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Tytuł:
Impact of mRNA chemistry and manufacturing process on innate immune activation.
Autorzy:
Nelson J; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Sorensen EW; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Mintri S; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Rabideau AE; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Zheng W; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Besin G; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Khatwani N; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Su SV; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Miracco EJ; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Issa WJ; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Hoge S; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Stanton MG; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
Joyal JL; Moderna Inc., 200 Technology Square, Cambridge, MA, USA.
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Źródło:
Science advances [Sci Adv] 2020 Jun 24; Vol. 6 (26), pp. eaaz6893. Date of Electronic Publication: 2020 Jun 24 (Print Publication: 2020).
Typ publikacji:
Journal Article; Research Support, Non-U.S. Gov't
Czasopismo naukowe
Tytuł:
Optimization of Lipid Nanoparticles for Intramuscular Administration of mRNA Vaccines.
Autorzy:
Hassett KJ; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Benenato KE; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Jacquinet E; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Lee A; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Woods A; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Yuzhakov O; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Himansu S; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Deterling J; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Geilich BM; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Ketova T; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Mihai C; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Lynn A; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
McFadyen I; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Moore MJ; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Senn JJ; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Stanton MG; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Almarsson Ö; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Ciaramella G; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Brito LA; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA. Electronic address: .
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Źródło:
Molecular therapy. Nucleic acids [Mol Ther Nucleic Acids] 2019 Apr 15; Vol. 15, pp. 1-11. Date of Electronic Publication: 2019 Feb 07.
Typ publikacji:
Journal Article
Czasopismo naukowe
Tytuł:
A Novel Amino Lipid Series for mRNA Delivery: Improved Endosomal Escape and Sustained Pharmacology and Safety in Non-human Primates.
Autorzy:
Sabnis S; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Kumarasinghe ES; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Salerno T; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Mihai C; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Ketova T; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Senn JJ; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Lynn A; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Bulychev A; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
McFadyen I; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Chan J; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Almarsson Ö; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Stanton MG; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA.
Benenato KE; Moderna Therapeutics, 200 Technology Square, Cambridge, MA 02139, USA. Electronic address: .
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Źródło:
Molecular therapy : the journal of the American Society of Gene Therapy [Mol Ther] 2018 Jun 06; Vol. 26 (6), pp. 1509-1519. Date of Electronic Publication: 2018 Mar 14.
Typ publikacji:
Journal Article
MeSH Terms:
Lipids/*chemistry
Nanoparticles/*chemistry
RNA, Messenger/*administration & dosage
RNA, Messenger/*chemistry
Animals ; Primates ; Rats
Czasopismo naukowe
Tytuł:
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Autorzy:
Katz JD; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address: jason_.
Haidle A; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Childers KK; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Zabierek AA; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Jewell JP; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hou Y; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Altman MD; Department of Structural Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Szewczak A; Department of In Vitro Sciences, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Chen D; Department of Drug Metabolism, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Harsch A; Department of Drug Metabolism, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hayashi M; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Warren L; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hutton M; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Nuthall H; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Su HP; Department of Structural Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
Munshi S; Department of Structural Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA.
Stanton MG; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Davies IW; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Munoz B; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Northrup A; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jan 01; Vol. 27 (1), pp. 114-120. Date of Electronic Publication: 2016 Oct 22.
Typ publikacji:
Journal Article
MeSH Terms:
Drug Design*
Protein Kinase Inhibitors/*pharmacology
Pyrimidinones/*pharmacology
Pyrroles/*pharmacology
Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Cell Line ; Crystallography, X-Ray ; Dose-Response Relationship, Drug ; Humans ; Models, Molecular ; Molecular Structure ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Serine-Threonine Kinases/antagonists & inhibitors ; Protein Serine-Threonine Kinases/metabolism ; Pyrimidinones/chemical synthesis ; Pyrimidinones/chemistry ; Pyrroles/chemical synthesis ; Pyrroles/chemistry ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł:
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Autorzy:
Haidle AM; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Childers KK; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Zabierek AA; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Katz JD; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Jewell JP; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hou Y; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Altman MD; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Szewczak A; Department of In Vitro Sciences, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Chen D; Department of Drug Metabolism, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Harsch A; Department of Drug Metabolism, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hayashi M; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Warren L; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Hutton M; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Nuthall H; Department of Neuroscience, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Stanton MG; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Davies IW; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Munoz B; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Northrup A; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jan 01; Vol. 27 (1), pp. 109-113. Date of Electronic Publication: 2016 Aug 25.
