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. 2020 Jan 10;13(8):749–763. doi: 10.4155/fmc-2019-0274

Figure 6. . Recruitment of reader proteins to specific genomic loci to control gene expression.

Figure 6. 

(A) General strategy of using bivalent molecules containing a BET bromodomain ligand and a genomic targeting moiety to site specifically recruit BRD4 to perturb gene expression. (B) Syn-TEF1 recruits BRD4 to the FXN gene by localizing to GAA repeats via its polyamide DNA-binding moiety, in turn activating FXN expression. (C) Mixing JQ1 fused to IntC with a guide RNA and dCas-IntN in cell media results in an assembled dCas-JQ1: guide RNA complex which can then be delivered to cells via cationic lipid-mediated delivery and localize to its target DNA sequence. (D) A dCas9-FKBP fusion protein targets CEM-87 to a gene of interest, which induces transcription at that loci through the recruitment of BRD4.

CEM: Chemical epigenetic modifier