Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor
Shultz, Michael D, Cheung, Atwood K, Kirby, Christina A, Firestone, Brant, Fan, Jianmei, Chen, Christine Hiu-Tung, Chen, Zhouliang, Chin, Donovan N, DiPietro, Lucian, Fazal, Aleem, Feng, Yun, Fortin, Pascal D, Gould, Ty, Lagu, Bharat, Lei, Huangshu, Lenoir, Francois, Majumdar, Dyuti, Ochala, Etienne, Palermo, M. G, Pham, Ly, Pu, Minying, Smith, Troy, Stams, Travis, Tomlinson, Ronald C, Touré, B. Barry, Visser, Michael, Wang, Run Ming, Waters, Nigel J, Shao, Wenlin
Published in Journal of medicinal chemistry (22.08.2013)
Published in Journal of medicinal chemistry (22.08.2013)
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The Role of the Acidity of N‑Heteroaryl Sulfonamides as Inhibitors of Bcl‑2 Family Protein–Protein Interactions
Touré, B. Barry, Miller-Moslin, Karen, Yusuff, Naeem, Perez, Lawrence, Doré, Michael, Joud, Carol, Michael, Walter, DiPietro, Lucian, van der Plas, Simon, McEwan, Michael, Lenoir, Francois, Hoe, Madelene, Karki, Rajesh, Springer, Clayton, Sullivan, John, Levine, Kymberly, Fiorilla, Catherine, Xie, Xiaoling, Kulathila, Raviraj, Herlihy, Kara, Porter, Dale, Visser, Michael
Published in ACS medicinal chemistry letters (14.02.2013)
Published in ACS medicinal chemistry letters (14.02.2013)
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Journal Article
Evaluation of Protein Kinase cAMP-Activated Catalytic Subunit Alpha as a Therapeutic Target for Fibrolamellar Carcinoma
Schalm, Stefanie S., O’Hearn, Erin, Wilson, Kevin, LaBranche, Timothy P., Silva, Grace, Zhang, Zhuo, DiPietro, Lucian, Bifulco, Neil, Woessner, Richard, Stransky, Nicolas, Sappal, Darshan, Campbell, Robert, Lobbardi, Riadh, Palmer, Michael, Kim, Joseph, Ye, Chaoyang, Dorsch, Marion, Lengauer, Christoph, Guzi, Timothy, Kadambi, Vivek, Garner, Andrew, Hoeflich, Klaus P.
Published in Gastro hep advances (2023)
Published in Gastro hep advances (2023)
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Journal Article
In vitro and in vivo anticancer activities of synthetic macrocyclic ketone analogues of halichondrin B
TOWLE, Murray J, SALVATO, Kathleen A, HABGOOD, Gregory J, SINGER, Lori A, DIPIETRO, Lucian V, YUAN WANG, CHEN, Jack J, QUINCY, David A, DAVIS, Ashley, YOSHIMATSU, Kentaro, KISHI, Yoshito, YU, Melvin J, BUDROW, Jacqueline, LITTLEFIELD, Bruce A, WELS, Bruce F, KUZNETSOV, Galina, AALFS, Kimberley K, WELSH, Susan, WANJUN ZHENG, SELETSKY, Boris M, PALME, Monica H
Published in Cancer research (Chicago, Ill.) (01.02.2001)
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Published in Cancer research (Chicago, Ill.) (01.02.2001)
Journal Article
Structurally simplified macrolactone analogues of halichondrin B
Seletsky, Boris M., Wang, Yuan, Hawkins, Lynn D., Palme, Monica H., Habgood, Gregory J., DiPietro, Lucian V., Towle, Murray J., Salvato, Kathleen A., Wels, Bruce F., Aalfs, Kimberley K., Kishi, Yoshito, Littlefield, Bruce A., Yu, Melvin J.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Journal Article
Precision Targeted Therapy with BLU-667 for RET -Driven Cancers
