Search Results - "Gaudino, John"

SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy by Drilon, Alexander, Sharma, Manish R, Johnson, Melissa L, Yap, Timothy A, Gadgeel, Shirish, Nepert, Dale, Feng, Gang, Reddy, Micaela B, Harney, Allison S, Elsayed, Mohamed, Cook, Adam W, Wong, Christina E, Hinklin, Ronald J, Jiang, Yutong, Brown, Eric N, Neitzel, Nickolas A, Laird, Ellen R, Wu, Wen-I, Singh, Anurag, Wei, Ping, Ching, Keith A, Gaudino, John J, Lee, Patrice A, Hartley, Dylan P, Rothenberg, S Michael

“…Rationally targeted therapies have transformed cancer treatment, but many patients develop resistance through bypass signaling pathway activation. PF-07284892…”
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Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA by 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.

“…HER2 overexpression and amplification have been identified as oncogenic drivers, and the development of therapies to treat tumors harboring these markers has…”
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Discovery of Potent and Selective Covalent Inhibitors of HER2 WT and HER2 YVMA by 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

“…HER2 overexpression and amplification have been identified as oncogenic drivers, and the development of therapies to treat tumors harboring these markers has…”
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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity by 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

“…KRAS is the most frequently mutated driver oncogene in human cancer, and KRAS mutations are commonly associated with poor prognosis and resistance to standard…”
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Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy by 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.

“…Mesenchymal-epithelial transition factor (MET) is a receptor tyrosine kinase that serves a critical function in numerous developmental, morphogenic, and…”
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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 by 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

“…RAF inhibitors have transformed treatment for patients with BRAFV600-mutant cancers, but clinical benefit is limited by adaptive induction of ERK signaling,…”
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Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2 by 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

“…Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent,…”
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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 by 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

“…The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by…”
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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2 by 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.

“…[Display omitted] The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors…”
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Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer by 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

“…Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new…”
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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 by 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.

“…Several toxicities are clearly driven by free drug concentrations in plasma, such as toxicities related to on-target exaggerated pharmacology or off-target…”
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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer by 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

“…Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new…”
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Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists by 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.

“…A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are…”
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Kilogram-Scale Asymmetric Ruthenium-Catalyzed Hydrogenation of a Tetrasubstituted Fluoroenamide by Stumpf, Andreas, Reynolds, Mark, Sutherlin, Daniel, Babu, Srinivasan, Bappert, Erhard, Spindler, Felix, Welch, Michael, Gaudino, John

“…Ruthenium‐catalyzed asymmetric homogeneous hydrogenation (AHH) is used as the key step of a multi‐kilogram scale synthesis of an enantiomeric fluoropiperidine…”
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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 by 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

“…Several N-acylglucosamine derivatives of sialyl Lewis X (1−3) were prepared using a combined chemical enzymatic approach and evaluated as an inhibitor of…”
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New approaches to enzyme regulators. Synthesis and enzymological activity of carbocyclic analogs of D-fructofuranose and D-fructofuranose-6-phosphate by Wilcox, Craig S, Gaudino, John J

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A Novel and Efficient Synthesis of Neolacto Series Gangliosides 3'-nLM1 and 6'-nLM1 by Gaudino, John J, Paulson, James C

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A concise approach to enantiomerically pure carbocyclic ribose analogs. Synthesis of (4S,5R,6R,7R)-7-(hydroxymethyl)spiro[2.4]heptane-4,5,6-triol 7-O-(dihydrogen phosphate) by Gaudino, John J, Wilcox, Craig S

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Abstract CT178: Phase 1 trial of PF-07799933 (ARRY-440), a next-generation BRAF inhibitor, for BRAF-mutant cancers by Yaeger, Rona, McKean, Meredith, Haq, Rizwan, Beck, Joseph T., Taylor, Matthew H., Cohen, Jonathan, Bowles, Daniel, 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, Gadal, Sunyana, Rosen, Neal, Gaudino, John J., Lee, Patrice A., Hartley, Dylan P., Rothenberg, Stephen Michael

“…BACKGROUND Approved BRAF inhibitors (BRAFi) have transformed the treatment of BRAF V600-mutant cancers. However, clinical benefit is limited by BRAF…”
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Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development by Robarge, Kirk, Schwarz, Jacob, Blake, Jim, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Gaudino, John, Gould, Stephen, Grina, Jonas, Linghu, Xin, Liu, Lichuan, Martinson, Matthew, Moreno, David A., Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Peter, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John G.

“…The extracellular-signal-regulated kinases (ERK1 and ERK2) represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that commonly is activated…”
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