CURRICULUM VITAE
`
`Jeffrey David Winkler
`
`Department of Chemistry
`University of Pennsylvania
`Philadelphia, PA 19104
`email: winkler@sas.upenn.edu
`
`(215) 898-0052
`
`
`
`
`2020
`
`
`
`2019
`
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`2019
`
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`2019
`
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`2018
`
`
`2018
`
`
`2018
`
`2018
`
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`
`
`NAME:
`
`ADDRESS:
`
`
`
`
`PHONE:
`
`LEGAL CONSULTING EXPERIENCE (last five years; on behalf of underlined):
`
`
`2020
`
`Cooley LLP Expert in organic chemistry (Liquidia Technologies v.
`United Therapeutics Corporation)
`
`Winston & Strawn Expert in organic chemistry
`(FWK Holdings, LLC, et. al. v. Merck, Glenmark Pharmaceuticals,
`et. al.)
`
`McNeely Hare and War Expert in organic chemistry
`(Amerigen Pharmaceuticals Ltd v. United Therapeutics Corporation)
`
`
`
`Womble Bond Dickinson Expert in organic chemistry
`(Ferring Pharmaceuticals Inc. et. al. v. Lupin Inc., No 19-cv-913 (D.
`Del))
`
`Bereskin & Parr (Canada) Expert in organic chemistry (ViiV
`Healthcare Co., Shionogi & Co., Ltd., and ViiV Healthcare UK (No. 3)
`Ltd. v. Gilead Sciences, Inc.)
`
`Baker Hostetler/McGuireWoods Expert in organic and medicinal
`chemistry (Eli Lilly v. Eagle Pharmaceuticals, Case No. 1:17-cv-1293;
`Expert Report, Deposition, Trial Testimony)
`
`Crowell & Moring Expert in organic chemistry (Chen v. Jung and
`Sawyers, Case No. 2:18-cv-02015-R-KS; Expert Report, Deposition and
`Trial Testimony)
`
`McCarthy Tetrault Expert in organic chemistry (Akebia v. FibroGen)
`
`Greenberg Traurig Expert in organic chemistry (Leo Pharma v. Actavis;
`Expert Reports and Deposition)
`
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`

`

`2018
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`2018
`
`2017
`
`2017
`
`2017
`
`2017
`
`2017
`
`2016
`
`2015
`
`2015
`
`Quinn Emanuel Expert in organic chemistry (Mitsubishi Tanabe Pharma
`Corp. and Janssen Pharmaceuticals v. Apotex, Aurobindo Pharma, Dr.
`Reddy’s Laboratories, Hetero USA, Indoco Remedies, InvaGen
`Pharmaceuticals, Inc., Laurus Labs, 4, Macleods Pharma, MSN
`Laboratories, Prinston Pharmaceuticals, Sandoz, Teva Pharmaceuticals
`and Zydus Pharmaceuticals)
`
`Quinn Emanuel Expert in organic chemistry (Celgene v. International
`Union of Bricklayers and Allied Craft Workers Local 1 Health Fund;
`Expert Report and Deposition)
`
`Polsinelli PC Expert in organic chemistry (Leo Pharma v. Perrigo; Expert
`Reports and Deposition)
`
`Jones Day Expert in organic chemistry (Accord Healthcare Limited v.
`Celgene Corporation, HP-2017-000036, HP-2017-000037)
`
`Gibbons P. C. Expert in organic chemistry (Cipla v. Sunovion Pharm.
`Inc.; 15-cv-424 (LPS) (D. Del., Expert Reports and Deposition)
`
`Durie Tangri Expert in organic chemistry (Plexxikon Inc. v. Novartis
`Pharmaceuticals Corporation)
`
`Arnold Porter Kaye Scholer Expert in organic chemistry (Pfizer v. Micro
`Labs, Sun, Prinston, Zydus and Breckenridge)
`
`Crowell Moring Expert in organic chemistry (Hetero Laboratories v.
`Boehringer Ingelheim)
`
`DLA Piper Expert in organic chemistry (SteadyMed Therapeutics, Inc. v.
`United Therapeutics Corp.; Expert Report and Deposition)
`
`Finnegan, Henderson, Farabow, Garrett & Dunner, LLP Expert in
`organic chemistry (Principia Biopharma)
`
`EDUCATION:
`
`Post-doctoral:
`
`Graduate:
`
`Columbia University. January 1982-August 1983.
`Research Director: Professor Ronald Breslow.
`
`Columbia University. September 1977-December 1981.
`M.A. 1978, M.Phil., Ph.D. 1981.
`Thesis Advisor: Professor Gilbert Stork.
`
`Undergraduate:
`
`Harvard College. September 1973-June 1977.
`A. B. cum laude in Chemistry, 1977.
