Search Results - "O'Connell, Shawn"

Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1) by Kanouni, Toufike, Severin, Christophe, Cho, Robert W, Yuen, Natalie Y.-Y, Xu, Jiangchun, Shi, Lihong, Lai, Chon, Del Rosario, Joselyn R, Stansfield, Ryan K, Lawton, Lee N, Hosfield, David, O’Connell, Shawn, Kreilein, Matt M, Tavares-Greco, Paula, Nie, Zhe, Kaldor, Stephen W, Veal, James M, Stafford, Jeffrey A, Chen, Young K

“…Histone demethylase LSDl (KDMlA) belongs to the flavin adenine dinucleotide (FAD) dependent family of monoamine oxidases and is vital in regulation of…”
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Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer by Dong, Qing, Dougan, Douglas R., Gong, Xianchang, Halkowycz, Petro, Jin, Bohan, Kanouni, Toufike, O’Connell, Shawn M., Scorah, Nicholas, Shi, Lihong, Wallace, Michael B., Zhou, Feng

“…A series of potent 8-methylpyrido[2,3- d]pyrimidine-4,7(3 H,8 H)-dione inhibitors of MEK kinase was designed and synthesized. Structural properties and…”
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Histone lysine acetyltransferase inhibitors: an emerging class of drugs for cancer therapy by White, Jeffrey, Derheimer, Frederick A., Jensen-Pergakes, Kristen, O’Connell, Shawn, Sharma, Shikhar, Spiegel, Noah, Paul, Thomas A.

“…Due to their important function in cancer, lysine acetyltransferases (KATs) are an emerging class of drug targets.Small-molecule KAT inhibitors have been…”
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Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides by Bressi, Jerome C., Jennings, Andy J., Skene, Robert, Wu, Yiqin, Melkus, Robert, Jong, Ron De, O’Connell, Shawn, Grimshaw, Charles E., Navre, Marc, Gangloff, Anthony R.

“…Substituted N-(2-aminophenyl)benzamides demonstrated time-dependent binding kinetics that is rationalized using a co-complex crystal structure of HDAC2 and…”
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Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models by Chen, Young K, Bonaldi, Tiziana, Cuomo, Alessandro, Del Rosario, Joselyn R, Hosfield, David J, Kanouni, Toufike, Kao, Shih-chu, Lai, Chon, Lobo, Neethan A, Matuszkiewicz, Jennifer, McGeehan, Andrew, O’Connell, Shawn M, Shi, Lihong, Stafford, Jeffrey A, Stansfield, Ryan K, Veal, James M, Weiss, Michael S, Yuen, Natalie Y, Wallace, Michael B

“…Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related processes. Herein, we describe our discovery of a series of potent…”
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Structure-based design and discovery of potent and selective KDM5 inhibitors by Nie, Zhe, Shi, Lihong, Lai, Chon, O'Connell, Shawn M., Xu, Jiangchun, Stansfield, Ryan K., Hosfield, David J., Veal, James M., Stafford, Jeffrey A.

“…[Display omitted] •KDM5A/5B have been identified as potential anti-cancer drug targets.•Compound 33 is an orally available, potent inhibitor of KDM5A/5B with…”
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Optimization of mTOR Inhibitors Using Property-Based Drug Design and Free–Wilson Analysis for Improved In Vivo Efficacy by Murphy, Sean T., Atienza, Joy, Brown, Jason W., Cheruvallath, Zacharia S., Cukierski, Matthew J., Fabrey, Robyn, Keung, Walter, Kwok, Lily, O’Connell, Shawn, Tang, Mingnam, Vanderpool, Darin L., Vincent, Patrick W., Zhang, Lilly, Marx, Matthew A.

“…The mTOR kinase regulates a variety of critical cellular processes and has become a target for the treatment of various cancers. Using a combination of…”
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Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy by Adams, Mark E., Wallace, Michael B., Kanouni, Toufike, Scorah, Nicholas, O’Connell, Shawn M., Miyake, Hiroshi, Shi, Lihong, Halkowycz, Petro, Zhang, Lilly, Dong, Qing

“…The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The…”
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Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors by Wallace, Michael B., Adams, Mark E., Kanouni, Toufike, Mol, Clifford D., Dougan, Douglas R., Feher, Victoria A., O’Connell, Shawn M., Shi, Lihong, Halkowycz, Petro, Dong, Qing

“…A series of potent pyrrole-based inhibitors of MEK kinase was designed and synthesized. Structural properties and biological activities are described. A novel…”
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Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors by Gangloff, Anthony R., Brown, Jason, de Jong, Ron, Dougan, Douglas R., Grimshaw, Charles E., Hixon, Mark, Jennings, Andy, Kamran, Ruhi, Kiryanov, Andre, O’Connell, Shawn, Taylor, Ewan, Vu, Phong

