Search Results - "Arnone, Marc"

Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions by King, Alastair J, Arnone, Marc R, Bleam, Maureen R, Moss, Katherine G, Yang, Jingsong, Fedorowicz, Kelly E, Smitheman, Kimberly N, Erhardt, Joseph A, Hughes-Earle, Angela, Kane-Carson, Laurie S, Sinnamon, Robert H, Qi, Hongwei, Rheault, Tara R, Uehling, David E, Laquerre, Sylvie G

“…Mitogen-Activated Protein Kinase (MAPK) pathway activation has been implicated in many types of human cancer. BRAF mutations that constitutively activate MAPK…”
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Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B‑Raf-Driven Tumors by Rheault, Tara R., Stellwagen, John C., Adjabeng, George M., Hornberger, Keith R., Petrov, Kimberly G., Waterson, Alex G., Dickerson, Scott H., Mook, Robert A., Laquerre, Sylvie G., King, Alastair J., Rossanese, Olivia W., Arnone, Marc R., Smitheman, Kimberly N., Kane-Carson, Laurie S., Han, Chao, Moorthy, Ganesh S., Moss, Katherine G., Uehling, David E.

“…Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-RafV600E mutated enzyme has been observed in a number of human…”
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A Biochemical Rationale for the Anticancer Effects of Hsp90 Inhibitors: Slow, Tight Binding Inhibition by Geldanamycin and Its Analogues by Gooljarsingh, Lata T., Fernandes, Christine, Yan, Kang, Zhang, Hong, Grooms, Michael, Johanson, Kyung, Sinnamon, Robert H., Kirkpatrick, Robert B., Kerrigan, John, Lewis, Tia, Arnone, Marc, King, Alastair J., Lai, Zhihong, Copeland, Robert A., Tummino, Peter J.

“…Heat shock protein (Hsp)90 is emerging as an important therapeutic target for the treatment of cancer. Two analogues of the Hsp90 inhibitor geldanamycin are…”
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Identification of Peptide Substrates for Human MMP-11 (Stromelysin-3) Using Phage Display by Pan, Weijun, Arnone, Marc, Kendall, Marvin, Grafstrom, Robert H., Seitz, Steven P., Wasserman, Zelda R., Albright, Charles F.

“…The MMP-11 proteinase, also known as stromelysin-3, probably plays an important role in human cancer because MMP-11 is frequently overexpressed in human tumors…”
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Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup by STELLWAGEN, John C, ADJABENG, George M, ROMINGER, Cynthia M, ROSSANESE, Olivia W, SMITHEMAN, Kimberly N, WATERSON, Alex G, UEHLING, David E, ARNONE, Marc R, DICKERSON, Scott H, CHAO HAN, HORNBERGER, Keith R, KING, Alastair J, MOOK, Robert A, PETROV, Kimberly G, RHEAULT, Tara R

“…A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability…”
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Abstract B88: A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation by Laquerre, Sylvie, Arnone, Marc, Moss, Katherine, Yang, Jingsong, Fisher, Kelly, Kane-Carson, Laurie S., Smitheman, Kimberly, Ward, Jessica, Heidrich, Bradley, Rheault, Tara, Adjabeng, George, Hornberger, Keith, Stellwagen, John, Waterson, Alex, Han, Chao, Mook, Robert A., Uehling, David, King, Alastair J.

“…Abstract Activation of the Ras-Raf-MEK-ERK pathway has been implicated in a large range of human cancers. Growth factor receptor stimulation by extracellular…”
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Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one Inhibitors of Cyclin-Dependent Kinases by Markwalder, Jay A, Arnone, Marc R, Benfield, Pamela A, Boisclair, Michael, Burton, Catherine R, Chang, Chong-Hwan, Cox, Sarah S, Czerniak, Philip M, Dean, Charity L, Doleniak, Deborah, Grafstrom, Robert, Harrison, Barbara A, Kaltenbach, Robert F, Nugiel, David A, Rossi, Karen A, Sherk, Susan R, Sisk, Lisa M, Stouten, Pieter, Trainor, George L, Worland, Peter, Seitz, Steven P

“…Using a high-throughput screening strategy, a series of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-ones was identified that inhibit the cyclin-dependent…”
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Putative identification of functional interactions between DNA intercalating agents and topoisomerase II using the V79 in vitro micronucleus assay by Snyder, Ronald D, Arnone, Marc R

“…Clastogenicity is frequently observed following treatment of mammalian cells with new chemical entities. This clastogenicity, unless proven otherwise, is…”
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Abstract 5035: Predictions of therapeutic doses of a B-Raf inhibitor, GSK2118436, based on exposure-response modeling of preclinical tumor biomarker and xenograft data by Ouellet, Daniele, Laquerre, Sylvie, Minthorn, Elisabeth, Arnone, Marc, Bleam, Maureen, Liu, Qi, Moss, Katherine, Lebowitz, Peter

“…Abstract Background: GSK2118436 is a potent inhibitor of B-Raf, a signal transduction kinase in the MAPK pathway that can be mutated to become an oncogenic…”
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Development of potent B-Raf super(V600E inhibitors containing an arylsulfonamide headgroup) by Stellwagen, John C, Adjabeng, George M, Arnone, Marc R, Dickerson, Scott H, Han, Chao, Hornberger, Keith R, King, Alastair J, Mook, Robert A, Petrov, Kimberly G, Rheault, Tara R, Rominger, Cynthia M, Rossanese, Olivia W, Smitheman, Kimberly N, Waterson, Alex G, Uehling, David E

“…A potent series of inhibitors against the B-Raf super(V600E kinase have been developed that show excellent activity in cellular assays and good oral…”
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Development of potent B-Raf V600E inhibitors containing an arylsulfonamide headgroup by Stellwagen, John C., Adjabeng, George M., Arnone, Marc R., Dickerson, Scott H., Han, Chao, Hornberger, Keith R., King, Alastair J., Mook, Robert A., Petrov, Kimberly G., Rheault, Tara R., Rominger, Cynthia M., Rossanese, Olivia W., Smitheman, Kimberly N., Waterson, Alex G., Uehling, David E.

“…A potent series of inhibitors against the B-Raf V600E kinase have been developed that show excellent activity in cellular assays and good oral bioavailability…”
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Putative identification of functional interactions between DNA intercalating agents and topoisomerase II using the V79 in vitro micronucleus assay by SNYDER, Ronald D, ARNONE, Marc R

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Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1 H -pyrazolo[3,4- d ]pyrimidin-4-one Inhibitors of Cyclin-Dependent Kinases by Markwalder, Jay A., Arnone, Marc R., Benfield, Pamela A., Boisclair, Michael, Burton, Catherine R., Chang, Chong-Hwan, Cox, Sarah S., Czerniak, Philip M., Dean, Charity L., Doleniak, Deborah, Grafstrom, Robert, Harrison, Barbara A., Kaltenbach, Robert F., Nugiel, David A., Rossi, Karen A., Sherk, Susan R., Sisk, Lisa M., Stouten, Pieter, Trainor, George L., Worland, Peter, Seitz, Steven P.

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