Search Results - "Tahir, Stephen K."

Potential mechanisms of resistance to venetoclax and strategies to circumvent it by Tahir, Stephen K, Smith, Morey L, Hessler, Paul, Rapp, Lisa Roberts, Idler, Kenneth B, Park, Chang H, Leverson, Joel D, Lam, Lloyd T

“…Venetoclax (ABT-199), a first-in-class orally bioavailable BCL-2-selective inhibitor, was recently approved by the FDA for use in patients with 17p-deleted…”
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Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy by Leverson, Joel D, Phillips, Darren C, Mitten, Michael J, Boghaert, Erwin R, Diaz, Dolores, Tahir, Stephen K, Belmont, Lisa D, Nimmer, Paul, Xiao, Yu, Ma, Xiaoju Max, Lowes, Kym N, Kovar, Peter, Chen, Jun, Jin, Sha, Smith, Morey, Xue, John, Zhang, Haichao, Oleksijew, Anatol, Magoc, Terrance J, Vaidya, Kedar S, Albert, Daniel H, Tarrant, Jacqueline M, La, Nghi, Wang, Le, Tao, Zhi-Fu, Wendt, Michael D, Sampath, Deepak, Rosenberg, Saul H, Tse, Chris, Huang, David C S, Fairbrother, Wayne J, Elmore, Steven W, Souers, Andrew J

“…The BCL-2/BCL-XL/BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical activity in lymphoid malignancies such as chronic lymphocytic leukemia…”
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ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor by Tse, Christin, Shoemaker, Alexander R, Adickes, Jessica, Anderson, Mark G, Chen, Jun, Jin, Sha, Johnson, Eric F, Marsh, Kennan C, Mitten, Michael J, Nimmer, Paul, Roberts, Lisa, Tahir, Stephen K, Xiao, Yu, Yang, Xiufen, Zhang, Haichao, Fesik, Stephen, Rosenberg, Saul H, Elmore, Steven W

“…Overexpression of the prosurvival Bcl-2 family members (Bcl-2, Bcl-xL, and Mcl-1) is commonly associated with tumor maintenance, progression, and…”
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Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins by Park, Cheol-Min, Bruncko, Milan, Adickes, Jessica, Bauch, Joy, Ding, Hong, Kunzer, Aaron, Marsh, Kennan C, Nimmer, Paul, Shoemaker, Alexander R, Song, Xiaohong, Tahir, Stephen K, Tse, Christin, Wang, Xilu, Wendt, Michael D, Yang, Xiufen, Zhang, Haichao, Fesik, Stephen W, Rosenberg, Saul H, Elmore, Steven W

“…Overexpression of prosurvival proteins such as Bcl-2 and Bcl-XL has been correlated with tumorigenesis and resistance to chemotherapy, and thus, the…”
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Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737 by TAHIR, Stephen K, XIUFEN YANG, ROSENBERG, Saul H, TSE, Christin, ANDERSON, Mark G, MORGAN-LAPPE, Susan E, SARTHY, Aparna V, JUN CHEN, WARNER, Robert B, NG, Shi-Chung, FESIK, Stephen W, ELMORE, Steve W

“…ABT-737 is a novel and potent Bcl-2 antagonist with single-agent activity against small-cell lung cancer (SCLC) cell lines. Here, we evaluated the contribution…”
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The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo by Ackler, Scott, Mitten, Michael J., Foster, Kelly, Oleksijew, Anatol, Refici, Marion, Tahir, Stephen K., Xiao, Yu, Tse, Christin, Frost, David J., Fesik, Stephen W., Rosenberg, Saul H., Elmore, Steven W., Shoemaker, Alexander R.

“…Purpose This study was designed to test the ability of the Bcl-2 family inhibitor ABT-263 to potentiate commonly used chemotherapeutic agents and regimens in…”
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Integrative Genomic Analysis of Small-Cell Lung Carcinoma Reveals Correlates of Sensitivity to Bcl-2 Antagonists and Uncovers Novel Chromosomal Gains by Olejniczak, Edward T, Van Sant, Charles, Anderson, Mark G, Wang, Gang, Tahir, Stephen K, Sauter, Guido, Lesniewski, Rick, Semizarov, Dimitri

“…Cancer is a highly heterogeneous disease in terms of the genetic profile and the response to therapeutics. An early identification of a genomic marker in drug…”
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Survivin Enhances Aurora-B Kinase Activity and Localizes Aurora-B in Human Cells by Chen, Jun, Jin, Sha, Tahir, Stephen K., Zhang, Haichao, Liu, Xuesong, Sarthy, Aparna V., McGonigal, Thomas P., Liu, Zhihong, Rosenberg, Saul H., Ng, Shi-Chung

“…Survivin, one of the most tumor-specific gene products, has been implicated in both anti-apoptosis and cytokinesis. However, the mechanism by which survivin…”
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A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies by Phillips, Darren C., Jin, Sha, Gregory, Gareth P., Zhang, Qi, Xue, John, Zhao, Xiaoxian, Chen, Jun, Tong, Yunsong, Zhang, Haichao, Smith, Morey, Tahir, Stephen K., Clark, Rick F., Penning, Thomas D., Devlin, Jennifer R., Shortt, Jake, Hsi, Eric D., Albert, Daniel H., Konopleva, Marina, Johnstone, Ricky W., Leverson, Joel D., Souers, Andrew J.

