G
Grogan Michael John
Researcher at Eli Lilly and Company
Publications - 6
Citations - 440
Grogan Michael John is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: In vivo & Cyclopamine. The author has an hindex of 6, co-authored 6 publications receiving 386 citations.
Papers
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Journal ArticleDOI
Discovery of a Potent and Orally Active Hedgehog Pathway Antagonist (IPI-926)
Martin R. Tremblay,Andre Lescarbeau,Grogan Michael John,Eddy Tan,Grace Lin,Brian C. Austad,Lin-Chen Yu,Mark L. Behnke,Somarajan J. Nair,Margit Hagel,Kerry White,James M. Conley,Joseph D. Manna,Teresa M. Alvarez-Diez,Jennifer Hoyt,Caroline N. Woodward,Jens Sydor,Melissa Pink,John R. MacDougall,Matthew Campbell,Jill Cushing,Jeanne A. Ferguson,Michael Curtis,Karen McGovern,Margaret A. Read,Vito J. Palombella,Julian Adams,Alfredo C. Castro +27 more
TL;DR: IPI-926 (compound 28), a novel semisynthetic cyclopamine analogue with substantially improved pharmaceutical properties and potency and a favorable pharmacokinetic profile relative tocyclopamine and compound 2, is discovered.
Journal ArticleDOI
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity
Zahid Quyoom Bonday,Cortez Guillermo S,Grogan Michael John,Stephen Antonysamy,Ken Weichert,Wayne P. Bocchinfuso,Fengling Li,Steven Kennedy,Binghui Li,Mary M. Mader,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Peter Brown,Mohammad S. Eram,Magdalena M. Szewczyk,Dalia Barsyte-Lovejoy,Masoud Vedadi,Masoud Vedadi,Ernesto Guccione,Robert M. Campbell +19 more
TL;DR: The identification and characterization of a novel and selective PRMT5 inhibitor with potent in vitro and in vivo activity is described and compound 1 showed antitumor activity in mouse xenografts when dosed orally and can serve as an excellent probe molecule for understanding the biological function ofPRMT5 in normal and cancer cells.
Patent
Inhibitors of fatty acid amide hydrolase
Julian Adams,Mark L. Behnke,Alfredo C. Castro,Catherine A. Evans,Louis Grenier,Grogan Michael John,Tao Liu,Daniel A. Snyder,Thomas T. Tibbitts +8 more
TL;DR: In this paper, the authors provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I, (II) or (III) and also provide methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound, or a pharmaceutical composition thereof, to a patient in need thereof.
Journal ArticleDOI
The pre-clinical absorption, distribution, metabolism and excretion properties of IPI-926, an orally bioavailable antagonist of the hedgehog signal transduction pathway.
Sherri Smith,Jennifer Hoyt,Nigel Whitebread,Joseph D. Manna,Marisa O. Peluso,Kerrie Faia,Veronica Campbell,Martin R. Tremblay,Somarajan J. Nair,Grogan Michael John,Alfredo C. Castro,Matthew Campbell,Jeanne A. Ferguson,Brendan Arsenault,Jylle Nevejans,Bennett Carter,John Lee,Joi Dunbar,Karen McGovern,Margaret A. Read,Julian Adams,Alexander Constan,Gordon Loewen,Jens Sydor,Vito J. Palombella,John Soglia +25 more
TL;DR: IPI-926 has desirable pre-clinical absorption, distribution, metabolism and excretion properties, and is both a substrate and inhibitor of P-glycoprotein.
Journal ArticleDOI
Development of a Multi Kilogram-Scale, Tandem Cyclopropanation Ring-Expansion Reaction en Route to Hedgehog Antagonist IPI-926
Brian C. Austad,Andrew B. Hague,Priscilla L. White,Stéphane Peluso,Somarajan J. Nair,Kristopher M. Depew,Grogan Michael John,André B. Charette,Lin-Chen Yu,Caroline D. Lory,Louis Grenier,Andre Lescarbeau,Benjamin S. Lane,Lombardy Richard John,Mark L. Behnke,Koney Nii O,James R. Porter,Matthew Campbell,Jeanne Shaffer,Jimin Xiong,Joseph Helble,Michael Foley,Julian Adams,Alfredo C. Castro,Martin R. Tremblay +24 more
TL;DR: In order to perform large-scale cyclopropanation reactions, new iodomethylzinc bis(aryl)phosphate reagents were developed that were found to be both effective and safe.