Search Results - "Buchanan, Fritz G."

ABT-414, an Antibody-Drug Conjugate Targeting a Tumor-Selective EGFR Epitope by Phillips, Andrew C, Boghaert, Erwin R, Vaidya, Kedar S, Mitten, Michael J, Norvell, Suzanne, Falls, Hugh D, DeVries, Peter J, Cheng, Dong, Meulbroek, Jonathan A, Buchanan, Fritz G, McKay, Laura M, Goodwin, Neal C, Reilly, Edward B

“…Targeting tumor-overexpressed EGFR with an antibody-drug conjugate (ADC) is an attractive therapeutic strategy; however, normal tissue expression represents a…”
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The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia by Pappano, William N, Guo, Jun, He, Yupeng, Ferguson, Debra, Jagadeeswaran, Sujatha, Osterling, Donald J, Gao, Wenqing, Spence, Julie K, Pliushchev, Marina, Sweis, Ramzi F, Buchanan, Fritz G, Michaelides, Michael R, Shoemaker, Alexander R, Tse, Chris, Chiang, Gary G

“…Histone methyltransferases are epigenetic regulators that modify key lysine and arginine residues on histones and are believed to play an important role in…”
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Characterization of ABBV-221, a Tumor-Selective EGFR-Targeting Antibody Drug Conjugate by Phillips, Andrew C, Boghaert, Erwin R, Vaidya, Kedar S, Falls, Hugh D, Mitten, Michael J, DeVries, Peter J, Benatuil, Lorenzo, Hsieh, Chung-Ming, Meulbroek, Jonathan A, Panchal, Sanjay C, Buchanan, Fritz G, Durbin, Kenneth R, Voorbach, Martin J, Reuter, David R, Mudd, Sarah R, Loberg, Lise I, Ralston, Sherry L, Cao, Diana, Gan, Hui K, Scott, Andrew M, Reilly, Edward B

“…Depatuxizumab mafodotin (depatux-m, ABT-414) is a tumor-selective antibody drug conjugate (ADC) comprised of the anti-EGFR antibody ABT-806 and the monomethyl…”
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Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours by Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, T. Matt, Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, J. William, Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Kluge, Arthur F., Patane, Michael A., Van Drie, John H., Wang, Ce, McElligott, David, Kesicki, Ed, Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, Bromberg, Kenneth D.

“…A potent and selective catalytic inhibitor of p300/CBP histone acetyltransferases suppresses tumour proliferation across multiple cell lineages, illustrating…”
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The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex by He, Yupeng, Selvaraju, Sujatha, Curtin, Michael L, Jakob, Clarissa G, Zhu, Haizhong, Comess, Kenneth M, Shaw, Bailin, The, Juliana, Lima-Fernandes, Evelyne, Szewczyk, Magdalena M, Cheng, Dong, Klinge, Kelly L, Li, Huan-Qiu, Pliushchev, Marina, Algire, Mikkel A, Maag, David, Guo, Jun, Dietrich, Justin, Panchal, Sanjay C, Petros, Andrew M, Sweis, Ramzi F, Torrent, Maricel, Bigelow, Lance J, Senisterra, Guillermo, Li, Fengling, Kennedy, Steven, Wu, Qin, Osterling, Donald J, Lindley, David J, Gao, Wenqing, Galasinski, Scott, Barsyte-Lovejoy, Dalia, Vedadi, Masoud, Buchanan, Fritz G, Arrowsmith, Cheryl H, Chiang, Gary G, Sun, Chaohong, Pappano, William N

“…A pyrrolidine-based small-molecule inhibitor competes with H3K27me3 for binding to EED leading to inactivation of PRC2 and global reduction in H3K27me3 levels…”
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Hexavalent TRAIL Fusion Protein Eftozanermin Alfa Optimally Clusters Apoptosis-Inducing TRAIL Receptors to Induce On-Target Antitumor Activity in Solid Tumors by Phillips, Darren C, Buchanan, Fritz G, Cheng, Dong, Solomon, Larry R, Xiao, Yu, Xue, John, Tahir, Stephen K, Smith, Morey L, Zhang, Haichao, Widomski, Deborah, Abraham, Vivek C, Xu, Nan, Liu, Zhihong, Zhou, Li, DiGiammarino, Enrico, Lu, Xin, Rudra-Ganguly, Nandini, Trela, Bruce, Morgan-Lappe, Susan E

“…TRAIL can activate cell surface death receptors, resulting in potent tumor cell death via induction of the extrinsic apoptosis pathway. Eftozanermin alfa…”
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Activity of eftozanermin alfa plus venetoclax in preclinical models and patients with acute myeloid leukemia by Tahir, Stephen K., Calvo, Emiliano, Carneiro, Benedito A., Yuda, Junichiro, Shreenivas, Aditya, Jongen-Lavrencic, Mojca, Gort, Eelke, Ishizawa, Kenichi, Morillo, Daniel, Biesdorf, Carla, Smith, Morey, Cheng, Dong, Motwani, Monica, Sharon, David, Uziel, Tamar, Modi, Dimple A., Buchanan, Fritz G., Morgan-Lappe, Susan, Medeiros, Bruno C., Phillips, Darren C.

