View in EDS HTML Full Text PDF Full Text

Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells.

Saved in:
Bibliographic Details
Title: Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells.
Authors: Uguen M; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Shell DJ; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Silva M; University of Toronto, Toronto, ON, Canada., Deng Y; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Li F; University of Toronto, Toronto, ON, Canada., Szewczyk MM; University of Toronto, Toronto, ON, Canada., Yang K; Department of Cell Biology, Harvard Medical School, Boston, MA, USA., Zhao Y; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Stashko MA; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Norris-Drouin JL; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Waybright JM; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Design Therapeutics, Carlsbad, CA, USA., Beldar S; University of Toronto, Toronto, ON, Canada., Rectenwald JM; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Mordant AL; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Webb TS; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Herring LE; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Arrowsmith CH; University of Toronto, Toronto, ON, Canada., Ackloo S; University of Toronto, Toronto, ON, Canada., Gygi SP; Department of Cell Biology, Harvard Medical School, Boston, MA, USA., McGinty RK; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Barsyte-Lovejoy D; University of Toronto, Toronto, ON, Canada., Liu P; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Halabelian L; University of Toronto, Toronto, ON, Canada., James LI; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA., Pearce KH; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA., Frye SV; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA. svfrye@email.unc.edu.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA. svfrye@email.unc.edu.
Source: Nature communications [Nat Commun] 2025 Feb 24; Vol. 16 (1), pp. 1905. Date of Electronic Publication: 2025 Feb 24.
Publication Type: Journal Article
Journal Info: Publisher: Nature Pub. Group Country of Publication: England NLM ID: 101528555 Publication Model: Electronic Cited Medium: Internet ISSN: 2041-1723 (Electronic) Linking ISSN: 20411723 NLM ISO Abbreviation: Nat Commun Subsets: MEDLINE
Database: MEDLINE Ultimate
Full text is not displayed to guests.
FullText Links:
  – Type: pdflink
Text:
  Availability: 1
Header DbId: mdl
DbLabel: MEDLINE Ultimate
An: 39994194
AccessLevel: 2
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
IllustrationInfo
Items – Name: Title
  Label: Title
  Group: Ti
  Data: Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells.
– Name: Author
  Label: Authors
  Group: Au
  Data: <searchLink fieldCode="AU" term="%22Uguen+M%22">Uguen M</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Shell+DJ%22">Shell DJ</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Silva+M%22">Silva M</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Deng+Y%22">Deng Y</searchLink>; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Li+F%22">Li F</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Szewczyk+MM%22">Szewczyk MM</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Yang+K%22">Yang K</searchLink>; Department of Cell Biology, Harvard Medical School, Boston, MA, USA.<br /><searchLink fieldCode="AU" term="%22Zhao+Y%22">Zhao Y</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Stashko+MA%22">Stashko MA</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Norris-Drouin+JL%22">Norris-Drouin JL</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Waybright+JM%22">Waybright JM</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Design Therapeutics, Carlsbad, CA, USA.<br /><searchLink fieldCode="AU" term="%22Beldar+S%22">Beldar S</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Rectenwald+JM%22">Rectenwald JM</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Mordant+AL%22">Mordant AL</searchLink>; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Webb+TS%22">Webb TS</searchLink>; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Herring+LE%22">Herring LE</searchLink>; UNC Metabolomics and Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Arrowsmith+CH%22">Arrowsmith CH</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Ackloo+S%22">Ackloo S</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Gygi+SP%22">Gygi SP</searchLink>; Department of Cell Biology, Harvard Medical School, Boston, MA, USA.<br /><searchLink fieldCode="AU" term="%22McGinty+RK%22">McGinty RK</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Barsyte-Lovejoy+D%22">Barsyte-Lovejoy D</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22Liu+P%22">Liu P</searchLink>; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.; Department of Biochemistry and Biophysics, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Halabelian+L%22">Halabelian L</searchLink>; University of Toronto, Toronto, ON, Canada.<br /><searchLink fieldCode="AU" term="%22James+LI%22">James LI</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Pearce+KH%22">Pearce KH</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.<br /><searchLink fieldCode="AU" term="%22Frye+SV%22">Frye SV</searchLink>; UNC Eshelman School of Pharmacy, Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA. svfrye@email.unc.edu.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA. svfrye@email.unc.edu.