“…Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic & cellular activities…”
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Antitumor activity of the MEK inhibitor TAK-733 against melanoma cell lines and patient-derived tumor explants by Micel, Lindsey N, Tentler, John J, Tan, Aik-Choon, Selby, Heather M, Brunkow, Kelsey L, Robertson, Kelli M, Davis, S Lindsey, Klauck, Peter J, Pitts, Todd M, Gangolli, Esha, Fabrey, Robyn, O'Connell, Shawn M, Vincent, Patrick W, Eckhardt, S Gail

“…The goal of this study was to investigate the activity of the selective MEK1/2 inhibitor TAK-733 in both melanoma cell lines and patient-derived melanoma…”
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Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors by Bennett, Michael J., Wu, Yiqin, Boloor, Amogh, Matuszkiewicz, Jennifer, O'Connell, Shawn M., Shi, Lihong, Stansfield, Ryan K., Del Rosario, Joselyn R., Veal, James M., Hosfield, David J., Xu, Jiangchun, Kaldor, Stephen W., Stafford, Jeffrey A., Betancort, Juan M.

“…[Display omitted] •Novel 4-phenylisoquinolinone BET bromodomain inhibitors are disclosed.•Structure guided SAR exploration resulted in >10,000-fold potency…”
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Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity by Bressi, Jerome C., Jong, Ron de, Wu, Yiqin, Jennings, Andy J., Brown, Jason W., O’Connell, Shawn, Tari, Leslie W., Skene, Robert J., Vu, Phong, Navre, Marc, Cao, Xiaodong, Gangloff, Anthony R.

“…A series of imidazole and benzimidazole compounds were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases, displaying…”
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Multistep signaling requirements for pituitary organogenesis in vivo by Treier, M, Gleiberman, A S, O'Connell, S M, Szeto, D P, McMahon, J A, McMahon, A P, Rosenfeld, M G

“…During development of the mammalian pituitary gland specific hormone-producing cell types, critical in maintaining homeostasis, emerge in a spatially and…”
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Pitx2 regulates lung asymmetry, cardiac positioning and pituitary and tooth morphogenesis by Izpisúa-Belmonte, Juan Carlos, Rosenfeld, Michael G, Lin, Chijen R, Kioussi, Chrissa, O'Connell, Shawn, Briata, Paola, Szeto, Daniel, Liu, Forrest

“…Pitx1 (refs 1,2,3) and Pitx2 (refs 4, 5) are highly homologous, bicoid-related transcription factors. Pitx2 was initially identified as the gene responsible…”
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Reciprocal Interactions of Pit1 and GATA2 Mediate Signaling Gradient–Induced Determination of Pituitary Cell Types by Dasen, Jeremy S, O’Connell, Shawn M, Flynn, Sarah E, Treier, Mathias, Gleiberman, Anatoli S, Szeto, Daniel P, Hooshmand, Farideh, Aggarwal, Aneel K, Rosenfeld, Michael G

“…The mechanisms by which transient gradients of signaling molecules lead to emergence of specific cell types remain a central question in mammalian…”
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Pituitary lineage determination by the Prophet of Pit-1 homeodomain factor defective in Ames dwarfism by Sornson, Mark W, Wu, Wei, Dasen, Jeremy S, Flynn, Sarah E, Norman, Deborah J, O'Connell, Shawn M, Gukovsky, Ilya, Carrière, Catherine, Ryan, Aimee K, Miller, Andrew P, Zuo, Lin, Gleiberman, Anatoli S, Andersen, Bogi, Beamer, Wes G, Rosenfeld, Michael G

“…The gene apparently responsible for a heritable form of murine pituitary-dependent dwarfism (Ames dwarf, df) has been positionally cloned, identifying a novel,…”
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Pax6 Is Essential for Establishing Ventral-Dorsal Cell Boundaries in Pituitary Gland Development by Kioussi, Chrissa, O'Connell, Shawn, St-Onge, Luc, Treier, Mathias, Gleiberman, Anatoli S., Gruss, Peter, Rosenfeld, Michael G.

“…Pax6, a highly conserved member of the paired homeodomain transcription factor family that plays essential roles in ocular, neural, and pancreatic development…”
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Role of the Bicoid-related homeodomain factor Pitx1 in specifying hindlimb morphogenesis and pituitary development by Szeto, D P, Rodriguez-Esteban, C, Ryan, A K, O'Connell, S M, Liu, F, Kioussi, C, Gleiberman, A S, Izpisúa-Belmonte, J C, Rosenfeld, M G

“…Pitx1 is a Bicoid-related homeodomain factor that exhibits preferential expression in the hindlimb, as well as expression in the developing anterior pituitary…”
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Role of transcription factors a Brn-3.1 and Brn-3.2 in auditory and visual system development by Erkman, Linda, McEvilly, Robert J, Luo, Lin, Ryan, Aimee K, Hooshmand, Farideh, O'Connell, Shawn M, Keithley, Elizabeth M, Rapaport, David H, Ryan, Alien F, Rosenfeld, Michael G

“…The neurally expressed genes Brn-3.1 and Brn-3.2 (refs 1-6) are mammalian orthologues of the Caenorhabditis elegans unc-86 gene that constitute, with Brn-3.0…”
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