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IRF4 in multiple myeloma

IRF4 is a transcription factor that is required at different stages of B cell development and, in particular, in the differentiation of B cells into plasma cells. In many MM, the malignant plasma cells are dependent on IRF4 for maintenance and survival despite the fact that the gene is not always mutated to an oncogenic form [17]. Hence this dependency is termed non-oncogene dependency. IRF4 is of notable significance because current treatments for MM are ineffective and the median survival time is only 3-4 years following initial treatment [43].

IRF4 is expressed in acutely activated B cells, and directs them to terminally differentiate into plasma cells by acting as a positive transcriptional regulator of genes involved in differentiation and proliferation. As many as 308 genes are direct or indirect targets of IRF4, of which 101 have been shown to be upregulated in MM cell lines [17]. This broad regulation stems from the fact that IRF4 is at the apex in the hierarchy of gene regulators in that it regulates expression of other transcription factors which then further regulate gene expression. Moreover MYC, one transcription factor upregulated by IRF4, is a direct positive regulator of IRF4 itself [17]. Thus, IRF4 may act in a positive feedback loop to maintain its own expression whilst driving cancer progression.

Dependence of MM on non-oncogenic IRF4 was demonstrated using short hairpin RNA (shRNA) screens with retroviral expression vectors [17]. Retroviruses carrying different shRNAs were transfected into MM cell lines and shRNA expression was induced by addition of doxycycline. Several shRNAs targeting IRF4 were identified that were able to kill ten different cell lines, each with a distinct molecular manifestation of MM. One particular shRNA targeting the 3’ untranslated region of IRF4 mRNA reduced its expression by 50-75%, and killed MM cells within 3 days.

IRF4 is only expressed in lymphoid and myeloid cells [44]. This tissue specificity makes IRF4 an attractive therapeutic target for MM as (1) the uptake of IRF4-targeting drugs by other tissues will be unlikely to induce significant adverse effects, and (2) healthy blood cells lost due to the action of these drugs can be regenerated by natural haematopoiesis

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