`
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`

`PROFESSIONAL
`EXPERIENCE:
`
`Undergraduate Chair, Department of Chemistry, University
`of Pennsylvania, July 2018-
`
`Merriam Professor of Chemistry,
`University of Pennsylvania, January 2001-
`
`Professor, University of Pennsylvania
`Department of Chemistry, July 1996-
`
`Founding Member, University of Pennsylvania
`Center for Cancer Pharmacology, May 1998-present
`
`Associate Professor, University of Pennsylvania,
`Department of Chemistry, July 1990-June 1996
`
`Member, University of Pennsylvania Cancer Center,
`July 1993-present
`
`Assistant Professor, University of Chicago,
`Department of Chemistry, September 1983-June 1990
`
`Ira H. Abrams Memorial Award for Distinguished Teaching, 2016
`Elected Member, John Morgan Society, 2014
`Visiting Scholar, Harbin University of Science and Technology, 2013
`Fellow, Japan Society for the Promotion of Science, 2010
`Lindback Award for Distinguished Teaching, 2007
`Philadelphia Organic Chemists’ Club Award, 2006
`American Chemical Society Cope Scholar Award, 2000
`Chairman, Philadelphia Organic Chemists' Club, 1995
`American Cyanamid Young Faculty Award, 1989-1992
`NIH-NCI Research Career Development Award, 1988-1993
`Alfred P. Sloan Research Fellow, 1987-1989
`Merck Foundation Award for Faculty Development, 1985
`American Cancer Society Postdoctoral Fellow, 1982-1983
`
`AWARDS & HONORS:
`
`PROFESSIONAL ACTIVITIES
`
`Member, Atrin Pharmaceuticals, Scientific Advisor Board, 2013-present
`Co-Founder, Pinpoint Therapeutics, 2018-present
`
`INVITED LECTURES SINCE 2002:
`
`2002-2003
`Plenary Lecturer, French-American Chemical Society, 2002
`Pfizer Lecturer, University of
`Waterloo, 2002
`
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`Novartis Lecturer, University of Texas at Austin
`University of Rochester
`Emory University
`Alan Johnson Lecturer, University of Sussex, UK
`Invited Speaker, Gordon Research Conference on Natural Products, July 2003
`
`2003-2004
`Stanford University
`University of California at Berkeley
`Glaxo Smith Kline
`Amgen
`Biogen
`Yale University
`Boston College
`State University of New York at Stony Brook
`
`2004-05
`Plenary Speaker, Belgian Organic Chemistry Symposium
`Abbott Laboratories Distinguished Lecturer in Organic Synthesis, Notre Dame University
`California Institute of Technology
`
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`2005-2006
`GlaxoSmithKline Symposium Lecture
`Wyeth Synthesis Course (Princeton, Collegeville, Pearl River, Cambridge)
`
`2006-2007
`Roche Lectureship, University of Colorado
`Invited Lecturer, 12th Brazilian Meeting on Organic Synthesis
`
`2007-2008
`Bristol-Myers Squibb
`University of Wisconsin-Madison
`
`2008-2009
`National Taiwan University
`National Tsing Hua University, Taiwan
`Keynote Speaker, 9th International Symposium on Organic Reactions, 2008 (Chiayi, Taiwan)
`
`2009-2010
`Hamilton College
`Kyoto University, Katsura Campus
`Kyoto University, Yoshida North Campus
`Tokyo Institute of Technology
`University of Tokyo
`Chiba University
`Hokkaido University
`Tohoku University
`Eli Lilly and Company
`Pfizer Cambridge
`
`2010-2011
`
`University of Cambridge
`University College London
`Imperial College London
`University of Cardiff
`Paristech
`University of Lyon
`ETH
`Invited Lecturer, Breslow Symposium, Anaheim, CA
`
`2011-2012
`
`Plenary Lecturer, 1st Korea International Forum on Organic Chemistry, Seoul
`Frontiers in Chemistry Lecture, Case Western Reserve University
`University of Iowa
`University of Maryland Eastern Shores
`Towson University
`
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`Liquidia - Exhibit 1003 - Page 6
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`Liquidia - Exhibit 1003 - Page 6
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`2012-2013
`
`Morgan State University
`University of Maryland Eastern Shores
`Plenary Lecture, Paquette Symposium, Ohio State University
`Amgen (Thousand Oaks, CA)
`Harbin Institute of Technology
`Shanghai Institute of Organic Chemistry
`Peking University
`Tsinghua University
`University of Science and Technology of China (USTC)
`Soochow University
`Glaxo (Shanghai)
`Fudan University
`
`2013-2014
`
`Muhlenberg College
`Cutaneous Oncology Retreat, Villanova Conference Center
`Invited Speaker, “PAINS, Promiscuity and Probes-Are Drug and Probe Development Mutually
`Exclusive?” 248th ACS National Meeting - San Francisco, CA - August 2014
`
`2014-2015
`
`Rider University
`University of Maryland Eastern Shores
`Wesleyan University
`
`2015-2016
`
`Incyte
`Bard College
`Michigan State University
`
`2016-2017
`Louisiana State University
`St. Johns University
`Hanoi National University
`
`2017-2018
`Cutaneous Oncology Retreat, Wistar Institute
`Radiobiology and Imaging Program, University of Pennsylvania and Abramson Cancer Center
`
`2018-2019
`Universite Cote dAzur
`Philipps-University Marburg
`Leibniz Universitat Hannover
`
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`ESPCI (Ecole Superiere de Physique et de Chimie Industrielles de La Ville de Paris)
`Ecole Polytechnique, Paris
`14th Winter Conference on Medicinal and Bioorganic Chemistry, Steamboat Springs, CO
`
`PUBLICATIONS:
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`1.
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`2.
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`3.
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`5.
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`7.
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`9.
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`L. Blaszczak, J. Winkler, S. O'Kuhn, "A New Synthesis of Olefins from Ketones via
`Coupling of Lithium Dialkylcuprates with Enol Phosphate Diesters," Tetrahedron
`Lett. 1976, 4405-4408.
`G. Stork, C. Shiner, J. Winkler, "Stereochemical Control of the Internal Michael
`Reaction. A New Construction of trans-Hydrindane Systems," J. Am. Chem. Soc.
`1982, 104, 310-312.
`G. Stork, J. Winkler, C. Shiner, "Stereochemical Control of Intramolecular Conjugate
`Addition. A Short, Highly Stereoselective Synthesis of Adrenosterone," J. Am.
