SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy
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Published in Cancer discovery (04.08.2023)
Published in Cancer discovery (04.08.2023)
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Discovery of Potent and Selective Covalent Inhibitors of HER2 WT and HER2 YVMA
Hicken, Erik J, Brown, Karin, Dwulet, Natalie C, Gaudino, John J, Hansen, Erik P, Hartley, Dylan P, Kowalski, John P, Laird, Ellen R, Lazzara, Nicholas C, Li, Bin, Mou, Tung-Chung, Mutryn, Marie F, Oko, Lauren, Pajk, Spencer, Pipal, Robert W, Rosen, Rachel Z, Shelp, Russell, Singh, Anurag, Wang, Jing, Wise, Courtney E, Wong, Christina, Wong, Jim Y
Published in Journal of medicinal chemistry (13.06.2024)
Published in Journal of medicinal chemistry (13.06.2024)
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Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA
Hicken, Erik J., Brown, Karin, Dwulet, Natalie C., Gaudino, John J., Hansen, Erik P., Hartley, Dylan P., Kowalski, John P., Laird, Ellen R., Lazzara, Nicholas C., Li, Bin, Mou, Tung-Chung, Mutryn, Marie F., Oko, Lauren, Pajk, Spencer, Pipal, Robert W., Rosen, Rachel Z., Shelp, Russell, Singh, Anurag, Wang, Jing, Wise, Courtney E., Wong, Christina, Wong, Jim Y.
Published in Journal of medicinal chemistry (13.06.2024)
Published in Journal of medicinal chemistry (13.06.2024)
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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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Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy
Bumpers, Quinn A., Pipal, Robert W., Benz-Weeden, Anna M., Brewster, James T., Cook, Adam, Crooks, Amy L., Cruz, Cole, Dwulet, Natalie C., Gaudino, John J., Golec, Daniel, Harrison, Jacqueline A., Hartley, Dylan P., Hassanien, Sherif H., Hicken, Erik J., Kahn, Dean, Laird, Ellen R., Lemieux, Christine, Lewandowski, Nicholas, McCown, Joseph, McDonald, Matthew G., McNulty, Oren, Mou, Tung-Chung, Nguyen, Phong, Oko, Lauren, Opie, Lisa Pieti, Otten, Jennifer, Peck, Spencer C., Polites, Viktor C., Randall, Samuel D., Rosen, Rachel Z., Savechenkov, Pavel, Simpson, Helen, Singh, Anurag, Sparks, Drew, Wickersham, Kyle, Wollenberg, Lance, Wong, Christina E., Wong, Jim, Wu, Wen-I, Elsayed, Mohamed S. A., Hinklin, Ronald J., Tang, Tony P.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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A Next-Generation BRAF Inhibitor Overcomes Resistance to BRAF Inhibition in Patients with BRAF-Mutant Cancers Using Pharmacokinetics-Informed Dose Escalation
Yaeger, Rona, McKean, Meredith A, Haq, Rizwan, Beck, J Thaddeus, Taylor, Matthew H, Cohen, Jonathan E, Bowles, Daniel W, Gadgeel, Shirish M, Mihalcioiu, Catalin, Papadopoulos, Kyriakos P, Diamond, Eli L, Sturtz, Keren B, Feng, Gang, Drescher, Stefanie K, Reddy, Micaela B, Sengupta, Bhaswati, Maity, Arnab K, Brown, Suzy A, Singh, Anurag, Brown, Eric N, Baer, Brian R, Wong, Jim, Mou, Tung-Chung, Wu, Wen-I, Kahn, Dean R, Gadal, Sunyana, Rosen, Neal, Gaudino, John J, Lee, Patrice A, Hartley, Dylan P, Rothenberg, S Michael
Published in Cancer discovery (04.09.2024)
Published in Cancer discovery (04.09.2024)
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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.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2
Ren, Li, Grina, Jonas, Moreno, David, Blake, James F, Gaudino, John J, Garrey, Rustam, Metcalf, Andrew T, Burkard, Michael, Martinson, Matthew, Rasor, Kevin, Chen, Huifen, Dean, Brian, Gould, Stephen E, Pacheco, Patricia, Shahidi-Latham, Sheerin, Yin, Jianping, West, Kristina, Wang, Weiru, Moffat, John G, Schwarz, Jacob B
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