Typ publikacji:
Journal Article
MeSH Terms:
Alzheimer Disease/*drug therapy
Protein Kinase Inhibitors/*pharmacology
Pyrimidinones/*pharmacology
Pyrroles/*pharmacology
Alzheimer Disease/metabolism ; Animals ; Dose-Response Relationship, Drug ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Molecular Structure ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/metabolism ; Protein Serine-Threonine Kinases/antagonists & inhibitors ; Protein Serine-Threonine Kinases/metabolism ; Pyrimidinones/chemistry ; Pyrimidinones/metabolism ; Pyrroles/chemistry ; Pyrroles/metabolism ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł:
Systematic chemical modifications of single stranded siRNAs significantly improved CTNNB1 mRNA silencing.
Autorzy:
Chang W; Discovery Chemistry, Merck Research Laboratories, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, United States. Electronic address: .
Pei Y; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
Guidry EN; Discovery Chemistry, Merck Research Laboratories, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, United States.
Zewge D; Process Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States.
Parish CA; Process Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States.
Sherer EC; Structural Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States.
DiMuzio J; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
Zhang H; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
South VJ; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
Strapps WR; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
Sepp-Lorenzino L; RNA Biology, Merck Research Laboratories, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, United States.
Colletti SL; Discovery Chemistry, Merck Research Laboratories, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, United States.
Stanton MG; Process Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States.
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Sep 15; Vol. 26 (18), pp. 4513-4517. Date of Electronic Publication: 2016 Jul 28.
Typ publikacji:
Journal Article
MeSH Terms:
Gene Silencing*
RNA, Messenger/*genetics
RNA, Small Interfering/*genetics
beta Catenin/*genetics
HEK293 Cells ; Humans
Czasopismo naukowe
Tytuł:
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Autorzy:
Sloman DL; Discovery Chemistry, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Noucti N; Discovery Chemistry, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Altman MD; Chemistry Modeling and Informatics, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Chen D; Drug Metabolism and Pharmacokinetics, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Mislak AC; Drug Metabolism and Pharmacokinetics, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Szewczak A; CNS Pharmacology, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Hayashi M; CNS Pharmacology, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Warren L; CNS Pharmacology, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Dellovade T; Core Pharmacology, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Wu Z; Core Pharmacology, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Marcus J; Neuroscience Drug Discovery, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Walker D; Pharmaceutical Research and Development, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Su HP; Structural Biology, 770 Sumneytown Pike, West Point, PA 19486, United States.
Edavettal SC; Structural Biology, 770 Sumneytown Pike, West Point, PA 19486, United States.
Munshi S; Structural Biology, 770 Sumneytown Pike, West Point, PA 19486, United States.
Hutton M; Neuroscience Drug Discovery, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Nuthall H; Neuroscience Drug Discovery, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
Stanton MG; Discovery Chemistry, Merck and Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02215, United States.
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Sep 01; Vol. 26 (17), pp. 4362-6. Date of Electronic Publication: 2016 Feb 06.
Typ publikacji:
Journal Article
MeSH Terms:
Enzyme Inhibitors/*chemical synthesis
Heterocyclic Compounds/*chemistry
Protein Serine-Threonine Kinases/*antagonists & inhibitors
Animals ; Crystallography, X-Ray ; Dogs ; Enzyme Activation/drug effects ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Heterocyclic Compounds/pharmacology ; Humans ; Inhibitory Concentration 50 ; Molecular Weight ; Rats ; Solubility
Czasopismo naukowe
Tytuł:
5'-(E)-Vinylphosphonate: A Stable Phosphate Mimic Can Improve the RNAi Activity of siRNA-GalNAc Conjugates.
Autorzy:
Parmar R; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Willoughby JL; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Liu J; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Foster DJ; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Brigham B; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Theile CS; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Charisse K; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Akinc A; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Guidry E; Merck and Co., Inc, 770 Sumneytown Pike, West Point, PA, 19486, USA.