`Chem. Soc. 1982, 104, 3767-3768.
`G. Stork, J. Winkler, N. Saccomano, "Stereochemical Control in the Construction of
`Vicinally Substituted Cyclopentanes and Cyclohexanes. Intramolecular Conjugate
`Addition of β-Ketoester Anions," Tetrahedron Lett. 1983, 465-468.
`J. Winkler, E.Coutouli-Argyropoulou, R. Leppkes, R. Breslow, "An Artificial
`Transaminase Carrying A Synthetic Macrocyclic Binding Group," J. Am. Chem. Soc.
`1983, 105, 7198-7199.
`6. W. Weiner, J. Winkler, S. Zimmerman, R. Breslow, "Mimics of Tryptophan Syn-
`thetase and of Biochemical Dehydroalanine Formation," J. Am. Chem. Soc. 1985,
`107, 4093-4094.
`R. Breslow, A. W. Czarnik, M. Lauer, H. Leppkes, J. Winkler, S. Zimmerman,
`"Mimics of Transaminase Enzymes," J. Am. Chem. Soc. 1986, 108, 1969-1979.
`J. Winkler, V. Sridar, "Stereochemical Control of Transannular Radical Cyclizations.
`A New Approach to the Synthesis of Linearly Fused Cyclopentanoids," J. Am. Chem.
`Soc. 1986, 108, 1708-1709.
`J. Winkler, J. Hey, P. Williard, "Inside-Outside Stereoisomerism: A Synthesis of
`trans-Bicyclo[5.3.1]undecan-11-one," J. Am. Chem. Soc. 1986, 108, 6425-6427.
`J. Winkler, P. Hershberger, J. Springer, "A Stereoselective Synthesis of the
`Azaspiroundecane Ring System of (-)-Histrionicotoxin from (+)-Glutamic Acid,"
`Tetrahedron Lett. 1986, 5177-5180.
`J. Winkler, J. Hey, S. Darling, "Studies Directed Towards the Synthesis of the
`Taxane Diterpenes: A Remarkable Rearrangement," Tetrahedron Lett. 1986, 5959-
`5962.
`J. Winkler, J. Hey, F. Hannon, P. Williard, "Intramolecular Photoaddition of Diox-
`olenones. An Efficient Method for the Synthesis of Medium-Sized Rings," Hete-
`rocycles 1987, 25, 55-60.
`J. Winkler, K. Deshayes, "Photodynamic Macrocycles," J. Am. Chem. Soc. 1987,
`109, 2190-2191.
`J. Winkler, K. Henegar, P. Williard, "Inside-Outside Stereoisomerism II. Synthesis of
`the Carbocyclic Ring System of the Ingenane Diterpenes via the Intramolecular
`Dioxolenone Photocycloaddition," J. Am. Chem. Soc. 1987, 109, 2850-2851.
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`10.
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`11.
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`12.
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`13.
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`14.
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`16.
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`19.
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`23.
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`24.
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`22.
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`15. K. Henegar, J. Winkler, "A New Method for the Synthesis of Dioxolenones via the
`Carboxylation of Ketone Enolates with Anisyl Cyanoformate," Tetrahedron Lett.
`1987, 1051-1054.
`J. Winkler, C. Muller, R. Scott, "A New Method for the Formation of Nitrogen-
`Containing Ring Systems via the Intramolecular Photocycloaddition of Vinylogous
`Amides. A Synthesis of Mesembrine," J. Am. Chem. Soc. 1988, 110, 4831-4832.
`J. Winkler, J. Hey, P. Williard, "Inside-Outside Stereoisomerism III. The Synthesis of
`trans-Bicyclo[4.3.1]Decan-10-one," Tetrahedron Lett. 1988, 4691-4694.
`J. Winkler, V. Sridar, "Eight-Membered Ring Templates for Stereoselective Radical
`Cyclizations," Tetrahedron Lett. 1988, 6219-6222.
`J. Winkler, K. Deshayes, B. Shao, "Photodynamic Systems for Metal Ion Transport,"
`J. Am. Chem. Soc. 1989, 111, 769-770.
`J. Winkler, P. Hershberger, "A Stereoselective Synthesis of (-)-Perhydrohistrioni-
`cotoxin," J. Am. Chem. Soc. 1989, 111, 4852-4856.
`J. Winkler, V. Sridar, L. Rubo, J. Hey, N. Haddad, "Inside-Outside Stereoisomerism
`IV. An Unusual Rearrangement of the trans-Bicyclo[5.3.1]Undecan-11-yl Radical,"
`J. Org. Chem. 1989, 54, 3004-3006.
`J. Winkler, C. Lee, L. Rubo, C. Muller, P. J. Squattrito, "Stereoselective Synthesis of
`the Tricyclic Skeleton of the Taxane Diterpenes. The First C-Silylation of a Ketone
`Enolate," J. Org. Chem. 1989, 54, 4491-4493.
`J. Winkler, V. Sridar, M. Siegel, "Ten-Membered Ring Templates for Stereoselective
`Radical Cyclizations," Tetrahedron Lett. 1989, 4943-4946.
`J. Winkler, C. Muller, J. Hey, R. Ogilvie, N. Haddad, P. Squattrito, P. Williard, "The
`Effect of Chromophore Transposition on the Stereochemical Outcome of the
`Intramolecular Dioxenone Photocycloaddition Reaction," Tetrahedron Lett. 1989,
`5211-5214.
`J. Winkler, N. Haddad, R. Ogilvie, "Intramolecular Photocycloaddition and Retro-
`Mannich Fragmentation of Tertiary Vinylogous Amides," Tetrahedron Lett. 1989,
`5703-5704.
