Search Results - "LEE, Leslie B"

GDC-0941, a Novel Class I Selective PI3K Inhibitor, Enhances the Efficacy of Docetaxel in Human Breast Cancer Models by Increasing Cell Death In Vitro and In Vivo by WALLIN, Jeffrey J, GUAN, Jane, PRIOR, Wei Wei, LEE, Leslie B, BERRY, Leanne, BELMONT, Lisa D, KOEPPEN, Hartmut, BELVIN, Marcia, FRIEDMAN, Lori S, SAMPATH, Deepak

“…Docetaxel is a front-line standard-of-care chemotherapeutic drug for the treatment of breast cancer. Phosphoinositide 3-kinases (PI3K) are lipid kinases that…”
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SU11248 Inhibits KIT and Platelet-derived Growth Factor Receptor β in Preclinical Models of Human Small Cell Lung Cancer by Abrams, Tinya J, Lee, Leslie B, Murray, Lesley J, Pryer, Nancy K, Cherrington, Julie M

“…The purpose of this study was to evaluate the activity of the indolinone kinase inhibitor SU11248 against the receptor tyrosine kinase KIT in vitro and in vivo…”
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Inhibition of platelet-derived growth factor signaling attenuates pulmonary fibrosis by Abdollahi, Amir, Li, Minglun, Ping, Gong, Plathow, Christian, Domhan, Sophie, Kiessling, Fabian, Lee, Leslie B, McMahon, Gerald, Gröne, Hermann-Josef, Lipson, Kenneth E, Huber, Peter E

“…Pulmonary fibrosis is the consequence of a variety of diseases with no satisfying treatment option. Therapy-induced fibrosis also limits the efficacy of…”
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Supplementation of Nicotinic Acid with NAMPT Inhibitors Results in Loss of In Vivo Efficacy in NAPRT1 -Deficient Tumor Models by O'Brien, Thomas, Oeh, Jason, Xiao, Yang, Liang, Xiaorong, Vanderbilt, Alexander, Qin, Ann, Yang, Lulu, Lee, Leslie B, Ly, Justin, Cosino, Ely, LaCap, Jennifer A, Ogasawara, Annie, Williams, Simon, Nannini, Michelle, Liederer, Bianca M, Jackson, Peter, Dragovich, Peter S, Sampath, Deepak

“…Abstract Nicotinamide adenine dinucleotide (NAD) is a metabolite essential for cell survival and generated de novo from tryptophan or recycled from…”
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Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with “standard of care” therapeutic agents for the treatment of breast cancer by Abrams, Tinya J, Murray, Lesley J, Pesenti, Enrico, Holway, Vicky Walker, Colombo, Tina, Lee, Leslie B, Cherrington, Julie M, Pryer, Nancy K

“…SU11248 is an oral multitargeted tyrosine kinase inhibitor with antitumor and antiangiogenic activities through targeting platelet-derived growth factor…”
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Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models by JIE LIN, SAMPATH, Deepak, LEE, Leslie B, RISOM, Tyler, GROSS, Stefan, LIEDERER, Bianca M, KOEPPEN, Hartmut, SKELTON, Nicholas J, WALLIN, Jeffrey J, BELVIN, Marcia, PUNNOOSE, Elizabeth, FRIEDMAN, Lori S, NANNINI, Michelle A, KUI LIN, LEE, Brian B, DEGTYAREV, Michael, OEH, Jason, SAVAGE, Heidi, ZHENGYU GUAN, HONG, Rebecca, KASSEES, Robert

“…We describe the preclinical pharmacology and antitumor activity of GDC-0068, a novel highly selective ATP-competitive pan-Akt inhibitor currently in clinical…”
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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326) by Heffron, Timothy P, Heald, Robert A, Ndubaku, Chudi, Wei, BinQing, Augistin, Martin, Do, Steven, Edgar, Kyle, Eigenbrot, Charles, Friedman, Lori, Gancia, Emanuela, Jackson, Philip S, Jones, Graham, Kolesnikov, Aleksander, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, McLean, Neville, Mörtl, Mario, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Staben, Steven T, Steinbacher, Stefan, Tsui, Vickie, Wallin, Jeffrey, Sampath, Deepak, Olivero, Alan G

