PHF19 Activators

Chemicals classified as PHF19 Activators are substances that can influence the activity of the PHF19 protein, which is a part of the Polycomb repressive complex 2 (PRC2). These substances primarily affect the broader Polycomb machinery, which includes other proteins and complexes that interact with or are part of the same signaling pathways as PHF19. Many of these substances function by inhibiting key components of the PRC2 complex, such as EZH2, EED, or WDR5, or of the related PRC1 complex, such as RING1B or BMI1. By inhibiting these proteins, the substances can alter the activity of the PRC2 complex as a whole, and thereby influence PHF19 function. This occurs because PHF19 does not act in isolation, but as a part of the PRC2 complex.

The subset of PHF19 Activators that inhibit EZH2, the catalytic component of the PRC2 complex,are particularly noteworthy. EZH2 is responsible for the trimethylation of histone H3 at lysine 27 (H3K27me3), a mark of gene repression. DZNep, GSK126, EPZ-6438, UNC1999, and EPZ005687 can reduce the levels of H3K27me3 by inhibiting EZH2, which can indirectly affect PHF19's role in the PRC2 complex. Other PHF19 Activators function by inhibiting components of the PRC1 complex, which also plays a role in gene silencing. These include PRT4165, PTC-209, and YUKA1, which inhibit the PRC1 components RING1B and BMI1. Although PRC1 is a separate complex, its function is intertwined with that of PRC2, and changes in PRC1 activity can indirectly influence PHF19 and the PRC2 complex. In addition to the substances that inhibit EZH2 and PRC1 components, there are also PHF19 Activators that inhibit other components of the PRC2 complex. For example, BI-9564 and A-395 inhibit PRDM9 and EED, respectively, while MM-102 inhibits WDR5. By targeting these components, these substances influence the activity of the entire PRC2 complex, including PHF19.