RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers
Nichols, Robert J., Haderk, Franziska, Stahlhut, Carlos, Schulze, Christopher J., Hemmati, Golzar, Wildes, David, Tzitzilonis, Christos, Mordec, Kasia, Marquez, Abby, Romero, Jason, Hsieh, Tientien, Zaman, Aubhishek, Olivas, Victor, McCoach, Caroline, Blakely, Collin M., Wang, Zhengping, Kiss, Gert, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Goldsmith, Mark A., Smith, Jacqueline A. M., Bivona, Trever G.
Published in Nature cell biology (01.09.2018)
Published in Nature cell biology (01.09.2018)
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Journal Article
Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)
Rice, Kenneth D, Aay, Naing, Anand, Neel K, Blazey, Charles M, Bowles, Owen J, Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K, Defina, Steven C, Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A, Kennedy, Abigail R, Kim, Angie I, Koltun, Elena S, Lougheed, Julie C, Manalo, Jean-Claire L, Martini, Jean-Francois, Nuss, John M, Peto, Csaba J, Tsang, Tsze H, Yu, Peiwen, Johnston, Stuart
Published in ACS medicinal chemistry letters (10.05.2012)
Published in ACS medicinal chemistry letters (10.05.2012)
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Journal Article
Discovery of XL413, a potent and selective CDC7 inhibitor
Koltun, Elena S., Tsuhako, Amy Lew, Brown, David S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Ferguson, Kim, Franzini, Maurizio, Galan, Adam, Holst, Charles R., Huang, Ping, Kane, Brian, Kim, Moon H., Li, Jia, Markby, David, Mohan, Manisha, Noson, Kevin, Plonowski, Arthur, Richards, Steven J., Robertson, Scott, Shaw, Kenneth, Stott, Gordon, Stout, Thomas J., Young, Jenny, Yu, Peiwen, Zaharia, Cristiana A., Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Xu, Wei, Kearney, Patrick C.
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment
Quintana, Elsa, Schulze, Christopher J., Myers, Darienne R., Choy, Tiffany J., Mordec, Kasia, Wildes, David, Shifrin, Nataliya Tobvis, Belwafa, Amira, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Kelsey, Stephen, Goldsmith, Mark A., Nichols, Robert, Smith, Jacqueline A.M.
Published in Cancer research (Chicago, Ill.) (01.07.2020)
Published in Cancer research (Chicago, Ill.) (01.07.2020)
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Journal Article
Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS
Schulze, Christopher J., Seamon, Kyle J., Zhao, Yulei, Yang, Yu C., Cregg, Jim, Kim, Dongsung, Tomlinson, Aidan, Choy, Tiffany J., Wang, Zhican, Sang, Ben, Pourfarjam, Yasin, Lucas, Jessica, Cuevas-Navarro, Antonio, Ayala-Santos, Carlos, Vides, Alberto, Li, Chuanchuan, Marquez, Abby, Zhong, Mengqi, Vemulapalli, Vidyasiri, Weller, Caroline, Gould, Andrea, Whalen, Daniel M., Salvador, Anthony, Milin, Anthony, Saldajeno-Concar, Mae, Dinglasan, Nuntana, Chen, Anqi, Evans, Jim, Knox, John E., Koltun, Elena S., Singh, Mallika, Nichols, Robert, Wildes, David, Gill, Adrian L., Smith, Jacqueline A. M., Lito, Piro
Published in Science (American Association for the Advancement of Science) (18.08.2023)
Published in Science (American Association for the Advancement of Science) (18.08.2023)
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Journal Article
Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy
Holderfield, Matthew, Lee, Bianca J., Jiang, Jingjing, Tomlinson, Aidan, Seamon, Kyle J., Mira, Alessia, Patrucco, Enrico, Goodhart, Grace, Dilly, Julien, Gindin, Yevgeniy, Dinglasan, Nuntana, Wang, Yingyun, Lai, Lick Pui, Cai, Shurui, Jiang, Lingyan, Nasholm, Nicole, Shifrin, Nataliya, Blaj, Cristina, Shah, Harshit, Evans, James W., Montazer, Nilufar, Lai, Oliver, Shi, Jade, Ahler, Ethan, Quintana, Elsa, Chang, Stephanie, Salvador, Anthony, Marquez, Abby, Cregg, Jim, Liu, Yang, Milin, Anthony, Chen, Anqi, Ziv, Tamar Bar, Parsons, Dylan, Knox, John E., Klomp, Jennifer E., Roth, Jennifer, Rees, Matthew, Ronan, Melissa, Cuevas-Navarro, Antonio, Hu, Feng, Lito, Piro, Santamaria, David, Aguirre, Andrew J., Waters, Andrew M., Der, Channing J., Ambrogio, Chiara, Wang, Zhengping, Gill, Adrian L., Koltun, Elena S., Smith, Jacqueline A. M., Wildes, David, Singh, Mallika
Published in Nature (London) (23.05.2024)
