Search Results - "SANTINI, Angelina" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

Identification of 4‑(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2)

Identification of 4‑(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2)

by Rowbottom, Martin W, Bain, Gretchen, Calderon, Imelda, Lasof, Taylor, Lonergan, David, Lai, Andiliy, Huang, Fei, Darlington, Janice, Prodanovich, Patricia, Santini, Angelina M, King, Christopher D, Goulet, Lance, Shannon, Kristen E, Ma, Gina L, Nguyen, Katherine, MacKenna, Deidre A, Evans, Jilly F, Hutchinson, John H
Published in Journal of medicinal chemistry (25.05.2017)

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Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis

Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis

by Povero, Davide, Lazic, Milos, McBride, Christopher, Ambrus-Aikelin, Geza, Stansfield, Ryan, Johnson, Casey D, Santini, Angelina M, Pranadinata, Rama F, McGeough, Matthew D, Stafford, Jeffrey A, Hoffman, Hal M, Feldstein, Ariel E, Veal, James M, Bain, Gretchen
Published in The Journal of pharmacology and experimental therapeutics (01.08.2023)

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JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

by Ambrus-Aikelin, Geza, Takeda, Katsuyuki, Joetham, Anthony, Lazic, Milos, Povero, Davide, Santini, Angelina M, Pranadinata, Rama, Johnson, Casey D, McGeough, Matthew D, Beasley, Federico C, Stansfield, Ryan, McBride, Christopher, Trzoss, Lynnie, Hoffman, Hal M, Feldstein, Ariel E, Stafford, Jeffrey A, Veal, James M, Bain, Gretchen, Gelfand, Erwin W
Published in Scientific reports (19.08.2023)

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Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis

Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis

by Bain, Gretchen, Shannon, Kristen E, Huang, Fei, Darlington, Janice, Goulet, Lance, Prodanovich, Patricia, Ma, Gina L, Santini, Angelina M, Stein, Adam J, Lonergan, Dave, King, Christopher D, Calderon, Imelda, Lai, Andiliy, Hutchinson, John H, Evans, Jilly F
Published in The Journal of pharmacology and experimental therapeutics (01.01.2017)

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Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

by Ambrus-Aikelin, Geza, Takeda, Katsuyuki, Joetham, Anthony, Lazic, Milos, Povero, Davide, Santini, Angelina M, Pranadinata, Rama, Johnson, Casey D, McGeough, Matthew D, Beasley, Federico C, Stansfield, Ryan, McBride, Christopher, Trzoss, Lynnie, Hoffman, Hal M, Feldstein, Ariel E, Stafford, Jeffrey A, Veal, James M, Bain, Gretchen, Gelfand, Erwin W
Published in Scientific reports (16.11.2023)

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Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding

Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding

by Stein, Adam J, Bain, Gretchen, Prodanovich, Pat, Santini, Angelina M, Darlington, Janice, Stelzer, Nina M P, Sidhu, Ranjinder S, Schaub, Jeffrey, Goulet, Lance, Lonergan, Dave, Calderon, Imelda, Evans, Jilly F, Hutchinson, John H
Published in Molecular pharmacology (01.12.2015)

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Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti‐inflammatory 5‐lipoxygenase‐activating protein inhibitor

Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti‐inflammatory 5‐lipoxygenase‐activating protein inhibitor

by Bain, Gretchen, King, Christopher D., Schaab, Kevin, Rewolinski, Melissa, Norris, Virginia, Ambery, Claire, Bentley, Jane, Yamada, Masanori, Santini, Angelina M., Wetering de Rooij, Jeroen, Stock, Nicholas, Zunic, Jasmine, Hutchinson, John H., Evans, Jilly F.
Published in British journal of clinical pharmacology (01.03.2013)

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Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung

Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung

by Stebbins, Karin J, Broadhead, Alex R, Baccei, Christopher S, Scott, Jill M, Truong, Yen P, Coate, Heather, Stock, Nicholas S, Santini, Angelina M, Fagan, Patrick, Prodanovich, Patricia, Bain, Gretchen, Stearns, Brian A, King, Christopher D, Hutchinson, John H, Prasit, Peppi, Evans, Jilly F, Lorrain, Daniel S
Published in The Journal of pharmacology and experimental therapeutics (01.03.2010)

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Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation

Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation

by Bain, Gretchen, Lorrain, Daniel S, Stebbins, Karin J, Broadhead, Alex R, Santini, Angelina M, Prodanovich, Pat, Darlington, Janice, King, Christopher D, Lee, Catherine, Baccei, Christopher, Stearns, Brian, Troung, Yen, Hutchinson, John H, Prasit, Peppi, Evans, Jilly F
Published in The Journal of pharmacology and experimental therapeutics (01.07.2011)

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Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation

Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation

by Lorrain, Daniel S., Bain, Gretchen, Correa, Lucia D., Chapman, Charles, Broadhead, Alex R., Santini, Angelina M., Prodanovich, Patricia P., Darlington, Janice V., Stock, Nicholas S., Zunic, Jasmine, King, Christopher D., Lee, Catherine, Baccei, Christopher S., Stearns, Brian, Roppe, Jeffrey, Hutchinson, John H., Prasit, Peppi, Evans, Jilly F.
Published in European journal of pharmacology (25.08.2010)

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Pharmacological Characterization of 3-[3-tert-Butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic Acid (AM103), a Novel Selective 5-Lipoxygenase-Activating Protein Inhibitor That Reduces Acute and Chronic Inflammation

Pharmacological Characterization of 3-[3-tert-Butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic Acid (AM103), a Novel Selective 5-Lipoxygenase-Activating Protein Inhibitor That Reduces Acute and Chronic Inflammation

by Lorrain, Daniel S, Bain, Gretchen, Correa, Lucia D, Chapman, Charles, Broadhead, Alex R, Santini, Angelina M, Prodanovich, Pat, Darlington, Janice V, Hutchinson, John H, King, Christopher, Lee, Catherine, Baccei, Christopher, Li, Yiwei, Arruda, Jeannie M, Evans, Jilly F
Published in The Journal of pharmacology and experimental therapeutics (01.12.2009)

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5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-(( S)-1-Acetyl-2,3-dihydro-1 H-indol-2-ylmethoxy)-3- tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1 H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)—A potent FLAP inhibitor

5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-(( S)-1-Acetyl-2,3-dihydro-1 H-indol-2-ylmethoxy)-3- tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1 H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)—A potent FLAP inhibitor

by Stock, Nicholas, Baccei, Christopher, Bain, Gretchen, Broadhead, Alex, Chapman, Charles, Darlington, Janice, King, Christopher, Lee, Catherine, Li, Yiwei, Lorrain, Daniel S., Prodanovich, Pat, Rong, Haojing, Santini, Angelina, Zunic, Jasmine, Evans, Jilly F., Hutchinson, John H., Prasit, Peppi
Published in Bioorganic & medicinal chemistry letters (2010)

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N-acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the α2δ subunit of voltage gated calcium channels

N-acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the α2δ subunit of voltage gated calcium channels

by JONGWON LIM, STOCK, Nicholas, AIYAR, Jayashree, VENKATRAMAN, Shankar, PRACITTO, Richard, BOUERES, Julia K, MUNOZ, Benito, CHAUDHARY, Ashok, SANTINI, Angelina M, ORR, Karia, SCHAFFHAUSER, Hervé, BEZVERKOV, Robert E
Published in Bioorganic & medicinal chemistry letters (19.04.2004)

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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

by McBride, Christopher, Trzoss, Lynnie, Povero, Davide, Lazic, Milos, Ambrus-Aikelin, Geza, Santini, Angelina, Pranadinata, Rama, Bain, Gretchen, Stansfield, Ryan, Stafford, Jeffrey A., Veal, James, Takahashi, Ryan, Ly, Justin, Chen, Shu, Liu, Liling, Nespi, Marika, Blake, Robert, Katewa, Arna, Kleinheinz, Tracy, Sujatha-Bhaskar, Swathi, Ramamoorthi, Nandhini, Sims, Jessica, McKenzie, Brent, Chen, Mark, Ultsch, Mark, Johnson, Matthew, Murray, Jeremy, Ciferri, Claudio, Staben, Steven T., Townsend, Michael J., Stivala, Craig E.
Published in Journal of medicinal chemistry (10.11.2022)

