Search Results - "ZARRINKAR, Patrick P"

Comprehensive analysis of kinase inhibitor selectivity by Davis, Mindy I, Hunt, Jeremy P, Herrgard, Sanna, Ciceri, Pietro, Wodicka, Lisa M, Pallares, Gabriel, Hocker, Michael, Treiber, Daniel K, Zarrinkar, Patrick P

“…Davis et al . extend their previous efforts to use inhibitor-kinase interactions to understand kinase inhibitor selectivity by profiling the binding of 72…”
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AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML) by Zarrinkar, Patrick P., Gunawardane, Ruwanthi N., Cramer, Merryl D., Gardner, Michael F., Brigham, Daniel, Belli, Barbara, Karaman, Mazen W., Pratz, Keith W., Pallares, Gabriel, Chao, Qi, Sprankle, Kelly G., Patel, Hitesh K., Levis, Mark, Armstrong, Robert C., James, Joyce, Bhagwat, Shripad S.

“…Activating mutations in the receptor tyrosine kinase FLT3 are present in up to approximately 30% of acute myeloid leukemia (AML) patients, implicating FLT3 as…”
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A quantitative analysis of kinase inhibitor selectivity by Zarrinkar, Patrick P, Karaman, Mazen W, Herrgard, Sanna, Treiber, Daniel K, Gallant, Paul, Atteridge, Corey E, Campbell, Brian T, Chan, Katrina W, Ciceri, Pietro, Davis, Mindy I, Edeen, Philip T, Faraoni, Raffaella, Floyd, Mark, Hunt, Jeremy P, Lockhart, Daniel J, Milanov, Zdravko V, Morrison, Michael J, Pallares, Gabriel, Patel, Hitesh K, Pritchard, Stephanie, Wodicka, Lisa M

“…Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets 1 , 2 . The biological consequences of multi-kinase activity…”
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High-throughput kinase profiling as a platform for drug discovery by Zarrinkar, Patrick P, Goldstein, David M, Gray, Nathanael S

“…High-throughput profiling of compound libraries against large panels of kinases is becoming technically feasible. In contrast to the traditional linear,…”
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Inhibition of Drug-Resistant Mutants of ABL, KIT, and EGF Receptor Kinases by Carter, Todd A., Wodicka, Lisa M., Shah, Neil P., Velasco, Anne Marie, Fabian, Miles A., Treiber, Daniel K., Milanov, Zdravko V., Atteridge, Corey E., Biggs, William H., Edeen, Philip T., Floyd, Mark, Ford, Julia M., Grotzfeld, Robert M., Herrgard, Sanna, Insko, Darren E., Mehta, Shamal A., Patel, Hitesh K., Pao, William, Sawyers, Charles L., Varmus, Harold, Zarrinkar, Patrick P., Lockhart, David J.

“…To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it is important to address the emergence of drug resistance in…”
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Outlier analysis of functional genomic profiles enriches for oncology targets and enables precision medicine by Zhu, Zhou, Ihle, Nathan T, Rejto, Paul A, Zarrinkar, Patrick P

“…Genome-scale functional genomic screens across large cell line panels provide a rich resource for discovering tumor vulnerabilities that can lead to the next…”
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Analysis of Gene Expression Profiles in Normal and Neoplastic Ovarian Tissue Samples Identifies Candidate Molecular Markers of Epithelial Ovarian Cancer by Welsh, John B., Zarrinkar, Patrick P., Sapinoso, Lisa M., Kern, Suzanne G., Behling, Cynthia A., Monk, Bradley J., Lockhart, David J., Burger, Robert A., Hampton, Garret M.

“…Epithelial ovarian cancer is the leading cause of death from gynecologic cancer, in part because of the lack of effective early detection methods. Although…”
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Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor by Janes, Matthew R., Zhang, Jingchuan, Li, Lian-Sheng, Hansen, Rasmus, Peters, Ulf, Guo, Xin, Chen, Yuching, Babbar, Anjali, Firdaus, Sarah J., Darjania, Levan, Feng, Jun, Chen, Jeffrey H., Li, Shuangwei, Li, Shisheng, Long, Yun O., Thach, Carol, Liu, Yuan, Zarieh, Ata, Ely, Tess, Kucharski, Jeff M., Kessler, Linda V., Wu, Tao, Yu, Ke, Wang, Yi, Yao, Yvonne, Deng, Xiaohu, Zarrinkar, Patrick P., Brehmer, Dirk, Dhanak, Dashyant, Lorenzi, Matthew V., Hu-Lowe, Dana, Patricelli, Matthew P., Ren, Pingda, Liu, Yi

“…KRASG12C was recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II…”
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KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition by Misale, Sandra, Fatherree, Jackson P, Cortez, Eliane, Li, Chendi, Bilton, Samantha, Timonina, Daria, Myers, David T, Lee, Dana, Gomez-Caraballo, Maria, Greenberg, Max, Nangia, Varuna, Greninger, Patricia, Egan, Regina K, McClanaghan, Joseph, Stein, Giovanna T, Murchie, Ellen, Zarrinkar, Patrick P, Janes, Matthew R, Li, Lian-Sheng, Liu, Yi, Hata, Aaron N, Benes, Cyril H

“…KRAS-mutant lung cancers have been recalcitrant to treatments including those targeting the MAPK pathway. Covalent inhibitors of KRAS p.G12C allele allow for…”
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Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia by Smith, Catherine C., Wang, Qi, Chin, Chen-Shan, Salerno, Sara, Damon, Lauren E., Levis, Mark J., Perl, Alexander E., Travers, Kevin J., Wang, Susana, Hunt, Jeremy P., Zarrinkar, Patrick P., Schadt, Eric E., Kasarskis, Andrew, Kuriyan, John, Shah, Neil P.