“…MCL-1 is one of the most frequently amplified genes in cancer, facilitating tumor initiation and maintenance and enabling resistance to anti-tumorigenic agents…”
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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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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity by Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J

“…Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein we report a…”
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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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Down-regulation of Survivin by Antisense Oligonucleotides Increases Apoptosis, Inhibits Cytokinesis and Anchorage-Independent Growth by Chen, Jun, Wu, Wei, Tahir, Stephen K., Kroeger, Paul E., Rosenberg, Saul H., Cowsert, Lex M., Bennett, Frank, Krajewski, Stanislaw, Krajewska, Maryla, Welsh, Kate, Reed, John C., Ng, Shi-Chung

“…Survivin, a member of the inhibitor of apoptosis protein (IAP) family, is detected in most common human cancers but not in adjacent normal cells. Previous…”
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Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors by Lam, Lloyd T, Lin, Xiaoyu, Faivre, Emily J, Yang, Ziping, Huang, Xiaoli, Wilcox, Denise M, Bellin, Richard J, Jin, Sha, Tahir, Stephen K, Mitten, Michael, Magoc, Terry, Bhathena, Anahita, Kati, Warren M, Albert, Daniel H, Shen, Yu, Uziel, Tamar

“…Ten percent to 15% of all lung cancers are small-cell lung cancer (SCLC). SCLC usually grows and metastasizes before it is diagnosed and relapses rapidly upon…”
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Quantification of BCL-2 Family Members by Flow Cytometry by Smith, Morey L, Tahir, Stephen K

“…Flow cytometry is a powerful technique for the detection and quantification of cell surface and intracellular proteins. It enables the ability to measure the…”
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A-432411, a novel indolinone compound that disrupts spindle pole formation and inhibits human cancer cell growth by Chen, Zehan, Merta, Philip J, Lin, Nan-Hong, Tahir, Stephen K, Kovar, Peter, Sham, Hing L, Zhang, Haiying

“…Microtubules are among the most successful targets for anticancer therapies and for the development of new anticancer drugs. A-432411 is a novel small molecule…”
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Synthesis and Biological Evaluation of 2-Indolyloxazolines as a New Class of Tubulin Polymerization Inhibitors. Discovery of A-289099 as an Orally Active Antitumor Agent by Li, Qun, Woods, Keith W., Claiborne, Akiyo, Gwaltney, II, Stephen L., Barr, Kenneth J., Liu, Gang, Gehrke, Laura, Credo, R.Bruce, Hui, Yu Hua, Lee, Jang, Warner, Robert B., Kovar, Peter, Nukkala, Michael A., Zielinski, Nicolette A., Tahir, Stephen K., Fitzgerald, Michael, Kim, Ki H., Marsh, Kennan, Frost, David, Ng, Shi-Chung, Rosenberg, Saul, Sham, Hing L.

“…A series of indole containing oxazolines has been discovered as a result of structural modifications of the lead compound A-105972. The compounds exert their…”
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Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity by Tao, Zhi-Fu, Hasvold, Lisa, Wang, Le, Wang, Xilu, Petros, Andrew M, Park, Chang H, Boghaert, Erwin R, Catron, Nathaniel D, Chen, Jun, Colman, Peter M, Czabotar, Peter E, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Hymowitz, Sarah G, Jin, Sha, Judge, Russell A, Koehler, Michael F. T, Kovar, Peter J, Lessene, Guillaume, Mitten, Michael J, Ndubaku, Chudi O, Nimmer, Paul, Purkey, Hans E, Oleksijew, Anatol, Phillips, Darren C, Sleebs, Brad E, Smith, Brian J, Smith, Morey L, Tahir, Stephen K, Watson, Keith G, Xiao, Yu, Xue, John, Zhang, Haichao, Zobel, Kerry, Rosenberg, Saul H, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J

“…A-1155463, a highly potent and selective BCL-XL inhibitor, was discovered through nuclear magnetic resonance (NMR) fragment screening and structure-based…”
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An inhibitor of Bcl-2 family proteins induces regression of solid tumours by Fesik, Stephen W, Rosenberg, Saul H, Oltersdorf, Tilman, Elmore, Steven W, Shoemaker, Alexander R, Armstrong, Robert C, Augeri, David J, Belli, Barbara A, Bruncko, Milan, Deckwerth, Thomas L, Dinges, Jurgen, Hajduk, Philip J, Joseph, Mary K, Kitada, Shinichi, Korsmeyer, Stanley J, Kunzer, Aaron R, Letai, Anthony, Li, Chi, Mitten, Michael J, Nettesheim, David G, Ng, ShiChung, Nimmer, Paul M, O'Connor, Jacqueline M, Oleksijew, Anatol, Petros, Andrew M, Reed, John C, Shen, Wang, Tahir, Stephen K, Thompson, Craig B, Tomaselli, Kevin J, Wang, Baole, Wendt, Michael D, Zhang, Haichao

“…Proteins in the Bcl-2 family are central regulators of programmed cell death, and members that inhibit apoptosis, such as Bcl-XL and Bcl-2, are overexpressed…”
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Genomic analysis and selective small molecule inhibition identifies BCL-XL as a critical survival factor in a subset of colorectal cancer by Zhang, Haichao, Xue, John, Hessler, Paul, Tahir, Stephen K, Chen, Jun, Jin, Sha, Souers, Andrew J, Leverson, Joel D, Lam, Lloyd T

“…Background Defects in programmed cell death, or apoptosis, are a hallmark of cancer. The anti-apoptotic B-cell lymphoma 2 (BCL-2) family proteins, including…”
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