Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo.

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Title: Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo.
Authors: Dubiella C; Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel., Pinch BJ; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.; Department of Chemistry and Chemical Biology, Department of Chemical Biology, Harvard University, Cambridge, MA, USA., Koikawa K; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Zaidman D; Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel., Poon E; Division of Clinical Studies, The Institute of Cancer Research, London, UK., Manz TD; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.; Department of Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbruecken, Germany., Nabet B; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA., He S; Department of Pediatric Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA., Resnick E; Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel., Rogel A; Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel., Langer EM; Department of Molecular and Medical Genetics, Oregon Health & Science University, Portland, OR, USA.; Knight Cancer Institute, Oregon Health & Science University, Portland, OR, USA., Daniel CJ; Department of Molecular and Medical Genetics, Oregon Health & Science University, Portland, OR, USA.; Knight Cancer Institute, Oregon Health & Science University, Portland, OR, USA., Seo HS; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA., Chen Y; College of Chemistry and Molecular Engineering, Peking University, Beijing, China., Adelmant G; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Blais Proteomics Center, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA., Sharifzadeh S; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Blais Proteomics Center, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA., Ficarro SB; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Blais Proteomics Center, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA., Jamin Y; Division of Radiotherapy and Imaging, The Institute of Cancer Research, London, UK., Martins da Costa B; Division of Clinical Studies, The Institute of Cancer Research, London, UK., Zimmerman MW; Department of Pediatric Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA., Lian X; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Kibe S; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Kozono S; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Doctor ZM; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA., Browne CM; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.; Discovery Biology, Discovery Sciences, Biopharmaceuticals R&D, AstraZeneca, Boston, MA, USA., Yang A; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA., Stoler-Barak L; Department of Immunology, The Weizmann Institute of Science, Rehovot, Israel., Shah RB; Department of Medicine, Division of Hematology and Medical Oncology, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.; Department of Cell, Developmental and Regenerative Biology, The Graduate School of Biomedical Sciences, Icahn School of Medicine at Mount Sinai, New York, NY, USA., Vangos NE; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA., Geffken EA; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA., Oren R; Department of Veterinary Resources, The Weizmann Institute of Science, Rehovot, Israel., Koide E; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA., Sidi S; Department of Medicine, Division of Hematology and Medical Oncology, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.; Department of Cell, Developmental and Regenerative Biology, The Graduate School of Biomedical Sciences, Icahn School of Medicine at Mount Sinai, New York, NY, USA., Shulman Z; Department of Immunology, The Weizmann Institute of Science, Rehovot, Israel., Wang C; College of Chemistry and Molecular Engineering, Peking University, Beijing, China., Marto JA; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.; Department of Oncologic Pathology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Blais Proteomics Center, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA., Dhe-Paganon S; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA., Look T; Department of Pediatric Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.; Division of Pediatric Hematology/Oncology Boston Children's Hospital, Boston, MA, USA., Zhou XZ; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Lu KP; Department of Medicine, Division of Translational Therapeutics, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Cancer Research Institute, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA.; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Sears RC; Department of Molecular and Medical Genetics, Oregon Health & Science University, Portland, OR, USA.; Knight Cancer Institute, Oregon Health & Science University, Portland, OR, USA.; Brenden-Colson Center for Pancreatic Care, Oregon Health & Science University, Portland, OR, USA., Chesler L; Division of Clinical Studies, The Institute of Cancer Research, London, UK., Gray NS; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA. nsgray01@stanford.edu.; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA. nsgray01@stanford.edu.; Department of Chemical and Systems Biology, Chem-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA. nsgray01@stanford.edu., London N; Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot, Israel. nir.london@weizmann.ac.il.
Source: Nature chemical biology [Nat Chem Biol] 2021 Sep; Vol. 17 (9), pp. 954-963. Date of Electronic Publication: 2021 May 10.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Journal Info: Publisher: Nature Pub. Group Country of Publication: United States NLM ID: 101231976 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1552-4469 (Electronic) Linking ISSN: 15524450 NLM ISO Abbreviation: Nat Chem Biol Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1552-4469
DOI:10.1038/s41589-021-00786-7