Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases
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Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
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MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition
Vande Walle, Lieselotte, Stowe, Irma B, Šácha, Pavel, Lee, Bettina L, Demon, Dieter, Fossoul, Amelie, Van Hauwermeiren, Filip, Saavedra, Pedro H V, Šimon, Petr, Šubrt, Vladimír, Kostka, Libor, Stivala, Craig E, Pham, Victoria C, Staben, Steven T, Yamazoe, Sayumi, Konvalinka, Jan, Kayagaki, Nobuhiko, Lamkanfi, Mohamed
Published in PLoS biology (16.09.2019)
Published in PLoS biology (16.09.2019)
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Monomeric Targeted Protein Degraders
Hanan, Emily J, Liang, Jun, Wang, Xiaojing, Blake, Robert A, Blaquiere, Nicole, Staben, Steven T
Published in Journal of medicinal chemistry (22.10.2020)
Published in Journal of medicinal chemistry (22.10.2020)
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Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study
Yamazoe, Sayumi, Tom, Jeffrey, Fu, Yue, Wu, Wenqiong, Zeng, Liang, Sun, Changlei, Liu, Qi, Lin, Jie, Lin, Kui, Fairbrother, Wayne J, Staben, Steven T
Published in Journal of medicinal chemistry (26.03.2020)
Published in Journal of medicinal chemistry (26.03.2020)
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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor
McBride, Christopher, Trzoss, Lynnie, Povero, Davide, Lazic, Milos, Ambrus-Aikelin, Geza, Santini, Angelina, Pranadinata, Rama, Bain, Gretchen, Stansfield, Ryan, Stafford, Jeffrey A., Veal, James, Takahashi, Ryan, Ly, Justin, Chen, Shu, Liu, Liling, Nespi, Marika, Blake, Robert, Katewa, Arna, Kleinheinz, Tracy, Sujatha-Bhaskar, Swathi, Ramamoorthi, Nandhini, Sims, Jessica, McKenzie, Brent, Chen, Mark, Ultsch, Mark, Johnson, Matthew, Murray, Jeremy, Ciferri, Claudio, Staben, Steven T., Townsend, Michael J., Stivala, Craig E.
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Selective activation of PFKL suppresses the phagocytic oxidative burst
Amara, Neri, Cooper, Madison P., Voronkova, Maria A., Webb, Bradley A., Lynch, Eric M., Kollman, Justin M., Ma, Taylur, Yu, Kebing, Lai, Zijuan, Sangaraju, Dewakar, Kayagaki, Nobuhiko, Newton, Kim, Bogyo, Matthew, Staben, Steven T., Dixit, Vishva M.
Published in Cell (19.08.2021)
Published in Cell (19.08.2021)
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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties
Dragovich, Peter S, Pillow, Thomas H, Blake, Robert A, Sadowsky, Jack D, Adaligil, Emel, Adhikari, Pragya, Bhakta, Sunil, Blaquiere, Nicole, Chen, Jinhua, dela Cruz-Chuh, Josefa, Gascoigne, Karen E, Hartman, Steven J, He, Mingtao, Kaufman, Susan, Kleinheinz, Tracy, Kozak, Katherine R, Liu, Liang, Liu, Liling, Liu, Qi, Lu, Ying, Meng, Fanwei, Mulvihill, Melinda M, O’Donohue, Aimee, Rowntree, Rebecca K, Staben, Leanna R, Staben, Steven T, Wai, John, Wang, Jian, Wei, BinQing, Wilson, Catherine, Xin, Jianfeng, Xu, Zijin, Yao, Hui, Zhang, Donglu, Zhang, Hongyan, Zhou, Hao, Zhu, Xiaoyu
Published in Journal of medicinal chemistry (11.03.2021)
Published in Journal of medicinal chemistry (11.03.2021)
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NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus
Brightbill, Hans D, Suto, Eric, Blaquiere, Nicole, Ramamoorthi, Nandhini, Sujatha-Bhaskar, Swathi, Gogol, Emily B, Castanedo, Georgette M, Jackson, Benjamin T, Kwon, Youngsu C, Haller, Susan, Lesch, Justin, Bents, Karin, Everett, Christine, Kohli, Pawan Bir, Linge, Sandra, Christian, Laura, Barrett, Kathy, Jaochico, Allan, Berezhkovskiy, Leonid M, Fan, Peter W, Modrusan, Zora, Veliz, Kelli, Townsend, Michael J, DeVoss, Jason, Johnson, Adam R, Godemann, Robert, Lee, Wyne P, Austin, Cary D, McKenzie, Brent S, Hackney, Jason A, Crawford, James J, Staben, Steven T, Alaoui Ismaili, Moulay H, Wu, Lawren C, Ghilardi, Nico
Published in Nature communications (12.01.2018)
Published in Nature communications (12.01.2018)
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Hanan, Emily J., Braun, Marie-Gabrielle, Heald, Robert A., MacLeod, Calum, Chan, Connie, Clausen, Saundra, Edgar, Kyle A., Eigenbrot, Charles, Elliott, Richard, Endres, Nicholas, Friedman, Lori S., Gogol, Emily, Gu, Xiao-Hui, Thibodeau, Rebecca Hong, Jackson, Philip S., Kiefer, James R., Knight, Jamie D., Nannini, Michelle, Narukulla, Raman, Pace, Amanda, Pang, Jodie, Purkey, Hans E., Salphati, Laurent, Sampath, Deepak, Schmidt, Stephen, Sideris, Steve, Song, Kyung, Sujatha-Bhaskar, Swathi, Ultsch, Mark, Wallweber, Heidi, Xin, Jianfeng, Yeap, SiewKuen, Young, Amy, Zhong, Yu, Staben, Steven T.
