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Blood, Vol. 110, Issue 12, 4055-4063, December 1, 2007

Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets
Blood Rix et al.
110: 4055
Supplemental materials for: Rix et al
Files in this Data Supplement:
- Table S1. Frequently observed proteins by chemical proteomics (JPG, 74.2 KB)
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Proteins listed are identified at least three times out of seven independent chemical proteomics experiments using compounds unrelated to BCR-ABL-inhibitors. The chemical proteomics experiments used for this analysis were performed with geldanaymcin, FK506, rapamycin (all K562 cells), cyclosporin A (U937 cells), fluoxetine, paroxetine and fluvoxamine (all Namalwa cells).

- Table S2. Proteins purified on imatinib-matrix (JPG, 69.5 KB)
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Proteins are ordered by their peptide counts. IPI-IDs are IPI protein database entries to which identified peptides were assigned. The BCR-ABL fusion protein, which as a whole is not represented by an IPI-ID, is split into its two components BCR and ABL1, the peptides of which were used to determine the listed BCR-ABL parameters (grey shading). ‘Unique peptides’ refers to the sum of unique peptides observed for a particular protein in both experiments. Protein scores and sequence coverage (‘SC’) are based on these unique peptides. The listed data refer to the experiments using K562 cells. Where applicable, the number of unique peptides seen in CML primary cells is shown in parenthesis. Protein scores are Mascot standard scores. MW: Molecular weight in kDa as defined by the particular IPI-ID.

- Table S3. Proteins purified on nilotinib-matrix (JPG, 73.8 KB)
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For a detailed description refer to Table S2.

- Table S4. Proteins purified on dasatinib-matrix (JPG, 170 KB)
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For a detailed description refer to Table S2. The table has been appended with kinases identified only from CML primary cells (unique peptides and sequence coverage in parenthesis). In addition, proteins from CML primary cells, which are described to be associated with ILK, are also listed (gene name in parenthesis).

- Table S5. Raw data sets of K562 core proteome and drug pulldown duplicate experiments (XLS, 1.19 MB)
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The IPI-ID of the anchor protein of each protein group, the specific IPI-ID of each protein, the protein description, species, protein length (in amino acids), presence of specific peptides for one particular IPI-ID, number of unique peptides and the amino acid sequences of all identified peptides are listed (from left to right).
- Figure S1. c-ABL inhibitory potential of truncated imatinib analogues is significantly impaired (JPG, 26.6 KB)
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Chemical structures of alternative coupleable imatinib analogues c-imatinib1 and c-imatinib2 and estimated IC50’s obtained by IMAP kinase inhibition assays with c-ABL kinase domain and AblTide substrate peptide.

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