Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivity
Safina, Brian S., Sweeney, Zachary K., Li, Jun, Chan, Bryan K., Bisconte, Angelina, Carrera, Diane, Castanedo, Georgette, Flagella, Michael, Heald, Robert, Lewis, Cristina, Murray, Jeremy M., Nonomiya, Jim, Pang, Jodie, Price, Steve, Reif, Karin, Salphati, Laurent, Seward, Eileen M., Wei, Binqing, Sutherlin, Daniel P.
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
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Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
Sutherlin, Daniel P., Baker, Stewart, Bisconte, Angelina, Blaney, Paul M., Brown, Anthony, Chan, Bryan K., Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M., Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C., Lewis, Cristina, Murray, Jeremy, Nadin, Alan J., Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S., Salphati, Laurent, Staben, Steven, Seward, Eileen M., Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K., Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
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Development of a Scalable Strategy for the Synthesis of PI3Kδ Inhibitors: Selective and Efficient Functionalization of Purine Derivatives
Carrera, Diane E, Sheng, PeiJue, Safina, Brian S, Li, Jun, Angelaud, Remy
Published in Organic process research & development (18.01.2013)
Published in Organic process research & development (18.01.2013)
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Journal Article
605 Systemically administered HER2-targeted ISACs provoke a rapid, local response that engages the innate and adaptive arms of the immune system to eradicate tumors in preclinical models
LeBlanc, Heidi, Pearson, Cecelia, Kenkel, Justin, Blum, LIsa, Ho, Po, Luo, Angela, Laura, Richard, Zhou, Matthew, Gregorio, Joshua, Luo, Andrew, Ackerman, Shelley, Safina, Brian, Dornan, David, Alonso, Michael, Kowanetz, Marcin
Published in Journal for immunotherapy of cancer (01.11.2020)
Published in Journal for immunotherapy of cancer (01.11.2020)
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784 BDC-2034: discovery of a CEA-targeting immune-stimulating antibody conjugate (ISAC) for solid tumors
Mallet, William, Gadkari, Rishali, Pearson, Cecelia, Torrez Dulgeroff, Laughing Bear, Luo, Angela, Luo, AAngela Luondrew, Melrose, Jennifer, Nolin, Jess, Lee, Arthur, Zhou, Matthew, Anand, Puneet, Sarma, Ganapathy, Henning, Karla, Blum, Lisa, Chapin, Steven, Bogaert, Liz, Ackerman, Shelley, Kudirka, Romas, Shen, Yuyi, Husain, Amreen, Perez, Edith, Kowanetz, Marcin, Alonso, Michael, Safina, Brian, Dornan, David
Published in Journal for immunotherapy of cancer (01.11.2021)
Published in Journal for immunotherapy of cancer (01.11.2021)
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Journal Article
A Biomimetically Inspired Synthesis of the Dehydropiperidine Domain of Thiostrepton
Nicolaou, K. C., Nevalainen, Marta, Safina, Brian S., Zak, Mark, Bulat, Stephan
Published in Angewandte Chemie International Edition (03.06.2002)
Published in Angewandte Chemie International Edition (03.06.2002)
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Synthetic Studies on Thiostrepton: Construction of Thiostrepton Analogues with the Thiazoline-Containing Macrocycle
Nicolaou, K. C., Nevalainen, Marta, Zak, Mark, Bulat, Stephan, Bella, Marco, Safina, Brian S.
Published in Angewandte Chemie International Edition (28.07.2003)
Published in Angewandte Chemie International Edition (28.07.2003)
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A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel
Liu, Chang, Reese, Rebecca, Vu, Simon, Rougé, Lionel, Shields, Shannon D., Kakiuchi-Kiyota, Satoko, Chen, Huifen, Johnson, Kevin, Shi, Yu Patrick, Chernov-Rogan, Tania, Greiner, Demi Maria Zabala, Kohli, Pawan Bir, Hackos, David, Brillantes, Bobby, Tam, Christine, Li, Tianbo, Wang, Jianyong, Safina, Brian, Magnuson, Steve, Volgraf, Matthew, Payandeh, Jian, Zheng, Jie, Rohou, Alexis, Chen, Jun
Published in Neuron (Cambridge, Mass.) (20.01.2021)
Published in Neuron (Cambridge, Mass.) (20.01.2021)
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Discovery of Acyl-sulfonamide Na(v)1.7 Inhibitors GDC-0276 and GDC-0310
Safina, Brian S., McKerrall, Steven J., Sun, Shaoyi, Chen, Chien-An, Chowdhury, Sultan, Jia, Qi, Li, Jun, Zenova, Alla Y., Andrez, Jean-Christophe, Bankar, Girish, Bergeron, Philippe, Chang, Jae H., Chang, Elaine, Chen, Jun, Dean, Richard, Decker, Shannon M., DiPasquale, Antonio, Focken, Thilo, Hemeon, Ivan, Khakh, Kuldip, Kim, Amy, Kwan, Rainbow, Lindgren, Andrea, Lin, Sophia, Maher, Jonathan, Mezeyova, Janette, Misner, Dinah, Nelkenbrecher, Karen, Pang, Jodie, Reese, Rebecca, Shields, Shannon D., Sojo, Luis, Sheng, Tao, Verschoof, Henry, Waldbrook, Matthew, Wilson, Michael S., Xie, Zhiwei, Young, Clint, Zabka, Tanja S., Hackos, David H., Ortwine, Daniel F., White, Andrew D., Johnson, J. P., Robinette, C. Lee, Dehnhardt, Christoph M., Cohen, Charles J., Sutherlin, Daniel P.
