Search Results - "Seward, Eileen M."

Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation by Hanan, Emily J, Eigenbrot, Charles, Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Dotson, Jennafer, Heald, Robert A, Jackson, Philip S, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Tam, Christine, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yin, Jianping, Yu, Christine, Zilberleyb, Inna, Heffron, Timothy P

“…Activating mutations within the epidermal growth factor receptor (EGFR) kinase domain, commonly L858R or deletions within exon 19, increase EGFR-driven cell…”
Get full text

Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta by Murray, Jeremy M, Sweeney, Zachary K, Chan, Bryan K, Balazs, Mercedesz, Bradley, Erin, Castanedo, Georgette, Chabot, Christine, Chantry, David, Flagella, Michael, Goldstein, David M, Kondru, Rama, Lesnick, John, Li, Jun, Lucas, Matthew C, Nonomiya, Jim, Pang, Jodie, Price, Stephen, Salphati, Laurent, Safina, Brian, Savy, Pascal P. A, Seward, Eileen M, Ultsch, Mark, Sutherlin, Daniel P

“…Inhibition of PI3Kδ is considered to be an attractive mechanism for the treatment of inflammatory diseases and leukocyte malignancies. Using a structure-based…”
Get full text

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor by Chan, Bryan K, Hanan, Emily J, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dela Vega, Trisha, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard L, Heald, Robert A, Jackson, Philip S, Knight, Jamie D, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P

“…Inhibitors targeting the activating mutants of the epidermal growth factor receptor (EGFR) have found success in the treatment of EGFR mutant positive…”
Get full text

Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition by Safina, Brian S, Baker, Stewart, Baumgardner, Matt, Blaney, Paul M, Chan, Bryan K, Chen, Yung-Hsiang, Cartwright, Matthew W, Castanedo, Georgette, Chabot, Christine, Cheguillaume, Arnaud J, Goldsmith, Paul, Goldstein, David M, Goyal, Bindu, Hancox, Timothy, Handa, Raj K, Iyer, Pravin S, Kaur, Jasmit, Kondru, Rama, Kenny, Jane R, Krintel, Sussie L, Li, Jun, Lesnick, John, Lucas, Matthew C, Lewis, Cristina, Mukadam, Sophie, Murray, Jeremy, Nadin, Alan J, Nonomiya, Jim, Padilla, Fernando, Palmer, Wylie S, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Salphati, Laurent, Savy, Pascal A, Seward, Eileen M, Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K, Tay, Suzanne, Tivitmahaisoon, Parcharee, Waszkowycz, Bohdan, Wei, Binqing, Yue, Qin, Zhang, Chenghong, Sutherlin, Daniel P

“…PI3Kδ is a lipid kinase and a member of a larger family of enzymes, PI3K class IA(α, β, δ) and IB (γ), which catalyze the phosphorylation of PIP2 to PIP3…”
Get full text

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles by Safina, Brian S, Elliott, Richard L, Forrest, Andrew K, Heald, Robert A, Murray, Jeremy M, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Seward, Eileen M, Staben, Steven T, Ultsch, Mark, Wei, Binqing, Yang, Wenqian, Sutherlin, Daniel P

“…A novel selective benzoxazepin inhibitor of PI3Kδ has been discovered. Beginning from compound 3, an αPI3K inhibitor, we utilized structure-based drug design…”
Get full text

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivity by Safina, Brian S., Sweeney, Zachary K., Li, Jun, Chan, Bryan K., Bisconte, Angelina, Carrera, Diane, Castanedo, Georgette, Flagella, Michael, Heald, Robert, Lewis, Cristina, Murray, Jeremy M., Nonomiya, Jim, Pang, Jodie, Price, Steve, Reif, Karin, Salphati, Laurent, Seward, Eileen M., Wei, Binqing, Sutherlin, Daniel P.

“…In an effort to identify potent and isoform selective inhibitors of PI3Kδ, GNE-293 (34) was identified. Inhibitor 2 was found to induce micronuclei formation…”
Get full text

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf by Sutherlin, Daniel P., Baker, Stewart, Bisconte, Angelina, Blaney, Paul M., Brown, Anthony, Chan, Bryan K., Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M., Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C., Lewis, Cristina, Murray, Jeremy, Nadin, Alan J., Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S., Salphati, Laurent, Staben, Steven, Seward, Eileen M., Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K., Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing

“…A potent inhibitor of PI3Kδ that is ⩾200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for…”
Get full text

Cyclophane-arene inclusion complexation in protic solvents: solvent effects versus electron donor-acceptor interactions by Ferguson, Stephen B, Sanford, Elizabeth M, Seward, Eileen M, Diederich, Francois

Get full text

Substituent Effects on Edge-to-Face Aromatic Interactions by Carver, Fiona J., Hunter, Christopher A., Livingstone, David J., McCabe, James F., Seward, Eileen M.