“…Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have received substantial attention for their potential use in cancer therapy. Despite…”
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Loss of oncogenic Notch1 with resistance to a PI3K inhibitor in T-cell leukaemia by Dail, Monique, Wong, Jason, Lawrence, Jessica, O’Connor, Daniel, Nakitandwe, Joy, Chen, Shann-Ching, Xu, Jin, Lee, Leslie B., Akagi, Keiko, Li, Qing, Aster, Jon C., Pear, Warren S., Downing, James R., Sampath, Deepak, Shannon, Kevin

“…Mutations that deregulate Notch1 and Ras/phosphoinositide 3 kinase (PI3K)/Akt signalling are prevalent in T-cell acute lymphoblastic leukaemia (T-ALL), and…”
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Isoform-Specific Phosphoinositide 3-Kinase Inhibitors Exert Distinct Effects in Solid Tumors by EDGAR, Kyle A, WALLIN, Jeffrey J, BERRY, Megan, LEE, Leslie B, PRIOR, Wei Wei, SAMPATH, Deepak, FRIEDMAN, Lori S, BELVIN, Marcia

“…Therapeutic inhibitors are being developed against the phosphoinositide 3-kinase (PI3K) pathway, the deregulation of which drives tumor growth and survival in…”
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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR by Heffron, Timothy P, Ndubaku, Chudi O, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Drobnick, Joy, Edgar, Kyle, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Plise, Emile G, Sideris, Steve, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin, Olivero, Alan G

“…Inhibition of phosphoinositide 3-kinase (PI3K) signaling is an appealing approach to treat brain tumors, especially glioblastoma multiforme (GBM). We…”
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Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma by Salphati, Laurent, Alicke, Bruno, Heffron, Timothy P, Shahidi-Latham, Sheerin, Nishimura, Merry, Cao, Tim, Carano, Richard A, Cheong, Jonathan, Greve, Joan, Koeppen, Hartmut, Lau, Shari, Lee, Leslie B, Nannini-Pepe, Michelle, Pang, Jodie, Plise, Emile G, Quiason, Cristine, Rangell, Linda, Zhang, Xiaolin, Gould, Stephen E, Phillips, Heidi S, Olivero, Alan G

“…Glioblastoma multiforme (GBM) is the most common primary brain tumor in adults. Limited treatment options have only marginally impacted patient survival over…”
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Bcl-2/Bcl-xL inhibition increases the efficacy of MEK inhibition alone and in combination with PI3 kinase inhibition in lung and pancreatic tumor models by Tan, Nguyen, Wong, Maureen, Nannini, Michelle A, Hong, Rebecca, Lee, Leslie B, Price, Stephen, Williams, Karen, Savy, Pierre Pascal, Yue, Peng, Sampath, Deepak, Settleman, Jeffrey, Fairbrother, Wayne J, Belmont, Lisa D

“…Although mitogen-activated protein (MAP)-extracellular signal-regulated kinase (ERK) kinase (MEK) inhibition is predicted to cause cell death by stabilization…”
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In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: Determination of a pharmacokinetic/pharmacodynamic relationship by MENDEL, Dirk B, LAIRD, A. Douglas, MURRAY, Lesley J, CARVER, Jeremy, CHAN, Emily, MOSS, Katherine G, HAZNEDAR, Joshua Ö, SUKBUNTHERNG, Juthamas, BLAKE, Robert A, LI SUN, CHO TANG, MILLER, Todd, XIAOHUA XIN, SHIRAZIAN, Sheri, MCMAHON, Gerald, CHERRINGTON, Julie M, LOUIE, Sharianne G, CHRISTENSEN, James G, GUANGMIN LI, SCHRECK, Randall E, ABRAMS, Tinya J, NGAI, Theresa J, LEE, Leslie B

