Search Results - "Medina, Jesús R."

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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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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Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1 by Medina, Jesús R

“…3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a protein target that has generated considerable interest in both academia and the pharmaceutical…”
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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells by Medina, Jesús R, Tian, Xinrong, Li, William H, Suarez, Dominic, Mack, James F, LaFrance, Louis, Martyr, Cuthbert, Brackley, James, Di Marco, Christina, Rivero, Ralph, Heerding, Dirk A, McHugh, Charles, Minthorn, Elisabeth, Bhaskar, Aishwarya, Rubin, Jacob, Butticello, Michael, Carpenter, Christopher, Nartey, Eldridge N, Berrodin, Thomas J, Kallal, Lorena A, Mangatt, Biju

“…Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacological…”
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Selective 3‑Phosphoinositide-Dependent Kinase 1 (PDK1) Inhibitors: Dissecting the Function and Pharmacology of PDK1: Miniperspective by Medina, Jesús R

“…3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a protein target that has generated considerable interest in both academia and the pharmaceutical…”
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Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors by Medina, Jesús R, Becker, Christopher J, Blackledge, Charles W, Duquenne, Celine, Feng, Yanhong, Grant, Seth W, Heerding, Dirk, Li, William H, Miller, William H, Romeril, Stuart P, Scherzer, Daryl, Shu, Arthur, Bobko, Mark A, Chadderton, Antony R, Dumble, Melissa, Gardiner, Christine M, Gilbert, Seth, Liu, Qi, Rabindran, Sridhar K, Sudakin, Valery, Xiang, Hong, Brady, Pat G, Campobasso, Nino, Ward, Paris, Axten, Jeffrey M

“…Phosphoinositide-dependent protein kinase-1(PDK1) is a master regulator of the AGC family of kinases and an integral component of the PI3K/AKT/mTOR pathway. As…”
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High-Throughput Screening and Triage Assays Identify Small Molecules Targeting c-MYC in Cancer Cells by Kallal, Lorena A, Waszkiewicz, Anna, Jaworski, Jon-Paul, Della Pietra, Anthony, Berrodin, Tom, Brady, Pat, Jurewicz, Anthony J, Zeng, Xin, Payne, Lisa, Medina, Jesús R, Doepner-Buser, Carolyn, Mangatt, Biju

“…While c-MYC is well established as a proto-oncogene, its structure and function as a transcription factor have made c-MYC a difficult therapeutic target. To…”
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9-Borabicyclo[3.3.2]decanes and the Asymmetric Hydroboration of 1,1-Disubstituted Alkenes by Gonzalez, Ana Z, Román, José G, Gonzalez, Eduvigis, Martinez, Judith, Medina, Jesus R, Matos, Karl, Soderquist, John A

“…The syntheses of the optically pure asymmetric hydroborating agents 1 (a, R = Ph; b, R = TMS) in both enantiomeric forms are reported. These reagents are…”
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Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery by Medina, Jesús R, Blackledge, Charles W, Heerding, Dirk A, Campobasso, Nino, Ward, Paris, Briand, Jacques, Wright, Lois, Axten, Jeffrey M

“…Fragment screening of phosphoinositide-dependent kinase-1 (PDK1) in a biochemical kinase assay afforded hits that were characterized and prioritized based on…”
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Acylprolinamides: A new class of peptide deformylase inhibitors with in vivo antibacterial activity by Axten, Jeffrey M., Medina, Jesús R., Blackledge, Charles W., Duquenne, Céline, Grant, Seth W., Bobko, Mark A., Peng, Tony, Miller, William H., Pinckney, Theresa, Gallagher, Timothy F., Kulkarni, Swarupa, Lewandowski, Thomas, Van Aller, Glenn S., Zonis, Rimma, Ward, Paris, Campobasso, Nino

“…A new class of PDF inhibitor with potent, broad spectrum antibacterial activity is described. Optimization of blood stability and potency provided compounds…”
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Design and synthesis of aminopyridine containing biaryls reducing c-MYC protein levels in cells by Di Marco, Christina N., Terrell, Lamont, Sanchez, Robert, Rueda, Lourdes, Shuster, Leanna, Nartey, Eldridge N., McHugh, Charles, Mack, James F., Shu, Arthur, Tian, Xinrong, Medina, Jesus R., Rivero, Ralph, Manetsch, Roman, Heerding, Dirk, Mangatt, Biju

