Search Results - "Come, Jon"

ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors by Bandarage, Upul K., Court, John, Gao, Huai, Nanthakumar, Suganthini, Come, Jon H., Giroux, Simon, Green, Jeremy

“…[Display omitted] Rho kinase (ROCK) inhibitors are of therapeutic value for the treatment of disorders such as hypertension and glaucoma, and potentially of…”
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ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors by Bandarage, Upul K., Cao, Jingrong, Come, Jon H., Court, John J., Gao, Huai, Jacobs, Marc D., Marhefka, Craig, Nanthakumar, Suganthi, Green, Jeremy

“…[Display omitted] •3-Substituted 7-azaindoles are shown to be bioisosteric replacements for 4-substituted pyridines.•Solubilizing groups are used to enhance…”
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Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3‑Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS) by Come, Jon H, Collier, Philip N, Henderson, James A, Pierce, Albert C, Davies, Robert J, Le Tiran, Arnaud, O’Dowd, Hardwin, Bandarage, Upul K, Cao, Jingrong, Deininger, David, Grey, Ron, Krueger, Elaine B, Lowe, Derek B, Liang, Jianglin, Liao, Yusheng, Messersmith, David, Nanthakumar, Suganthi, Sizensky, Emmanuelle, Wang, Jian, Xu, Jinwang, Chin, Elaine Y, Damagnez, Veronique, Doran, John D, Dworakowski, Wojciech, Griffith, James P, Jacobs, Marc D, Khare-Pandit, Suvarna, Mahajan, Sudipta, Moody, Cameron S, Aronov, Alex M

“…The lipid kinase phosphoinositide 3-kinase γ (PI3Kγ) has attracted attention as a potential target to treat a variety of autoimmune disorders, including…”
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Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1 by Come, Jon H, Senter, Timothy J, Clark, Michael P, Court, John J, Gale-Day, Zachary, Gu, Wenxin, Krueger, Elaine, Liang, Jianglin, Morris, Mark, Nanthakumar, Suganthini, O’Dowd, Hardwin, Maltais, Francois, Iyer, Ganesh, Andreassi, John, Boucher, Christina, Considine, Tony, Moody, Cameron S, Taylor, William, Mohanty, Arun K, Huang, Yulin, Zuccola, Harmon, Coll, Joyce, Bonanno, Kenneth C, Gagnon, Kevin J, Gan, Lu, Lu, Fan, Gao, Hong, Chakilam, Ananthisrinivas, Engtrakul, Juntyma, Song, Bin, Crawford, Dan, Doyle, Elisabeth, Kramer, Tal, Vought, Bryan, Phillips, Jonathan, Kemper, Raymond, Sanders, Martin, Swett, Rebecca, Furey, Brinley, Winquist, Ray, Bunnage, Mark E, Jackson, Katrina L, Charifson, Paul S, Magavi, Sanjay S

“…Accumulation of very long chain fatty acids (VLCFAs) due to defects in ATP binding cassette protein D1 (ABCD1) is thought to underlie the pathologies observed…”
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Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors by Bandarage, Upul K, Aronov, Alex M, Cao, Jingrong, Come, Jon H, Cottrell, Kevin M, Davies, Robert J, Giroux, Simon, Jacobs, Marc, Mahajan, Sudipta, Messersmith, David, Moody, Cameron S, Swett, Rebecca, Xu, Jinwang

“…Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation,…”
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Cell-free formation of protease-resistant prion protein by Kocisko, D.A, Come, J.H, Priola, S.A, Chesebro, B, Raymond, G.J, Lansbury, P.T, Caughey, B

“…The infectious agent (or 'prion') of the transmissible spongiform encephalopathies (TSEs) such as scrapie resembles a virus in that it replicates in vivo and…”
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Novel thiol-based TACE inhibitors: Rational design, synthesis, and SAR of thiol-containing aryl sulfonamides by Govinda Rao, B., Bandarage, Upul K., Wang, Tiansheng, Come, Jon H., Perola, Emanuele, Wei, Yunyi, Tian, Shi-Kai, Saunders, Jeffrey O.

