EZH2.md
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## Experimental Evidence
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Mutations at the main hotspot and some less common hotspots lead to enhanced methylation by PRC2.[@yapSomaticMutationsEZH22011b]
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-Pharmacologic inhibitors of this activity such as tazemetostat have shown benefit in FL.[@morinTreatingLymphomaNow2021]
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+A number of small molecule/pharmacologic inhibitors of EZH2 activity have been described.[@garapaty-raoIdentificationEZH2EZH12013; @knutsonSelectiveInhibitionEZH22014] At least one of these, tazemetostat, has shown benefit in FL.[@morinTreatingLymphomaNow2021]
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+Combination therapies including EZH2 inhibitors are also under exploration for DLBCL patients with mutant EZH2.[@scholzeCombinedEZH2Bcl22020b]
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## History
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```mermaid
morinlab.bib
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+@article{scholzeCombinedEZH2Bcl22020b,
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+ title = {Combined {{EZH2}} and {{Bcl-2}} Inhibitors as Precision Therapy for Genetically Defined {{DLBCL}} Subtypes.},
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+ author = {Scholze, Hanna and Stephenson, Regan E. and Reynolds, Raymond and Shah, Shivem B. and Puri, R. and Butler, Scott D. and Trujillo-Alonso, Vicenta and Teater, Matt and family=Besien, given=Herman, prefix=van, useprefix=false and Gibbs-Curtis, Destini and Ueno, H. and Parvin, S. and Letai, A. and Mathew, S. and Singh, Ankur and Cesarman, E. and Melnick, A. and Giulino‐Roth, L.},
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+ date = {2020},
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+ journaltitle = {Blood Advances},
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+ shortjournal = {Blood advances},
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+ volume = {4 20},
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+ pages = {5226--5231},
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+ doi = {10.1182/bloodadvances.2020002580}
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+}
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@article{yapSomaticMutationsEZH22011b,
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title = {Somatic Mutations at {{EZH2 Y641}} Act Dominantly through a Mechanism of Selectively Altered {{PRC2}} Catalytic Activity, to Increase {{H3K27}} Trimethylation},