“…[Display omitted] The c-MYC oncogene transcription factor has been implicated in cell cycle regulation controlling cell growth and proliferation. It is tightly…”
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Discovery of a new series of Aurora inhibitors through truncation of GSK1070916 by Medina, Jesus R., Grant, Seth W., Axten, Jeffrey M., Miller, William H., Donatelli, Carla A., Hardwicke, Mary Ann, Oleykowski, Catherine A., Liao, Qiaoyin, Plant, Ramona, Xiang, Hong

“…The SAR results from this investigation will be presented with an emphasis on the impact structural changes have on the cellular phenotype. Novel Aurora…”
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Benzyl 2-Cyano-3,3-Dimethyl-1-pyrrolidinecarboxylate, a Versatile Intermediate for the Synthesis of 3,3-Dimethylproline Derivatives by Medina, Jesus R, Blackledge, Charles W, Erhard, Karl F, Axten, Jeffrey M, Miller, William H

“…The synthesis of racemic nitrile (±)-9 was accomplished in four steps and 58% overall yield from the known pyrrolidinone 5. Nitrile (±)-9 was resolved via…”
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New Δ5,9 Fatty Acids in the Phospholipids of the Sea Anemone Stoichactis helianthus by Carballeira, Néstor M, Medina, Jesús R

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Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1 H -indol-5-yl)-7 H -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.

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New Direct 11B NMR-Based Analysis of Organoboranes through Their Potassium Borohydrides by Medina, Jesus R, Cruz, Gabriel, Cabrera, Carlos R, Soderquist, John A

“…Representative organoborane mixtures were quantitatively converted to their borohydrides through their reaction with activated KH (KH*), permitting their…”
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Abstract 2919: Discovery of small-molecule compounds targeting c-MYC using a novel cell-based screen by Mangatt, Biju, Pietra, Anthony D., Waszkiewicz, Anna, Jaworski, Jon-Paul, Ghidelli-Disse, Sonja, Berrodin, Thomas J., Sherk, Christian S., Meinhold, Derrick W., Rutkowska-Klute, Anna, Sundaram, Shanker K., Ganji, Gopinath, Halsey, Wendy S., Livi, George P., Li, William, Mack, James, Romeril, Stuart P., Minthorn, Elisabeth A., Kumar, Rakesh, Drewes, Gerard C., Heerding, Dirk A., Kallal, Lorena A., Buser, Carolyn A., Medina, Jesus R.

“…Elevated expression of the c-MYC oncogene (either due to gene amplification, translocation, abnormality in upstream signaling pathways and/or protein…”
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Abstract LB-42: PDK1 knockdown selectively inhibits growth of cancer cells harboring activating mutations involved in MAPK signaling by DeYoung, M. Phillip, Gardiner, Christine M., Chadderton, Antony R., Medina, Jesus R., Axten, Jeffrey M., Rabindran, Sridhar K.

“…Phosphoinositide-dependent protein kinase-1 (PDK1) is a master regulator of the AGC family of kinases and an integral component of the PI3K/AKT/mTOR pathway…”
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A mild and general method for the synthesis of 2-substituted-5-hydroxypyrimidines by Medina, Jesus R., Henry, Theresa A., Axten, Jeffrey M.

“…5-Bromopyrimidines are converted to 5-hydroxypyrimidines using a mild synthetic procedure. The method is general and can be applied to compounds containing…”
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Abstract LB-116: GSK2334470: A potent and highly selective inhibitor of PDK1 by Axten, Jeffrey M., Medina, Jesus R., Shu, Arthur, Li, William H., Feng, Yanhong, DeYoung, M. Phillip, Gardiner, Christine M., Chadderton, Antony R., Dumble, Melissa, Liu, Qi, Rabindran, Sridhar

“…Phosphoinositide-dependent protein kinase-1 (PDK1) is a master regulator of the AGC family of kinases and an integral component of the PI3K/AKT/mTOR pathway…”
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