Stuart L Schreiber

Stuart L Schreiber

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Stuart L Schreiber

Stuart L Schreiber

Publications by authors named "Stuart L Schreiber"

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Recent achievements and current trajectories of diversity-oriented synthesis.

Curr Opin Chem Biol 2019 Oct 14;56:1-9. Epub 2019 Oct 14.

Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138, USA; Chemical Biology and Therapeutics Science Program, Broad Institute, 415 Main Street, Cambridge, MA 02142, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S13675931193010
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http://dx.doi.org/10.1016/j.cbpa.2019.08.008DOI Listing
October 2019

6-Phosphogluconate Dehydrogenase Links Cytosolic Carbohydrate Metabolism to Protein Secretion via Modulation of Glutathione Levels.

Cell Chem Biol 2019 Sep 13;26(9):1306-1314.e5. Epub 2019 Jun 13.

Broad Institute of Harvard and MIT, Cambridge, MA 02142, USA; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.05.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6754299PMC
September 2019

DNA Barcoding a Complete Matrix of Stereoisomeric Small Molecules.

J Am Chem Soc 2019 Jul 25;141(26):10225-10235. Epub 2019 Jun 25.

Department of Chemistry and Chemical Biology , Harvard University , 12 Oxford Street , Cambridge , Massachusetts 02138 , United States.

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http://dx.doi.org/10.1021/jacs.9b01203DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6681660PMC
July 2019

1980s Camelot.

J Antibiot (Tokyo) 2019 06 27;72(6):323. Epub 2019 May 27.

Harvard University, Broad Institute, Cambridge, MA, USA.

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http://dx.doi.org/10.1038/s41429-019-0174-zDOI Listing
June 2019

DNA-Compatible [3 + 2] Nitrone-Olefin Cycloaddition Suitable for DEL Syntheses.

Org Lett 2019 03 14;21(5):1325-1330. Epub 2019 Feb 14.

Department of Chemistry and Chemical Biology , Harvard University , 12 Oxford Street , Cambridge , Massachusetts 02138 , United States.

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http://pubs.acs.org/doi/10.1021/acs.orglett.9b00017
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http://dx.doi.org/10.1021/acs.orglett.9b00017DOI Listing
March 2019

A Chemical Biology View of Bioactive Small Molecules and a Binder-Based Approach to Connect Biology to Precision Medicines.

Isr J Chem 2019 Feb 30;59(1-2):52-59. Epub 2018 Oct 30.

Department of Chemistry and Chemical Biology Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA and Chemical Biology and Therapeutics Science Program Broad Institute, 415 Main Street, Cambridge, Massachusetts 02142, USA.

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http://dx.doi.org/10.1002/ijch.201800113DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6528670PMC
February 2019

RWEN: response-weighted elastic net for prediction of chemosensitivity of cancer cell lines.

Bioinformatics 2018 10;34(19):3332-3339

Chemical Biology & Therapeutics Science Program, Broad Institute of Harvard and MIT, Cambridge, MA, USA.

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http://dx.doi.org/10.1093/bioinformatics/bty199DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6157095PMC
October 2018

High Throughput Screen Identifies Interferon γ-Dependent Inhibitors of Toxoplasma gondii Growth.

ACS Infect Dis 2018 10 28;4(10):1499-1507. Epub 2018 Aug 28.

Department of Molecular Microbiology , Washington University in Saint Louis School of Medicine , 660 S. Euclid Avenue , St. Louis , Missouri 63110 , United States.

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http://pubs.acs.org/doi/10.1021/acsinfecdis.8b00135
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http://dx.doi.org/10.1021/acsinfecdis.8b00135DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6200635PMC
October 2018

Synergistic Effects of Stereochemistry and Appendages on the Performance Diversity of a Collection of Synthetic Compounds.

J Am Chem Soc 2018 09 6;140(37):11784-11790. Epub 2018 Sep 6.