`J. Winkler, M. Finck-Estes, "Carbon-Carbon Bond Formation Under Aqueous
`Reaction Conditions Using Sulfonium and Selenonium Salt Electrophiles,"
`Tetrahedron Lett. 1989, 7293-7296.
`J. Winkler, R. Scott, P. Williard, "Asymmetric Induction in the Vinylogous Amide
`Photocycloaddition. A Formal Synthesis of Vindorosine," J. Am. Chem. Soc. 1990,
`112, 8971-8975.
`J. Winkler, B. Hong, "Inside-Outside Stereoisomerism V. Synthesis and Reactivity
`of Bicyclo[n.3.1]alkanones with trans Intrabridgehead Stereochemistry," J. Am.
`Chem. Soc. 1991, 113, 8839-8846.
`J. Winkler, E. Gretler, "Stereoselective Cyclopropanation of Homoallylic Alcohols.
`Formal Attachment of a Cyclopropane to a Preexisting Ring," Tetrahedron Lett.
`1991, 5733-36.
`J. Winkler and D. Subrahmanyam, "Studies Directed Towards the Synthesis of
`Taxol: Preparation of C-13 Oxygenated Taxane Congeners," Tetrahedron 1992,
`48, 7049-7056.
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`25.
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`26.
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`27.
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`28.
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`29.
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`30.
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`32.
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`39.
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`31.
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`J. Winkler, E. Gretler, P. Williard,"Studies Directed Towards the Synthesis of the
`Ingenane Diterpenes. An Unexpected Synthesis of trans-Bicyclo[5.3.0]Decanes,"
`J. Org. Chem. 1993, 58, 1973-1975.
`J. Winkler, B. Hong, A. Bahador, M. Kazanietz, P. Blumberg, "Synthesis of Ingenol
`Analogs with Affinity for Protein Kinase C," Bioorg. Med. Chem. Lett. 1993, 3, 577-
`580.
`J. Winkler, B. Shao, "On the Stereoselectivity of the Intramolecular Dioxenone
`Photocycloaddition Reaction," Tetrahedron Lett. 1993, 3355-3358.
`J. Winkler, M. Siegel, and J. Stelmach, "A Highly Stereoselective Approach to the
`Synthesis of the Manzamine Alkaloids via the Intramolecular Vinylogous Amide
`Photocycloaddition," Tetrahedron Lett. 1993, 6509-6512.
`J. Winkler, K. Deshayes and Bin Shao, "Photochemical Binding, Release and
`Transport of Metal Ions." In Bioorganic Photochemistry, 1993, Volume II, H.
`Morrison, Ed., Wiley, New York, Chapter 3, pp. 169-196.
`J. Winkler, M. Siegel, "A Novel Photochemical Synthesis of Pyrroles from β-
`Ketoviny-logous Amides," Tetrahedron Lett. 1993, 7697-7700.
`37. M. Siegel and J. Winkler, "Photochemistry of Enamines and Enaminones" In The
`Chemistry of Enamines, 1994, S. Patai and Z. Rappaport, Eds., Wiley, New York,
`637-679.
`J. Winkler, K. Henegar, B. Hong and P. Williard, "Inside-Outside Stereoisomerism.
`6. Synthesis of trans-Bicyclo[4.4.1]Undecan-11-one and the First Stereoselective
`Construction of the Ingenane Nucleus," J. Am. Chem. Soc. 1994, 116, 4183-4188.
`J. Winkler, B. Hong, "Trans-Bicyclo-[5.3.1]undecan-11-one," in Photochemical Key
`Steps in Organic Synthesis 1994, J. Mattay and A. Griesbeck, Eds., VCH, Weinheim,
`109-111.
`40. K. Davis, T. Berrodin, T., J. Stelmach, J. Winkler, M. Lazar, "Endogenous RXRs can
`function as hormone receptors in pituitary cells," Molecular and Cell Biology 1994,
`14, 7105-7110.
`J. Winkler, S. Kim, K. Condroski, A. Asensio, K. N. Houk, "Stereoselective
`Synthesis of Polycyclic Ring Systems via the Tandem Diels-Alder Reaction," J. Org.
`Chem. 1994, 59, 6879-6881.
`J. Winkler, B. Hong, "Transannular Radical Reactions in Bicycloalkanes with
`‘Inside-Outside’ Stereochemistry. An Unusual Bridgehead Hydroxylation,"
`Tetrahedron Lett. 1995, 683-686.
`J. Winkler, H. Kim, S. Kim, "A Highly Efficient Synthesis of Taxanes via the
`Tandem Diels-Alder Reaction,” Tetrahedron Lett. 1995, 687-691.
`J. Winkler, B. Hong, A. Bahador, M. Kazanietz, P. Blumberg, "Methodology for the
`Synthesis of 3-Oxygenated Ingenanes--The First Ingenol Analogs with High Affinity
`for Protein Kinase C," J. Org. Chem. 1995, 60, 1381-1390.
`J. Winkler, S. Bhattacharya, F. Liotta, R. Batey, G. Heffernan, D. Cladingboel, R.
`Kelly, "Stereoselective Synthesis of A Synthon for the A-Ring of Taxol from R-(+)-
`Verbenone," Tetrahedron Lett. 1995, 2211-2215.
`J. Winkler, B. Hong, S. Kim, N. Lewin, P. Blumberg, "On the Protein Kinase C
`Pharmacophore: Synthesis and Biological Activity of 4-Hydroxylated Analogs of
`Ingenol," Synlett 1995, 533-535.
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`41.
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`42.
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`43.