“…A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated…”
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4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Potent and selective p70S6 kinase inhibitors by Bandarage, Upul, Hare, Brian, Parsons, Jonathan, Pham, Ly, Marhefka, Craig, Bemis, Guy, Tang, Qing, Moody, Cameron Stuver, Rodems, Steve, Shah, Sundeep, Adams, Chris, Bravo, Jose, Charonnet, Emmanuelle, Savic, Vladimir, Come, Jon H., Green, Jeremy

“…We report herein the design and synthesis of 4-(benzimidazol-2-yl)-1,2,5-oxadiazol-3-amine derivatives as inhibitors of p70S6 kinase. Screening hits containing…”
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Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones by Bandarage, Upul K., Wang, Tiansheng, Come, Jon H., Perola, Emanuele, Wei, Yunyi, Rao, B. Govinda

“…A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In…”
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A Kinetic Model for Amyloid Formation in the Prion Diseases: Importance of Seeding by Come, Jon H., Fraser, Paul E., Lansbury, Peter T.

“…The transmissible spongiform encephalopathies (TSEs) are neurodegenerative diseases characterized by amyloid formation in the brain. The major amyloid protein…”
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Predisposition of prion protein homozygotes to Creutzfeldt-Jakob disease can be explained by a nucleation-dependent polymerization mechanism by Come, Jon H, Lansbury, Peter T

“…The transmissible spongiform encephalopathies (e.g., scrapie, Creutzfeldt-Jakob disease (CJD), and Gerstmann-Strauessler-Scheinker disease (GSS)), like…”
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Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1 by Boyd, Michael J, Collier, Philip N, Clark, Michael P, Deng, Hongbo, Kesavan, Sarathy, Ronkin, Steven M, Waal, Nathan, Wang, Jian, Cao, Jingrong, Li, Pan, Come, Jon, Davies, Ioana, Duffy, John P, Cochran, John E, Court, John J, Chandupatla, Kishan, Jackson, Katrina L, Maltais, Francois, O’Dowd, Hardwin, Boucher, Christina, Considine, Tony, Taylor, William P, Gao, Hong, Chakilam, Ananthisrinivas, Engtrakul, Juntyma, Crawford, Dan, Doyle, Elizabeth, Phillips, Jonathan, Kemper, Raymond, Swett, Rebecca, Empfield, James, Bunnage, Mark E, Charifson, Paul S, Magavi, Sanjay Shivayogi

“…In our efforts to identify novel small molecule inhibitors for the treatment of adrenoleukodystrophy (ALD), we conducted a high-throughput radiometric screen…”
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Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3‑Kinase γ by Collier, Philip N., Messersmith, David, Le Tiran, Arnaud, Bandarage, Upul K., Boucher, Christina, Come, Jon, Cottrell, Kevin M., Damagnez, Veronique, Doran, John D., Griffith, James P., Khare-Pandit, Suvarna, Krueger, Elaine B., Ledeboer, Mark W., Ledford, Brian, Liao, Yusheng, Mahajan, Sudipta, Moody, Cameron S., Roday, Setu, Wang, Tiansheng, Xu, Jinwang, Aronov, Alex M.

“…A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase…”
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Abstract 3363: LIG1 inactivation selectively inhibits growth of BRCA1 mutant cells in vitro and in vivo by Martires, Lauren, Ahronian, Leanne G., Pratt, Charlotte, Das, Nikitha, Zhang, Xiaobin, Whittington, Douglas A., Zhang, Hongxiang, Shen, Binzhang, Come, Jon, McCarren, Patrick, Liu, Mu-Sen, Min, Chengyin, Feng, Tianshu, Jahic, Haris, Brophy, Eric, Aird, Daniel, Andersen, Jannik N., Huang, Alan, Li, Fang, Mallender, William D., Nicholson, Hilary E.