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Gold(I)-Catalyzed Stereoselective Olefin Cyclopropanation
Johansson, Magnus J, Gorin, David J, Staben, Steven T, Toste, F. Dean
Published in Journal of the American Chemical Society (28.12.2005)
Published in Journal of the American Chemical Society (28.12.2005)
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Identifying transcriptional programs underlying cancer drug response with TraCe-seq
Chang, Matthew T, Shanahan, Frances, Nguyen, Thi Thu Thao, Staben, Steven T, Gazzard, Lewis, Yamazoe, Sayumi, Wertz, Ingrid E, Piskol, Robert, Yang, Yeqing Angela, Modrusan, Zora, Haley, Benjamin, Evangelista, Marie, Malek, Shiva, Foster, Scott A, Ye, Xin
Published in Nature biotechnology (01.01.2022)
Published in Nature biotechnology (01.01.2022)
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Targeted degradation via direct 26S proteasome recruitment
Bashore, Charlene, Prakash, Sumit, Johnson, Matthew C, Conrad, Ryan J, Kekessie, Ivy A, Scales, Suzie J, Ishisoko, Noriko, Kleinheinz, Tracy, Liu, Peter S, Popovych, Nataliya, Wecksler, Aaron T, Zhou, Lijuan, Tam, Christine, Zilberleyb, Inna, Srinivasan, Rajini, Blake, Robert A, Song, Aimin, Staben, Steven T, Zhang, Yingnan, Arnott, David, Fairbrother, Wayne J, Foster, Scott A, Wertz, Ingrid E, Ciferri, Claudio, Dueber, Erin C
Published in Nature chemical biology (01.01.2023)
Published in Nature chemical biology (01.01.2023)
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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)
Dragovich, Peter S., Adhikari, Pragya, Blake, Robert A., Blaquiere, Nicole, Chen, Jinhua, Cheng, Yun-Xing, den Besten, Willem, Han, Jinping, Hartman, Steven J., He, Jintang, He, Mingtao, Rei Ingalla, Ellen, Kamath, Amrita V., Kleinheinz, Tracy, Lai, Tommy, Leipold, Douglas D., Li, Chun Sing, Liu, Qi, Lu, Jiawei, Lu, Ying, Meng, Fanwei, Meng, Lingyao, Ng, Carl, Peng, Kaishan, Lewis Phillips, Gail, Pillow, Thomas H., Rowntree, Rebecca K., Sadowsky, Jack D., Sampath, Deepak, Staben, Leanna, Staben, Steven T., Wai, John, Wan, Kunpeng, Wang, Xinxin, Wei, BinQing, Wertz, Ingrid E., Xin, Jianfeng, Xu, Keyang, Yao, Hui, Zang, Richard, Zhang, Donglu, Zhou, Hao, Zhao, Yongxin
Published in Bioorganic & medicinal chemistry letters (15.02.2020)
Published in Bioorganic & medicinal chemistry letters (15.02.2020)
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Au(I)-Catalyzed Ring Expanding Cycloisomerizations: Total Synthesis of Ventricosene
Sethofer, Steven G, Staben, Steven T, Hung, Olivia Y, Toste, F. Dean
Published in Organic letters (02.10.2008)
Published in Organic letters (02.10.2008)
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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy
Song, Kyung W, Edgar, Kyle A, Hanan, Emily J, Hafner, Marc, Oeh, Jason, Merchant, Mark, Sampath, Deepak, Nannini, Michelle A, Hong, Rebecca, Phu, Lilian, Forrest, William F, Stawiski, Eric, Schmidt, Stephen, Endres, Nicholas, Guan, Jane, Wallin, Jeffrey J, Cheong, Jonathan, Plise, Emile G, Lewis Phillips, Gail D, Salphati, Laurent, Heffron, Timothy P, Olivero, Alan G, Malek, Shiva, Staben, Steven T, Kirkpatrick, Donald S, Dey, Anwesha, Friedman, Lori S
Published in Cancer discovery (01.01.2022)
Published in Cancer discovery (01.01.2022)
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Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability
Ladi, Ena, Everett, Christine, Stivala, Craig E, Daniels, Blake E, Durk, Matthew R, Harris, Seth F, Huestis, Malcolm P, Purkey, Hans E, Staben, Steven T, Augustin, Martin, Blaesse, Michael, Steinbacher, Stefan, Eidenschenk, Celine, Pappu, Rajita, Siu, Michael
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity
Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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Heteroarylation of Azine N-Oxides
Gosselin, Francis, Savage, Scott J, Blaquiere, Nicole, Staben, Steven T
Published in Organic letters (03.02.2012)
Published in Organic letters (03.02.2012)
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