Search Results - "DeFina, Steven C"

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973) by Rice, Kenneth D, Aay, Naing, Anand, Neel K, Blazey, Charles M, Bowles, Owen J, Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K, Defina, Steven C, Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A, Kennedy, Abigail R, Kim, Angie I, Koltun, Elena S, Lougheed, Julie C, Manalo, Jean-Claire L, Martini, Jean-Francois, Nuss, John M, Peto, Csaba J, Tsang, Tsze H, Yu, Peiwen, Johnston, Stuart

“…The ERK/MAP kinase cascade is a key mechanism subject to dysregulation in cancer and is constitutively activated or highly upregulated in many tumor types…”
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Discovery of XL888: A novel tropane-derived small molecule inhibitor of HSP90 by Bussenius, Joerg, Blazey, Charles M., Aay, Naing, Anand, Neel K., Arcalas, Arlyn, Baik, TaeGon, Bowles, Owen J., Buhr, Chris A., Costanzo, Simona, Curtis, Jeffrey K., DeFina, Steven C., Dubenko, Larisa, Heuer, Timothy S., Huang, Ping, Jaeger, Christopher, Joshi, Anagha, Kennedy, Abigail R., Kim, Angie I., Lara, Katherine, Lee, Jae, Li, Jonathan, Lougheed, Julie C., Ma, Sunghoon, Malek, Shiva, Manalo, Jean-Claire L., Martini, Jean-Francois, McGrath, Garth, Nicoll, Monique, Nuss, John M., Pack, Michael, Peto, Csaba J., Tsang, Tsze H., Wang, Longcheng, Womble, Scott W., Yakes, Michael, Zhang, Wentao, Rice, Kenneth D.

“…Lead optimization of tropane-derived HTS hits driven by traditional SAR and X-ray crystallography led to the identification of clinical candidate 12i (XL888)…”
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Recognition of Planar and Nonplanar Ligands in the Malachite Green-RNA Aptamer Complex by Flinders, Jeremy, DeFina, Steven C, Brackett, David M, Baugh, Chris, Wilson, Charles, Dieckmann, Thorsten

“…Ribonucleic acids are an attractive drug target owing to their central role in many pathological processes. Notwithstanding this potential, RNA has only rarely…”
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Pyrazolopyrimidines as dual Akt/p70S6K inhibitors by Rice, Kenneth D., Kim, Moon H., Bussenius, Joerg, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Canne-Bannen, Lynne, Chan, Diva S.-M., Chen, Baili, Co, Erick W., Costanzo, Simona, DeFina, Steven C., Dubenko, Larisa, Engst, Stefan, Franzini, Maurizio, Huang, Ping, Jammalamadaka, Vasu, Khoury, Richard G., Klein, Rhett R., Laird, A.Douglas, Le, Donna T., Mac, Morrison B., Matthews, David J., Markby, David, Miller, Nicole, Nuss, John M., Parks, Jason J., Tsang, Tsze H., Tsuhako, Amy L., Wang, Yong, Xu, Wei

“…Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6Kinase, which is the last kinase in the…”
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Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors by Bussenius, Joerg, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Bannen, Lynne Canne, Chan, Diva S.-M., Chen, Baili, Co, Erick W., Costanzo, Simona, DeFina, Steven C., Dubenko, Larisa, Engst, Stefan, Franzini, Maurizio, Huang, Ping, Jammalamadaka, Vasu, Khoury, Richard G., Kim, Moon H., Klein, Rhett R., Laird, Douglas, Le, Donna T., Mac, Morrison B., Matthews, David J., Markby, David, Miller, Nicole, Nuss, John M., Parks, Jason J., Tsang, Tsze H., Tsuhako, Amy L., Wang, Yong, Xu, Wei, Rice, Kenneth D.

“…The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K…”
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Binding to an RNA Aptamer Changes the Charge Distribution and Conformation of Malachite Green by Nguyen, Dat H, DeFina, Steven C, Fink, William H, Dieckmann, Thorsten

“…RNA plays a central role in many biological processes and is therefore an important target for drug development. In recent years an increasing wealth of…”
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Synthesis of selectively 15N- or 13C-labelled malachite green by DeFina, Steven C., Dieckmann, Thorsten

“…Two complimentary syntheses of selectively 15N‐ or 13C‐labelled malachite green hydrochloride were developed in order to provide labelled ligands for…”
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Serotonin transporter inhibitors: synthesis and binding potency of 2′-methyl- and 3′-methyl-6-nitroquipazine by Gerdes, John M, DeFina, Steven C, Wilson, Paul A, Taylor, Scott E

“…Racemic 2′-methyl- and 3′-methyl-6-nitroquipazine ligands were selected as targets, synthesized and evaluated at the serotonin transporter employing an in…”
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Synthesis of selectively 15 N‐ or 13 C‐labelled malachite green by DeFina, Steven C., Dieckmann, Thorsten

“…Two complimentary syntheses of selectively 15 N‐ or 13 C‐labelled malachite green hydrochloride were developed in order to provide labelled ligands for…”
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