“…One challenging aspect in the clinical development of molecularly targeted therapies, which represent a new and promising approach to treating cancers, has…”
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SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo by O'Farrell, Anne-Marie, Abrams, Tinya J., Yuen, Helene A., Ngai, Theresa J., Louie, Sharianne G., Yee, Kevin W.H., Wong, Lily M., Hong, Weiru, Lee, Leslie B., Town, Ajia, Smolich, Beverly D., Manning, William C., Murray, Lesley J., Heinrich, Michael C., Cherrington, Julie M.

“…FLT3 (fms-related tyrosine kinase/Flk2/Stk-2) is a receptor tyrosine kinase (RTK) primarily expressed on hematopoietic cells. In blasts from acute myelogenous…”
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The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α by Heffron, Timothy P, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Dotson, Jennafer, Edgar, Kyle, Goldsmith, Richard, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Ndubaku, Chudi, Nonomiya, Jim, Olivero, Alan G, Pang, Jodie, Plise, Emile G, Sideris, Steve, Trapp, Sean, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin

“…Inhibition of phosphoinositide 3-kinase (PI3K) signaling through PI3Kα has received significant attention for its potential in cancer therapy. While the PI3K…”
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Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier by SALPHATI, Laurent, HEFFRON, Timothy P, KOEPPEN, Hartmut, LAU, Shari, LEE, Leslie B, PANG, Jodie, PLISE, Emile G, POKORNY, Jenny L, BOU RESLAN, Hani, SARKARIA, Jann N, WALLIN, Jeffrey J, XIAOLIN ZHANG, ALICKE, Bruno, GOULD, Stephen E, OLIVERO, Alan G, PHILLIPS, Heidi S, NISHIMURA, Merry, BARCK, Kai, CARANO, Richard A, CHEONG, Jonathan, EDGAR, Kyle A, GREVE, Joan, KHARBANDA, Samir

“…Glioblastoma (GBM), the most common primary brain tumor in adults, presents a high frequency of alteration in the PI3K pathway. Our objectives were to identify…”
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Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human by Salphati, Laurent, Pang, Jodie, Plise, Emile G, Lee, Leslie B, Olivero, Alan G, Prior, Wei Wei, Sampath, Deepak, Wong, Susan, Zhang, Xiaolin

“…(S)-1-{4-[2-(2-Amino-pyrimidin-5-yl)-7-methyl-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl]-piperazin-1-yl}-2-hydroxy-propan-1-one (GDC-0980) is a potent…”
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Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941 by Salphati, Laurent, Lee, Leslie B, Pang, Jodie, Plise, Emile G, Zhang, Xiaolin

“…2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) is a novel small molecule inhibitor of the…”
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Proof of target for SU11654: Inhibition of KIT phosphorylation in canine mast cell tumors by PRYER, Nancy K, LEE, Leslie B, ZADOVASKAYA, Regina, XIAOMING YU, SUKBUNTHERNG, Juthamas, CHERRINGTON, Julie M, LONDON, Cheryl A

“…The purpose of this study was to evaluate the effect of the receptor tyrosine kinase inhibitor SU11654 on the activity of its molecular target KIT in canine…”
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Loss of oncogenic notchl with resistance to a PI3K inhibitor in t-cell leukaemia by Dail, Monique, Wong, Jason, Lawrence, Jessica, O'Connor, Daniel, Nakitandwe, Joy, Chen, Shann-Ching, Xu, Jin, Lee, Leslie B, Akagi, Keiko, Li, Qing, Aster, Jon C, Pear, Warren S, Downing, James R, Sampath, Deepak, Shannon, Kevin

“…Mutations that deregulate Notch1 and Ras/phosphoinositide 3 kinase (PI3K)/Akt signalling are prevalent in T-cell acute lymphoblastic leukaemia (T-ALL), and…”
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