Search Results - "Kahler, Jennifer"

Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib by CAREY, Kendall D, GARTON, Andrew J, ROMERO, Maria S, KAHLER, Jennifer, THOMSON, Stuart, ROSS, Sarajane, PARK, Frances, HALEY, John D, GIBSON, Neil, SLIWKOWSKI, Mark X

“…We show that two commonly occurring epidermal growth factor receptor (EGFR) somatic mutations, L858R and an in-frame deletion mutant, Del(746-750), exhibit…”
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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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Enhanced Antitumor Activity of an Anti-5T4 Antibody-Drug Conjugate in Combination with PI3K/mTOR inhibitors or Taxanes by Shor, Boris, Kahler, Jennifer, Dougher, Maureen, Xu, Jane, Mack, Michelle, Rosfjord, Ed, Wang, Fang, Melamud, Eugene, Sapra, Puja

“…Targeted treatment of solid or liquid tumors with antibody-drug conjugates (ADCs) can lead to promising clinical benefit. The aim of the study is to…”
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Development of Highly Optimized Antibody-Drug Conjugates against CD33 and CD123 for Acute Myeloid Leukemia by Han, Yoon-Chi, Kahler, Jennifer, Piché-Nicholas, Nicole, Hu, Wenyue, Thibault, Stephane, Jiang, Fan, Leal, Mauricio, Katragadda, Madan, Maderna, Andreas, Dushin, Russell, Prashad, Nadira, Charati, Manoj B, Clark, Tracey, Tumey, L Nathan, Tan, Xingzhi, Giannakou, Andreas, Rosfjord, Edward, Gerber, Hans-Peter, Tchistiakova, Lioudmila, Loganzo, Frank, O'Donnell, Christopher J, Sapra, Puja

“…Mortality due to acute myeloid leukemia (AML) remains high, and the management of relapsed or refractory AML continues to be therapeutically challenging. The…”
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Novel DNA-Damaging Linker Payloads Are Active in Models of Acquired Resistance to Calicheamicin and Standard of Care by Kahler, Jennifer, Dougher, Maureen, Lu, Jia, Xu, Jane, Kausar, Tasneem, Lemon, Luanna, Zhong, Wenyan, Lucas, Judy, Sung, Matthew, Sapra, Puja

“…Gemtuzumab ozogamicin (GO) is an FDA-approved antibody-drug conjugate that has shown clinical benefit in acute myeloid leukemia (AML) patients but has been…”
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Abstract 3095: The development of CPI as a novel, next-generation DNA-targeting payload for ADCs by Kahler, Jennifer, Dougher, Maureen, Xu, Jane, Doroski, Matthew, Maderna, Andreas, Dushin, Russell, Thibault, Stephane, Leal, Mauricio, Katragadda, Madan, O'Donnell, Christopher J., Sung, Matthew, Sapra, Puja

“…Abstract DNA targeting drugs represent one of cornerstones of anti-cancer therapy for both hematologic and solid tumor indications. Low potency anti-DNA…”
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Abstract 2463: Enhanced anti-tumor activity of an Auristatin-based antibody-drug conjugate in combination with PI3K/mTOR inhibitors or taxanes: Translational implications and mechanistic insights by Sapra, Puja, Shor, Boris, Dougher, Maureen, Kahler, Jennifer, Mack, Michelle, Xu, Jane, Lu, Shuyan, Melamud, Eugene, Wang, Fang, Rosfjord, Edward

“…Abstract Targeted treatment with antibody-drug conjugates (ADCs) can lead to dramatic regressions of solid tumors; combination therapies with the ADCs that…”
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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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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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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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Abstract 4487: OSI-027, a potent and selective small molecule mTORC1/mTORC2 kinase inhibitor is mechanistically distinct from rapamycin by Bhagwat, Shripad V., Crew, Andrew P., Gokhale, Praful C., Yao, Yan, Kahler, Jennifer, Epstein, David M., Wild, Robert, Pachter, Jonathan A.

“…Abstract The PI3K/AKT/mTOR pathway is frequently activated in many human cancers and mTOR has been clinically validated as an effective anti-cancer target by…”
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High-throughput screening for mTORC1/mTORC2 kinase inhibitors using a chemiluminescence-based ELISA assay by Bhagwat, Shripad V, Kahler, Jennifer, Yao, Yan, Maresca, Paul, Brooks, Maureen, Crew, Andy, Boisclair, Michael, Pachter, Jonathan A

“…A high-throughput chemiluminescence and ELISA-based biochemical assay to identify mTORC1/mTORC2 kinase inhibitors is described. These mTOR complexes were…”
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Therapeutic interventions in the treatment of dissociative disorders by Turkus, Joan A, Kahler, Jennifer Aloe

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