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Discovery of (S)‑1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl‑1H‑pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)‑one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
Blake, James F, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Dudley, Danette A, Gaudino, John J, Gould, Stephen E, Grina, Jonas, Hunsaker, Thomas, Liu, Lichuan, Martinson, Matthew, Moreno, David, Mueller, Lars, Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Robarge, Kirk, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Jianping, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John, Schwarz, Jacob B
Published in Journal of medicinal chemistry (23.06.2016)
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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
Blake, James F., Gaudino, John J., De Meese, Jason, Mohr, Peter, Chicarelli, Mark, Tian, Hongqi, Garrey, Rustam, Thomas, Allen, Siedem, Christopher S., Welch, Michael B., Kolakowski, Gabrielle, Kaus, Robert, Burkard, Michael, Martinson, Matthew, Chen, Huifen, Dean, Brian, Dudley, Danette A., Gould, Stephen E., Pacheco, Patricia, Shahidi-Latham, Sheerin, Wang, Weiru, West, Kristina, Yin, Jianping, Moffat, John, Schwarz, Jacob B.
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
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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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Pharmacokinetic drivers of toxicity for basic molecules: Strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor
Diaz, Dolores, Ford, Kevin A., Hartley, Dylan P., Harstad, Eric B., Cain, Gary R., Achilles-Poon, Kirsten, Nguyen, Trung, Peng, Jing, Zheng, Zhong, Merchant, Mark, Sutherlin, Daniel P., Gaudino, John J., Kaus, Robert, Lewin-Koh, Sock C., Choo, Edna F., Liederer, Bianca M., Dambach, Donna M.
Published in Toxicology and applied pharmacology (01.01.2013)
Published in Toxicology and applied pharmacology (01.01.2013)
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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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KRAS G12C 억제제
HINKLIN RONALD JAY, MEJIA MACEDONIO J, VIGERS GUY P.A, FISCHER JOHN P, LEE MATTHEW RANDOLF, FELL JAY BRADFORD, GAUDINO JOHN J, ZECCA HENRY J, TANG TONY P, BLAKE JAMES F, CHRISTENSEN JAMES GAIL, HICKEN ERIK JAMES, MARX MATTHEW ARNOLD, CHICARELLI MARK JOSEPH, BURGESS LAURENCE E, SAVECHENKOV PAVEL
Year of Publication 12.04.2019
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Year of Publication 12.04.2019
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Ligand Interactions with E-Selectin. Identification of a New Binding Site for Recognition of N-Acyl Aromatic Glucosamine Substituents of Sialyl Lewis X
Ramphal, John Y, Hiroshige, Mariann, Lou, Boliang, Gaudino, John J, Hayashi, Masaji, Chen, Shiow Meei, Chiang, Lin C, Gaeta, Federico C. A, DeFrees, Shawn A
Published in Journal of medicinal chemistry (29.03.1996)
Published in Journal of medicinal chemistry (29.03.1996)
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A Novel and Efficient Synthesis of Neolacto Series Gangliosides 3'-nLM1 and 6'-nLM1
Gaudino, John J, Paulson, James C
Published in Journal of the American Chemical Society (01.02.1994)
Published in Journal of the American Chemical Society (01.02.1994)
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SERINE/THREONINE KINASE INHIBITORS
DEMEESE JASON, MOHR PETER J, KOLAKOWSKI GABRIELLE R, GARREY RUSTAM, GAUDINO JOHN J, WENGLOWSKY STEVEN MARK, THOMAS ALLEN A, BLAKE JAMES F, WALLACE ELI, KAUS ROBERT J, REN LI, SCHWARZ JACOB, MARLOW ALLISON L, CHEN HUIFEN, CHICARELLI MARK JOSEPH, SIEDEM CHRISTOPHER S
Year of Publication 05.02.2014
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Year of Publication 05.02.2014
Patent