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Overcoming Preclinical Safety Obstacles to Discover ( S )- N -((1,2,3,5,6,7-Hexahydro- s -indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5 H -pyrazolo[5,1- b ][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Overcoming Preclinical Safety Obstacles to Discover ( S )- N -((1,2,3,5,6,7-Hexahydro- s -indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5 H -pyrazolo[5,1- b ][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

by McBride, Christopher, Trzoss, Lynnie, Povero, Davide, Lazic, Milos, Ambrus-Aikelin, Geza, Santini, Angelina, Pranadinata, Rama, Bain, Gretchen, Stansfield, Ryan, Stafford, Jeffrey A., Veal, James, Takahashi, Ryan, Ly, Justin, Chen, Shu, Liu, Liling, Nespi, Marika, Blake, Robert, Katewa, Arna, Kleinheinz, Tracy, Sujatha-Bhaskar, Swathi, Ramamoorthi, Nandhini, Sims, Jessica, McKenzie, Brent, Chen, Mark, Ultsch, Mark, Johnson, Matthew, Murray, Jeremy, Ciferri, Claudio, Staben, Steven T., Townsend, Michael J., Stivala, Craig E.
Published in Journal of medicinal chemistry (10.11.2022)

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Abstract 2083: Discovery of ETX-19477, a novel and selective PARG inhibitor with high potency against tumors with underlying replication stress

Abstract 2083: Discovery of ETX-19477, a novel and selective PARG inhibitor with high potency against tumors with underlying replication stress

by Holleran, John P., Rodems, Tamara S., Sharma, Shweta, Santini, Angelina M., Wuerz, Cindy, Liu, Juping, Tian, Lu, Dosch, Joseph, Nader, Joy, Rivera, Richard, Herath, Shyama, Marakovits, Joseph, McBride, Christopher, Stansfield, Ryan, Salyards, Amy, Veal, James M., Stafford, Jeffrey A., Bain, Gretchen
Published in Cancer research (Chicago, Ill.) (22.03.2024)

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5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor

5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor

by Stock, Nicholas S, Bain, Gretchen, Zunic, Jasmine, Li, Yiwei, Ziff, Jeannie, Roppe, Jeffrey, Santini, Angelina, Darlington, Janice, Prodanovich, Pat, King, Christopher D, Baccei, Christopher, Lee, Catherine, Rong, Haojing, Chapman, Charles, Broadhead, Alex, Lorrain, Dan, Correa, Lucia, Hutchinson, John H, Evans, Jilly F, Prasit, Peppi
Published in Journal of medicinal chemistry (08.12.2011)

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5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3- tert -Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1 H -indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor

5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3- tert -Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1 H -indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor

by Stock, Nicholas S., Bain, Gretchen, Zunic, Jasmine, Li, Yiwei, Ziff, Jeannie, Roppe, Jeffrey, Santini, Angelina, Darlington, Janice, Prodanovich, Pat, King, Christopher D., Baccei, Christopher, Lee, Catherine, Rong, Haojing, Chapman, Charles, Broadhead, Alex, Lorrain, Dan, Correa, Lucia, Hutchinson, John H., Evans, Jilly F., Prasit, Peppi
Published in Journal of medicinal chemistry (08.12.2011)

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Pharmacology of AM211, a Potent and Selective Prostaglandin D 2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation

Pharmacology of AM211, a Potent and Selective Prostaglandin D 2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation

by Bain, Gretchen, Lorrain, Daniel S., Stebbins, Karin J., Broadhead, Alex R., Santini, Angelina M., Prodanovich, Pat, Darlington, Janice, King, Christopher D., Lee, Catherine, Baccei, Christopher, Stearns, Brian, Troung, Yen, Hutchinson, John H., Prasit, Peppi, Evans, Jilly F.
Published in The Journal of pharmacology and experimental therapeutics (01.07.2011)

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5-Lipoxygenase-Activating Protein Inhibitors: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic Acid (AM103)

5-Lipoxygenase-Activating Protein Inhibitors: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic Acid (AM103)

by Hutchinson, John H, Li, Yiwei, Arruda, Jeannie M, Baccei, Christopher, Bain, Gretchen, Chapman, Charles, Correa, Lucia, Darlington, Janice, King, Christopher D, Lee, Catherine, Lorrain, Dan, Prodanovich, Pat, Rong, Haojing, Santini, Angelina, Stock, Nicholas, Prasit, Peppi, Evans, Jilly F
Published in Journal of medicinal chemistry (08.10.2009)

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