Search Results - "Bittner, Mark"

Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin by Bhagwat, Shripad V, Gokhale, Prafulla C, Crew, Andrew P, Cooke, Andy, Yao, Yan, Mantis, Christine, Kahler, Jennifer, Workman, Jennifer, Bittner, Mark, Dudkin, Lorina, Epstein, David M, Gibson, Neil W, Wild, Robert, Arnold, Lee D, Houghton, Peter J, Pachter, Jonathan A

“…The phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway is frequently activated in human cancers, and mTOR is a clinically validated target. mTOR forms two…”
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Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors by Jin, Meizhong, Wang, Jing, Kleinberg, Andrew, Kadalbajoo, Mridula, Siu, Kam W., Cooke, Andrew, Bittner, Mark A., Yao, Yan, Thelemann, April, Ji, Qunsheng, Bhagwat, Shripad, Mulvihill, Kristen M., Rechka, Josef A., Pachter, Jonathan A., Crew, Andrew P., Epstein, David, Mulvihill, Mark J.

“…This Letter describes the medicinal chemistry effort towards a series of novel imidazo[1,5-a]pyrazine derived inhibitors of ACK1. Virtual screening led to the…”
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Imidazo[1,5- a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2 by Crew, Andrew P., Bhagwat, Shripad V., Dong, Hanqing, Bittner, Mark A., Chan, Anna, Chen, Xin, Coate, Heather, Cooke, Andrew, Gokhale, Prafulla C., Honda, Ayako, Jin, Meizhong, Kahler, Jennifer, Mantis, Christine, Mulvihill, Mark J., Tavares-Greco, Paula A., Volk, Brian, Wang, Jing, Werner, Douglas S., Arnold, Lee D., Pachter, Jonathan A., Wild, Robert, Gibson, Neil W.

“…The discovery of a selective and orally efficacious imidazo[1,5- a]pyrazine mTOR inhibitor ( 4c) via optimization of an HTS hit is described. The discovery and…”
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Discovery of Novel Insulin-Like Growth Factor‑1 Receptor Inhibitors with Unique Time-Dependent Binding Kinetics by Jin, Meizhong, Petronella, Brenda A, Cooke, Andy, Kadalbajoo, Mridula, Siu, Kam W, Kleinberg, Andrew, May, Earl W, Gokhale, Prafulla C, Schulz, Ryan, Kahler, Jennifer, Bittner, Mark A, Foreman, Kenneth, Pachter, Jonathan A, Wild, Robert, Epstein, David, Mulvihill, Mark J

“…This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure–activity and…”
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OSI-930 : A novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models by GARTON, Andrew J, CREW, Andrew P. A, BITTNER, Mark A, KEILY, John F, BRINER, Paul, HIDDEN, Chris, SREBERNAK, Mary C, PIRRIT, Carrie, O'CONNOR, Matthew, ANNA CHAN, VULEVIC, Bojana, HENNINGER, Dwight, FRANKLIN, Maryland, HART, Karen, SENNELLO, Regina, LI, An-Hu, TAO ZHANG, RICHARDSON, Frank, EMERSON, David L, CASTELHANO, Arlindo L, ARNOLD, Lee D, GIBSON, Neil W, COOKE, Andrew R, WYNNE, Graham M, CASTALDO, Linda, KAHLER, Jennifer, WINSKI, Shannon L, FRANKS, April, BROWN, Eric N

“…OSI-930 is a novel inhibitor of the receptor tyrosine kinases Kit and kinase insert domain receptor (KDR), which is currently being evaluated in clinical…”
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Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy by Jin, Meizhong, Kleinberg, Andrew, Cooke, Andy, Gokhale, Prafulla C., Foreman, Kenneth, Dong, Hanqing, Siu, Kam W., Bittner, Mark A., Mulvihill, Kristen M., Yao, Yan, Landfair, Darla, O’Connor, Matthew, Mak, Gilda, Pachter, Jonathan A., Wild, Robert, Rosenfeld-Franklin, Maryland, Ji, Qunsheng, Mulvihill, Mark J.

