Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase
Baltgalvis, Kristen A, Lamb, Kelsey N, Symons, Kent T, Wu, Chu-Chiao, Hoffman, Melissa A, Snead, Aaron N, Song, Xiaodan, Glaza, Thomas, Kikuchi, Shota, Green, Jason C, Rogness, Donald C, Lam, Betty, Rodriguez-Aguirre, Maria E, Woody, David R, Eissler, Christie L, Rodiles, Socorro, Negron, Seth M, Bernard, Steffen M, Tran, Eileen, Pollock, Jonathan, Tabatabaei, Ali, Contreras, Victor, Williams, Heather N, Pastuszka, Martha K, Sigler, John J, Pettazzoni, Piergiorgio, Rudolph, Markus G, Classen, Moritz, Brugger, Doris, Claiborne, Christopher, Plancher, Jean-Marc, Cuartas, Isabel, Seoane, Joan, Burgess, Laurence E, Abraham, Robert T, Weinstein, David S, Simon, Gabriel M, Patricelli, Matthew P, Kinsella, Todd M
Published in Nature (London) (09.05.2024)
Published in Nature (London) (09.05.2024)
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Author Correction: Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase
Baltgalvis, Kristen A, Lamb, Kelsey N, Symons, Kent T, Wu, Chu-Chiao, Hoffman, Melissa A, Snead, Aaron N, Song, Xiaodan, Glaza, Thomas, Kikuchi, Shota, Green, Jason C, Rogness, Donald C, Lam, Betty, Rodriguez-Aguirre, Maria E, Woody, David R, Eissler, Christie L, Rodiles, Socorro, Negron, Seth M, Bernard, Steffen M, Tran, Eileen, Pollock, Jonathan, Tabatabaei, Ali, Contreras, Victor, Williams, Heather N, Pastuszka, Martha K, Sigler, John J, Pettazzoni, Piergiorgio, Rudolph, Markus G, Classen, Moritz, Brugger, Doris, Claiborne, Christopher, Plancher, Jean-Marc, Cuartas, Isabel, Seoane, Joan, Burgess, Laurence E, Abraham, Robert T, Weinstein, David S, Simon, Gabriel M, Patricelli, Matthew P, Kinsella, Todd M
Published in Nature (London) (18.07.2024)
Published in Nature (London) (18.07.2024)
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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity
Fell, Jay B, Fischer, John P, Baer, Brian R, Ballard, Joshua, Blake, James F, Bouhana, Karyn, Brandhuber, Barbara J, Briere, David M, Burgess, Laurence E, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Davidson, Kevin, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hee, Kenneth, Hicken, Erik J, Hinklin, Ronald J, Marx, Matthew A, Mejia, Macedonio J, Olson, Peter, Savechenkov, Pavel, Sudhakar, Niranjan, Tang, Tony P, Vigers, Guy P, Zecca, Henry, Christensen, James G
Published in ACS medicinal chemistry letters (13.12.2018)
Published in ACS medicinal chemistry letters (13.12.2018)
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Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists
Newhouse, Bradley, Allen, Shelley, Fauber, Benjamin, Anderson, Aaron S., Eary, C. Todd, Hansen, Joshua D., Schiro, Justin, Gaudino, John J., Laird, Ellen, Chantry, David, Eberhardt, Christine, Burgess, Laurence E.
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Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia
Bachegowda, Lohith, Morrone, Kerry, Winski, Shannon L, Mantzaris, Ioannis, Bartenstein, Matthias, Ramachandra, Nandini, Giricz, Orsi, Sukrithan, Vineeth, Nwankwo, George, Shahnaz, Samira, Bhagat, Tushar, Bhattacharyya, Sanchari, Assal, Amer, Shastri, Aditi, Gordon-Mitchell, Shanisha, Pellagatti, Andrea, Boultwood, Jacqueline, Schinke, Carolina, Yu, Yiting, Guha, Chandan, Rizzi, James, Garrus, Jennifer, Brown, Suzy, Wollenberg, Lance, Hogeland, Grant, Wright, Dale, Munson, Mark, Rodriguez, Mareli, Gross, Stefan, Chantry, David, Zou, Yiyu, Platanias, Leonidas, Burgess, Laurence E, Pradhan, Kith, Steidl, Ulrich, Verma, Amit
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Potent Selective Nonpeptidic Inhibitors of Human Lung Tryptase
Burgess, Laurence E., Newhouse, Bradley J., Ibrahim, Prabha, Rizzi, James, Kashem, Mohammed A., Hartman, Ann, Brandhuber, Barbara J., Wright, Clifford D., Thomson, David S., Guy P. A. Vigers, Koch, Kevin
Published in Proceedings of the National Academy of Sciences - PNAS (20.07.1999)
Published in Proceedings of the National Academy of Sciences - PNAS (20.07.1999)
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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer
Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
Eary, C. Todd, Jones, Zachary S., Groneberg, Robert D., Burgess, Laurence E., Mareska, David A., Drew, Mark D., Blake, James F., Laird, Ellen R., Balachari, Devan, O’Sullivan, Michael, Allen, Andrew, Marsh, Vivienne
Published in Bioorganic & medicinal chemistry letters (01.05.2007)
Published in Bioorganic & medicinal chemistry letters (01.05.2007)
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Asymmetric synthesis of .gamma.,.gamma.-dialkyl-.gamma.-aminobutyric acid analogs and 2,2-disubstituted pyrrolidines. Control of stereochemistry in aminal ring opening by varying the extent of allylic 1,3 strain
Burgess, Laurence E, Meyers, A. I
Published in Journal of the American Chemical Society (01.12.1991)
Published in Journal of the American Chemical Society (01.12.1991)
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Discovery of a Novel Class of Imidazo[1,2‑a]Pyridines with Potent PDGFR Activity and Oral Bioavailability
Hicken, Erik J, Marmsater, Fred P, Munson, Mark C, Schlachter, Stephen T, Robinson, John E, Allen, Shelley, Burgess, Laurence E, DeLisle, Robert Kirk, Rizzi, James P, Topalov, George T, Zhao, Qian, Hicks, Julie M, Kallan, Nicholas C, Tarlton, Eugene, Allen, Andrew, Callejo, Michele, Cox, April, Rana, Sumeet, Klopfenstein, Nathalie, Woessner, Richard, Lyssikatos, Joseph P
Published in ACS medicinal chemistry letters (09.01.2014)
Published in ACS medicinal chemistry letters (09.01.2014)
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5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor
Bach, Peter, Boström, Jonas, Brickmann, Kay, Burgess, Laurence E, Clarke, David, Groneberg, Robert D, Harvey, Darren M, Laird, Ellen R, O'Sullivan, Michael, Zetterberg, Fredrik
Published in Future medicinal chemistry (01.11.2013)
Published in Future medicinal chemistry (01.11.2013)
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Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists
Allen, Shelley, Newhouse, Bradley, Anderson, Aaron S., Fauber, Benjamin, Allen, Andrew, Chantry, David, Eberhardt, Christine, Odingo, Joshua, Burgess, Laurence E.
