Search Results - "Merritt, Hanne"

RAF Inhibitors Activate the MAPK Pathway by Relieving Inhibitory Autophosphorylation by Holderfield, Matthew, Merritt, Hanne, Chan, John, Wallroth, Marco, Tandeske, Laura, Zhai, Huili, Tellew, John, Hardy, Stephen, Hekmat-Nejad, Mohammad, Stuart, Darrin D., McCormick, Frank, Nagel, Tobi E.

“…ATP competitive inhibitors of the BRAFV600E oncogene paradoxically activate downstream signaling in cells bearing wild-type BRAF (BRAFWT). In this study, we…”
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The structural mechanism of human glycogen synthesis by the GYS1-GYG1 complex by Fastman, Nathan M., Liu, Yuxi, Ramanan, Vyas, Merritt, Hanne, Ambing, Eileen, DePaoli-Roach, Anna A., Roach, Peter J., Hurley, Thomas D., Mellem, Kevin T., Ullman, Julie C., Green, Eric, Morgans, David, Tzitzilonis, Christos

“…Glycogen is the primary energy reserve in mammals, and dysregulation of glycogen metabolism can result in glycogen storage diseases (GSDs). In muscle, glycogen…”
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Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer by Burger, Matthew T, Pecchi, Sabina, Wagman, Allan, Ni, Zhi-Jie, Knapp, Mark, Hendrickson, Thomas, Atallah, Gordana, Pfister, Keith, Zhang, Yanchen, Bartulis, Sarah, Frazier, Kelly, Ng, Simon, Smith, Aaron, Verhagen, Joelle, Haznedar, Joshua, Huh, Kay, Iwanowicz, Ed, Xin, Xiaohua, Menezes, Daniel, Merritt, Hanne, Lee, Isabelle, Wiesmann, Marion, Kaufman, Susan, Crawford, Kenneth, Chin, Michael, Bussiere, Dirksen, Shoemaker, Kevin, Zaror, Isabel, Maira, Sauveur-Michel, Voliva, Charles F

“…Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein…”
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Bioluminescent Assay for the Quantification of Cellular Glycogen Levels by Leippe, Donna, Choy, Rebeca, Vidugiris, Gediminas, Merritt, Hanne, Mellem, Kevin T., Beattie, David T., Ullman, Julie C., Vidugiriene, Jolanta

“…Glycogen is a large polymer of glucose that functions as an important means of storing energy and maintaining glucose homeostasis. Glycogen synthesis and…”
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Isolation of picomolar affinity anti-c-erbB-2 single-chain Fv by molecular evolution of the complementarity determining regions in the center of the antibody binding site by Schier, R, McCall, A, Adams, G P, Marshall, K W, Merritt, H, Yim, M, Crawford, R S, Weiner, L M, Marks, C, Marks, J D

“…We determined the extent to which additional binding energy could be achieved by diversifying the complementarity determining regions (CDRs) located in the…”
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In-vitro characterization of MZE001, an orally active GYS1 inhibitor to treat Pompe disease by Choy, Rebeca, Reiton, Daniel, Merritt, Hanne, Gujral, Tarunmeet, Ganesh, Sandya, Denisin, Aleksandra, Powers, Hannah, Won, Walter, Satterfield, Terrence, Ullman, Julie, Mellem, Kevin, Green, Eric, Morgans, David, Beattie, David

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Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis by Han, Wooseok, Ma, Xiaolei, Balibar, Carl J, Baxter Rath, Christopher M, Benton, Bret, Bermingham, Alun, Casey, Fergal, Chie-Leon, Barbara, Cho, Min-Kyu, Frank, Andreas O, Frommlet, Alexandra, Ho, Chi-Min, Lee, Patrick S, Li, Min, Lingel, Andreas, Ma, Sylvia, Merritt, Hanne, Ornelas, Elizabeth, De Pascale, Gianfranco, Prathapam, Ramadevi, Prosen, Katherine R, Rasper, Dita, Ruzin, Alexey, Sawyer, William S, Shaul, Jacob, Shen, Xiaoyu, Shia, Steven, Steffek, Micah, Subramanian, Sharadha, Vo, Jason, Wang, Feng, Wartchow, Charles, Uehara, Tsuyoshi

