Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)
Axten, Jeffrey M, Medina, Jesús R, Feng, Yanhong, Shu, Arthur, Romeril, Stuart P, Grant, Seth W, Li, William Hoi Hong, Heerding, Dirk A, Minthorn, Elisabeth, Mencken, Thomas, Atkins, Charity, Liu, Qi, Rabindran, Sridhar, Kumar, Rakesh, Hong, Xuan, Goetz, Aaron, Stanley, Thomas, Taylor, J. David, Sigethy, Scott D, Tomberlin, Ginger H, Hassell, Annie M, Kahler, Kirsten M, Shewchuk, Lisa M, Gampe, Robert T
Published in Journal of medicinal chemistry (23.08.2012)
Published in Journal of medicinal chemistry (23.08.2012)
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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development
Axten, Jeffrey M, Romeril, Stuart P, Shu, Arthur, Ralph, Jeffrey, Medina, Jesús R, Feng, Yanhong, Li, William Hoi Hong, Grant, Seth W, Heerding, Dirk A, Minthorn, Elisabeth, Mencken, Thomas, Gaul, Nathan, Goetz, Aaron, Stanley, Thomas, Hassell, Annie M, Gampe, Robert T, Atkins, Charity, Kumar, Rakesh
Published in ACS medicinal chemistry letters (10.10.2013)
Published in ACS medicinal chemistry letters (10.10.2013)
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Structure of Rev-erbα bound to N-CoR reveals a unique mechanism of nuclear receptor–co-repressor interaction
Phelan, Caroline A, Gampe, Robert T, Lambert, Millard H, Parks, Derek J, Montana, Valerie, Bynum, Jane, Broderick, Timothy M, Hu, Xiao, Williams, Shawn P, Nolte, Robert T, Lazar, Mitchell A
Published in Nature structural & molecular biology (01.07.2010)
Published in Nature structural & molecular biology (01.07.2010)
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Journal Article
Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance
He, Bin, Gampe, Robert T., Kole, Adam J., Hnat, Andrew T., Stanley, Thomas B., An, Gang, Stewart, Eugene L., Kalman, Rebecca I., Minges, John T., Wilson, Elizabeth M.
Published in Molecular cell (05.11.2004)
Published in Molecular cell (05.11.2004)
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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists
Zuercher, William J, Buckholz, Richard G, Campobasso, Nino, Collins, Jon L, Galardi, Cristin M, Gampe, Robert T, Hyatt, Stephen M, Merrihew, Susan L, Moore, John T, Oplinger, Jeffrey A, Reid, Paul R, Spearing, Paul K, Stanley, Thomas B, Stewart, Eugene L, Willson, Timothy M
Published in Journal of medicinal chemistry (22.04.2010)
Published in Journal of medicinal chemistry (22.04.2010)
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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
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Probing the Functional Link between Androgen Receptor Coactivator and Ligand-binding Sites in Prostate Cancer and Androgen Insensitivity
He, Bin, Gampe, Robert T., Hnat, Andrew T., Faggart, Jonathan L., Minges, John T., French, Frank S., Wilson, Elizabeth M.
Published in The Journal of biological chemistry (10.03.2006)
Published in The Journal of biological chemistry (10.03.2006)
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Synthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators
Lamotte, Yann, Martres, Paul, Faucher, Nicolas, Laroze, Alain, Grillot, Didier, Ancellin, Nicolas, Saintillan, Yannick, Beneton, Véronique, Gampe, Robert T.
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
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Journal Article
Structural Determinants of Ligand Binding Selectivity between the Peroxisome Proliferator-Activated Receptors
Xu, H. Eric, Lambert, Millard H., Montana, Valerie G., Plunket, Kelli D., Moore, Linda B., Collins, Jon L., Oplinger, Jeffery A., Kliewer, Steven A., Gampe, Robert T., McKee, David D., Moore, John T., Willson, Timothy M.
Published in Proceedings of the National Academy of Sciences - PNAS (20.11.2001)
Published in Proceedings of the National Academy of Sciences - PNAS (20.11.2001)
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Journal Article
BacMam production and crystal structure of nonglycosylated apo human furin at 1.89 Å resolution
Pearce, Kenneth H., Overton, Laurie K., Gampe, Robert T., Barrett, George B., Taylor, J. David, McKee, David D., Campobasso, Nino, Nolte, Robert T., Reid, Robert A.
