Search Results - "Laquerre, Sylvie G"

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…”
Get full text

Distinct Concentration-Dependent Effects of the Polo-like Kinase 1―Specific Inhibitor GSK461364A, Including Differential Effect on Apoptosis by GILMARTIN, Aidan G, BLEAM, Maureen R, SUTTON, David, DIAMOND, Melody A, JACKSON, Jeffrey R, LAQUERRE, Sylvie G, RICHTER, Mark C, ERSKINE, Symon G, KRUGER, Ryan G, MADDEN, Lenore, HASSLER, Daniel F, SMITH, Gary K, GONTAREK, Richard R, COURTNEY, Mary P

“…Polo-like kinase 1 (Plk1) is a conserved serine/threonine kinase that plays an essential role in regulating the many processes involved in mitotic entry and…”
Get full text

Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate) by Abe, Hiroyuki, Kikuchi, Shinichi, Hayakawa, Kazuhide, Iida, Tetsuya, Nagahashi, Noboru, Maeda, Katsuya, Sakamoto, Johei, Matsumoto, Noriaki, Miura, Tomoya, Matsumura, Koji, Seki, Noriyoshi, Inaba, Takashi, Kawasaki, Hisashi, Yamaguchi, Takayuki, Kakefuda, Reina, Nanayama, Toyomichi, Kurachi, Hironori, Hori, Yoshikazu, Yoshida, Takayuki, Kakegawa, Junya, Watanabe, Yoshihiro, Gilmartin, Aidan G, Richter, Mark C, Moss, Katherine G, Laquerre, Sylvie G

“…Inhibition of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) represents a promising strategy for the discovery of a new…”
Get full text

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition by GILMARTIN, Aidan G, BLEAM, Maureen R, ZAPPACOSTA, Francesca, ANNAN, Roland, SUTTON, David, LAQUERRE, Sylvie G, GROY, Arthur, MOSS, Katherine G, MINTHORN, Elisabeth A, KULKARNI, Swarupa G, ROMINGER, Cynthia M, ERSKINE, Symon, FISHER, Kelly E, JINGSONG YANG

“…Despite their preclinical promise, previous MEK inhibitors have shown little benefit for patients. This likely reflects the narrow therapeutic window for MEK…”
Get full text

Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations by Greger, James G, Eastman, Stephen D, Zhang, Vivian, Bleam, Maureen R, Hughes, Ashley M, Smitheman, Kimberly N, Dickerson, Scott H, Laquerre, Sylvie G, Liu, Li, Gilmer, Tona M

“…Recent results from clinical trials with the BRAF inhibitors GSK2118436 (dabrafenib) and PLX4032 (vemurafenib) have shown encouraging response rates; however,…”
Get full text

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…”
Get full text

Abstract C74: Reassessing IKKε as a novel oncology target by Richter, Mark C., Groy, Arthur X., Wang, Da-Yuan, Lu, Quinn, Holbrook, Joanna D., Sarpong, Martha A., Seefeld, Mark A., Smith, Danielle M., Laquerre, Sylvie G., Gilmartin, Aidan G.

“…Abstract Recent years have seen increasing efforts to employ integrative genomic approaches to identify novel oncogenes. In this manner, IKBKE coding for IKKε…”
Get full text