“…Internal tandem duplication mutations in FLT3, known to be associated with a poor prognosis in acute myeloid leukaemia, are now shown to be a valid therapeutic…”
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Kinetic Intermediates Trapped by Native Interactions in RNA Folding by Treiber, Daniel K., Rook, Martha S., Zarrinkar, Patrick P., Williamson, James R.

“…In the magnesium ion-dependent folding of the Tetrahymena ribozyme, a kinetic intermediate accumulates in which the P4-P6 domain is formed, but the P3-P7…”
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An Internally Controlled Quantitative Target Occupancy Assay for Covalent Inhibitors by Hansen, Rasmus, Firdaus, Sarah J., Li, Shuangwei, Janes, Matthew R., Zhang, Jingchuan, Liu, Yi, Zarrinkar, Patrick P.

“…Assessing target occupancy is critical for establishing proof-of-mechanism for novel inhibitors and to determine whether robust target inhibition can be…”
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Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor by Chao, Qi, Sprankle, Kelly G, Grotzfeld, Robert M, Lai, Andiliy G, Carter, Todd A, Velasco, Anne Marie, Gunawardane, Ruwanthi N, Cramer, Merryl D, Gardner, Michael F, James, Joyce, Zarrinkar, Patrick P, Patel, Hitesh K, Bhagwat, Shripad S

“…Treatment of AML patients with small molecule inhibitors of FLT3 kinase has been explored as a viable therapy. However, these agents are found to be less than…”
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A small molecule-kinase interaction map for clinical kinase inhibitors by Zarrinkar, Patrick P, Floyd, Mark, Lai, Andiliy G, Atteridge, Corey E, Carter, Todd A, Galvin, Margaret, Mehta, Shamal A, Lélias, Jean-Michel, Wodicka, Lisa M, Benedetti, Michael G, Azimioara, Mihai D, Treiber, Daniel K, Insko, Darren E, Insko, Michael A, Edeen, Philip T, Gerlach, Jay L, Fabian, Miles A, Grotzfeld, Robert M, Lockhart, David J, Patel, Hitesh K, Milanov, Zdravko V, Ciceri, Pietro, Biggs, William H, Herrgard, Sanna, Velasco, Anne Marie, Ford, Julia M

“…Kinase inhibitors show great promise as a new class of therapeutics. Here we describe an efficient way to determine kinase inhibitor specificity by measuring…”
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The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors by Hansen, Rasmus, Peters, Ulf, Babbar, Anjali, Chen, Yuching, Feng, Jun, Janes, Matthew R., Li, Lian-Sheng, Ren, Pingda, Liu, Yi, Zarrinkar, Patrick P.

“…Activating mutations in KRAS are among the most common tumor driver mutations. Until recently, KRAS had been considered undruggable with small molecules; the…”
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Structure of the kinase domain of an imatinib-resistant abl mutant in complex with the aurora kinase inhibitor VX-680 by YOUNG, Matthew A, SHAH, Neil P, SAWYERS, Charles L, KURIYAN, John, CHAO, Luke H, SEELIGER, Markus, MILANOV, Zdravko V, BIGGS, William H, TREIBER, Daniel K, PATEL, Hitesh K, ZARRINKAR, Patrick P, LOCKHART, David J

“…We present a high-resolution (2.0 A) crystal structure of the catalytic domain of a mutant form of the Abl tyrosine kinase (H396P; Abl-1a numbering) that is…”
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Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors by Liu, Gang, Abraham, Sunny, Liu, Xing, Xu, Shimin, Rooks, Allison M., Nepomuceno, Ron, Dao, Alan, Brigham, Daniel, Gitnick, Dana, Insko, Darren E., Gardner, Michael F., Zarrinkar, Patrick P., Christopher, Ron, Belli, Barbara, Armstrong, Robert C., Holladay, Mark W.

“…[Display omitted] Based on a putative binding mode of quizartinib (AC220, 1), a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clinical…”
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Tuning a Three-Component Reaction For Trapping Kinase Substrate Complexes by Statsuk, Alexander V, Maly, Dustin J, Seeliger, Markus A, Fabian, Miles A, Biggs, William H, Lockhart, David J, Zarrinkar, Patrick P, Kuriyan, John, Shokat, Kevan M

“…The upstream protein kinases responsible for thousands of phosphorylation events in the phosphoproteome remain to be discovered. We developed a three-component…”
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Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry by Wodicka, Lisa M., Ciceri, Pietro, Davis, Mindy I., Hunt, Jeremy P., Floyd, Mark, Salerno, Sara, Hua, Xuequn H., Ford, Julia M., Armstrong, Robert C., Zarrinkar, Patrick P., Treiber, Daniel K.

“…Interactions between kinases and small molecule inhibitors can be activation state dependent. A detailed understanding of inhibitor binding therefore requires…”
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Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors by Patel, Hitesh K., Grotzfeld, Robert M., Lai, Andiliy G., Mehta, Shamal A., Milanov, Zdravko V., Chao, Qi, Sprankle, Kelly G., Carter, Todd A., Velasco, Anne Marie, Fabian, Miles A., James, Joyce, Treiber, Daniel K., Lockhart, David J., Zarrinkar, Patrick P., Bhagwat, Shripad S.

“…A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral…”
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