“…Preclinical and emerging clinical evidence suggests that inhibiting insulin-like growth factor 1 receptor (IGF-1R) signaling may offer a promising therapeutic…”
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Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR by Jin, Meizhong, Gokhale, Prafulla C, Cooke, Andy, Foreman, Kenneth, Buck, Elizabeth, May, Earl W, Feng, Lixin, Bittner, Mark A, Kadalbajoo, Mridula, Landfair, Darla, Siu, Kam W, Stolz, Kathryn M, Werner, Douglas S, Laufer, Radoslaw S, Li, An-Hu, Dong, Hanqing, Steinig, Arno G, Kleinberg, Andrew, Yao, Yan, Pachter, Jonathan A, Wild, Robert, Mulvihill, Mark J

“…This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor…”
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Men in Early Childhood Education: Their Emergent Issues by Cooney, Margaret H, Bittner, Mark T

“…Focus groups were used to explore emergent issues for men in early childhood education. Preservice teachers, classroom teachers, and male professors identified…”
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Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: Optimization of kinase selectivity and pharmacokinetics by Hornberger, Keith R., Chen, Xin, Crew, Andrew P., Kleinberg, Andrew, Ma, Lifu, Mulvihill, Mark J., Wang, Jing, Wilde, Victoria L., Albertella, Mark, Bittner, Mark, Cooke, Andrew, Kadhim, Salam, Kahler, Jennifer, Maresca, Paul, May, Earl, Meyn, Peter, Romashko, Darlene, Tokar, Brianna, Turton, Roy

“…The kinase selectivity and pharmacokinetic optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. The intersection of insights…”
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Temperament and School-Aged Children's Coping Abilities and Responses to Stress by Carson, David K., Bittner, Mark T.

“…To measure children's temperament and coping abilities, we administered the Stress Impact Scale to sixty 9- to 12-year-old children. Trained observers also…”
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Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 by Hornberger, Keith R., Berger, Dan M., Crew, Andrew P., Dong, Hanqing, Kleinberg, Andrew, Li, An-Hu, Medeiros, Matthew R., Mulvihill, Mark J., Siu, Kam, Tarrant, James, Wang, Jing, Weng, Felix, Wilde, Victoria L., Albertella, Mark, Bittner, Mark, Cooke, Andrew, Gray, Michael J., Maresca, Paul, May, Earl, Meyn, Peter, Peick, William, Romashko, Darlene, Tanowitz, Michael, Tokar, Brianna

“…The discovery and potency optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput…”
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Abstract 2463: Discovery of imidazo[1,5- a ]pyrazine derived potent, selective and orally bioavailable ACK1 inhibitors by Jin, Meizhong, Wang, Jing, Kleinberg, Andrew, Kadalbajoo, Mridula, Siu, Kam W., Cooke, Andrew, Bittner, Mark, Yao, Yan, Thelemann, April, Ji, Qunsheng, Bhagwat, Shripad, Mulvihill, Kristen M., Rechka, Josef A., Pachter, Jonathan A., Crew, Andrew P., Epstein, David, Mulvihill, Mark J.

“…Abstract Activated Cdc42-associated kinase (ACK1) is a non-receptor tyrosine kinase originally identified by virtue of its binding to GTP-bound small GTPase…”
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Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases by Steinig, Arno G., Li, An-Hu, Wang, Jing, Chen, Xin, Dong, Hanqing, Ferraro, Caterina, Jin, Meizhong, Kadalbajoo, Mridula, Kleinberg, Andrew, Stolz, Kathryn M., Tavares-Greco, Paula A., Wang, Ti, Albertella, Mark R., Peng, Yue, Crew, Linda, Kahler, Jennifer, Kan, Julie, Schulz, Ryan, Cooke, Andy, Bittner, Mark, Turton, Roy W., Franklin, Maryland, Gokhale, Prafulla, Landfair, Darla, Mantis, Christine, Workman, Jen, Wild, Robert, Pachter, Jonathan, Epstein, David, Mulvihill, Mark J.