– Name: TitleSource
  Label: Source
  Group: Src
  Data: <searchLink fieldCode="JN" term="%22101528555%22">Nature communications</searchLink> [Nat Commun] 2025 Feb 24; Vol. 16 (1), pp. 1905. <i>Date of Electronic Publication: </i>2025 Feb 24.
– Name: TypePub
  Label: Publication Type
  Group: TypPub
  Data: Journal Article
– Name: TitleSource
  Label: Journal Info
  Group: Src
  Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22Nature+Pub%2E+Group%22">Nature Pub. Group </searchLink><i>Country of Publication: </i>England <i>NLM ID: </i>101528555 <i>Publication Model: </i>Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>2041-1723 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2220411723%22">20411723 </searchLink><i>NLM ISO Abbreviation: </i>Nat Commun <i>Subsets: </i>MEDLINE
PLink https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=39994194
RecordInfo BibRecord:
  BibEntity:
    Identifiers:
      – Type: doi
        Value: 10.1038/s41467-025-57005-3
    Languages:
      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        StartPage: 1905
    Titles:
      – TitleFull: Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells.
        Type: main
  BibRelationships:
    HasContributorRelationships:
      – PersonEntity:
          Name:
            NameFull: Uguen M
      – PersonEntity:
          Name:
            NameFull: Shell DJ
      – PersonEntity:
          Name:
            NameFull: Silva M
      – PersonEntity:
          Name:
            NameFull: Deng Y
      – PersonEntity:
          Name:
            NameFull: Li F
      – PersonEntity:
          Name:
            NameFull: Szewczyk MM
      – PersonEntity:
          Name:
            NameFull: Yang K
      – PersonEntity:
          Name:
            NameFull: Zhao Y
      – PersonEntity:
          Name:
            NameFull: Stashko MA
      – PersonEntity:
          Name:
            NameFull: Norris-Drouin JL
      – PersonEntity:
          Name:
            NameFull: Waybright JM
      – PersonEntity:
          Name:
            NameFull: Beldar S
      – PersonEntity:
          Name:
            NameFull: Rectenwald JM
      – PersonEntity:
          Name:
            NameFull: Mordant AL
      – PersonEntity:
          Name:
            NameFull: Webb TS
      – PersonEntity:
          Name:
            NameFull: Herring LE
      – PersonEntity:
          Name:
            NameFull: Arrowsmith CH
      – PersonEntity:
          Name:
            NameFull: Ackloo S
      – PersonEntity:
          Name:
            NameFull: Gygi SP
      – PersonEntity:
          Name:
            NameFull: McGinty RK
      – PersonEntity:
          Name:
            NameFull: Barsyte-Lovejoy D
      – PersonEntity:
          Name:
            NameFull: Liu P
      – PersonEntity:
          Name:
            NameFull: Halabelian L
      – PersonEntity:
          Name:
            NameFull: James LI
      – PersonEntity:
          Name:
            NameFull: Pearce KH
      – PersonEntity:
          Name:
            NameFull: Frye SV
    IsPartOfRelationships:
      – BibEntity:
          Dates:
            – D: 24
              M: 02
              Text: 2025 Feb 24
              Type: published
              Y: 2025
          Identifiers:
            – Type: issn-electronic
              Value: 2041-1723
          Numbering:
            – Type: volume
              Value: 16
            – Type: issue
              Value: 1
          Titles:
            – TitleFull: Nature communications
              Type: main
ResultId 1