Department of Chemistry and Chemical Biology , Harvard University , Cambridge , Massachusetts 02138 , United States.

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http://pubs.acs.org/doi/10.1021/jacs.8b07319
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http://dx.doi.org/10.1021/jacs.8b07319DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6644712PMC
September 2018

Chemical probes and drug leads from advances in synthetic planning and methodology.

Nat Rev Drug Discov 2018 05 13;17(5):333-352. Epub 2018 Apr 13.

Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA, USA.

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http://www.nature.com/doifinder/10.1038/nrd.2018.53
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http://dx.doi.org/10.1038/nrd.2018.53DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6707071PMC
May 2018

Targeting Dependency on the GPX4 Lipid Peroxide Repair Pathway for Cancer Therapy.

Biochemistry 2018 04 27;57(14):2059-2060. Epub 2018 Mar 27.

Department of Chemistry , Columbia University , New York , New York 10027 , United States.

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http://pubs.acs.org/doi/10.1021/acs.biochem.8b00307
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http://dx.doi.org/10.1021/acs.biochem.8b00307DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5962875PMC
April 2018

Drug-tolerant persister cancer cells are vulnerable to GPX4 inhibition.

Nature 2017 11 1;551(7679):247-250. Epub 2017 Nov 1.

Department of Microbiology and Immunology, University of California San Francisco, 513 Parnassus Avenue, San Francisco, California 94143, USA.

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http://www.nature.com/doifinder/10.1038/nature24297
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http://dx.doi.org/10.1038/nature24297DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5933935PMC
November 2017

Stereospecific Palladium-Catalyzed C-H Arylation of Pyroglutamic Acid Derivatives at the C3 Position Enabled by 8-Aminoquinoline as a Directing Group.

Org Lett 2017 09 15;19(17):4424-4427. Epub 2017 Aug 15.

Department of Chemistry and Chemical Biology, Harvard University , Cambridge, Massachusetts 02138, United States.

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http://dx.doi.org/10.1021/acs.orglett.7b01776DOI Listing
September 2017

Synthesis of a Bicyclic Azetidine with In Vivo Antimalarial Activity Enabled by Stereospecific, Directed C(sp)-H Arylation.

J Am Chem Soc 2017 08 7;139(32):11300-11306. Epub 2017 Aug 7.

Department of Chemistry and Chemical Biology, Harvard University , Cambridge, Massachusetts 02138, United States.

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http://dx.doi.org/10.1021/jacs.7b06994DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561537PMC
August 2017

Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit Dihydroorotate Dehydrogenase.

ACS Med Chem Lett 2017 Apr 27;8(4):438-442. Epub 2017 Feb 27.

Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States.

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.7b00030
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http://dx.doi.org/10.1021/acsmedchemlett.7b00030DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5392761PMC
April 2017

US immigration order strikes against biotech.