“…Abstract Women harboring a mutation in the BRCA1 gene have a >7X increased risk of developing breast cancer and >35X increased risk of developing ovarian…”
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Abstract 3242: TNG917 is a clinical-grade, potent and selective inhibitor of EHMT1/2 for the treatment of immune cold tumors by Lu, Alvin, Haines, Brian, Lei, Ji, Zhang, Wenhai, Zhang, Minjie, Whittington, Douglas A., Ferdinez, Maria Lucia, Yu, Yi, Meier, Samuel R., Choi, Ashley, Bejnood, Alborz, Bandi, Madhavi, Lazarides, Katherine, Pan, Xuewen, Gu, Lina, Tsai, Alice W., Sudsakorn, Sirimas, Liang, Colin, Come, Jon, Williams, Brett, Throner, Scott, Vacca, Joseph, Maxwell, John P., Anderson, Jannik N., Huang, Alan, Min, Chengyin, Chen, Yingnan P.

“…Abstract CRISPR-based functional genomics screening can be designed to identify novel cancer cell intrinsic targets that increase tumor immunogenicity. Using a…”
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Abstract LB-B15: A novel PI3K gamma isoform selective small molecule kinase inhibitor demonstrates single agent anti-tumor activity and enhanced combination activity with checkpoint blockade in syngeneic mouse models of cancer by Saha, Saurabh, Zhang, Linping, Hoock, Thomas, Aronov, Alex, Mahajan, Sudipta, Boyd, Michael, Come, Jon, Damagnez, Veronique, Dworakowski, Wojciech, Khare-Pandit, Suvarna, LeTiran, Arnaud, Moody, Cameron, O'Dowd, Harwin, Prezioso, Joseph, Roday, Setu, Zhang, Xiaoyan M.

“…Abstract Immune checkpoint inhibitors have generated impressive clinical responses, however, a number of patients and cancer types remain resistant to…”
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A Three-Hybrid Approach to Scanning the Proteome for Targets of Small Molecule Kinase Inhibitors by Becker, Frank, Murthi, Krishna, Smith, Chase, Come, Jon, Costa-Roldán, Nuria, Kaufmann, Christine, Hanke, Urs, Degenhart, Carsten, Baumann, Sabine, Wallner, Wolfgang, Huber, Andrea, Dedier, Severine, Dill, Simone, Kinsman, David, Hediger, Mark, Bockovich, Nicholas, Meier-Ewert, Sebastian, Kluge, Arthur F, Kley, Nikolai

“…In this study, we explored the application of a yeast three-hybrid (Y3H)-based compound/protein display system to scanning the proteome for targets of kinase…”
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Convenient synthesis of N-(4-(2-aminopyridin-4-yl)thiazol-2-yl)-2-phenylacetamides by Bandarage, Upul K., Come, Jon H., Green, Jeremy

“…We report a facile one-pot, three-step synthesis of N-(4-(2-aminopyridin-4-yl)thiazol-2-yl)-2-phenylacetamides via condensation of 2-…”
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Mechanistic and preparative studies of the intramolecular photocyclization of methylated 2-(4-pentenyl)tropones by Feldman, Ken S, Come, Jon H, Kosmider, Benedict J, Smith, Pamela M, Rotella, David P, Wu, Ming Jung

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2-Aminopyrazolo[1,5- a]pyrimidines as potent and selective inhibitors of JAK2 by Ledeboer, Mark W., Pierce, Albert C., Duffy, John P., Gao, Huai, Messersmith, David, Salituro, Francesco G., Nanthakumar, Suganthini, Come, Jon, Zuccola, Harmon J., Swenson, Lora, Shlyakter, Dina, Mahajan, Sudipta, Hoock, Thomas, Fan, Bin, Tsai, Wan-Jung, Kolaczkowski, Elaine, Carrier, Scott, Hogan, James K., Zessis, Richard, Pazhanisamy, S., Bennani, Youssef L.

“…The discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5- a]pyrimidines of potent and selective inhibitors of JAK2 is…”
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