“…The lipopolysaccharide biosynthesis pathway is considered an attractive drug target against the rising threat of multi-drug-resistant Gram-negative bacteria…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic by Ramurthy, Savithri, Taft, Benjamin R, Aversa, Robert J, Barsanti, Paul A, Burger, Matthew T, Lou, Yan, Nishiguchi, Gisele A, Rico, Alice, Setti, Lina, Smith, Aaron, Subramanian, Sharadha, Tamez, Victoriano, Tanner, Huw, Wan, Lifeng, Hu, Cheng, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Tellew, John E, Huang, Shenlin, Yue, Qin, Chaudhary, Apurva, Tian, Hung, Iyer, Raman, Hassan, A. Quamrul, Mathews Griner, Lesley A, La Bonte, Laura R, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Mishina, Yuji, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Sellers, William R, Lees, Emma, Shao, Wenlin, Dillon, Michael P, Stuart, Darrin D

“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Small molecule inhibition of glycogen synthase 1 restores autophagolysosomal and metabolic pathway dysfunction in a mouse model of Pompe disease by Ullman, Julie C., Xi, Yannan, Mellem, Kevin T., Merritt, Hanne, Choy, Rebeca, Gujral, Taru, Blake, Kerrigan, Tep, Samnang, O'Regan, Adam, Wong, Perryn, Wong, Casper, Pang, Lisa, Satterfield, Terrence F., Lin, Baiwei, Situ, Eva, Hoek, Maarten, Chandriani, Sanjay J., Bainer, Russell, Sinz, Christopher, Dick, Ryan, Noonberg, Sarah B., Beattie, David, Morgans, David J., Green, Eric M.

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Small-molecule inhibition of glycogen synthase 1 for the treatment of Pompe disease and other glycogen storage disorders by Ullman, Julie C, Mellem, Kevin T, Xi, Yannan, Ramanan, Vyas, Merritt, Hanne, Choy, Rebeca, Gujral, Tarunmeet, Young, Lyndsay E A, Blake, Kerrigan, Tep, Samnang, Homburger, Julian R, O'Regan, Adam, Ganesh, Sandya, Wong, Perryn, Satterfield, Terrence F, Lin, Baiwei, Situ, Eva, Yu, Cecile, Espanol, Bryan, Sarwaikar, Richa, Fastman, Nathan, Tzitzilonis, Christos, Lee, Patrick, Reiton, Daniel, Morton, Vivian, Santiago, Pam, Won, Walter, Powers, Hannah, Cummings, Beryl B, Hoek, Maarten, Graham, Robert R, Chandriani, Sanjay J, Bainer, Russell, DePaoli-Roach, Anna A, Roach, Peter J, Hurley, Thomas D, Sun, Ramon C, Gentry, Matthew S, Sinz, Christopher, Dick, Ryan A, Noonberg, Sarah B, Beattie, David T, Morgans, Jr, David J, Green, Eric M

“…Glycogen synthase 1 (GYS1), the rate-limiting enzyme in muscle glycogen synthesis, plays a central role in energy homeostasis and has been proposed as a…”
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Abstract 4945: Inhibition of wild-type PI3Kα signaling is required for durable efficacy in PI3Kα mutant cancer cells due to robust re-activation of wild-type PI3Kα signaling by MacDougall, John R., Zhong, Mengqi, Merritt, Hanne, Cid, Joselyn S. Del, Bradley, John, Mak, Raymond, Dhawan, Neil, Chen, Wei

“…Abstract PI3Kα is the most mutated oncogene with a high mutation rate in breast, lung, colorectal, gastric, bladder, and other tumor types. However, current…”
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Substrate reduction therapy for Pompe disease: Small molecule inhibition of glycogen synthase 1 in preclinical models by Ullman, Julie C., Mellem, Kevin T., Xi, Yannan, Satterfield, Terrence F., Gujral, Tarunmeet, Choy, Rebeca, Homburger, Julian R., Merritt, Hanne, Reiton, Daniel, Tep, Samnang, Lin, Baiwei, Yu, Cecile, Situ, Eva, Won, Walter, Powers, Hannah, Ramanan, Vyas, Hoek, Maarten, Graham, Robert, Chandriani, Sanjay J., Sinz, Christopher, Dick, Ryan A., Noonberg, Sarah B., Beattie, David T., Morgans, David J., Jr, Green, Eric M.

