Search Results - "Mcgrath, Mary E."

Structural basis for RNA replication by the hepatitis C virus polymerase by Appleby, Todd C., Perry, Jason K., Murakami, Eisuke, Barauskas, Ona, Feng, Joy, Cho, Aesop, Fox, David, Wetmore, Diana R., McGrath, Mary E., Ray, Adrian S., Sofia, Michael J., Swaminathan, S., Edwards, Thomas E.

“…Nucleotide analog inhibitors have shown clinical success in the treatment of hepatitis C virus (HCV) infection, despite an incomplete mechanistic understanding…”
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A structural role for hormone in the thyroid hormone receptor by Wagner, Richard L, Apriletti, James W, McGrath, Mary E, West, Brian L, Baxter, John D, Fletterick, Robert J

“…The crystal structure of the rat alpha 1 thyroid hormone receptor ligand-binding domain bound with a thyroid hormone agonist reveals that ligand is completely…”
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Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ by Somoza, John R., Koditek, David, Villaseñor, Armando G., Novikov, Nikolai, Wong, Melanie H., Liclican, Albert, Xing, Weimei, Lagpacan, Leanna, Wang, Ruth, Schultz, Brian E., Papalia, Giuseppe A., Samuel, Dharmaraj, Lad, Latesh, McGrath, Mary E.

“…Idelalisib (also known as GS-1101, CAL-101, IC489666, and Zydelig) is a PI3Kδ inhibitor that has recently been approved for the treatment of several…”
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Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3‑Kinase (PI3K) β Inhibitor by Chandrasekhar, Jayaraman, Dick, Ryan, Van Veldhuizen, Joshua, Koditek, David, Lepist, Eve-Irene, McGrath, Mary E, Patel, Leena, Phillips, Gary, Sedillo, Kassandra, Somoza, John R, Therrien, Joseph, Till, Nicholas A, Treiberg, Jennifer, Villaseñor, Armando G, Zherebina, Yelena, Perreault, Stephane

“…Atropisomerism is a type of axial chirality in which enantiomers or diastereoisomers arise due to hindered rotation around a bond axis. In this manuscript, we…”
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The Structure of the Extracellular Region of Human Hepsin Reveals a Serine Protease Domain and a Novel Scavenger Receptor Cysteine-Rich (SRCR) Domain by Somoza, John R, Ho, Joseph D, Luong, Christine, Ghate, Manjiri, Sprengeler, Paul A, Mortara, Kyle, Shrader, William D, Sperandio, David, Chan, Hedy, McGrath, Mary E, Katz, Bradley A

“…Hepsin is an integral membrane protein that may participate in cell growth and in maintaining proper cell morphology and is overexpressed in a number of…”
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Discovery of a Phosphoinositide 3‑Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856 by Perreault, Stephane, Chandrasekhar, Jayaraman, Cui, Zhi-Hua, Evarts, Jerry, Hao, Jia, Kaplan, Joshua A, Kashishian, Adam, Keegan, Kathleen S, Kenney, Thomas, Koditek, David, Lad, Latesh, Lepist, Eve-Irene, McGrath, Mary E, Patel, Leena, Phillips, Bart, Therrien, Joseph, Treiberg, Jennifer, Yahiaoui, Anella, Phillips, Gary

“…Phosphoinositide 3-kinase (PI3K) β signaling is required to sustain cancer cell growth in which the tumor suppressor phosphatase and tensin homolog (PTEN) has…”
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Discovery of Orally Efficacious Phosphoinositide 3‑Kinase δ Inhibitors with Improved Metabolic Stability by Patel, Leena, Chandrasekhar, Jayaraman, Evarts, Jerry, Forseth, Kristen, Haran, Aaron C, Ip, Carmen, Kashishian, Adam, Kim, Musong, Koditek, David, Koppenol, Sandy, Lad, Latesh, Lepist, Eve-Irene, McGrath, Mary E, Perreault, Stephane, Puri, Kamal D, Villaseñor, Armando G, Somoza, John R, Steiner, Bart H, Therrien, Joseph, Treiberg, Jennifer, Phillips, Gary

“…Aberrant signaling of phosphoinositide 3-kinase δ (PI3Kδ) has been implicated in numerous pathologies including hematological malignancies and rheumatoid…”
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2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors by Patel, Leena, Chandrasekhar, Jayaraman, Evarts, Jerry, Haran, Aaron C, Ip, Carmen, Kaplan, Joshua A, Kim, Musong, Koditek, David, Lad, Latesh, Lepist, Eve-Irene, McGrath, Mary E, Novikov, Nikolai, Perreault, Stephane, Puri, Kamal D, Somoza, John R, Steiner, Bart H, Stevens, Kirk L, Therrien, Joseph, Treiberg, Jennifer, Villaseñor, Armando G, Yeung, Arthur, Phillips, Gary

“…Inhibition of phosphoinositide 3-kinase δ (PI3Kδ) is an appealing target for several hematological malignancies and inflammatory diseases. Herein, we describe…”
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Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif by Perreault, Stephane, Arjmand, Fatima, Chandrasekhar, Jayaraman, Hao, Jia, Keegan, Kathleen S., Koditek, David, Lepist, Eve-Irene, Matson, Clinton K., McGrath, Mary E., Patel, Leena, Sedillo, Kassandra, Therrien, Joseph, Till, Nicholas A., Tomkinson, Adrian, Treiberg, Jennifer, Zherebina, Yelena, Phillips, Gary