Authors:
Jeremy M Levin Steven H Holtzman John Maraganore Paul J Hastings Ron Cohen Bassil Dahiyat Julian Adams Chris Adams Brett Ahrens Jeff Albers Mara G Aspinall James E Audia Martin Babler Peter Barrett Zoe Barry Nessan Bermingham Stephen Bloch Robert I Blum Paul B Bolno Michael W Bonney Bruce Booth Daniel M Bradbury Steven K Brauer Brook Byers Pablo J Cagnoni Brian M Cali Isaac Ciechanover Chip Clark Michael D Clayman Jeff L Cleland Paula Cobb Ron Cooper Mark G Currie John Diekman Eric L Dobmeier Doug Doerfler Elizabeth Lr Donley Deborah Dunsire Matthew During Jens W Eckstein Eric Elenko Neil A Exter Jonathan J Fleming Gregory J Flesher Jean-Francois Formela Robert Forrester Cedric Francois Heather Franklin Mason W Freeman Howard Furst Leonard Patrick Gage Nicholas Galakatos Brian M Gallagher James A Geraghty Simba Gill David V Goeddel Mark A Goldsmith Maxine Gowen Vikas Goyal Tom Graney David Grayzel Barry Greene Paul Grint J C Gutierrez-Ramos Bill Haney Tuan Ha-Ngoc Tim Harris Faheem Hasnain Yujiro Steve Hata Peter Hecht Leslie Henshaw Rich Heyman Herve Hoppenot H Robert Horvitz Thomas E Hughes Wende S Hutton Stephen T Isaacs Annalisa Jenkins Jeff Jonker Jeff Kaplan Perry Karsen Jeb Keiper Jean Kim Jeff Kindler Rachel King Vanessa King Nina Kjellson Scott Koenig Gerhard Koenig Peter Kolchinsky Paul Laikind Robert Bob Langer John J Lee Jonathan S Leff Bruce A Leicher Nick Leschly Andrew Levin Mark Levin Arnold J Levine Alan Levy David R Liu Harvey F Lodish Uri Lopatin Ted W Love Guy Macdonald Gail J Maderis Ankit Mahadevia Nagesh K Mahanthappa Joel F Martin Alex Martin W Eddie Martucci James G McArthur Corey M McCann Sean A McCarthy C Geoffrey McDonough John Mendlein Larry Miller Diego Miralles Kenneth I Moch Bob More Andrew G Myers Michael A Narachi Amir Nashat Wendy Nelson William J Newell Bernat Olle John E Osborn Julia C Owens Atul Pande Stelios Papadopoulos H Stewart Parker Kush M Parmar Matthew R Patterson Steve M Paul Rob Perez Matthew Perry Cary G Pfeffer Mike Powell Mark Pruzanski Dennis J Purcell Amit Rakhit Kartik Ramamoorthi William Rastetter Adrian Ad Rawcliffe Laurence E Reid Ron C Renaud Jason P Rhodes William J Rieflin Chad Robins Scott M Rocklage Michael Rosenblatt Jonathan G Rosin William J Rutter Saurabh Saha Camille Samuels Vicki L Sato George Scangos John A Scarlett David Schenkein Stuart L Schreiber Andrew Schwab Paul Sekhri Rajeev Shah Thomas Shenk Clay B Siegall Nick J Simon Nancy Simonian Jeff Stein Michael Su Mary T Szela Marco Taglietti Nina Tandon Henri Termeer Nancy A Thornberry Martin Tolar Richard Ulevitch Akshay K Vaishnaw Anne VanLent Martin Varsavsky George P Vlasuk Michel Vounatsos Samuel G Waksal Neil Warma Ryan J Watts Yaron Werber Christoph Westphal Wendell Wierenga Doug E Williams Lewis Rusty Williams Kleanthis G Xanthopoulos Daphne Zohar Sandford Sandy Zweifach

Nat Biotechnol 2017 03;35(3):204-206

Nuvelution Pharmaceuticals, Inc., South San Francisco, California, USA.

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http://dx.doi.org/10.1038/nbt.3824DOI Listing
March 2017

Divergent Synthesis and Real-Time Biological Annotation of Optically Active Tetrahydrocyclopenta[c]pyranone Derivatives.

Org Lett 2016 12 7;18(24):6280-6283. Epub 2016 Dec 7.

Howard Hughes Medical Institute and Center for the Science of Therapeutics, The Broad Institute of Harvard and MIT , 415 Main Street, Cambridge, Massachusetts 02142, United States.

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http://dx.doi.org/10.1021/acs.orglett.6b03118DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5171204PMC
December 2016

Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia.

ACS Med Chem Lett 2016 Dec 28;7(12):1112-1117. Epub 2016 Sep 28.

Center for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States; Howard Hughes Medical Institute, Cambridge, Massachusetts 02138, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00316DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5150668PMC
December 2016

Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.

ACS Med Chem Lett 2016 Oct 18;7(10):944-949. Epub 2016 Aug 18.