Subbiah, Vivek, Gainor, Justin F, Rahal, Rami, Brubaker, Jason D, Kim, Joseph L, Maynard, Michelle, Hu, Wei, Cao, Qiongfang, Sheets, Michael P, Wilson, Douglas, Wilson, Kevin J, DiPietro, Lucian, Fleming, Paul, Palmer, Michael, Hu, Mimi I, Wirth, Lori, Brose, Marcia S, Ou, Sai-Hong Ignatius, Taylor, Matthew, Garralda, Elena, Miller, Stephen, Wolf, Beni, Lengauer, Christoph, Guzi, Timothy, Evans, Erica K
Published in Cancer discovery (01.07.2018)
Published in Cancer discovery (01.07.2018)
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Journal Article
A precision therapy against cancers driven by KIT/PDGFRA mutations
Evans, Erica K, Gardino, Alexandra K, Kim, Joseph L, Hodous, Brian L, Shutes, Adam, Davis, Alison, Zhu, Xing Julia, Schmidt-Kittler, Oleg, Wilson, Doug, Wilson, Kevin, DiPietro, Lucian, Zhang, Yulian, Brooijmans, Natasja, LaBranche, Timothy P, Wozniak, Agnieszka, Gebreyohannes, Yemarshet K, Schöffski, Patrick, Heinrich, Michael C, DeAngelo, Daniel J, Miller, Stephen, Wolf, Beni, Kohl, Nancy, Guzi, Timothy, Lydon, Nicholas, Boral, Andy, Lengauer, Christoph
Published in Science translational medicine (01.11.2017)
Published in Science translational medicine (01.11.2017)
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Journal Article
Abstract P5-16-10: RLY-2608: The first allosteric mutant- and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models
Pazolli, Ermira, Kipp, Randy, Boezio, Alessandro, Gunaydin, Hakan, Iskandar, Amanda, Zubrowski, Matthew, Williams, Bret, Shortsleeves, Kelley, Larivee, Alexandre, McLean, Tom, Michelsen, Klaus, Zeng, Hongtao, LaRochelle, Jonathan, Manna, Joe, DiPietro, Lucian, Lescarbeau, Andre, Mader, Mary, Bennet, Bindu, Wilbur, Jeremy, Wang, Qi, Pierce, Levi, Martin, Iain, Watters, James, Fortin, Pascal, Bergstrom, Donald
Published in Cancer research (Chicago, Ill.) (15.02.2022)
Published in Cancer research (Chicago, Ill.) (15.02.2022)
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Journal Article
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia
Varkaris, Andreas, Pazolli, Ermira, Gunaydin, Hakan, Wang, Qi, Pierce, Levi, Boezio, Alessandro A, Bulku, Artemisa, DiPietro, Lucian, Fridrich, Cary, Frost, Adam, Giordanetto, Fabrizio, Hamilton, Erika P, Harris, Katherine, Holliday, Michael, Hunter, Tamieka L, Iskandar, Amanda, Ji, Yongli, Larivée, Alexandre, LaRochelle, Jonathan R, Lescarbeau, André, Llambi, Fabien, Lormil, Brenda, Mader, Mary M, Mar, Brenton G, Martin, Iain, McLean, Thomas H, Michelsen, Klaus, Pechersky, Yakov, Puente-Poushnejad, Erika, Raynor, Kevin, Rogala, Dipali, Samadani, Ramin, Schram, Alison M, Shortsleeves, Kelley, Swaminathan, Sweta, Tajmir, Shahein, Tan, Gege, Tang, Yong, Valverde, Roberto, Wehrenberg, Bryan, Wilbur, Jeremy, Williams, Bret R, Zeng, Hongtao, Zhang, Hanmo, Walters, W Patrick, Wolf, Beni B, Shaw, David E, Bergstrom, Donald A, Watters, James, Fraser, James S, Fortin, Pascal D, Kipp, D Randal
Published in Cancer discovery (08.02.2024)
Published in Cancer discovery (08.02.2024)
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Journal Article