Pei Y; Merck and Co., Inc, 770 Sumneytown Pike, West Point, PA, 19486, USA.
Strapps W; Merck and Co., Inc, 770 Sumneytown Pike, West Point, PA, 19486, USA.
Cancilla M; Merck and Co., Inc, 770 Sumneytown Pike, West Point, PA, 19486, USA.
Stanton MG; Merck and Co., Inc, 770 Sumneytown Pike, West Point, PA, 19486, USA.
Rajeev KG; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Sepp-Lorenzino L; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Manoharan M; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Meyers R; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Maier MA; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA.
Jadhav V; Alnylam Pharmaceuticals, 300 Third Street, Cambridge, MA, 02142, USA. .
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Źródło:
Chembiochem : a European journal of chemical biology [Chembiochem] 2016 Jun 02; Vol. 17 (11), pp. 985-9. Date of Electronic Publication: 2016 Apr 28.
Typ publikacji:
Journal Article
MeSH Terms:
RNA Interference*
Acetylgalactosamine/*chemistry
Organophosphonates/*chemistry
RNA, Small Interfering/*chemistry
Vinyl Compounds/*chemistry
Animals ; Apolipoproteins B/antagonists & inhibitors ; Apolipoproteins B/genetics ; Apolipoproteins B/metabolism ; Argonaute Proteins/antagonists & inhibitors ; Argonaute Proteins/genetics ; Argonaute Proteins/metabolism ; Cells, Cultured ; Factor IX/antagonists & inhibitors ; Factor IX/genetics ; Factor IX/metabolism ; Hepatocytes/cytology ; Hepatocytes/drug effects ; Hepatocytes/metabolism ; Humans ; Lipoproteins, LDL/blood ; Mice ; Mice, Inbred C57BL ; Organophosphonates/pharmacology ; RNA, Small Interfering/metabolism ; RNA-Binding Proteins ; RNA-Induced Silencing Complex/chemistry ; RNA-Induced Silencing Complex/metabolism ; Transcription Factors/metabolism ; Vinyl Compounds/pharmacology
Czasopismo naukowe
Tytuł:
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Autorzy:
Methot JL; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hoffman DM; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Witter DJ; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Stanton MG; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Harrington P; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hamblett C; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Siliphaivanh P; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Wilson K; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hubbs J; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Heidebrecht R; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Kral AM; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Ozerova N; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Fleming JC; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Wang H; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Szewczak AA; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Middleton RE; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Hughes B; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Cruz JC; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Haines BB; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Chenard M; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Kenific CM; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Harsch A; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Secrist JP; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
Miller TA; Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
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Źródło:
ACS medicinal chemistry letters [ACS Med Chem Lett] 2014 Jan 02; Vol. 5 (4), pp. 340-5. Date of Electronic Publication: 2014 Jan 02 (Print Publication: 2014).
Typ publikacji:
Journal Article
Czasopismo naukowe
Tytuł:
Medicinal chemistry of siRNA delivery.
Autorzy:
Stanton MG; Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., West Point, Pennsylvania 19486, USA. matthew_stanton@merck.com
Colletti SL
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Źródło:
Journal of medicinal chemistry [J Med Chem] 2010 Nov 25; Vol. 53 (22), pp. 7887-901. Date of Electronic Publication: 2010 Aug 31.
Typ publikacji:
Journal Article
MeSH Terms:
Drug Carriers*
RNA, Small Interfering/*administration & dosage
Animals ; Drug Discovery ; Humans ; Lipids/chemistry ; Nanoparticles ; Polymers/chemistry ; RNA, Small Interfering/chemistry ; RNA, Small Interfering/pharmacokinetics ; Structure-Activity Relationship ; Transfection
Czasopismo naukowe
Tytuł:
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Autorzy:
Stanton MG; Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. matthew_stanton@merck.com
Hubbs J
Sloman D
Hamblett C
Andrade P
Angagaw M
Bi G
Black RM
Crispino J
Cruz JC
Fan E
Farris G
Hughes BL
Kenific CM
Middleton RE
Nikov G
Sajonz P
Shah S
Shomer N
Szewczak AA
Tanga F
Tudge MT
Shearman M
Munoz B
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Jan 15; Vol. 20 (2), pp. 755-8. Date of Electronic Publication: 2009 Nov 13.