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`48.
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`51.
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`53.
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`54.
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`49.
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`47. H. Li, S. Narasimhulu, L. Havran, J. Winkler, T. Poulos, "Crystal Structure of
`Cytochrome P-450 Complexed with Its Catalytic Product, 5-Exo-
`Hydroxycamphor," J. Am. Chem. Soc. 1995, 117, 6297-6299.
`J. Winkler, C. Mazur, and F. Liotta, "[2+2]Photocycloaddition-Fragmentation
`Strategies for the Synthesis of Natural and Unnatural Products,” Chem. Rev. 1995,
`95, 2003-2020.
`J. Winkler, "The Tandem Diels-Alder Reaction," Chem. Rev. 1996, 96, 167-176.
`J. Winkler, J. Stelmach, J. Axten, "Two Highly Efficient Syntheses of Scalemic
`Azocines," Tetrahedron Lett. 1996, 4317-4320.
`J. Winkler, S. Bhattacharya, R. Batey, "Synthesis of a Taxinine Congener via the
`Intramolecular Diels-Alder Cycloaddition," Tetrahedron Lett. 1996, 8069-8072.
`J. Winkler, J. Holland, D. Peters, "Synthesis of Cyclopropyl Taxane Analogs via
`Sequential Diels-Alder Reactions," J. Org. Chem. 1996, 61, 9074-9075.
`J. Winkler and P. Axelsen, "A Model for the Taxol/Epothilone Pharmacophore,"
`Bioorg. Med. Chem. Lett. 1996, 6, 2963-2966.
`J. Winkler, H. Kim, S. Kim. K. Ando, K. Houk, "Stereoselective Synthesis of the
`Taxane Ring System via the Tandem Diels-Alder Cycloaddition," J. Org. Chem.
`1997, 62, 2957-2962.
`J. Winkler, J. Stelmach, M. Siegel, N. Haddad, J. Axten, W. Dailey, "An Approach
`to the Synthesis of the Manzamine Alkaloids via the Vinylogous Amide
`Photocycloaddition-retro-Mannich Fragmentation-Mannich Closure Cascade," Isr.
`J. Chem. 1997, 37, 47-67.
`S. Kim, J. Winkler, "Approaches to the Synthesis of Ingenol," Chem. Soc. Rev.
`1997, 26, 387-400.
`J. Winkler, E. Doherty, "Control of Relative Stereochemistry of Quaternary Carbon
`Centers via the Intramolecular Dioxenone Photocycloaddition: An Approach to the
`Synthesis of Saudin," Tetrahedron Lett. 1998, 2253-2256.
`J. Winkler, C. Bowen, V. Michelet, "Photodynamic Fluorescent Metal Ion Sensors
`with ppb Sensitivity," J. Am. Chem. Soc. 1998, 120, 3237-3242.
`S. Narasimhulu, L. Havran, P. Axelsen, J. Winkler, “Interactions of Substrate and
`Product with Cytochrome P450,” Arch. Biochem. Biophys. 1998, 353, 228-238.
`J. Winkler, J. Axten, H. Hammach, Y. Kwak, M. Lucero, K. Houk,
`"Stereoselective Synthesis of the Tetracyclic Core of the Manzamine Alkaloids via
`the Vinylogous Amide Photocycloaddition Cascade: A Remarkable Effect of
`Azocine Unsaturation on the Stereochemical Outcome of the Photocycloaddition
`Reaction," Tetrahedron 1998, 54, 7045-7056.
`J. Winkler, W. McCoull, "Diels-Alder Reaction on Solid Supports Using Polymer-
`Bound Oxazolidinones," Tetrahedron Lett. 1998, 4935-4936.
`J. Winkler, J. Axten, "The First Total Syntheses of Ircinol A, Ircinal A, and
`Manzamines A and D," J. Am. Chem. Soc. 1998, 120, 6425-6426.
`J. Winkler, Y. Kwak, “An Approach to Controlled Oligomerization via Iterative
`Diels-Alder Cycloadditions on Solid Supports,” J. Org. Chem. 1998, 63, 8634-
`8635.
`J. Axten, L. Krim, H. Kung, J. Winkler, “An Improved Synthesis of dl-threo-
`Methylphenidate. Preparation and Biological Evaluation of Novel Analogs,” J.
`Org. Chem 1998, 63, 9628-9629.
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`67.
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`65.
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`J. Winkler, S. Kim, S. Harrison, N. Lewin, P. Blumberg, "Synthesis and Biological
`Evaluation of Highly Functionalized Analogs of Ingenol: The Importance of
`Hydrophobic Effects on Binding to Protein Kinase C," J. Am. Chem. Soc., 1999,
`121, 296-300.
`66. G. Collins, L. Choi, K. Ewing, V. Michelet, C. Bowen, and J. Winkler,
`“Photoinduced Switching of Metal Complexation by Quinolinospiropyranindolines
`in Polar Solvents,” J. Chem. Soc., Chem. Commun. 1999, 321-322.
`J. Winkler, J. Holland, J. Kasparec, and P. Axelsen, “Synthesis and Biological
`Evaluation of Constrained Epothilone Analogs: The Efficient Synthesis of Eleven-
`Membered Rings by Olefin Metathesis,” Tetrahedron (invited contribution to
`Symposium-in-Print on Olefin Metathesis in Synthesis) 1999, 55, 8199-8214.
`J. Axten, R. Ivy, L. Krim, J. Winkler, “An Enantioselective Synthesis of d-threo-
`Methylphenidate," J. Am. Chem. Soc. 1999, 121, 6511-6512.