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism
Chernov-Rogan, Tania, Gianti, Eleonora, Liu, Chang, Villemure, Elisia, Cridland, Andrew P., Hu, Xiaoyu, Ballini, Elisa, Lange, Wienke, Deisemann, Heike, Li, Tianbo, Ward, Stuart I., Hackos, David H., Magnuson, Steven, Safina, Brian, Klein, Michael L., Volgraf, Matthew, Carnevale, Vincenzo, Chena, Jun
Published in Proceedings of the National Academy of Sciences - PNAS (17.12.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (17.12.2019)
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IMMUNOCONJUGATES
DAVID Y JACKSON, MICHAEL N ALONSO, EDGAR GEORGE ENGLEMAN, BRIAN SAFINA, SHELLEY ERIN ACKERMAN
Year of Publication 01.05.2024
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Year of Publication 01.05.2024
Patent
Discovery of Peptidomimetic Antibody–Drug Conjugate Linkers with Enhanced Protease Specificity
Wei, BinQing, Gunzner-Toste, Janet, Yao, Hui, Wang, Tao, Wang, Jing, Xu, Zijin, Chen, Jinhua, Wai, John, Nonomiya, Jim, Tsai, Siao Ping, Chuh, Josefa, Kozak, Katherine R, Liu, Yichin, Yu, Shang-Fan, Lau, Jeff, Li, Guangmin, Phillips, Gail D, Leipold, Doug, Kamath, Amrita, Su, Dian, Xu, Keyang, Eigenbrot, Charles, Steinbacher, Stefan, Ohri, Rachana, Raab, Helga, Staben, Leanna R, Zhao, Guiling, Flygare, John A, Pillow, Thomas H, Verma, Vishal, Masterson, Luke A, Howard, Philip W, Safina, Brian
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)methane-sulfonamidesas Potent and Selective hNa(v)1.7 Inhibitors for the Treatment of Pain
Focken, Thilo, Chowdhury, Sultan, Zenova, Alla, Grimwood, Michael E., Chabot, Christine, Sheng, Tao, Hemeon, Ivan, Decker, Shannon M., Wilson, Michael, Bichler, Paul, Jia, Qi, Sun, Shaoyi, Young, Clint, Lin, Sophia, Goodchild, Samuel J., Shuart, Noah G., Chang, Elaine, Xie, Zhiwei, Li, Bowen, Khakh, Kuldip, Bankar, Girish, Waldbrook, Matthew, Kwan, Rainbow, Nelkenbrecher, Karen, Tari, Parisa Karimi, Chahal, Navjot, Sojo, Luis, Robinette, C. Lee, White, Andrew D., Chen, Chien-An, Zhang, Yi, Pang, Jodie, Chang, Jae H., Hackos, David H., Johnson, J. P., Cohen, Charles J., Ortwine, Daniel F., Sutherlin, Daniel P., Dehnhardt, Christoph M., Safina, Brian S.
Published in Journal of medicinal chemistry (14.06.2018)
Published in Journal of medicinal chemistry (14.06.2018)
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Journal Article
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of Na(V)1.7 with Efficacy in Rodent Pain Models
Focken, Thilo, Liu, Shifeng, Chahal, Navjot, Dauphinais, Maxim, Grimwood, Michael E., Chowdhury, Sultan, Hemeon, Ivan, Bichler, Paul, Bogucki, David, Waldbrook, Matthew, Bankar, Girish, Sojo, Luis E., Young, Clint, Lin, Sophia, Shuart, Noah, Kwan, Rainbow, Pang, Jodie, Chang, Jae H., Safina, Brian S., Sutherlin, Daniel P., Johnson, J. P., Dehnhardt, Christoph M., Mansour, Tarek S., Oballa, Renata M., Cohen, Charles J., Robinette, C. Lee
Published in ACS medicinal chemistry letters (01.03.2016)
Published in ACS medicinal chemistry letters (01.03.2016)
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Antibody–Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo
Su, Dian, Chen, Jinhua, Cosino, Ely, dela Cruz-Chuh, Josefa, Davis, Helen, Del Rosario, Geoffrey, Figueroa, Isabel, Goon, Leanne, He, Jintang, Kamath, Amrita V, Kaur, Surinder, Kozak, Katherine R, Lau, Jeffrey, Lee, Donna, Lee, M. Violet, Leipold, Douglas, Liu, Luna, Liu, Peter, Lu, Guo-Liang, Nelson, Chris, Ng, Carl, Pillow, Thomas H, Polakis, Paul, Polson, Andrew G, Rowntree, Rebecca K, Saad, Ola, Safina, Brian, Stagg, Nicola J, Tercel, Moana, Vandlen, Richard, Vollmar, Breanna S, Wai, John, Wang, Tao, Wei, BinQing, Xu, Keyang, Xue, Juanjuan, Xu, Zijin, Yan, Gang, Yao, Hui, Yu, Shang-Fan, Zhang, Donglu, Zhong, Fiona, Dragovich, Peter S
Published in Bioconjugate chemistry (15.05.2019)
Published in Bioconjugate chemistry (15.05.2019)
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