“…•The antitumorigenic activity of eftoza is enhanced in combination with venetoclax in preclinical models of AML.•Eftoza-venetoclax combination is well…”
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Discovery of Potent Azetidine-Benzoxazole MerTK Inhibitors with In Vivo Target Engagement by Frey, Robin R., Jana, Navendu, Gorman, Jacob V., Wang, Jin, Smith, Heath A., Bromberg, Kenneth D., Thakur, Ashish, Doktor, Stella Z., Indulkar, Anura S., Jakob, Clarissa G., Upadhyay, Anup K., Qiu, Wei, Manaves, Vlasios, Gambino, Frank, Valentino, Stephen A., Montgomery, Debra, Zhou, Yebin, Li, Tao, Buchanan, Fritz G., Ferguson, Debra C., Kurnick, Matthew D., Kapecki, Nicolas, Lai, Albert, Michaelides, Michael R., Penning, Thomas D.

“…Inhibition of the receptor tyrosine kinase MerTK by small molecules has the potential to augment the immune response to tumors. Potent, selective inhibitors…”
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Discovery of A‑910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor by Yu, Yiyun, Jang, Miyeon, Miyashiro, Julie, Clark, Richard F., Zhu, Gui-Dong, Gong, Jane, Dai, Yujia, Frey, Robin R., Penning, Thomas D., Kim, Hadong, Lee, Hyung Ki, Kim, Jin Kwan, Ryu, Ki Moon, Park, Seong Jin, Yoon, Taeyoung, Li, Tao, Kurnick, Matthew D., Kapecki, Nicolas J., Li, Leiming, Gorman, Jacob V., Montgomery, Debra A., Manaves, Vlasios, Bromberg, Kenneth D., Doktor, Stella Z., Thakur, Ashish, Wang, Jin, Smith, Heath A., Buchanan, Fritz G., Ferguson, Debra C., Torrent, Maricel, Jakob, Clarissa G., Qiu, Wei, Upadhyay, Anup K., Martin, Ruth L., Lai, Albert, Michaelides, Michael R.

“…TAM receptor tyrosine kinases have emerged as promising therapeutic targets for cancer treatment due to their roles in both tumor intrinsic survival mechanisms…”
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Characterization of ABT-806, a Humanized Tumor-Specific Anti-EGFR Monoclonal Antibody by Reilly, Edward B, Phillips, Andrew C, Buchanan, Fritz G, Kingsbury, Gillian, Zhang, Yumin, Meulbroek, Jonathan A, Cole, Todd B, DeVries, Peter J, Falls, Hugh D, Beam, Christine, Gu, Jinming, Digiammarino, Enrico L, Palma, Joann P, Donawho, Cherrie K, Goodwin, Neal C, Scott, Andrew M

“…Despite clinical efficacy, current approved agents targeting EGFR are associated with on-target toxicities as a consequence of disrupting normal EGFR function…”
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Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605 by Pappano, William N, Jung, Paul M, Meulbroek, Jonathan A, Wang, Yi-Chun, Hubbard, Robert D, Zhang, Qian, Grudzien, Meagan M, Soni, Niru B, Johnson, Eric F, Sheppard, George S, Donawho, Cherrie, Buchanan, Fritz G, Davidsen, Steven K, Bell, Randy L, Wang, Jieyi

“…The insulin-like growth factor (IGF) axis is an important signaling pathway in the growth and survival of many cell and tissue types. This pathway has also…”
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Utilization of 18 F-Fluorodeoxyglucose-Positron Emission Tomography To Understand the Mechanism of Nicotinamide Phosphoribosyltransferase Inhibitors In Vivo by Mudd, Sarah R, Voorbach, Martin J, Cheng, Dong, Cheng, Min, Guo, Jun, Gao, Wenqing, Buchanan, Fritz G, Tse, Chris, Wilsbacher, Julie

“…Cancer cells are highly dependent on NAD /NADH produced via the nicotinamide salvage pathway. The rate-limiting enzyme in this pathway is the nicotinamide…”
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Corrigendum to “Investigation of biaryl heterocycles as inhibitors of Wee1 kinase” [Bioorg. Med. Chem. Lett. 29 (2019) 1481–1486] by Mastracchio, Anthony, Lai, Chunqiu, Torrent, Maricel, Bromberg, Kenneth, Buchanan, Fritz G., Ferguson, Debra, Bontcheva, Velitchka, Johnson, Eric F., Lasko, Loren, Maag, David, Shoemaker, Alexander R., Penning, Thomas D.