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
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Tryptase activates peripheral blood mononuclear cells causing the synthesis and release of TNF-α, IL-6 and IL-1β: possible relevance to multiple sclerosis
Malamud, Vivian, Vaaknin, Ady, Abramsky, Oded, Mor, Michal, Burgess, Laurence E., Ben-Yehudah, Ahmi, Lorberboum-Galski, Haya
Published in Journal of neuroimmunology (01.05.2003)
Published in Journal of neuroimmunology (01.05.2003)
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Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor Antagonist with Anti-Inflammatory Activity
D'Amico, Derin C, Aya, Toshi, Human, Jason, Fotsch, Christopher, Chen, Jian Jeffrey, Biswas, Kaustav, Riahi, Bobby, Norman, Mark H, Willoughby, Christopher A, Hungate, Randall, Reider, Paul J, Biddlecome, Gloria, Lester-Zeiner, Dianna, Van Staden, Carlo, Johnson, Eileen, Kamassah, Augustus, Arik, Leyla, Wang, Judy, Viswanadhan, Vellarkad N, Groneberg, Robert D, Zhan, James, Suzuki, Hideo, Toro, Andras, Mareska, David A, Clarke, David E, Harvey, Darren M, Burgess, Laurence E, Laird, Ellen R, Askew, Benny, Ng, Gordon
Published in Journal of medicinal chemistry (22.02.2007)
Published in Journal of medicinal chemistry (22.02.2007)
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Potent Nonpeptide Antagonists of the Bradykinin B1 Receptor: Structure−Activity Relationship Studies with Novel Diaminochroman Carboxamides
Biswas, Kaustav, Li, Aiwen, Chen, Jian Jeffrey, D'Amico, Derin C, Fotsch, Christopher, Han, Nianhe, Human, Jason, Liu, Qingyian, Norman, Mark H, Riahi, Bobby, Yuan, Chester, Suzuki, Hideo, Mareska, David A, Zhan, James, Clarke, David E, Toro, Andras, Groneberg, Robert D, Burgess, Laurence E, Lester-Zeiner, Dianna, Biddlecome, Gloria, Manning, Barton H, Arik, Leyla, Dong, Hong, Huang, Ming, Kamassah, Augustus, Loeloff, Richard, Sun, Hong, Hsieh, Feng-Yin, Kumar, Gondi, Ng, Gordon Y, Hungate, Randall W, Askew, Benny C, Johnson, Eileen
Published in Journal of medicinal chemistry (03.05.2007)
Published in Journal of medicinal chemistry (03.05.2007)
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Identification of the Clinical Development Candidate MRTX849, a Covalent KRAS(G12C) Inhibitor for the Treatment of Cancer
Fell, Jay B., Fischer, John P., Baer, Brian R., Blake, James F., Bouhana, Karyn, Briere, David M., Brown, Karin D., Burgess, Laurence E., Burns, Aaron C., Burkard, Michael R., Chiang, Harrah, Chicarelli, Mark J., Cook, Adam W., Gaudino, John J., Hallin, Jill, Hanson, Lauren, Hartley, Dylan P., Hicken, Erik J., Hingorani, Gary P., Hinklin, Ronald J., Mejia, Macedonio J., Olson, Peter, Otten, Jennifer N., Rhodes, Susan P., Rodriguez, Martha E., Savechenkov, Pavel, Smith, Darin J., Sudhakar, Niranjan, Sullivan, Francis X., Tang, Tony P., Vigers, Guy P., Wollenberg, Lance, Christensen, James G., Marx, Matthew A.
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Inhibition of allergen-induced pulmonary responses by the selective tryptase inhibitor 1,5-bis-{4-[(3-carbamimidoyl-benzenesulfonylamino)-methyl]-phenoxy}-pentane (AMG-126737)
Wright, Clifford D, Havill, Andrew M, Middleton, Scot C, Kashem, Mohammed A, Dripps, David J, Abraham, William M, Thomson, David S, Burgess, Laurence E
Published in Biochemical pharmacology (15.12.1999)
Published in Biochemical pharmacology (15.12.1999)
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