Abstract
Disclosed in this specification is a method for inhibiting the formation of SET1 family core complexes. A guanidinium-containing molecule is used to competitively inhibit the binding of the N-SET region of a SET1 protein to WDR5, thus inhibiting the formation of the SET1 family core complex. The guanidinium-containing molecule may be, for example, an arginine-containing peptide. When bound to WDR5, the guanidinium moiety is bound between the F-133 and F-263 residues of the WDR5 when a crystal structure of the bound complex is obtained.
| Original language | English (US) |
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| Patent number | 8,133,690 |
| State | Published - Feb 28 2010 |