Published in Nature (London) (23.05.2024)
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Journal Article
Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers
Jiang, Jingjing, Jiang, Lingyan, Maldonato, Benjamin J, Wang, Yingyun, Holderfield, Matthew, Aronchik, Ida, Winters, Ian P, Salman, Zeena, Blaj, Cristina, Menard, Marie, Brodbeck, Jens, Chen, Zhe, Wei, Xing, Rosen, Michael J, Gindin, Yevgeniy, Lee, Bianca J, Evans, James W, Chang, Stephanie, Wang, Zhican, Seamon, Kyle J, Parsons, Dylan, Cregg, James, Marquez, Abby, Tomlinson, Aidan C A, Yano, Jason K, Knox, John E, Quintana, Elsa, Aguirre, Andrew J, Arbour, Kathryn C, Reed, Abby, Gustafson, W Clay, Gill, Adrian L, Koltun, Elena S, Wildes, David, Smith, Jacqueline A M, Wang, Zhengping, Singh, Mallika
Published in Cancer discovery (09.04.2024)
Published in Cancer discovery (09.04.2024)
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Journal Article
The design, synthesis, and biological evaluation of PIM kinase inhibitors
Tsuhako, Amy Lew, Brown, David S., Koltun, Elena S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Franzini, Maurizio, Galan, Adam, Huang, Ping, Johnston, Stuart, Kane, Brian, Kim, Moon H., Douglas Laird, A., Lin, Rui, Mock, Lillian, Ngan, Iris, Pack, Michael, Stott, Gordon, Stout, Thomas J., Yu, Peiwen, Zaharia, Cristiana, Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Kearney, Patrick C., Xu, Wei
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Discovery and Characterization of an Inhibitor of Glucosylceramide Synthase
Richards, Steven, Larson, Christopher J, Koltun, Elena S, Hanel, Art, Chan, Vicky, Nachtigall, Jason, Harrison, Amanda, Aay, Naing, Du, Hongwang, Arcalas, Arlyn, Galan, Adam, Zhang, Jeff, Zhang, Wentao, Won, Kwang-Ai, Tam, Danny, Qian, Fawn, Wang, Tao, Finn, Patricia, Ogilvie, Kathy, Rosen, Jon, Aoyama, Ron, Plonowski, Artur, Cancilla, Belinda, Bentzien, Frauke, Yakes, Michael, Mohan, Raju, Lamb, Peter, Nuss, John, Kearney, Patrick
Published in Journal of medicinal chemistry (10.05.2012)
Published in Journal of medicinal chemistry (10.05.2012)
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Journal Article
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors
Forsyth, Timothy, Kearney, Patrick C., Kim, Byung Gyu, Johnson, Henry W.B., Aay, Naing, Arcalas, Arlyn, Brown, David S., Chan, Vicky, Chen, Jeff, Du, Hongwang, Epshteyn, Sergey, Galan, Adam A., Huynh, Tai P., Ibrahim, Mohamed A., Kane, Brian, Koltun, Elena S., Mann, Grace, Meyr, Lisa E., Lee, Matthew S., Lewis, Gary L., Noguchi, Robin T., Pack, Michael, Ridgway, Brian H., Shi, Xian, Takeuchi, Craig S., Zu, Peiwen, Leahy, James W., Nuss, John M., Aoyama, Ron, Engst, Stefan, Gendreau, Steven B., Kassees, Robert, Li, Jia, Lin, Shwu-Hwa, Martini, Jean-Francois, Stout, Thomas, Tong, Philip, Woolfrey, John, Zhang, Wentao, Yu, Peiwen
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
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Journal Article
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Year of Publication 31.05.2024
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Year of Publication 11.01.2024
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SHP2 25- 3- 256-3 3- 25-DISUBSTITUTED 3-METHYL PYRAZINES AND 256- TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS
BUCKL ANDREAS, KISS GERT, WON WALTER, KOLTUN ELENA S, SEMKO CHRISTOPHER, JOGALEKAR ASHUTOSH, AAY NAING, MELLEM KEVIN, GILL ADRIAN
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Year of Publication 13.11.2023
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Year of Publication 28.05.2024
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암의 치료를 위한 RAS 억제제
BUCKL ANDREAS, EDWARDS ANNE V, BURNETT G. LESLIE, KOLTUN ELENA S, SEMKO CHRISTOPHER, GILL ADRIAN L, CREGG JAMES, PITZEN JENNIFER, KNOX JOHN E
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Year of Publication 08.02.2024
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RAS 억제제
BUCKL ANDREAS, BURNETT G. LESLIE, KOLTUN ELENA S, GILL ADRIAN L, CREGG JAMES, PITZEN JENNIFER, LIU YANG, KNOX JOHN E, AGGEN JAMES
Year of Publication 04.08.2022
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Year of Publication 04.08.2022
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