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Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activit...

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Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activit...

https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_11463403

Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activity in Cells

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United States: Cold Spring Harbor Laboratory

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A promising drug target, SETDB1, is a dual Kme reader and methyltransferase, which has been implicated in cancer and neurodegenerative disease progression. To help understand the role of the triple Tudor domain (3TD) of SETDB1, its Kme reader, we first identified a low micromolar small molecule ligand, UNC6535, which occupies simultaneously both th...

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Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activity in Cells

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TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_11463403

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https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_11463403

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ISSN

2692-8205

E-ISSN

2692-8205

DOI

10.1101/2024.09.27.615363

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