M
Marie A. Holahan
Researcher at Merck & Co.
Publications - 65
Citations - 2200
Marie A. Holahan is an academic researcher from Merck & Co.. The author has contributed to research in topics: In vivo & Glycoprotein IIb/IIIa inhibitors. The author has an hindex of 26, co-authored 64 publications receiving 1912 citations. Previous affiliations of Marie A. Holahan include United States Military Academy.
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Journal ArticleDOI
Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
Robert W. Myers,Hong-Ping Guan,Juliann Ehrhart,Aleksandr Petrov,Srinivasa Prahalada,Effie Tozzo,Xiaodong Yang,Marc M. Kurtz,Maria E. Trujillo,Dinko Gonzalez Trotter,Danqing Feng,Shiyao Xu,George J. Eiermann,Marie A. Holahan,Daniel Rubins,Stacey Conarello,Xiaoda Niu,Sandra C. Souza,Corin O. Miller,Jinqi Liu,Ku Lu,Wen Feng,Ying Li,Ronald E. Painter,James A. Milligan,Huaibing He,Franklin Liu,Aimie Ogawa,Douglas Wisniewski,Rory J. Rohm,Liyang Wang,Michelle Bunzel,Ying Qian,Wei Zhu,Hongwu Wang,Bindu Bennet,Lisa LaFranco Scheuch,Guillermo Fernandez,Cai Li,Michael Klimas,Gaochao Zhou,Margaret van Heek,Tesfaye Biftu,Ann E. Weber,David E. Kelley,Nancy A. Thornberry,Mark D. Erion,Daniel M. Kemp,Iyassu K. Sebhat +48 more
TL;DR: MK-8722 is developed, a potent, direct, allosteric activator of all 12 mammalian AMPK complexes that induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia in rodents and rhesus monkeys.
Journal ArticleDOI
Preclinical Characterization of 18F-MK-6240, a Promising PET Tracer for In Vivo Quantification of Human Neurofibrillary Tangles.
Eric D. Hostetler,Abbas Walji,Zhizhen Zeng,Patricia Miller,Idriss Bennacef,Cristian Salinas,Brett Connolly,Liza Gantert,Hyking Haley,Marie A. Holahan,Mona Purcell,Kerry Riffel,Talakad G. Lohith,Paul J. Coleman,Aileen Soriano,Aimie Ogawa,Serena Xu,Xiaoping Zhang,Elizabeth Joshi,Joseph Della Rocca,David Hesk,David J. Schenk,Jeffrey L. Evelhoch +22 more
TL;DR: 18F-MK-6240 is a promising PET tracer for the in vivo quantification of NFTs in AD patients, indicating favorable tracer kinetics and distribution in the brain.
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Discovery of 6-(Fluoro-18F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([18F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs)
Abbas Walji,Eric D. Hostetler,Harold G. Selnick,Zhizhen Zeng,Patricia Miller,Idriss Bennacef,Cristian Salinas,Brett Connolly,Liza Gantert,Marie A. Holahan,Stacey O'Malley,Mona Purcell,Kerry Riffel,Jing Li,Jaume Balsells,Julie A. O'Brien,Stacey Melquist,Aileen Soriano,Xiaoping Zhang,Aimie Ogawa,Serena Xu,Elizabeth Joshi,Joseph Della Rocca,Fred Hess,Joel B. Schachter,David Hesk,David J. Schenk,Arie Struyk,Kerim Babaoglu,Talakad G. Lohith,Yaode Wang,Kun Yang,Jianmin Fu,Jeffrey L. Evelhoch,Paul J. Coleman +34 more
TL;DR: 6 exhibits high specificity and selectivity for binding to NFTs, with suitable physicochemical properties and in vivo pharmacokinetics.
Journal ArticleDOI
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines
Christopher S. Burgey,Robinson Kyle A,Terry A. Lyle,Sanderson Philip E,S. Dale Lewis,Bobby J. Lucas,Julie A. Krueger,Rominder Singh,Cynthia Miller-Stein,Rebecca B. White,Bradley K. Wong,Elizabeth A. Lyle,Peter D. Williams,Craig A. Coburn,Bruce D. Dorsey,James C. Barrow,Maria T. Stranieri,Marie A. Holahan,G. R. Sitko,Jacquelynn J. Cook,Daniel R. McMasters,Colleen M. McDonough,William M. Sanders,Audrey A. Wallace,Franklin C. Clayton,Dennis L. Bohn,Yvonne M. Leonard,Theodore J. Detwiler,Joseph J. Lynch,Youwei Yan,Zhongguo Chen,Lawrence Kuo,Stephen J. Gardell,Jules A. Shafer,Joseph P. Vacca +34 more
TL;DR: A metabolism-based approach to the optimization of the 3-(2-phenethylamino)-6-methylpyrazinone acetamide template resulted in the modification of each of the three principal components comprising this series.
Journal ArticleDOI
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sethu Sankaranarayanan,Marie A. Holahan,Dennis Colussi,Ming-Chih Crouthamel,Viswanath Devanarayan,Joan D. Ellis,Amy S. Espeseth,Adam Gates,Samuel L. Graham,Allison R. Gregro,Daria J. Hazuda,Jerome Hochman,M. Katharine Holloway,Lixia Jin,Jason Kahana,Ming-Tain Lai,Janet Lineberger,Georgia B. McGaughey,Keith P. Moore,Philippe G. Nantermet,Beth Pietrak,Eric A. Price,Hemaka A. Rajapakse,Shaun R. Stauffer,Melissa A. Steinbeiser,Guy R. Seabrook,Harold G. Selnick,Xiao-Ping Shi,Matthew G. Stanton,John Swestock,Katherine Tugusheva,Keala X. Tyler,Joseph P. Vacca,Jacky Wong,Guoxin Wu,Min Xu,Jacquelynn J. Cook,Adam J. Simon +37 more
TL;DR: In vivo proof of concept of CSF Aβ lowering after oral administration of a BACE1 inhibitor in a nonhuman primate is demonstrated, demonstrating excellent concordance with its potency in a cell-based assay.