Published in Acta crystallographica. Section F, Structural biology communications (01.04.2019)
Published in Acta crystallographica. Section F, Structural biology communications (01.04.2019)
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Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors
Davis, Stephen T., Benson, Bill G., Bramson, H. Neal, Chapman, Dennis E., Dickerson, Scott H., Dold, Karen M., Eberwein, Derek J., Edelstein, Mark, Frye, Stephen V., Gampe, Robert T., Griffin, Robert J., Harris, Philip A., Hassell, Anne M., Holmes, William D., Hunter, Robert N., Knick, Victoria B., Lackey, Karen, Lovejoy, Brett, Luzzio, Michael J., Murray, Doris, Parker, Patricia, Rocque, Warren J., Shewchuk, Lisa, Veal, James M., Walker, Duncan H., Kuyper, Lee F.
Published in Science (American Association for the Advancement of Science) (05.01.2001)
Published in Science (American Association for the Advancement of Science) (05.01.2001)
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Journal Article
Crystallization of protein-ligand complexes
Hassell, Anne M., An, Gang, Bledsoe, Randy K., Bynum, Jane M., Carter III, H. Luke, Deng, Su-Jun J., Gampe, Robert T., Grisard, Tamara E., Madauss, Kevin P., Nolte, Robert T., Rocque, Warren J., Wang, Liping, Weaver, Kurt L., Williams, Shawn P., Wisely, G. Bruce, Xu, Robert, Shewchuk, Lisa M.
Published in Acta crystallographica. Section D, Biological crystallography. (01.01.2007)
Published in Acta crystallographica. Section D, Biological crystallography. (01.01.2007)
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Journal Article
Structure-Based Design of Potent Retinoid X Receptor α Agonists
Haffner, Curt D., Lenhard, James M., Miller, Aaron B., McDougald, Darryl L., Dwornik, Kate, Ittoop, Olivia R., Gampe, Robert T., Xu, H. Eric, Blanchard, Steve, Montana, Valerie G., Consler, Tom G., Bledsoe, Randy K., Ayscue, Andrea, Croom, Dallas
Published in Journal of medicinal chemistry (08.04.2004)
Published in Journal of medicinal chemistry (08.04.2004)
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Journal Article
Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix
Gampe, Jr, R T, Montana, V G, Lambert, M H, Wisely, G B, Milburn, M V, Xu, H E
Published in Genes & development (01.09.2000)
Published in Genes & development (01.09.2000)
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Journal Article
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Adkison, Kim K., Barrett, David G., Deaton, David N., Gampe, Robert T., Hassell, Anne M., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Payne, J. Alan, Shewchuk, Lisa M., Wells-Knecht, Kevin J., Willard, Derril H., Wright, Lois L.
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
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Journal Article
A knowledge-based, structural-aided discovery of a novel class of 2-phe-nylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
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Journal Article
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators
Lamotte, Yann, Martres, Paul, Faucher, Nicolas, Laroze, Alain, Grillot, Didier, Ancellin, Nicolas, Saintillan, Yannick, Beneton, Véronique, Gampe, Jr, Robert T
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
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Journal Article
Structure of Rev-erbalpha bound to N-CoR reveals a unique mechanism of nuclear receptor-co-repressor interaction
Phelan, Caroline A, Gampe, Jr, Robert T, Lambert, Millard H, Parks, Derek J, Montana, Valerie, Bynum, Jane, Broderick, Timothy M, Hu, Xiao, Williams, Shawn P, Nolte, Robert T, Lazar, Mitchell A
Published in Nature structural & molecular biology (01.07.2010)
Published in Nature structural & molecular biology (01.07.2010)
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Journal Article
Accounting for spin diffusion in the analysis of 2D NOE data
Olejniczak, Edward T, Gampe, Robert T, Fesik, Stephen W
Published in Journal of magnetic resonance (1969) (01.03.1986)
Published in Journal of magnetic resonance (1969) (01.03.1986)
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