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17 results on '"Ackler, Scott"'

1. Supplementary Figure 1 from The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

Author

Chen, Jun, primary, Jin, Sha, primary, Abraham, Vivek, primary, Huang, Xiaoli, primary, Liu, Bernard, primary, Mitten, Michael J., primary, Nimmer, Paul, primary, Lin, Xiaoyu, primary, Smith, Morey, primary, Shen, Yu, primary, Shoemaker, Alexander R., primary, Tahir, Stephen K., primary, Zhang, Haichao, primary, Ackler, Scott L., primary, Rosenberg, Saul H., primary, Maecker, Heather, primary, Sampath, Deepak, primary, Leverson, Joel D., primary, Tse, Chris, primary, and Elmore, Steven W., primary

Published
2023
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2. Data from The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

Author

Chen, Jun, primary, Jin, Sha, primary, Abraham, Vivek, primary, Huang, Xiaoli, primary, Liu, Bernard, primary, Mitten, Michael J., primary, Nimmer, Paul, primary, Lin, Xiaoyu, primary, Smith, Morey, primary, Shen, Yu, primary, Shoemaker, Alexander R., primary, Tahir, Stephen K., primary, Zhang, Haichao, primary, Ackler, Scott L., primary, Rosenberg, Saul H., primary, Maecker, Heather, primary, Sampath, Deepak, primary, Leverson, Joel D., primary, Tse, Chris, primary, and Elmore, Steven W., primary

Published
2023
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3. Supplementary Table 1, Figure Legends 1-2 from The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

Author

Chen, Jun, primary, Jin, Sha, primary, Abraham, Vivek, primary, Huang, Xiaoli, primary, Liu, Bernard, primary, Mitten, Michael J., primary, Nimmer, Paul, primary, Lin, Xiaoyu, primary, Smith, Morey, primary, Shen, Yu, primary, Shoemaker, Alexander R., primary, Tahir, Stephen K., primary, Zhang, Haichao, primary, Ackler, Scott L., primary, Rosenberg, Saul H., primary, Maecker, Heather, primary, Sampath, Deepak, primary, Leverson, Joel D., primary, Tse, Chris, primary, and Elmore, Steven W., primary

Published
2023
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4. Supplementary Figure 2 from The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

Author

Chen, Jun, primary, Jin, Sha, primary, Abraham, Vivek, primary, Huang, Xiaoli, primary, Liu, Bernard, primary, Mitten, Michael J., primary, Nimmer, Paul, primary, Lin, Xiaoyu, primary, Smith, Morey, primary, Shen, Yu, primary, Shoemaker, Alexander R., primary, Tahir, Stephen K., primary, Zhang, Haichao, primary, Ackler, Scott L., primary, Rosenberg, Saul H., primary, Maecker, Heather, primary, Sampath, Deepak, primary, Leverson, Joel D., primary, Tse, Chris, primary, and Elmore, Steven W., primary

Published
2023
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5. Supplementary Fig. S1 from ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

Author

Ackler, Scott, primary, Xiao, Yu, primary, Mitten, Michael J., primary, Foster, Kelly, primary, Oleksijew, Anatol, primary, Refici, Marion, primary, Schlessinger, Sally, primary, Wang, Baole, primary, Chemburkar, Sanjay R., primary, Bauch, Joy, primary, Tse, Christin, primary, Frost, David J., primary, Fesik, Stephen W., primary, Rosenberg, Saul H., primary, Elmore, Steven W., primary, and Shoemaker, Alex R., primary

Published
2023
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6. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

Author

Souers, Andrew J., Leverson, Joel D., Boghaert, Erwin R., Ackler, Scott L., Catron, Nathaniel D., Chen, Jun, Dayton, Brian D., Ding, Hong, Enschede, Sari H., Fairbrother, Wayne J., Huang, David C.S., Hymowitz, Sarah G., Jin, Sha, Khaw, Seong Lin, Kovar, Peter J., Lam, Lloyd T., Lee, Jackie, Maecker, Heather L., Marsh, Kennan C., Mason, Kylie D., Mitten, Michael J., Nimmer, Paul M., Oleksijew, Anatol, Park, Chang H., Park, Cheol-Min, Phillips, Darren C., Roberts, Andrew W., Sampath, Deepak, Seymour, John F., Smith, Morey L., Sullivan, Gerard M., Tahir, Stephen K., Tse, Chris, Wendt, Michael D., Xiao, Yu, Xue, John C., Zhang, Haichao, Humerickhouse, Rod A., Rosenberg, Saul H., and Elmore, Steven W.

Subjects
Physiological aspects, Health aspects, Blood platelets -- Physiological aspects -- Health aspects, B cells -- Physiological aspects -- Health aspects, Blood proteins -- Physiological aspects -- Health aspects, Antineoplastic agents -- Physiological aspects -- Health aspects, Antimitotic agents -- Physiological aspects -- Health aspects
Abstract

Apoptosis, or programmed cell death, is a conserved and regulated process that is the primary mechanism for the removal of aged, damaged and unnecessary cells. The ability to block apoptotic [...], Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic process. This family comprises proapoptotic and prosurvival proteins, and shifting the balance toward the latter is an established mechanism whereby cancer cells evade apoptosis. The therapeutic potential of directly inhibiting prosurvival proteins was unveiled with the development of navitoclax, a selective inhibitor of both BCL-2 and BCL-2-like 1 ([BCL-X.sub.L]), which has shown clinical efficacy in some BCL-2-dependent hematological cancers. However, concomitant on-target thrombocytopenia caused by [BCL-X.sub.L] inhibition limits the efficacy achievable with this agent. Here we report the re-engineering of navitoclax to create a highly potent, orally bioavailable and BCL-2-selective inhibitor, ABT-199. This compound inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicate that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2-dependent hematological cancers.