`J. Winkler, E. Doherty, “ The First Total Synthesis of (+)-Saudin," J. Am. Chem.
`Soc. 1999, 121, 7425-7426.
`L. Evans, G. Collins, R. Shaffer, V. Michelet, J. Winkler, :Selective Metals
`Determination with a Photoreversible Spirobenzopyran," Anal. Chem. 1999, 71,
`5322. 5327.
`J. Winkler, E. Piatnitski, J. Mehlmann, J. Kasparec, P. Axelsen, “Design and
`Synthesis of Novel Foldamers Based on an Anthracene Diels-Alder Adduct,”
`Angew. Chem. Int. Ed. Engl. 2001, 40, 743-745.
`72. Y. Kwak, J. Winkler, "Synthesis of 6-Aza-Bicyclo[3.2.1]Octan-3-Ones via
`Vinylogous Imide Photochemistry: An Approach to the Synthesis of the Hetisine
`Alkaloids," J. Am. Chem. Soc. 2001, 123, 7429-7430.
`F. Ichinose, J. Erana-Garcia, J. Hromi, Y. Raveh, R. Jones, L. Krim, M. Clark, J.
`Winkler, K. Bloch, W. Zapol, “Nebulized sildenafil is a selective pulmonary
`vasodilator in lambs with acute pulmonary hypertension,” Critical Care Medicine
`2001, 29, 1000-1005.
`G. Collins, R. Morris, J. Wei, M. Smith, M. Hammond, V. Michelet, J. Winkler,
`“Spectrophotometric Detection of Trace Copper Levels in Jet Fuel,” Energy &
`Fuels 2002, in press.
`J. Winkler, M. Rouse, M. Greaney, S. Harrison, Y. Jeon, “The First Total Synthesis
`of Ingenol, J. Am. Chem. Soc. 2002, 124, 9726-9728.
`J. Winkler, S. Harrison, M. Greaney, M. Rouse, “Mechanistic Observations on the
`Unusual Reactivity of Dioxenone Photosubstrates in the Synthesis of Ingenol,”
`Synthesis (Special Issue Dedicated to Professor Dieter Seebach) 2002, 2150.
`J. Winkler, K. Quinn, C. MacKinnon, S. Hiscock, E. McLaughlin, “Tandem Diels-
`Alder Approach to the Synthesis of Eleutherobin,” Org. Lett. 2003, 5, 1805.
`R. Doerksen, B. Chen, J. Yuan, J. Winkler, M. Klein, “Novel Conformationally-
`Constrained β-Peptides Characterized by 1H NMR Chemical Shifts,,” Chem.
`Commun., 2003, 2534-2535.
`D. Liu; S. Choi; B. Chen; R.J. Doerksen; D.J. Clements; J.D. Winkler; M.L. Klein;
`W.F. DeGrado. “Nontoxic Membrane-Active Antimicrobial Arylamide Oligomers,”
`Angew. Chem. Int. Ed. 2004, 43, 1158-1162.
`J. Winkler, P. Mikochik, “Synthesis of Cyclic Hemiketals and Spiroketals from
`Dioxanorbornanes,” Org. Lett, 2004, 6, 3735-3737.
`
`73.
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`74.
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`75.
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`76.
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`77.
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`78.
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`79.
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`81.
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`82.
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`83.
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`84.
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`85.
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`86.
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`87.
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`J. Winkler, S. Asselin, S. Shepard, J. Yuan, “Metathesis Approach to the Synthesis
`of Polyheterocyclic Structures from Oxanorbornenes,” Org. Lett, 2004, 6, 3821-
`3824.
`H. Kung, S. Newman, S. Choi, S. Oya, C. Hou, Z. Zhuang, P. Acton, K. Ploessl, J.
`Winkler, M. Kung, “2-(2-(Dimethylaminomethyl)phenoxy)-5-iodophenylamine: An
`Improved Serotonin Transporter Imaging Agent,” J. Med. Chem. 2004, 47, 5258-
`5264.
`J. Winkler, E. McLaughlin, “Intramolecular Photocycloaddition of Dioxenones
`with Alkynes: Formation of Secondary Photoproducts from Cyclobutene
`Photoadducts,” Org. Lett, 2005, 7, 227-229.
`J. Winkler, K. Oh, S. Asselin, “Synthesis of Highly Functionalized Furanones via
`Aldol Reaction of 3-Silyloxyfurans,” Org. Lett, 2005, 7, 387-389.
`J. Winkler, E. Lee, L. Nevels, “A Pauson-Khand Approach to the Synthesis of
`Ingenol,” Org. Lett., 2005, 7, 1489-1491.
`J. Winkler, K. Oh, “A One-Step Synthesis of 2,3-Dihydro-4H-pyran-4-ones from
`3-Ethoxy α,β -Unsaturated Lactones,” Org. Lett. 2005, 7, 2421-2423.
`S. Choi, D. Clements, V. Pophristic, I. Ivanov, S. Vemparala, J. Bennett, M. Klein,
`J. Winkler, W. DeGrado, “The Design and Evaluation of Heparin-Binding
`Foldamers,” Angew. Chem. Int. Ed. 2005, 44, 6685-6689.
`88. W. Wang, W. Ho, D. Dicker, C. MacKinnon, J. Winkler, R. Marmorstein, W. El-
`Deiry, “Acridine Derivatives Activate p53 and Induce Tumor Cell Death Through
`Bax,” Cancer Biology and Therapy 2005, i, 893-898.
`J. Winkler, E. Lee, “Photochemical Route to the Synthesis of Thiolane 1-Oxides,”
`J. Am. Chem. Soc. 2006, 128, 9040-9041.