“…Chemical double mutant cycles have been used to measure the magnitude of edge‐to‐face aromatic interactions in hydrogen‐bonded zipper complexes as a function…”
Get full text

Redox-dependent binding ability of a flavin cyclophane in aqueous solution: hydrophobic stacking versus cavity-inclusion complexation by Seward, Eileen M, Hopkins, R. Bruce, Sauerer, Wolfgang, Tam, Suk Wah, Diederich, Francois

Get full text

Molecular receptors. Synthesis and x-ray crystal structure of a calix[4] arene tetracarbonate-acetonitrile (1:1) clathrate by McKervey, M. Anthony, Seward, Eileen M, Ferguson, George, Ruhl, Barbara L

Get full text

Spirocyclic NK1 antagonists I:[4.5] and [5.5]-spiroketals by SEWARD, Eileen M, CARLSON, Emma, SADOWSKI, Sharon J, SWAIN, Christopher J, WILLIAMS, Brian J, HARRISON, Timothy, HAWORTH, Karen E, HERBERT, Richard, KELLEHER, Fintan J, KURTZ, Marc M, MOSELEY, Jonathan, OWEN, Simon N, OWENS, Andrew P

Get full text

Substituent effects on edge-to-face aromatic interactions by Carver, Fiona J, Hunter, Christopher A, Livingstone, David J, McCabe, James F, Seward, Eileen M

“…Chemical double mutant cycles have been used to measure the magnitude of edge-to-face aromatic interactions in hydrogen-bonded zipper complexes as a function…”
Get full text

Potent and selective inhibitors of PI3KI': Obtaining isoform selectivity from the affinity pocket and tryptophan shelf by Sutherlin, Daniel P, Baker, Stewart, Bisconte, Angelina, Blaney, Paul M, Brown, Anthony, Chan, Bryan K, Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M, Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C, Lewis, Cristina, Murray, Jeremy, Nadin, Alan J, Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S, Salphati, Laurent, Staben, Steven, Seward, Eileen M, Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K, Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing

“…A potent inhibitor of PI3KI' that is aCO34200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis…”
Get full text

Quantitative Measurements of Edge-to-Face Aromatic Interactions by Using Chemical Double-Mutant Cycles by Carver, Fiona J., Hunter, Christopher A., Jones, Philip S., Livingstone, David J., McCabe, James F., Seward, Eileen M., Tiger, Pascale, Spey, Sharon E.

“…Synthetic H‐bonded zipper complexes have been used to quantify the magnitude of an edge‐to‐face aromatic interaction between a benzoyl group and an aniline…”
Get full text

Synthesis, x-ray crystal structures, and cation-binding properties of alkyl calixaryl esters and ketones, a new family of macrocyclic molecular receptors by Arnaud-Neu, Francoise, Collins, Elizabeth M, Deasy, Mary, Ferguson, George, Harris, Stephen J, Kaitner, Branko, Lough, Alan J, McKervey, M. Anthony, Marques, Elizabeth

Get full text

Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals by Seward, Eileen M, Carlson, Emma, Harrison, Timothy, Haworth, Karen R, Herbert, Richard, Kelleher, Fintan J, Kurtz, Marc M, Moseley, Jonathan, Owen, Simon N, Owens, Andrew P, Sadowski, Sharon J, Swain, Christopher J, Williams, Brian J

“…A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed,…”
Get full text

Spirocyclic NK 1 antagonists I: [4.5] and [5.5]-Spiroketals by Seward, Eileen M, Carlson, Emma, Harrison, Timothy, Haworth, Karen E, Herbert, Richard, Kelleher, Fintan J, Kurtz, Marc M, Moseley, Jonathan, Owen, Simon N, Owens, Andrew P, Sadowski, Sharon J, Swain, Christopher J, Williams, Brian J

“…A series of novel spiroketal-based NK 1 antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed,…”
Get full text