Typ publikacji:
Journal Article
MeSH Terms:
Acetates/*chemistry
Amyloid Precursor Protein Secretases/*metabolism
Fluorine/*chemistry
Piperidines/*chemistry
Acetates/chemical synthesis ; Acetates/pharmacokinetics ; Amyloid beta-Peptides/genetics ; Amyloid beta-Peptides/metabolism ; Animals ; Diazonium Compounds/chemistry ; Disease Models, Animal ; Mice ; Mice, Transgenic ; Peptide Fragments/genetics ; Peptide Fragments/metabolism ; Piperidines/chemical synthesis ; Piperidines/pharmacokinetics ; Rats ; Receptors, Notch/metabolism
Czasopismo naukowe
Tytuł:
Quantitative analysis of histone deacetylase-1 selective histone modifications by differential mass spectrometry.
Autorzy:
Lee AY; Department of Proteomics, Merck Research Laboratories, Merck & Co. Inc., Rahway, New Jersey 07065, USA.
Paweletz CP
Pollock RM
Settlage RE
Cruz JC
Secrist JP
Miller TA
Stanton MG
Kral AM
Ozerova ND
Meng F
Yates NA
Richon V
Hendrickson RC
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Źródło:
Journal of proteome research [J Proteome Res] 2008 Dec; Vol. 7 (12), pp. 5177-86.
Typ publikacji:
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:
Gene Expression Regulation, Enzymologic*
Histone Deacetylases/*metabolism
Histones/*chemistry
Mass Spectrometry/*methods
Proteomics/*methods
Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Chromatography, Liquid/methods ; False Positive Reactions ; Histones/metabolism ; Humans ; Peptides/chemistry ; Protein Isoforms ; Proteome ; ROC Curve ; Spectrometry, Mass, Electrospray Ionization
Czasopismo naukowe
Tytuł:
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Autorzy:
Methot JL; Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. joey_ />Chakravarty PK
Chenard M
Close J
Cruz JC
Dahlberg WK
Fleming J
Hamblett CL
Hamill JE
Harrington P
Harsch A
Heidebrecht R
Hughes B
Jung J
Kenific CM
Kral AM
Meinke PT
Middleton RE
Ozerova N
Sloman DL
Stanton MG
Szewczak AA
Tyagarajan S
Witter DJ
Secrist JP
Miller TA
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 01; Vol. 18 (3), pp. 973-8. Date of Electronic Publication: 2008 Jan 07.
Typ publikacji:
Journal Article
MeSH Terms:
Histone Deacetylase Inhibitors*
Models, Molecular*
Benzene Derivatives/*chemical synthesis
Benzene Derivatives/*pharmacology
Benzene Derivatives/chemistry ; Binding Sites/drug effects ; Histone Deacetylase 1 ; Histone Deacetylase 2 ; Histone Deacetylases/chemistry ; Histone Deacetylases/metabolism ; Humans ; Molecular Structure ; Protein Isoforms ; Repressor Proteins ; Structure-Activity Relationship
Czasopismo naukowe
Czasopismo naukowe
Tytuł:
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.
Autorzy:
Sanderson PE; Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. phil_ />Stanton MG
Dorsey BD
Lyle TA
McDonough C
Sanders WM
Savage KL
Naylor-Olsen AM
Krueger JA
Lewis SD
Lucas BJ
Lynch JJ
Yan Y
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Źródło:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Mar 10; Vol. 13 (5), pp. 795-8.
Typ publikacji:
Comparative Study; Journal Article
MeSH Terms:
Aza Compounds/*chemistry
Aza Compounds/*pharmacology
Enzyme Inhibitors/*chemistry
Enzyme Inhibitors/*pharmacology
Indoles/*chemistry
Indoles/*pharmacology
Thrombin/*antagonists & inhibitors
Administration, Oral ; Animals ; Aza Compounds/pharmacokinetics ; Dogs ; Enzyme Inhibitors/pharmacokinetics ; Humans ; Indoles/pharmacokinetics ; Models, Molecular ; Partial Thromboplastin Time ; Pyridines/chemistry ; Pyridines/pharmacology ; Structure-Activity Relationship ; Substrate Specificity ; Thrombin/metabolism ; Trypsin/metabolism
Czasopismo naukowe

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