“…A series of PI3Kβ selective inhibitors derived from a novel 4-(1H-benzo[d]imidazol-1-yl)quinoline chemotype has been rationally designed. Crucial to achieving…”
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Crystal Structure of Phenylmethanesulfonyl Fluoride-Treated Human Chymase at 1.9 Å by McGrath, Mary E, Mirzadegan, Tara, Schmidt, Brian F

“…The X-ray crystal structure of human chymase has been determined to 1.9 Å resolution using molecular replacement methods. This first structure of human chymase…”
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Visualizing the Molecular Interactions of a Nucleotide Analog, GS-9148, with HIV-1 Reverse Transcriptase–DNA Complex by Lansdon, Eric B., Samuel, Dharmaraj, Lagpacan, Leanna, Brendza, Katherine M., White, Kirsten L., Hung, Magdeleine, Liu, Xiaohong, Boojamra, Constantine G., Mackman, Richard L., Cihlar, Tomas, Ray, Adrian S., McGrath, Mary E., Swaminathan, S.

“…GS-9148 ([5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid) is a dAMP (2′-deoxyadenosine monophosphate) analog that maintains…”
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Identification of a potent and selective non-basic cathepsin K inhibitor by Li, Chun Sing, Deschenes, Denis, Desmarais, Sylvie, Falgueyret, Jean-Pierre, Gauthier, Jacques Yves, Kimmel, Donald. B., Léger, Serge, Massé, Frédéric, McGrath, Mary E., McKay, Daniel J., Percival, M. David, Riendeau, Denis, Rodan, Sevgi B., Thérien, Michel, Truong, Vouy-Linh, Wesolowski, Gregg, Zamboni, Robert, Black, W. Cameron

“…Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound…”
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THE LYSOSOMAL CYSTEINE PROTEASES by McGrath, Mary E

“…A significant number of exciting papain-like cysteine protease structures have been determined by crystallographic methods over the last several years. This…”
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Perturbing the polar environment of Asp102 in trypsin: consequences of replacing conserved Ser214 by McGrath, Mary E, Vasquez, John R, Craik, Charles S, Yang, A. S, Honig, Barry, Fletterick, Robert J

“…Much of the catalytic power of trypsin is derived from the unusual buried, charged side chain of Asp102. A polar cave provides the stabilization for…”
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Production of crystallizable human chymase from a Bacillus subtilis system by McGrath, Mary E, Osawa, A.Edward, Barnes, Michael G, Clark, James M, Mortara, Kyle D, Schmidt, Brian F

“…A Bacillus subtilis strain deficient in seven extracellular proteases was used to produce human mast cell chymase and is a viable expression system for serine…”
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Peptide Ketobenzoxazole Inhibitors Bound to Cathepsin K by McGrath, Mary E, Sprengeler, Paul A, Hill, Craig M, Martichonok, Valeri, Cheung, Harry, Somoza, John R, Palmer, James T, Janc, James W

“…Potent inhibitors of human cysteine proteases of the papain family have been made and assayed versus a number of relevant family members. We describe the…”
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Dissecting and Designing Inhibitor Selectivity Determinants at the S1 Site Using an Artificial Ala190 Protease (Ala190 uPA) by Katz, Bradley A., Luong, Christine, Ho, Joseph D., Somoza, John R., Gjerstad, Erik, Tang, Jie, Williams, Steven R., Verner, Erik, Mackman, Richard L., Young, Wendy B., Sprengeler, Paul A., Chan, Hedy, Mortara, Kyle, Janc, James W., McGrath, Mary E.

“…A site-directed mutant of the serine protease urokinase-type plasminogen activator (uPA), was produced to assess the contribution of the Ser190 side-chain to…”
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Structure-Guided Design of Peptide-Based Tryptase Inhibitors by McGrath, Mary E, Sprengeler, Paul A, Hirschbein, Bernard, Somoza, John R, Lehoux, Isabelle, Janc, James W, Gjerstad, Erik, Graupe, Michael, Estiarte, Angeles, Venkataramani, Chandru, Liu, Yang, Yee, Robb, Ho, Joseph D, Green, Michael J, Lee, Chang-Sun, Liu, Liang, Tai, Vincent, Spencer, Jeffrey, Sperandio, David, Katz, Bradley A

“…Improved peptide-based inhibitors of human β tryptase were discovered using information gleaned from tripeptide library screening and structure-guided design…”
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Design of novel, potent, and selective human β-tryptase inhibitors based on α-keto-[1,2,4]-oxadiazoles by Lee, Chang-Sun, Liu, Weili, Sprengeler, Paul A., Somoza, John R., Janc, James W., Sperandio, David, Spencer, Jeffrey R., Green, Michael J., McGrath, Mary E.

“…A series of novel α-keto-[1,2,4]-oxadiazoles has been synthesized as human tryptase inhibitors for evaluation as a new class of anti-asthmatic agent. The…”
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Crystal Structure of Human Cathepsin V by Somoza, John R, Zhan, Hangjun, Bowman, Krista K, Yu, Lily, Mortara, Kyle D, Palmer, James T, Clark, James M, McGrath, Mary E

“…Cathepsin V is a lysosomal cysteine protease that is expressed in the thymus, testis and corneal epithelium. We have determined the 1.6 Å resolution crystal…”
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