Center for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States; Howard Hughes Medical Institute, Cambridge, Massachusetts 02138, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00264DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5066158PMC
October 2016

Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia.

Cell 2016 Sep 15;167(1):171-186.e15. Epub 2016 Sep 15.

Center for Regenerative Medicine, Massachusetts General Hospital, Boston, MA 02114, USA; Cancer Center, Massachusetts General Hospital, Boston, MA 02114, USA; Department of Stem Cell and Regenerative Biology, Harvard University, Cambridge, MA 02138, USA; Harvard Stem Cell Institute, Cambridge, MA 02138, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00928674163115
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http://dx.doi.org/10.1016/j.cell.2016.08.057DOI Listing
September 2016

Gene Expression-Based Screen for Parkinson's Disease Identifies GW8510 as a Neuroprotective Agent.

ACS Chem Neurosci 2016 07 9;7(7):857-63. Epub 2016 Jun 9.

Center for the Science of Therapeutics, Broad Institute of Harvard and MIT , Cambridge, Massachusetts 02142, United States.

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http://dx.doi.org/10.1021/acschemneuro.6b00076DOI Listing
July 2016

Real-Time Biological Annotation of Synthetic Compounds.

J Am Chem Soc 2016 07 11;138(28):8920-7. Epub 2016 Jul 11.

Department of Chemistry and Chemical Biology, Harvard University , 12 Oxford Street, Cambridge, Massachusetts 02138, United States.

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http://dx.doi.org/10.1021/jacs.6b04614DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4976700PMC
July 2016

High-Throughput Luciferase-Based Assay for the Discovery of Therapeutics That Prevent Malaria.

ACS Infect Dis 2016 Apr 10;2(4):281-293. Epub 2016 Feb 10.

School of Medicine, Department of Pediatrics, Pharmacology & Drug Discovery, University of California, San Diego , 9500 Gilman Drive, La Jolla, California 92093, United States.

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http://dx.doi.org/10.1021/acsinfecdis.5b00143DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4890880PMC
April 2016

High-Throughput Assay and Discovery of Small Molecules that Interrupt Malaria Transmission.

Cell Host Microbe 2016 Jan 31;19(1):114-26. Epub 2015 Dec 31.

Division of Pharmacology and Drug Discovery, Department of Pediatrics, University of California San Diego School of Medicine, 9500 Gilman Drive, La Jolla, CA 92093, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chom.2015.12.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4723716PMC
January 2016

High-Throughput Screen in Identifies a Novel Molecular Scaffold That Inhibits Cell Wall Integrity Pathway Signaling.

ACS Infect Dis 2016 Jan 6;2(1):93-102. Epub 2015 Nov 6.

Department of Pediatrics and Department of Microbiology/Immunology, University of Rochester School of Medicine and Dentistry, 601 Elmwood Avenue, Rochester, New York 14642, United States; Department of Pediatrics and Department of Microbiology/Immunology, University of Rochester School of Medicine and Dentistry, 601 Elmwood Avenue, Rochester, New York 14642, United States.

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http://dx.doi.org/10.1021/acsinfecdis.5b00111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4709821PMC
January 2016

The Power of Sophisticated Phenotypic Screening and Modern Mechanism-of-Action Methods.

Cell Chem Biol 2016 Jan;23(1):3-9

Center for the Science of Therapeutics, Broad Institute, Cambridge, MA 02142, USA; Department of Chemistry and Chemical Biology, Howard Hughes Medical Institute, Harvard University, Cambridge, MA 02138, USA.

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http://dx.doi.org/10.1016/j.chembiol.2015.11.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4779180PMC
January 2016

Small-molecule enhancers of autophagy modulate cellular disease phenotypes suggested by human genetics.

Proc Natl Acad Sci U S A 2015 Aug 20;112(31):E4281-7. Epub 2015 Jul 20.

