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Home > Curated Information Page > PubMed Id: 20145145
Pan BS, et al. (2010) MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res 70, 1524-33 20145145
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.
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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 mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 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 mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

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 mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

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 mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

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 mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y653-p - FGFR1 (human)
Modsite: RDIHHIDyykKTTNG SwissProt Entrez-Gene
Orthologous residues
FGFR1 (human): Y653‑p, FGFR1 iso2 (human): Y651‑p, FGFR1 iso14 (human): Y562‑p, FGFR1 iso21 (human): Y684‑p, FGFR1 (mouse): Y653‑p, FGFR1 (rat): Y560‑p, FGFR1 iso2 (rat): Y653‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y654-p - FGFR1 (human)
Modsite: DIHHIDyykKTTNGR SwissProt Entrez-Gene
Orthologous residues
FGFR1 (human): Y654‑p, FGFR1 iso2 (human): Y652‑p, FGFR1 iso14 (human): Y563‑p, FGFR1 iso21 (human): Y685‑p, FGFR1 (mouse): Y654‑p, FGFR1 (rat): Y561‑p, FGFR1 iso2 (rat): Y654‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y1003-p - Met (human)
Modsite: VsNEsVDyRAtFPED SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1003‑p, Met iso2 (human): Y1021‑p, Met (mouse): Y1001‑p, Met (rat): Y1004‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y1230-p - Met (human)
Modsite: FGLARDMyDkEyysV SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1230‑p, Met iso2 (human): Y1248‑p, Met (mouse): Y1228‑p, Met (rat): Y1231‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Enzymes shown to modify site in vitro
Type Enzyme
KINASE Met (human)

Y1234-p - Met (human)
Modsite: RDMyDkEyysVHNkt SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1234‑p, Met iso2 (human): Y1252‑p, Met (mouse): Y1232‑p, Met (rat): Y1235‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Enzymes shown to modify site in vitro
Type Enzyme
KINASE Met (human)

Y1235-p - Met (human)
Modsite: DMyDkEyysVHNktG SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1235‑p, Met iso2 (human): Y1253‑p, Met (mouse): Y1233‑p, Met (rat): Y1236‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Enzymes shown to modify site in vitro
Type Enzyme
KINASE Met (human)

Y1349-p - Met (human)
Modsite: stFIGEHyVHVNAty SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1349‑p, Met iso2 (human): Y1367‑p, Met (mouse): Y1347‑p, Met (rat): Y1350‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Enzymes shown to modify site in vitro
Type Enzyme
KINASE Met (human)
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y1365-p - Met (human)
Modsite: NVKCVAPyPsLLssE SwissProt Entrez-Gene
Orthologous residues
Met (human): Y1365‑p, Met iso2 (human): Y1383‑p, Met (mouse): Y1363‑p, Met (rat): Y1366‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Enzymes shown to modify site in vitro
Type Enzyme
KINASE Met (human)
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease

Y849-p - PDGFRA (human)
Modsite: DIMHDsNyVsKGSTF SwissProt Entrez-Gene
Orthologous residues
PDGFRA (human): Y849‑p, PDGFRA (mouse): Y849‑p, PDGFRA (rat): Y848‑p
Characterization
Methods used to characterize site in vivo mass spectrometry, phospho-antibody, western blotting
Disease tissue studied:  gastric cancer, gastric carcinoma, lung cancer, non-small cell lung cancer, non-small cell lung adenocarcinoma, non-small cell squamous cell lung carcinoma
Relevant cell lines - cell types - tissues:  A549 (pulmonary), GTL-16 (gastric), KATO III (gastric), NCI-H1703 (squamous)
Cellular systems studied:  cell lines
Species studied:  human
Comments:  including xenografts using GTL-16 cells
Upstream Regulation
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
MK-2461 decrease