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Investigation of biaryl heterocycles as inhibitors of Wee1 kinase by Mastracchio, Anthony, Lai, Chunqiu, Torrent, Maricel, Bromberg, Kenneth, Buchanan, Fritz G., Ferguson, Debra, Bontcheva, Velitchka, Johnson, Eric F., Lasko, Loren, Maag, David, Shoemaker, Alexander R., Penning, Thomas D.

“…[Display omitted] In continuation of our previous research towards the discovery of potent, selective and drug-like Wee1 inhibitors, 2 novel series of biaryl…”
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Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours by Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, T. Matt, Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, J. William, Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Kluge, Arthur F., Patane, Michael A., Van Drie, John H., Wang, Ce, McElligott, David, Kesicki, Edward A., Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, Bromberg, Kenneth D.

“…In the originally published version of this Letter, the authors Arthur F. Kluge, Michael A. Patane and Ce Wang were inadvertently omitted from the author list…”
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Pyrimidine-Based Tricyclic Molecules as Potent and Orally Efficacious Inhibitors of Wee1 Kinase by Tong, Yunsong, Torrent, Maricel, Florjancic, Alan S, Bromberg, Kenneth D, Buchanan, Fritz G, Ferguson, Debra C, Johnson, Eric F, Lasko, Loren M, Maag, David, Merta, Philip J, Olson, Amanda M, Osterling, Donald J, Soni, Nirupama, Shoemaker, Alexander R, Penning, Thomas D

“…Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure–activity…”
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Optimization of Phenyl-Substituted Benzimidazole Carboxamide Poly(ADP-Ribose) Polymerase Inhibitors: Identification of (S)-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a Highly Potent and Efficacious Inhibitor by Penning, Thomas D, Zhu, Gui-Dong, Gong, Jianchun, Thomas, Sheela, Gandhi, Viraj B, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F, Park, Chang H, Fry, Elizabeth H, Donawho, Cherrie K, Frost, David J, Buchanan, Fritz G, Bukofzer, Gail T, Rodriguez, Luis E, Bontcheva-Diaz, Velitchka, Bouska, Jennifer J, Osterling, Donald J, Olson, Amanda M, Marsh, Kennan C, Luo, Yan, Giranda, Vincent L

“…We have developed a series of phenylpyrrolidine- and phenylpiperidine-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase (PARP) inhibitors with…”
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Optimization of Phenyl-Substituted Benzimidazole Carboxamide Poly(ADP-Ribose) Polymerase Inhibitors: Identification of ( S )-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1 H -benzimidazole-4-carboxamide (A-966492), a Highly Potent and Efficacious Inhibitor by Penning, Thomas D., Zhu, Gui-Dong, Gong, Jianchun, Thomas, Sheela, Gandhi, Viraj B., Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F., Park, Chang H., Fry, Elizabeth H., Donawho, Cherrie K., Frost, David J., Buchanan, Fritz G., Bukofzer, Gail T., Rodriguez, Luis E., Bontcheva-Diaz, Velitchka, Bouska, Jennifer J., Osterling, Donald J., Olson, Amanda M., Marsh, Kennan C., Luo, Yan, Giranda, Vincent L.

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Abstract LB-A23: Discovery of a potent catalytic p300/CBP inhibitor that targets lineage-specific tumors by Bromberg, Kenneth D., Lasko, Loren M., Jakob, Clarissa G., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, Todd M., Risi, Roberto M., Frey, Robin R., Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Favire, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert

“…Abstract The dynamic and reversible acetylation of proteins catalyzed by histone acetyltransferases (HATs) and histone deacetylases (HDACs) is a major…”
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Abstract 4718: ABBV-075, a novel BET family bromodomain inhibitor, represents a promising therapeutic agent for a broad spectrum of cancer indications by Sarthy, Aparna, Li, Leiming, Albert, Daniel H., Lin, Xiaoyu, Scott, Warder, Faivre, Emily, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise M., Magoc, Terry, Buchanan, Fritz G., Tapang, Paul, Sheppard, George S., Wang, Le, Fidanze, Steve D., Pratt, John, Liu, Dachun, Hasvold, Lisa, Hessler, Paul, Uziel, Tamar, Lam, Lloyd, Rajaraman, Ganesh, Fang, Guowei, Elmore, Steven W., Rosenberg, Saul H., McDaniel, Keith, Kati, Warren, Shen, Yu

“…Abstract Small molecule inhibitors of the bromodomain and extraterminal domain (BET) proteins have emerged as a promising option for cancer therapy. ABBV-075…”
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