As a predominant type II protein arginine methyltransferase,
PRMT5
plays critical roles in various normal cellular processes by catalyzing
the mono- and symmetrical dimethylation of a wide range of histone
and nonhistone substrates. Clinical studies have revealed that high
expression of PRMT5 is observed in different solid tumors and hematological
malignancies and is closely associated with cancer initiation and
progression. Accordingly, PRMT5 is becoming a promising anticancer
target and has received great attention in both the pharmaceutical
industry and the academic community. In this Perspective, we comprehensively
summarize recent advances in the development of first-generation PRMT5
enzymatic inhibitors and highlight novel strategies targeting PRMT5
in the past 5 years. We also discuss the challenges and opportunities
of PRMT5 inhibition, with the aim of shedding light on future PRMT5
drug discovery.
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