Abstract P251: Discovery and characterization of RLY-2608: The first allosteric, mutant, and isoform-selective inhibitor of PI3Kα
Pazolli, Ermira, Kipp, Randy, Boezio, Alessandro, Gunaydin, Hakan, Iskandar, Amanda, Zubrowski, Matthew, Williams, Bret, Shortsleeves, Kelley, Larivee, Alexandre, McLean, Tom, Michelsen, Klaus, Zeng, Hongtao, LaRochelle, Jonathan, Manna, Joe, DiPietro, Lucian, Mader, Mary, Bennet, Bindu, Wilbur, Jeremy, Wang, Qi, Pierce, Levi, Martin, Iain, Watters, James, Fortin, Pascal, Bergstrom, Donald
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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Journal Article
Abstract B01: BLU-667: A highly selective RET inhibitor to target RET-driven NSCLC
Rahal, Rami, Maynard, Michelle, Hu, Wei, Brubaker, Jason, Cao, Qiangfang, Kim, Joseph L., Sheets, Michael P., Wilson, Douglas P., Wilson, Kevin J., DiPietro, Lucian, LaBranche, Timothy, Wolf, Beni, Guzi, Timothy, Lengauer, Christoph, Evans, Erica K.
Published in Clinical cancer research (01.09.2018)
Published in Clinical cancer research (01.09.2018)
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Journal Article
Abstract B127: Evaluating PRKACA as a therapeutic target for Fibrolamellar Carcinoma
Schalm, Stefanie S, O’Hearn, Erin, Wilson, Kevin, LaBranche, Timothy, Silva, Grace, DiPietro, Lucian, Bifulco, Neil, Woessner, Richard, Stransky, Nicolas, Sappal, Darshan, Shutes, Adam, Campbell, Robert, Lobbardi, Riadh, Palmer, Michael, Kim, Joseph, Miller, Stephen, Dorsch, Marion, Lengauer, Christoph, Guzi, Timothy, Kadambi, Vivek, Garner, Andrew, Hoeflich, Klaus P
Published in Molecular cancer therapeutics (01.12.2019)
Published in Molecular cancer therapeutics (01.12.2019)
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Journal Article
Abstract B151: BLU-667 is a potent and highly selective RET inhibitor being developed for RET -driven cancers
Rahal, Rami, Maynard, Michelle, Hu, Wei, Brubaker, Jason, Cao, Qiongfang, Kim, Joseph L., Sheets, Michael P., Wilson, Douglas P., Wilson, Kevin J., DiPietro, Lucian, Fleming, Paul, LaBranche, Timothy P., Wolf, Beni, Guzi, Timothy, Lengauer, Christoph, Evans, Erica K.
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Journal Article
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors
Potashman, Michele H, Bready, James, Coxon, Angela, DeMelfi, Thomas M, DiPietro, Lucian, Doerr, Nicholas, Elbaum, Daniel, Estrada, Juan, Gallant, Paul, Germain, Julie, Gu, Yan, Harmange, Jean-Christophe, Kaufman, Stephen A, Kendall, Rick, Kim, Joseph L, Kumar, Gondi N, Long, Alexander M, Neervannan, Seshadri, Patel, Vinod F, Polverino, Anthony, Rose, Paul, van der Plas, Simon, Whittington, Douglas, Zanon, Roger, Zhao, Huilin
Published in Journal of medicinal chemistry (06.09.2007)
Published in Journal of medicinal chemistry (06.09.2007)
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Journal Article
Abstract LB-324: First isoform selective inhibitor of FGFR4 for the treatment of genomically defined patients with hepatocellular carcinoma
