Search Results - "Gampe, Robert T."

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) by 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

“…Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous…”
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Modulation of Androgen Receptor Activation Function 2 by Testosterone and Dihydrotestosterone by Askew, Emily B., Gampe, Robert T., Stanley, Thomas B., Faggart, Jonathan L., Wilson, Elizabeth M.

“…The androgen receptor (AR) is transcriptionally activated by high affinity binding of testosterone (T) or its 5α-reduced metabolite, dihydrotestosterone (DHT),…”
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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development by 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

“…We recently reported the discovery of GSK2606414 (1), a selective first in class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK),…”
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Structure of Rev-erbα bound to N-CoR reveals a unique mechanism of nuclear receptor–co-repressor interaction by 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

“…The ligand binding domain of nuclear receptor Rev-Erbα recruits corepressor NCoR to regulate target gene expression. Here the crystal structure of Rev-Erbα LBD…”
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Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance by 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.

“…The androgen receptor (AR) is required for male sex development and contributes to prostate cancer cell survival. In contrast to other nuclear receptors that…”
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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists by 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

“…Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased…”
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Structural Determinants of Ligand Binding Selectivity between the Peroxisome Proliferator-Activated Receptors by 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.

“…The peroxisome proliferator-activated receptors (PPARs) are transcriptional regulators of glucose, lipid, and cholesterol metabolism. We report the x-ray…”
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Probing the Functional Link between Androgen Receptor Coactivator and Ligand-binding Sites in Prostate Cancer and Androgen Insensitivity by He, Bin, Gampe, Robert T., Hnat, Andrew T., Faggart, Jonathan L., Minges, John T., French, Frank S., Wilson, Elizabeth M.

“…The androgen receptor (AR) is a ligand-activated transcription factor required for male sex development and virilization and contributes to prostate cancer…”
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Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors by 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.

“…Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of…”
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Crystallization of protein-ligand complexes by 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.

“…Obtaining diffraction‐quality crystals has long been a bottleneck in solving the three‐dimensional structures of proteins. Often proteins may be stabilized…”
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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 by 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.

“…Through an internal virtual screen performed at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were…”
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Structure-Based Design of Potent Retinoid X Receptor α Agonists by 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

“…A series of tetrahydrobenzofuranyl and tetrahydrobenzothienyl propenoic acids that showed potent agonist activity against RXRα were synthesized via a…”
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Synthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators by Lamotte, Yann, Martres, Paul, Faucher, Nicolas, Laroze, Alain, Grillot, Didier, Ancellin, Nicolas, Saintillan, Yannick, Beneton, Véronique, Gampe, Robert T.

“…Starting from the structure of Telmisartan, a new series of potent and selective PPARγ modulators was identified. The synthesis, in vitro and in vivo…”
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BacMam production and crystal structure of nonglycosylated apo human furin at 1.89 Å resolution by 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.

“…Furin, also called proprotein convertase subtilisin/kexin 3 (PCSK3), is a calcium‐dependent serine endoprotease that processes a wide variety of proproteins…”
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Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix by Gampe, Jr, R T, Montana, V G, Lambert, M H, Wisely, G B, Milburn, M V, Xu, H E

“…The 9-cis-retinoic acid receptors (RXRalpha, RXRbeta, and RXRgamma) are nuclear receptors that play key roles in multiple hormone-signaling pathways…”
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Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? by 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.

“…Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of…”
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Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators by Lamotte, Yann, Martres, Paul, Faucher, Nicolas, Laroze, Alain, Grillot, Didier, Ancellin, Nicolas, Saintillan, Yannick, Beneton, Véronique, Gampe, Jr, Robert T

“…Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo…”
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Structure of Rev-erbalpha bound to N-CoR reveals a unique mechanism of nuclear receptor-co-repressor interaction by 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

“…Repression of gene transcription by the nuclear receptor Rev-erbalpha plays an integral role in the core molecular circadian clock. We report the crystal…”
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Asymmetry in the PPARγ/RXRα Crystal Structure Reveals the Molecular Basis of Heterodimerization among Nuclear Receptors by Gampe, Robert T., Montana, Valerie G., Lambert, Millard H., Miller, Aaron B., Bledsoe, Randy K., Milburn, Michael V., Kliewer, Steven A., Willson, Timothy M., Xu, H.Eric

“…The nuclear receptor PPAR gamma /RXR alpha heterodimer regulates glucose and lipid homeostasis and is the target for the antidiabetic drugs GI262570 and the…”
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1-Methylphenanthro[3,4-b]thiophene: Determination of the tertiary structure in solution and in the crystalline state by NMR spectroscopy and X-ray diffraction by Musmar, M. J., Martin, Gary E., Gampe Jr, Robert T., Lynch, Vincent M., Simonsen, Stanley H., Lee, Milton L., Tedjamulia, Marvin L., Castle, Raymond N.

“…1‐Methylphenanthro[3,4‐b]thiophene was prepared by the photocyclization of 1‐(4′‐methyl‐2′‐thienyl)‐2‐(2″‐naphthyl)ethene. The 1H and 13C‐nmr spectra were…”
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