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Recruitment of FBXO22 for targeted degradation of NSD2.

Autor: Nie DY; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Tabor JR; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Li J; University of Florida Health Cancer Center, Gainesville, FL, USA.; Department of Pharmacology, Physiology, and Cancer Biology, Sidney Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA, USA., Kutera M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., St-Germain J; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada., Hanley RP; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; C4 Therapeutics, Watertown, MA, USA., Wolf E; Department of Chemistry, York University, Toronto, Ontario, Canada., Paulakonis E; Department of Pharmacology, University of North Carolina, Chapel Hill, NC, USA., Kenney TMG; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Duan S; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada., Shrestha S; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada., Owens DDG; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Amphista Therapeutics, Cambridge, UK., Maitland MER; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Pon A; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Szewczyk M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Lamberto AJ; University of Florida Health Cancer Center, Gainesville, FL, USA., Menes M; University of Florida Health Cancer Center, Gainesville, FL, USA., Li F; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Penn LZ; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Barsyte-Lovejoy D; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Department of Pharmacology & Toxicology, University of Toronto, Toronto, Ontario, Canada., Brown NG; Department of Pharmacology, University of North Carolina, Chapel Hill, NC, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Barsotti AM; Deerfield Discovery and Development, Deerfield Management, New York, NY, USA., Stamford AW; Deerfield Discovery and Development, Deerfield Management, New York, NY, USA., Collins JL; Office of the Vice Chancellor for Research, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Wilson DJ; Department of Chemistry, York University, Toronto, Ontario, Canada., Raught B; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Licht JD; University of Florida Health Cancer Center, Gainesville, FL, USA., James LI; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA. ingerman@email.unc.edu.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA. ingerman@email.unc.edu., Arrowsmith CH; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada. cheryl.arrowsmith@uhn.ca.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, Canada. cheryl.arrowsmith@uhn.ca.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada. cheryl.arrowsmith@uhn.ca.

Publikováno v: Nature chemical biology [Nat Chem Biol] 2024 Dec; Vol. 20 (12), pp. 1597-1607. Date of Electronic Publication: 2024 Jul 04.

Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2.

Autor: Hanley RP; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Nie DY; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario M5G 1L7, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Tabor JR; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Li F; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Sobh A; University of Florida Health Cancer Center, The University of Florida Cancer and Genetics Research Complex, Gainesville, Florida 32610, United States., Xu C; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States.; Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States., Barker NK; UNC Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Dilworth D; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Hajian T; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Gibson E; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Szewczyk MM; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Brown PJ; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada., Barsyte-Lovejoy D; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.; Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario M5S 1A8, Canada., Herring LE; UNC Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Wang GG; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States.; Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States.; Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States., Licht JD; University of Florida Health Cancer Center, The University of Florida Cancer and Genetics Research Complex, Gainesville, Florida 32610, United States., Vedadi M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.; Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario M5S 1A8, Canada., Arrowsmith CH; Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.; Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario M5G 1L7, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario M5G 1L7, Canada., James LI; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States.

Publikováno v: Journal of the American Chemical Society [J Am Chem Soc] 2023 Apr 12; Vol. 145 (14), pp. 8176-8188. Date of Electronic Publication: 2023 Mar 28.

A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.

Autor: Dilworth D; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada. david.dilworth@utoronto.ca.; BlueRock Therapeutics, Toronto, Ontario, Canada. david.dilworth@utoronto.ca., Hanley RP; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; C4 Therapeutics, Watertown, MA, USA., Ferreira de Freitas R; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Rua Arcturus 3, São Bernardo do Campo, Brazil., Allali-Hassani A; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Incyte, Wilmington, DE, USA., Zhou M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Hubei Key Laboratory of Genetic Regulation and Integrative Biology, School of Life Sciences, Central China Normal University, Wuhan, China., Mehta N; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Nurix Therapeutics, San Francisco, CA, USA., Marunde MR; EpiCypher Inc., Durham, NC, USA., Ackloo S; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Carvalho Machado RA; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Khalili Yazdi A; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Owens DDG; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Vu V; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Nie DY; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Alqazzaz M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Marcon E; Donnelly Centre, University of Toronto, Toronto, Ontario, Canada., Li F; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Chau I; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Bolotokova A; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Qin S; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Life Science Research Center, Southern University of Science and Technology, Shenzhen, China., Lei M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Hubei Key Laboratory of Genetic Regulation and Integrative Biology, School of Life Sciences, Central China Normal University, Wuhan, China., Liu Y; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; College of Pharmaceutical Sciences, Soochow University, Suzhou, China., Szewczyk MM; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Dong A; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Kazemzadeh S; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Abramyan T; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.; Atomwise, San Francisco, CA, USA., Popova IK; EpiCypher Inc., Durham, NC, USA., Hall NW; EpiCypher Inc., Durham, NC, USA., Meiners MJ; EpiCypher Inc., Durham, NC, USA., Cheek MA; EpiCypher Inc., Durham, NC, USA., Gibson E; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Kireev D; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Greenblatt JF; Donnelly Centre, University of Toronto, Toronto, Ontario, Canada., Keogh MC; EpiCypher Inc., Durham, NC, USA., Min J; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Hubei Key Laboratory of Genetic Regulation and Integrative Biology, School of Life Sciences, Central China Normal University, Wuhan, China., Brown PJ; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada., Vedadi M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada., Arrowsmith CH; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.; Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada., Barsyte-Lovejoy D; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada. d.barsyte@utoronto.ca.; Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada. d.barsyte@utoronto.ca., James LI; Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA. ingerman@email.unc.edu., Schapira M; Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada. matthieu.schapira@utoronto.ca.; Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada. matthieu.schapira@utoronto.ca.

Publikováno v: Nature chemical biology [Nat Chem Biol] 2022 Jan; Vol. 18 (1), pp. 56-63. Date of Electronic Publication: 2021 Nov 15.

Targeting Regorafenib-Induced Toxicity through Inhibition of Gut Microbial β-Glucuronidases.

Autor: Ervin SM; Department of Chemistry , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Hanley RP; Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Lim L; Department of Chemistry , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Walton WG; Department of Chemistry , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Pearce KH; Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Bhatt AP; Department of Medicine , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., James LI; Center for Integrative Chemical Biology and Drug Discovery, Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States., Redinbo MR; Department of Chemistry , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States.; Integrated Program for Biological and Genome Sciences and Departments of Biochemistry and Microbiology , University of North Carolina at Chapel Hill , Chapel Hill , North Carolina 27599 , United States.

Publikováno v: ACS chemical biology [ACS Chem Biol] 2019 Dec 20; Vol. 14 (12), pp. 2737-2744. Date of Electronic Publication: 2019 Nov 12.