`J. Winkler, A. Londregan, M. Hamann, “Antimalarial Activity of a New Family of
`Analogs of Manzamine A,” Org. Lett., 2006, 8, 2591-2594.
`J. Winkler, A. Londregan, J. Ragains, M. Hamann, “Synthesis and Biological
`Evaluation of Manzamine Analogues,” Org. Lett., 2006, 8, 3407-3409.
`J. Winkler, J. Ragains, “Intramolecular Photocycloaddition of Vinylogous Amides
`with Allenes: A Novel Approach to the Synthesis of Pyrroles,” Org. Lett., 2006, 8,
`4031-33.
`J. Winkler, S. Asselin, “Synthesis of Novel Heterocyclic Structures via Reaction of
`Isocyanides with S-trans-Enones,” Org. Lett., 2006, 8, 3975-77.
`J. Ragains, J. Winkler, “Pseudosymmetry in azabicyclo[2.1.1.]hexanes. A
`Stereoselective Construction of the Bicyclic Core of the Ring System of
`Peduncularine,” Org. Lett., 2006, 8, 4437-4440.
`95. W. Jiang, P. Mikochik, J. Ra, H. Lei, K. Flaherty, J. Winkler, F. Spitz, “HIV
`Protease Inhibitor Nelfinavir Inhibits Growth of Human Melanoma Cells by
`Induction of Cell Cycle Arrest,” Cancer Research 2007, 67, 1221-1227.
`J. Winkler, A. Londregan, M. Hamann, “Synthetic Modification of Manzmaine A
`via Grubbs Metathesis. Novel Structures with Enhanced Antibacterial and
`Antiprotozoal Properties,” Org. Lett. 2007, 9, 4467-4469.
`S. Choi, G. Vilaire, C. Marcinkiewicz, J. Winkler, J. Bennett, W. Degrado, “Small
`Molecule Inhibitors of Integrin a2b1,” J. Med. Chem. 2007, 50, 5457-5462.
`J. Winkler, M. Fitzgerald, “Stereoselective Synthesis of 8-Substituted 6-
`Azabicyclo[3.2.1]-octan-3-ones,” Synlett 2009, 562-564.
`
`89.
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`90.
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`91.
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`92.
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`93.
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`94.
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`96.
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`99.
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`101.
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`S. Choi, A. Isaacs, D. Clements, D. Liu, H. Kim. R. Scott, J. Winkler, W. Degrado,
`“De Novo Design and in vivo Activity of Conformationally Restrained
`Antimicrobial Arylamide Foldamers,” Proc. Natl. Acad. Sci, 2009, 106, 6968-6973.
`100. H. Jo, M. Fitzgerald, J. Winkler, “An Unusual Pathway to Cyclobutane Formation
`via Desulfurative Intramolecular Photocycloaddition to an Enone Benzothiazoline
`Pair,” Org. Lett 2009, 11, 1685-1687.
`J. Winkler, A. Isaacs, L. Holderbaum. V. Tatard, N. Dahmane, “Design and
`Synthesis of Inhibitors of Hedgehog Signaling Based on the Alkaloid Cyclopamine
`Org. Lett 2009, 11, 2824-2827.
`102. T. Yano, S. Kassovska-Bratinova, J. Teh, J. Winkler, K. Sullivan, A. Isaacs, N.
`Schechter, H. Rubin, “Reduction of Clofazimine by Mycobaterial Type 2
`NADH:Quinone Oxidoreductase: A Pathway for the Generation of Bactericidal
`Levels of Reactive Oxygen Species,” J. Biol. Chem. 2011, 286, 10276-10287 (doi:
`10.1074/ jbc.M110. 200501).
`103. T. Haimowitz, M. Fitzgerald, J. Winkler, “Studies Directed Toward the Synthesis
`of Nakadomarin A,” Tetrahedron Lett. 2011, 52, 2162-2164 (invited contribution in
`honor of Professor Harry Wasserman).
`104. A. Adeniji, B. Twenter, M. Byrns, Y. Jin, J. Winkler, T. Penning, “Discovery of
`Substituted 3-(Phenylamino)benzoic acids as Potent and Selective Inhibitors of
`Type 5 17β-Hydroxysteroid Dehydrogenase (AKR1C3),” Bioorg. Med. Chem. Lett,
`2011, 21, 1464-1468.
`105. Z. Zhang, V. Baubet, C. Ventocilla, C. Xiang, N. Dahmane, J. Winkler,
`“Stereoselective Synthesis of F-Ring Saturated Estrone-Derived Inhibitors of
`Hedgehog Signaling Based on Cyclopamine,” Org. Lett 2011, 13, 4786-4789.
`106. A. Isaacs, C. Xiang, V. Baubet, N. Dahmane, J. Winkler, “Studies Directed toward
`the Eludication of the Pharmacophore of Steroid-Based Hedgehog Signaling
`Inhibitors,” Org. Lett 2011, 13, 5140-5143.
`J. Winkler, A. Isaacs, C. Xiang, V. Baubet, N. Dahmane, “Design, Synthesis and
`Biological Evaluation of Estrone-Derived Hedgehog Signaling Inhibitors,”
`Tetrahedron 2011, 67, 10261-10266 (invited contribution in honor of Professor
`Gilbert Stork).
`J. Winkler, B. Twenter, T. Gendrineau, “Synthesis of Substituted Phenazines via
`Palladium-Catalyzed Aryl Ligation,” Heterocycles, 2012, 84, 1345-1353 (invited
`contribution in honor of Professor Albert Padwa).