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Pharmacology of small molecule inhibitors of GYS1 in a mouse model of Pompe disease by Xi, Yannan, Satterfield, Terrence F., Choy, Rebeca, Gujral, Tarunmeet, Situ, Eva, Tep, Samnang, Morton, Vivian, Yu, Cecile, Reiton, Daniel, Lin, Baiwei, Merritt, Hanne, Santiago, Pam, Espanol, Bryan, Dick, Ryan A., Ullman, Julie C., Mellem, Kevin T., Noonberg, Sarah B., Green, Eric M., Morgans, David J., Chandriani, Sanjay J., Beattie, David T.

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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers by Nishiguchi, Gisele A, Rico, Alice, Tanner, Huw, Aversa, Robert J, Taft, Benjamin R, Subramanian, Sharadha, Setti, Lina, Burger, Matthew T, Wan, Lifeng, Tamez, Victoriano, Smith, Aaron, Lou, Yan, Barsanti, Paul A, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Dix, Ina, Tellew, John E, Huang, Shenlin, Mathews Griner, Lesley A, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Ma, Sylvia, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Jansen, Johanna M, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Lees, Emma, Shao, Wenlin, Stuart, Darrin D, Dillon, Michael P, Ramurthy, Savithri

“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model by Han, Wooseok, Menezes, Daniel L., Xu, Yongjin, Knapp, Mark S., Elling, Robert, Burger, Matthew T., Ni, Zhi-Jie, Smith, Aaron, Lan, Jiong, Williams, Teresa E., Verhagen, Joelle, Huh, Kay, Merritt, Hanne, Chan, John, Kaufman, Susan, Voliva, Charles F., Pecchi, Sabina

“…[Display omitted] Alterations in PI3K/AKT signaling are known to be implicated with tumorigenesis. The PI3 kinases family of lipid kinases has been an…”
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Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors by Smith, Aaron, Ni, Zhi-Jie, Poon, Daniel, Huang, Zilin, Chen, Zheng, Zhang, Qiong, Tandeske, Laura, Merritt, Hanne, Shoemaker, Kevin, Chan, John, Kaufman, Susan, Huh, Kay, Murray, Jeremy, Appleton, Brent A., Cowan-Jacob, Sandra W., Scheufler, Clemens, Kanazawa, Takanori, Jansen, Johanna M., Stuart, Darrin, Shafer, Cynthia M.

“…A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs were designed as inhibitors of B-RAFV600E. Medicinal chemistry techniques were employed to explore the…”
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Abstract LB-54: Identification of a RAF inhibitory auto-phosphorylation site by Holderfield, Matthew, Merritt, Hanne, Lin, Julie, Gao, Zenhai, Stuart, Darrin, McCormick, Frank

“…Abstract Preclinical studies have demonstrated that BRAF wild-type cancer cells are not only refractory but paradoxically activate the MAPK pathway when…”
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Expression, purification and characterization of inactive and active forms of ERK2 from insect expression system by Yan, Kelly, Merritt, Hanne, Crawford, Kenneth, Pardee, Gwynn, Cheng, Jan Marie, Widger, Stephania, Hekmat-Nejad, Mohammad, Zaror, Isabel, Sim, Janet

“…•Inactive and active ERK2 production method in insect system is newly developed.•Inactive ERK2 expressed in insect system is homogenously…”
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Abstract LB-121: Dissecting MAPK pathway in BRAFmut melanoma: Intricacies of ERK1 and ERK2 by Zavorotinskaya, Tatiana, Mehra, Upasana, Dai, Yumin, Faure, Michel, Crawford, Ken, Yu, Karen, Cheng, Jan Marie, Ma, Xiaolei, Xuan, Jan, Yan, Kelly, Hekmat-Nejad, Mohammad, Merritt, Hanne, Stuart, Darrin, Voliva, Charles

“…Abstract The MAPK signaling cascade, comprised of the RAS GTPases, the RAF, MEK1/2 and ERK1/2 kinases is frequently deregulated in cancer. ERK1 and ERK2…”
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Identification and structure–activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors by Pecchi, Sabina, Renhowe, Paul A., Taylor, Clarke, Kaufman, Susan, Merritt, Hanne, Wiesmann, Marion, Shoemaker, Kevin R., Knapp, Mark S., Ornelas, Elizabeth, Hendrickson, Thomas F., Fantl, Wendy, Voliva, Charles F.

“…PI3 Kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration, and differentiation. The PI3 kinase pathway is…”
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