Search Results - "Rana, Sumeet"

ARRY-520, a Novel KSP Inhibitor with Potent Activity in Hematological and Taxane-resistant Tumor Models by RICHARD WOESSNER, BRIAN TUNQUIST, CHRISTINE LEMIEUX, ELIZABETH CHLIPALA, STEVE JACKINSKY, WALTER DEWOLF, JR, WALTER VOEGTLI, APRIL COX, SUMEET RANA, PATRICE LEE, DUNCAN WALKER

“…Aim: Profiling the efficacy and pharmacodynamic activity of the kinesin spindle protein (KSP) inhibitor ARRY-520 will aid the identification of responsive…”
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Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors by Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A, Laird, Ellen R, Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J, Choo, Edna F, Dinkel, Victoria, Feng, Bainian, Gloor, Susan L, Gould, Stephen E, Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D, Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J, Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T, Shrag, Michael, Song, Kyung, Sturgis, Hillary L, Voegtli, Walter C, Wen, Zhaoyang, Willis, Brandon S, Woessner, Richard D, Wu, Wen-I, Young, Wendy B, Grina, Jonas

“…The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using…”
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Inflammatory Biomarkers of Sulfur Mustard Analog 2-Chloroethyl Ethyl Sulfide–Induced Skin Injury in SKH-1 Hairless Mice by Tewari-Singh, Neera, Rana, Sumeet, Gu, Mallikarjuna, Pal, Arttatrana, Orlicky, David J., White, Carl W., Agarwal, Rajesh

“…Sulfur mustard (HD) is an alkylating and cytotoxic chemical warfare agent, which inflicts severe skin toxicity and an inflammatory response. Effective medical…”
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Spirocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid β in a Higher Species by Hunt, Kevin W, Cook, Adam W, Watts, Ryan J, Clark, Christopher T, Vigers, Guy, Smith, Darin, Metcalf, Andrew T, Gunawardana, Indrani W, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Thomas, Allen A, Rana, Sumeet, Kallan, Nicholas C, DeLisle, Robert K, Rizzi, James P, Regal, Kelly, Sammond, Douglas, Groneberg, Robert, Siu, Michael, Purkey, Hans, Lyssikatos, Joseph P, Marlow, Allison, Liu, Xingrong, Tang, Tony P

“…A hallmark of Alzheimer’s disease is the brain deposition of amyloid beta (Aβ), a peptide of 36–43 amino acids that is likely a primary driver of…”
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Discovery of 7‑Tetrahydropyran-2-yl Chromans: β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors That Reduce Amyloid β‑Protein (Aβ) in the Central Nervous System by Thomas, Allen A, Hunt, Kevin W, Volgraf, Matthew, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Sammond, Douglas, Tang, Tony P, Rhodes, Susan P, Metcalf, Andrew T, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Do, Mary K. Geck, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P, Gunawardana, Indrani W

“…In an attempt to increase selectivity vs Cathepsin D (CatD) in our BACE1 program, a series of 1,3,4,4a,10,10a-hexahydropyrano[4,3-b]chromene analogues was…”
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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase by Wenglowsky, Steve, Ren, Li, Grina, Jonas, Hansen, Joshua D, Laird, Ellen R, Moreno, David, Dinkel, Victoria, Gloor, Susan L, Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Sturgis, Hillary L, Voegtli, Walter C, Vigers, Guy, Willis, Brandon, Mathieu, Simon, Rudolph, Joachim

“…Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based…”
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8‑Tetrahydropyran-2-yl Chromans: Highly Selective Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors by Thomas, Allen A, Hunt, Kevin W, Newhouse, Brad, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Rhodes, Susan P, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Liao, Jiangpeng, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P

“…A series of 2,3,4,4a,10,10a-hexahydropyrano[3,2-b]chromene analogs was developed that demonstrated high selectivity (>2000-fold) for BACE1 vs Cathepsin D…”
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Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors by Volgraf, Matthew, Chan, Lina, Huestis, Malcolm P., Purkey, Hans E., Burkard, Michael, Geck Do, Mary, Harris, Julie, Hunt, Kevin W., Liu, Xingrong, Lyssikatos, Joseph P., Rana, Sumeet, Thomas, Allen A., Vigers, Guy P.A., Siu, Michael

“…The development of 1,3,4,4a,5,10a-hexahydropyrano[3,4-b]chromene analogs as BACE1 inhibitors is described. Introduction of the spirocyclic pyranochromene…”
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Abstract 2550: Combination of the KSP inhibitor ARRY-520 with bortezomib causes sustained tumor regressions and significantly increased time to regrowth in bortezomib sensitive and resistant models of multiple myeloma by Woessner, Richard, Tunquist, Brian, Walker, Duncan, Rana, Sumeet, Orlowski, Robert, Kuhn, Deborah

