez-Gene
Orthologous residues
ERK1 (human): T202‑p, ERK1 iso2 (human): T202‑p, ERK1 iso3 (human): T202‑p, ERK1 (mouse): T203‑p, ERK1 (rat): T203‑p, ERK1 (hamster): T192‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 no change compared to control

Y204-p - ERK1 (human)
Modsite: HtGFLtEyVAtRWyr SwissProt Entrez-Gene
Orthologous residues
ERK1 (human): Y204‑p, ERK1 iso2 (human): Y204‑p, ERK1 iso3 (human): Y204‑p, ERK1 (mouse): Y205‑p, ERK1 (rat): Y205‑p, ERK1 (hamster): Y194‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 no change compared to control

T185-p - ERK2 (human)
Modsite: HDHtGFLtEyVAtRW SwissProt Entrez-Gene
Orthologous residues
ERK2 (human): T185‑p, ERK2 (mouse): T183‑p, ERK2 (rat): T183‑p, ERK2 (chicken): T193‑p, ERK2 (cow): T185‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 no change compared to control

Y187-p - ERK2 (human)
Modsite: HtGFLtEyVAtRWyr SwissProt Entrez-Gene
Orthologous residues
ERK2 (human): Y187‑p, ERK2 (mouse): Y185‑p, ERK2 (rat): Y185‑p, ERK2 (chicken): Y195‑p, ERK2 (cow): Y187‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 no change compared to control

T32-p - FOXO3A (human)
Modsite: QsRPRsCtWPLQRPE SwissProt Entrez-Gene
Orthologous residues
FOXO3A (human): T32‑p, FOXO3A (mouse): T32‑p, FOXO3A (rat): T32‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease

S21-p - GSK3A (human)
Modsite: sGrARtssFAEPGGG SwissProt Entrez-Gene
Orthologous residues
GSK3A (human): S21‑p, GSK3A (mouse): S21‑p, GSK3A (rat): S21‑p, GSK3A (cow): S21‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease
siRNA increase p70S6K siRNA
KP-372-1 decrease
siRNA KP-372-1 inhibit treatment-induced decrease p70S6K siRNA

S9-p - GSK3B (human)
Modsite: SGRPRttsFAEsCkP SwissProt Entrez-Gene
Orthologous residues
GSK3B (human): S9‑p, GSK3B iso2 (human): S9‑p, GSK3B (mouse): S9‑p, GSK3B (rat): S9‑p, GSK3B (rabbit): S9‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease
siRNA increase p70S6K siRNA
KP-372-1 decrease
siRNA KP-372-1 inhibit treatment-induced decrease p70S6K siRNA

T412-p - p70S6K (human)
Modsite: NQVFLGFtyVAPsVL SwissProt Entrez-Gene
Orthologous residues
p70S6K (human): T412‑p, p70S6K iso2 (human): T389‑p, p70S6K (mouse): T412‑p, p70S6K (rat): T412‑p, p70S6K iso2 (rat): T389‑p, p70S6K (fruit fly): T398‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 decrease

S241-p - PDK1 (human)
Modsite: skQARANsFVGtAQy SwissProt Entrez-Gene
Orthologous residues
PDK1 (human): S241‑p, PDK1 iso2 (human): S191‑p, PDK1 iso4 (human): S114‑p, PDK1 iso5 (human): S241‑p, PDK1 (mouse): S244‑p, PDK1 (rat): S244‑p
Characterization
Methods used to characterize site in vivo phospho-antibody
Disease tissue studied:  breast cancer, leukemia, acute myelogenous leukemia, acute erythroid leukemias, including erythroleukemia (M6a) and very rare pure erythroid leukemia (M6b), lymphoma
Relevant cell lines - cell types - tissues:  KG-1 (myeloid), MCF-7 (breast cell), NB-4 (myeloid), TF-1 (erythroid), U-937 (myeloid)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
KP-372-1 no change compared to control