Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties von 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

Volltext

MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition von 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

Volltext

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases von Blaquiere, Nicole, Villemure, Elisia, Staben, Steven T

Volltext

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... von 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.

Volltext

Monomeric Targeted Protein Degraders von Hanan, Emily J, Liang, Jun, Wang, Xiaojing, Blake, Robert A, Blaquiere, Nicole, Staben, Steven T

Volltext

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study von Yamazoe, Sayumi, Tom, Jeffrey, Fu, Yue, Wu, Wenqiong, Zeng, Liang, Sun, Changlei, Liu, Qi, Lin, Jie, Lin, Kui, Fairbrother, Wayne J, Staben, Steven T

Volltext

Four-Component Synthesis of Fully Substituted 1,2,4-Triazoles von Staben, Steven T, Blaquiere, Nicole

Volltext

Selective activation of PFKL suppresses the phagocytic oxidative burst von 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.

Volltext

Gold(I)-Catalyzed Stereoselective Olefin Cyclopropanation von Johansson, Magnus J, Gorin, David J, Staben, Steven T, Toste, F. Dean

Volltext

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα) von 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

Volltext

A General Strategy for the Construction of Functionalized Azaindolines via Domino Palladium-Catalyzed Heck Cyclization/Suzuki Coupling von Schempp, Tabitha T, Daniels, Blake E, Staben, Steven T, Stivala, Craig E

Volltext

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus von 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

Volltext

Au(I)-Catalyzed Ring Expanding Cycloisomerizations: Total Synthesis of Ventricosene von Sethofer, Steven G, Staben, Steven T, Hung, Olivia Y, Toste, F. Dean

Volltext

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα von 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.

Volltext

Targeted degradation via direct 26S proteasome recruitment von 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.

Volltext

Identifying transcriptional programs underlying cancer drug response with TraCe-seq von 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

Volltext

Gold(I)-Catalyzed Ring Expansion of Cyclopropanols and Cyclobutanols von Markham, Jordan P, Staben, Steven T, Toste, F. Dean

Volltext

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy von 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

Volltext

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... von 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

Volltext

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability von 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

Volltext