“…Abstract The allosteric kinesin spindle protein (KSP) inhibitor ARRY-520 has potent antitumor activity as a single agent in xenograft models of multiple…”
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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf super(V600E) kinase by Wenglowsky, Steve, Ren, Li, Grina, Jonas, Hansen, Joshua D, Laird, Ellen R, Moreno, David, Dinkel, Victoria, Gloor, Susan L, Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Sturgis, Hillary L, Voegtli, Walter C, Vigers, Guy, Willis, Brandon, Mathieu, Simon, Rudolph, Joachim

“…Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based…”
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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-RafV600E kinase by Wenglowsky, Steve, Ren, Li, Grina, Jonas, Hansen, Joshua D., Laird, Ellen R., Moreno, David, Dinkel, Victoria, Gloor, Susan L., Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Sturgis, Hillary L., Voegtli, Walter C., Vigers, Guy, Willis, Brandon, Mathieu, Simon, Rudolph, Joachim

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Abstract 2514: ARRY-162, A Potent and Selective MEK 1/2 Inhibitor, Shows Enhanced Efficacy in Combination with Other Targeted Kinase Inhibitors and with Chemotherapy by Woessner, Richard, Winski, Shannon, Rana, Sumeet, Anderson, Deborah, Winkler, James D., Lee, Patrice A.

“…Abstract MAPK kinase pathway-activation is implicated in uncontrolled cell proliferation and tumor growth in numerous tumor types. Targeting MEK may inhibit…”
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Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors by Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A, Laird, Ellen R, Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J, Choo, Edna F, Dinkel, Victoria, Feng, Bainian, Gloor, Susan L, Gould, Stephen E, Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D, Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J, Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T, Shrag, Michael, Song, Kyung, Sturgis, Hillary L, Voegtli, Walter C, Wen, Zhaoyang, Willis, Brandon S, Woessner, Richard D, Wu, Wen-I, Young, Wendy B, Grina, Jonas

“…The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using…”
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Combination of the KSP Inhibitor ARRY-520 with Bortezomib or Revlimid Causes Sustained Tumor Regressions and Significantly Increased Time to Regrowth in Models of Multiple Myeloma by Woessner, Richard, Tunquist, Brian, Cox, April, Rana, Sumeet, Walker, Duncan, Lee, Patrice A.

“…Abstract 2858 Poster Board II-834 The allosteric kinesin spindle protein (KSP) inhibitor ARRY-520 has potent antitumor activity as a single agent in xenograft…”
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Discovery of a Novel Class of Imidazo[1,2‑a]Pyridines with Potent PDGFR Activity and Oral Bioavailability by Hicken, Erik J, Marmsater, Fred P, Munson, Mark C, Schlachter, Stephen T, Robinson, John E, Allen, Shelley, Burgess, Laurence E, DeLisle, Robert Kirk, Rizzi, James P, Topalov, George T, Zhao, Qian, Hicks, Julie M, Kallan, Nicholas C, Tarlton, Eugene, Allen, Andrew, Callejo, Michele, Cox, April, Rana, Sumeet, Klopfenstein, Nathalie, Woessner, Richard, Lyssikatos, Joseph P

“…The in silico construction of a PDGFRβ kinase homology model and ensuing medicinal chemistry guided by molecular modeling, led to the identification of potent,…”
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Abstract 2515: Preclinical Development of ARRY-162, A Potent and Selective MEK 1/2 Inhibitor by Lee, Patrice A., Wallace, Eli, Marlow, Allison, Yeh, Tammie, Marsh, Vivienne, Anderson, Deborah, Woessner, Richard, Hurley, Brian, Lyssikatos, Joseph, Poch, Gregory, Gross, Stefan, Rana, Sumeet, Winski, Shannon, Koch, Kevin

“…Abstract Activation of the Ras/Raf/MEK/MAP kinase pathway is implicated in uncontrolled cell proliferation and tumor growth. Inappropriate activation of the…”
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The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase by Ren, Li, Ahrendt, Kateri A., Grina, Jonas, Laird, Ellen R., Buckmelter, Alex J., Hansen, Joshua D., Newhouse, Brad, Moreno, David, Wenglowsky, Steve, Dinkel, Victoria, Gloor, Susan L., Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Risom, Tyler, Sturgis, Hillary L., Voegtli, Walter C., Mathieu, Simon

“…Herein we describe the discovery of a novel series of ATP competitive B-Raf inhibitors via structure based drug design (SBDD). These pyridopyrimidin-7-one…”
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Pyrazolopyridine Inhibitors of B-Raf V600E . Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors by Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A., Laird, Ellen R., Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J., Choo, Edna F., Dinkel, Victoria, Feng, Bainian, Gloor, Susan L., Gould, Stephen E., Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D., Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J., Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T., Shrag, Michael, Song, Kyung, Sturgis, Hillary L., Voegtli, Walter C., Wen, Zhaoyang, Willis, Brandon S., Woessner, Richard D., Wu, Wen-I, Young, Wendy B., Grina, Jonas

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