Center for Computational and Integrative Biology, Massachusetts General Hospital, Boston, MA 02114; Program in Medical and Population Genetics, Broad Institute, Cambridge, MA 02142; Center for the Study of Inflammatory Bowel Disease, Massachusetts General Hospital, Boston, MA 02114;

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http://dx.doi.org/10.1073/pnas.1512289112DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4534235PMC
August 2015

Discovery of a Small-Molecule Probe for V-ATPase Function.

J Am Chem Soc 2015 Apr 20;137(16):5563-8. Epub 2015 Apr 20.

∥Center for Computational and Integrative Biology, Massachusetts General Hospital, 185 Cambridge Street, Boston, Massachusetts 02114, United States.

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http://dx.doi.org/10.1021/jacs.5b02150DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4416280PMC
April 2015

HDAC6 inhibitors modulate Lys49 acetylation and membrane localization of β-catenin in human iPSC-derived neuronal cells.

ACS Chem Biol 2015 Mar 8;10(3):883-90. Epub 2015 Jan 8.

†Center for Experimental Drugs and Diagnostics, Psychiatric and Neurodevelopmental Genetics Unit, Center for Human Genetic Research, Harvard Medical School and Massachusetts General Hospital, Boston, Massachusetts 02114, United States.

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http://dx.doi.org/10.1021/cb500838rDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4372110PMC
March 2015

Synthesis of oxazocenones via gold(I)-catalyzed 8-endo-dig hydroalkoxylation of alkynamides.

Org Lett 2015 Feb 8;17(3):418-21. Epub 2015 Jan 8.

Center for the Science of Therapeutics, Broad Institute , 415 Main Street, Cambridge, Massachusetts 02142, United States.

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http://dx.doi.org/10.1021/ol503273vDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4323038PMC
February 2015

Target-based identification of whole-cell active inhibitors of biotin biosynthesis in Mycobacterium tuberculosis.

Chem Biol 2015 Jan 31;22(1):76-86. Epub 2014 Dec 31.

Center for Drug Design, University of Minnesota, Minneapolis, MN 55455, USA; Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2014.11.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4305006PMC
January 2015

Small-molecule control of cytokine function: new opportunities for treating immune disorders.

Curr Opin Chem Biol 2014 Dec 15;23:23-30. Epub 2014 Sep 15.

Center for the Science of Therapeutics, Broad Institute, Cambridge, MA 02142, USA. Electronic address:

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5087273PMC
http://dx.doi.org/10.1016/j.cbpa.2014.08.013DOI Listing
December 2014

Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).

Bioorg Med Chem Lett 2014 Dec 28;24(24):5801-5804. Epub 2014 Oct 28.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Ste 327 Johnson, 847, Monroe, Memphis, TN 38163, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0960894X140108
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http://dx.doi.org/10.1016/j.bmcl.2014.10.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5695681PMC
December 2014

NAMPT is the cellular target of STF-31-like small-molecule probes.

ACS Chem Biol 2014 Oct 7;9(10):2247-54. Epub 2014 Aug 7.

Center for the Science of Therapeutics and ∥Howard Hughes Medical Institute, Broad Institute , 7 Cambridge Center, Cambridge, Massachusetts 02142, United States.

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http://dx.doi.org/10.1021/cb500347pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4201331PMC
October 2014

Atg16L1 T300A variant decreases selective autophagy resulting in altered cytokine signaling and decreased antibacterial defense.

Proc Natl Acad Sci U S A 2014 May 12;111(21):7741-6. Epub 2014 May 12.

Broad Institute, Cambridge, MA 02142;Center for Computational and Integrative Biology, Massachusetts General Hospital, Boston, MA 02114;Gastrointestinal Unit, Massachusetts General Hospital, Harvard Medical School, Boston, MA 02114;Center for the Study of Inflammatory Bowel Disease, Massachusetts General Hospital, Boston, MA 02114;

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http://dx.doi.org/10.1073/pnas.1407001111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4040621PMC
May 2014