“…A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure–activity…”
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Abstract 3900: Discovery of FQIT: An imidazo[5,1- f ][1,2,4]triazine derived dual IGF-1R/IR inhibitor by Jin, Meizhong, Gokhale, Prafulla, Cooke, Andy, Foreman, Kenneth, Buck, Elizabeth, May, Earl, Feng, Lixing, Bittner, Mark, Kadalbajoo, Mridula, Landfair, Darla, Siu, Kam, Stolz, Kathryn, Werner, Douglas, Laufer, Radoslaw, Li, An-Hu, Dong, Hanqing, Steinig, Arno, Kleinberg, Andrew, Yao, Yan, Pachter, Jonathan, Wild, Robert, Mulvihill, Mark

“…Abstract Insulin-like growth factor-1 receptor (IGF-1R) has been recognized as a major target in cancer drug discovery due to its strong implications in…”
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Abstract 2915: Discovery and characterization of OSI-296, a dual inhibitor of cMET and RON kinases by Steinig, Arno G., Li, An-Hu, Wang, Jing, Kleinberg, Andrew, Dong, Hanqing, Wang, Ti, Gavagan, Kathryn M. Stolz, Jin, Meizhong, Tavares-Greco, Paula, Peng, Yue, Kahler, Jen, Castaldo, Linda, McCormack, Siobhan, Kan, Julie, Albertella, Mark, Cooke, Andy, Turton, Roy, Bittner, Mark, Franklin, Maryland, Landfair, Darla, Gokhale, Prafulla, Wild, Robert, Pachter, Jonathan, Epstein, David, Mulvihill, Mark J.

“…Abstract cMET and RON are receptor tyrosine kinases of the MET proto-oncogene family that are activated by their respective ligands HGF and MSP. Signaling…”
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Abstract 4486: OSI-027, a selective dual mTORC1/TORC2 kinase inhibitor displays broad spectrum anti-tumor activity in preclinical models of human cancer by Gokhale, Prafulla C., Bhagwat, Shripad V., Crew, Andrew P., Cooke, Andrew, Mantis, Christine, Workman, Jennifer E., Landfair, Darla, Bittner, Mark, Epstein, David M., Pachter, Jonathan A., Wild, Robert

“…Abstract The mammalian target of rapamycin (mTOR) protein kinase plays a central role in regulating cell proliferation and cell survival. The PI3K/AKT…”
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Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs) by Mulvihill, Mark J., Kan, Julie L.C., Beck, Patricia, Bittner, Mark, Cesario, Cara, Cooke, Andrew, Keane, David M., Nigro, Anthony I., Nillson, Christy, Smith, Vanessa, Srebernak, Mary, Sun, Feng-Lei, Vrkljan, Michael, Winski, Shannon L., Castelhano, Arlindo L., Emerson, David, Gibson, Neil

“…A series of [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines were designed and synthesized as CYP26 inhibitors, serving as…”
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3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent by Mulvihill, Mark J., Kan, Julie L.C., Cooke, Andrew, Bhagwat, Shripad, Beck, Patricia, Bittner, Mark, Cesario, Cara, Keane, David, Lazarescu, Viorica, Nigro, Anthony, Nillson, Christy, Panicker, Bijoy, Smith, Vanessa, Srebernak, Mary, Sun, Feng-Lei, O’Connor, Matthew, Russo, Suzanne, Fischetti, Gia, Vrkljan, Michael, Winski, Shannon, Castelhano, Arlindo L., Emerson, David, Gibson, Neil W.

“…3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid and analogs were designed and synthesized as highly potent and…”
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Turn Taking: A Dialogue on Past, Present, and Future Collaboration by Cooney, Margaret, Bittner, Mark

“…Most of the games children play require learning and practicing the concept of give and take, or turn taking, a crucial element in play/life. This article…”
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Male Teachers and Gender Balance in Early Childhood Programs--Facing Gender Balance Issues: Our Need for Male Teachers Is Critical by Bittner, Mark T, Cooney, Margaret H

“…Discusses three benefits of recruiting male early childhood teachers: creating a gender fair classroom, offering positive male role models, and improving wages…”
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