Hagel, Margit, Miduturu, Chandra, Sheets, Mike, Weng, Weifan, Rubin, Nooreen, Bifulco, Neil, DiPietro, Lucian, Kim, Joseph, Brooijmans, Natasja, Stransky, Nicolas, Winter, Christopher, Lengauer, Christoph, Guzi, Timothy
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors
Rahal, Rami, Evans, Erica K., Hu, Wei, Maynard, Michelle, Fleming, Paul, DiPietro, Lucian, Kim, Joseph L., Sheets, Michael P., Wilson, Doug P., Wilson, Kevin J., Stransky, Nicolas, Brubaker, Jason D., Guzi, Timothy, Kohl, Nancy E., Lengauer, Christoph
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Journal Article
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluations
Harmange, Jean-Christophe, Weiss, Matthew M., Germain, Julie, Polverino, Anthony J., Borg, George, Bready, James, Chen, Danlin, Choquette, Deborah, Coxon, Angela, DeMelfi, Tom, DiPietro, Lucian, Doerr, Nicholas, Estrada, Juan, Flynn, Julie, Graceffa, Russell F., Harriman, Shawn P., Kaufman, Stephen, La, Daniel S., Long, Alexander, Martin, Matthew W., Neervannan, Sesha, Patel, Vinod F., Potashman, Michele, Regal, Kelly, Roveto, Phillip M., Schrag, Michael L., Starnes, Charlie, Tasker, Andrew, Teffera, Yohannes, Wang, Ling, White, Ryan D., Whittington, Douglas A., Zanon, Roger
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Journal Article
RET의 저해제
WILSON DOUGLAS, BRUBAKER JASON D, KIM JOSEPH L, DIPIETRO LUCIAN V, WILSON KEVIN J
Year of Publication 02.07.2018
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Year of Publication 02.07.2018
Patent
Identification of Potent and Selective Amidobipyridyl Inhibitors of Protein Kinase D
Meredith, Erik L, Beattie, Kimberly, Burgis, Robin, Capparelli, Michael, Chapo, Joseph, DiPietro, Lucian, Gamber, Gabriel, Enyedy, Istvan, Hood, David B, Hosagrahara, Vinayak, Jewell, Charles, Koch, Keith A, Lee, Wendy, Lemon, Douglas D, McKinsey, Timothy A, Miranda, Karl, Pagratis, Nikos, Phan, Dillon, Plato, Craig, Rao, Chang, Rozhitskaya, Olga, Soldermann, Nicolas, Springer, Clayton, van Eis, Maurice, Vega, Richard B, Yan, Wanlin, Zhu, Qingming, Monovich, Lauren G
Published in Journal of medicinal chemistry (12.08.2010)
Published in Journal of medicinal chemistry (12.08.2010)
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Journal Article
PI3Kα 억제제 및 이의 사용 방법
WALTERS W. PATRICK, GELOZIA SHORENA, DENINNO MICHAEL PAUL, KURUKULASURIYA RAVI, LEE JESSICA, LEPITRE THOMAS, TAYLOR ALEXANDER M, BOEZIO ALESSANDRO, BURNIE ANDREW J, STURINO CLAUDIO, PIERCE LEVI CHARLES THOMAS, MOHAMED TAREK, THORAT RAKESH, KRUEGER ELAINE B, GIGUERE JEAN BENOIT, RAYNOR KEVIN DAVID, LARIVEE ALEXANDRE, LANDAGARAY ELODIE, CHEN FEI, PAL MOHAN, FRIDRICH CARY GRIFFIN, GUNAYDIN HAKAN, MAERTENS GAETAN, SHORTSLEEVES KELLEY C, MCLEAN THOMAS H, WANG QI, JOBIN DES LAURIERS ANTOINE, DIPIETRO LUCIAN V, PAN YUE, GIORDANETTO FABRIZIO, OUTIN JOHANNE, MADER MARY M, ATIENZA BREN JORDAN, BERTRAND LAPERLE MEGAN, VEMULA NARESH, TANVEER KASHIF, ZHANG HANMO, BOUSQUET YVES, LESCARBEAU ANDRE, TANG YONG, PECHERSKY YAKOV, CHITALE SAMPADA
Year of Publication 15.02.2023
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Year of Publication 15.02.2023
Patent