`109. A. Adeniji, B. Twenter, M. Byrns, U. Jin, M. Chen, J. Winkler, T. Penning,
`“Development of Potent and Selective Inhibitors of Aldo-Keto Reductase 1C3 (type
`5 17β-hydroxysteroid dehydrogenase) Based on N-Phenyl-Aminobenzoates and
`Their Structure Activity Relationships,” J. Med. Chem. 2012, 55, 2311-2323
`110. Q. McAfee, Z. Zhang, A. Samanta, S. Levi, X. Ma, S. Piao, J. Lynch, T. Uehara, A.
`Sepulveda, L. Davis, J. Winkler, R. Amaravadi, “A Novel Autophagy Inhibitor with
`Single Agent Antitumor Activity Reproduces the Phenotype of a Genetic
`Autophagy Deficiency,” Proc. Natl. Acad. Sci. 2012, 109, 8253-8258.
`J. Qin, P. Xie, C. Ventochilla, G. Zhou, A. Vultur, Q. Chen, Q. Liu, M. Herlyn, J.
`Winkler, R. Marmorstein, “Identification of a Novel Family of BRAF(V600E)
`Inhibitors, J. Med. Chem. 2012, 55, 5220-5230.
`112. M. Chen, A. Adeniji, B. Twenter, J. Winkler, D. Christianson, T. Penning, “Crystal
`Structures of AKR1C3 Containing an N-(Aryl)amino-benzoate Inhibitor and a
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`108.
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`120.
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`Bifunctional AKR1C3 Inhibitor and Androgen Receptor Antagonist. Therapeutic
`Leads for Castrate Resistant Prostate Cancer,” Bioorg. Med. Chem. Lett. 2012, 22,
`3492-3497.
`113. R. Amaravadi, J. Winkler, “Lys05: A New Lysosomal Autophagy Inhibitor,”
`Autophagy 2012, 8, 1383-1384.
`114. X. Ma, S. Piao, S. Dey, Q. Mcafee, G. Karakousis, J. Villaneuva, L. Hart, S. Levi,
`J. Hu, G. Zhang, R. Lazova, V. Klump, J. Pawalek, X. Xu, W. Xu, L. Schuchter, M.
`Davies, M. Herlyn, J. Winkler, C. Koumenis, R. Amaravadi, “ Targeting ER
`Stress-Induced Autophagy Overcomes BRAF Inhibitor Resistance in Melanoma,” J.
`Clin. Invest. 2014, 124, 1406-1417.
`115. V. Hubbard-Lucey, Y. Shono, K. Maurer, M. West, N. Singer, C. Ziegler, C.
`Lezcano, A. Motta, K. Schmid, S. Levi, G. Murphy, C. Liu, J. Winkler, R.
`Amaravadi, G. Rogler, A. Dickinson, E. Holler, M. van den Brink, K. Cadwell,
`“Autophagy Gene Atg16l1 Prevents Lethal T Cell Alloreactivity Mediated by
`Dendritic Cells,” Immunity, 2014, 4, 579-591.
`J. Chatwichien, S. Basu, M. Murphy, M. Hamann, J. Winkler, “Design, Synthesis
`and Biological Evaluation of β-Carboline Dimers Based on the Structure of
`Neokauluamine,” “Tet. Lett. 2015, 56, 3515-3517.
`117. Y. Nishimura, N. McLaughlin, J. Pan, S. Goldstein, S. Hafenstein, H. Shimizu, J.
`Winkler, J. Bergelson, “The Suramin Derivative NF449 Interacts with the 5-Fold
`Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and
`Heparan Sulfate,” PLOS Pathogens 2015, 11 (10): e1005184.
`I. Vasilevskaya, M. Selvakumaran, L. Hierro, S. Goldstein, J. Winkler. P.
`O’Dwyer, “Inhibition of JNK Sensitizes Hypoxic Colon Cancer Cells to DNA
`Damaging Agents, “ Clin. Cancer Res. 2015, 21, 4143-4152.
`119. C. Natale, E. Duperret, J. Zhang, R. Sadeghi, D. Ankit, K. O’Brien, R. Cookson, J.
`Winkler, T. Ridky “Sex Steroids Regulate Skin Pigmentation Through Nonclassical
`Membrane-Bound Receptors,” eLife, 2016, 5, e15164. PMID: 27115344.
`J. Chatwichien, S. Basu, A. Budina-Kolomets, M. Murphy and J. Winkler,
`“PUMA-Dependent Apoptosis in NSCLC Cancer Cells by a Dimeric β-Carboline,
`Bioorg. Med. Chem. Lett. 2016, 26, 4884-4887.
`121. M. Grasso, M. Estrada, C. Ventocilla, M. Samanta, J. Maksimoska, J. Villaneuva,
`J. Winkler, R. Marmorstein, “Chemically Linked Vemurafenib Inhibitors Promote
`an Inactive BRAF/V600E Conformation,” ACS Chemical Biology 2016, 11, 2876-
`2888.
`122. L. DeVorkin, M. Hattersley, P. Kim, J. Ries, J. Lum, J. Spowart, M. Anglesio, D.
`Huntsman, S. Levi, J. Winkler, R. Amaravadi, A. Tinker, “Autophagy Inhibition
`Enhances Sunitinib Efficacy in Clear Cell Ovarian Carcinoma,” Molecular Cancer
`Research 2017, 15, 250-258.
`123. T. Gade, E. Tucker, M. Nakazawa, S. Hunt. W. Wong, B. Krock, C. Weber, G.
`Madolski, J. Winkler, R. Amaravadi, M. Simon, “Ischemia Induces Quiescence and
`Autophagy Dependence in Hepatocellular Carcinoma,” Radi