Published
2013
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11. Clearance of systemic hematologic tumors by venetoclax (Abt‐199) and navitoclax

Author

Ackler, Scott, primary, Oleksijew, Anatol, additional, Chen, Jun, additional, Chyla, Brenda J., additional, Clarin, Jerry, additional, Foster, Kelly, additional, McGonigal, Thomas, additional, Mishra, Sasmita, additional, Schlessinger, Sally, additional, Smith, Morey L., additional, Tahir, Stephen K., additional, Leverson, Joel D., additional, Souers, Andrew J., additional, Boghaert, Erwin R., additional, and Hickson, Jonathan, additional

Published
2015
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12. Abstract C249: Detection of tissue and bone marrow clearance of systemically engrafted hematologic tumors by ABT-199 and navitoclax using bioluminescent imaging.

Author

Ackler, Scott L., primary, Oleksijew, Anatol, additional, Chen, Jun, additional, Chyla, Brenda J., additional, Clarin, Jerry, additional, Foster, Kelly, additional, McGonigal, Thomas, additional, Mishra, Sasmita, additional, Schlessinger, Sally, additional, Smith, Morey L., additional, Tahir, Stephen K., additional, Leverson, Joel, additional, Souers, Andrew J., additional, Boghaert, Erwin R., additional, and Hickson, Jonathan, additional

Published
2013
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13. The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

Author

Chen, Jun, primary, Jin, Sha, additional, Abraham, Vivek, additional, Huang, Xiaoli, additional, Liu, Bernard, additional, Mitten, Michael J., additional, Nimmer, Paul, additional, Lin, Xiaoyu, additional, Smith, Morey, additional, Shen, Yu, additional, Shoemaker, Alexander R., additional, Tahir, Stephen K., additional, Zhang, Haichao, additional, Ackler, Scott L., additional, Rosenberg, Saul H., additional, Maecker, Heather, additional, Sampath, Deepak, additional, Leverson, Joel D., additional, Tse, Chris, additional, and Elmore, Steven W., additional

Published
2011
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14. Characterization of the PKB/AKT Pathway in the Role of Tumorigenesis and Transformation of MCF10A Human Mammary Epithelial Cells

Author

GEORGETOWN UNIV WASHINGTON DC MEDICAL CENTER, Ackler, Scott L., GEORGETOWN UNIV WASHINGTON DC MEDICAL CENTER, and Ackler, Scott L.

Abstract

The Akt homology domain (AM) of Akt has been identified as a potential dimerization site within the kinase, and potentially could serve as a selective inhibitor of these kinases. We fused the AM domains of Akt1 (AH1) and Akt2 (AH2) to EGFP and performed expression studies with these constructs. Overexpression of both in PTEN deficient U87 cells sensitized these cells to apoptosis from camptothecin treatment, while neither was able to do this in PTEN+ MCF-7 cells. AH2 was able to block overexpressed Aktl and endogenous Akts inhibition of AFX as measured by an AFX reporter assay, but not when Akt2 was overexpressed. AFX disinhibition in U87 and MCF-7 cells patterned their effects in the cytotoxicity assay. Finally, we were able to demonstrate that AH2 bound to Akt1 and Akt2, but AHl only bound to Akt1 using co-immunoprecipitation assays; both bound to PDK1. Binding of AH domains to Akt decreased phosphorylation within the activation loop of Akts. We hypothesize that the AH2 domain binds to the AM domain within Akts, and this blocks access either to 3'OH-phosphoinositides or PDK1, and thereby inhibits Akt activation. We further hypothesize that PTEN deficient cells are more susceptible to Akt inhibition PTEN expressing cells.

Published
2003

15. ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

Author

Ackler, Scott, primary, Xiao, Yu, additional, Mitten, Michael J., additional, Foster, Kelly, additional, Oleksijew, Anatol, additional, Refici, Marion, additional, Schlessinger, Sally, additional, Wang, Baole, additional, Chemburkar, Sanjay R., additional, Bauch, Joy, additional, Tse, Christin, additional, Frost, David J., additional, Fesik, Stephen W., additional, Rosenberg, Saul H., additional, Elmore, Steven W., additional, and Shoemaker, Alex R., additional

Published
2008
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16. Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models

Author

Shoemaker, Alex R., primary, Mitten, Michael J., additional, Adickes, Jessica, additional, Ackler, Scott, additional, Refici, Marion, additional, Ferguson, Debra, additional, Oleksijew, Anatol, additional, O'Connor, Jacqueline M., additional, Wang, Baole, additional, Frost, David J., additional, Bauch, Joy, additional, Marsh, Kennan, additional, Tahir, Steven K., additional, Yang, Xiufen, additional, Tse, Christin, additional, Fesik, Stephen W., additional, Rosenberg, Saul H., additional, and Elmore, Steven W., additional

Published
2008
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17. The Bcl-2 Family Inhibitor ABT-263 Shows Significant Anti-Tumor Efficacy in Models of B Cell Non-Hodgkin’s Lymphoma.

Author

Shoemaker, Alex R., primary, Mitten, Michael J., additional, Oleksijew, Anatol, additional, O’Connor, Jacqeuline M., additional, Wang, Baole, additional, Ackler, Scott, additional, Joseph, Mary, additional, Zhang, Haichao, additional, Nimmer, Paul, additional, Xiao, Yu, additional, Tse, Christin, additional, Frost, David J., additional, Fesik, Stephen W., additional, Rosenberg, Saul H., additional, and Elmore, Steven W., additional

Published
2006
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