Search Results - "Fischer, Eric S"

Plasticity in binding confers selectivity in ligand-induced protein degradation by Nowak, Radosław P., DeAngelo, Stephen L., Buckley, Dennis, He, Zhixiang, Donovan, Katherine A., An, Jian, Safaee, Nozhat, Jedrychowski, Mark P., Ponthier, Charles M., Ishoey, Mette, Zhang, Tinghu, Mancias, Joseph D., Gray, Nathanael S., Bradner, James E., Fischer, Eric S.

“…Heterobifunctional small-molecule degraders that induce protein degradation through ligase-mediated ubiquitination have shown considerable promise as a new…”
Get full text

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery by Wu, Tao, Yoon, Hojong, Xiong, Yuan, Dixon-Clarke, Sarah E., Nowak, Radosław P., Fischer, Eric S.

“…Controlled perturbation of protein activity is essential to study protein function in cells and living organisms. Small molecules that hijack the cellular…”
Get full text

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15 by Faust, Tyler B., Yoon, Hojong, Nowak, Radosław P., Donovan, Katherine A., Li, Zhengnian, Cai, Quan, Eleuteri, Nicholas A., Zhang, Tinghu, Gray, Nathanael S., Fischer, Eric S.

“…The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the degradation of the splicing factor RBM39 in a proteasome-dependent…”
Get full text

Structure of the Human cGAS–DNA Complex Reveals Enhanced Control of Immune Surveillance by Zhou, Wen, Whiteley, Aaron T., de Oliveira Mann, Carina C., Morehouse, Benjamin R., Nowak, Radosław P., Fischer, Eric S., Gray, Nathanael S., Mekalanos, John J., Kranzusch, Philip J.

“…Cyclic GMP–AMP synthase (cGAS) recognition of cytosolic DNA is critical for immune responses to pathogen replication, cellular stress, and cancer. Existing…”
Get full text

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation by Olson, Calla M, Jiang, Baishan, Erb, Michael A, Liang, Yanke, Doctor, Zainab M, Zhang, Zinan, Zhang, Tinghu, Kwiatkowski, Nicholas, Boukhali, Myriam, Green, Jennifer L, Haas, Wilhelm, Nomanbhoy, Tyzoon, Fischer, Eric S, Young, Richard A, Bradner, James E, Winter, Georg E, Gray, Nathanael S

“…A selective small-molecule degrader of CDK9 was generated by conjugating an imide to SNS-032, a promiscuous ATP-site-directed CDK binder. The pharmacological…”
Get full text

Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML by Brand, Matthias, Jiang, Baishan, Bauer, Sophie, Donovan, Katherine A, Liang, Yanke, Wang, Eric S, Nowak, Radosław P, Yuan, Jingting C, Zhang, Tinghu, Kwiatkowski, Nicholas, Müller, André C, Fischer, Eric S, Gray, Nathanael S, Winter, Georg E

“…The design of selective small molecules is often stymied by similar ligand binding pockets. Here, we report BSJ-03-123, a phthalimide-based degrader that…”
Get more information

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader by Huang, Hai-Tsang, Dobrovolsky, Dennis, Paulk, Joshiawa, Yang, Guang, Weisberg, Ellen L, Doctor, Zainab M, Buckley, Dennis L, Cho, Joong-Heui, Ko, Eunhwa, Jang, Jaebong, Shi, Kun, Choi, Hwan Geun, Griffin, James D, Li, Ying, Treon, Steven P, Fischer, Eric S, Bradner, James E, Tan, Li, Gray, Nathanael S

“…Heterobifunctional molecules that recruit E3 ubiquitin ligases, such as cereblon, for targeted protein degradation represent an emerging pharmacological…”
Get more information

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations by de Wispelaere, Mélissanne, Du, Guangyan, Donovan, Katherine A., Zhang, Tinghu, Eleuteri, Nicholas A., Yuan, Jingting C., Kalabathula, Joann, Nowak, Radosław P., Fischer, Eric S., Gray, Nathanael S., Yang, Priscilla L.

“…Targeted protein degradation is a promising drug development paradigm. Here we leverage this strategy to develop a new class of small molecule antivirals that…”
Get full text

Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome by Donovan, Katherine A, An, Jian, Nowak, Radosław P, Yuan, Jingting C, Fink, Emma C, Berry, Bethany C, Ebert, Benjamin L, Fischer, Eric S

“…In historical attempts to treat morning sickness, use of the drug thalidomide led to the birth of thousands of children with severe birth defects. Despite…”
Get full text

Small molecule modulation of protein polymerization by Fischer, Eric S, Jones, Lyn H

“…The modulation of protein surface physicochemistry through single point mutations can trigger polymerization, which is facilitated by subunit repetition within…”
Get more information

Bruton tyrosine kinase degradation as a therapeutic strategy for cancer by Dobrovolsky, Dennis, Wang, Eric S., Morrow, Sara, Leahy, Catharine, Faust, Tyler, Nowak, Radosław P., Donovan, Katherine A., Yang, Guang, Li, Zhengnian, Fischer, Eric S., Treon, Steven P., Weinstock, David M., Gray, Nathanael S.

“…The covalent Bruton tyrosine kinase (BTK) inhibitor ibrutinib is highly efficacious against multiple B-cell malignancies. However, it is not selective for BTK,…”
Get full text

Chemo-proteomics exploration of HDAC degradability by small molecule degraders by Xiong, Yuan, Donovan, Katherine A, Eleuteri, Nicholas A, Kirmani, Nadia, Yue, Hong, Razov, Anthony, Krupnick, Noah M, Nowak, Radosław P, Fischer, Eric S

“…Targeted protein degradation refers to the use of small molecules that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent…”
Get more information

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK) by Powell, Chelsea E, Gao, Yang, Tan, Li, Donovan, Katherine A, Nowak, Radosław P, Loehr, Amanda, Bahcall, Magda, Fischer, Eric S, Jänne, Pasi A, George, Rani E, Gray, Nathanael S

“…We present the development of the first small molecule degraders that can induce anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung…”
Get full text

Crystal structure of the human COP9 signalosome by Lingaraju, Gondichatnahalli M., Bunker, Richard D., Cavadini, Simone, Hess, Daniel, Hassiepen, Ulrich, Renatus, Martin, Fischer, Eric S., Thomä, Nicolas H.

“…Ubiquitination is a crucial cellular signalling process, and is controlled on multiple levels. Cullin–RING E3 ubiquitin ligases (CRLs) are regulated by the…”
Get full text

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models by Silva, M Catarina, Ferguson, Fleur M, Cai, Quan, Donovan, Katherine A, Nandi, Ghata, Patnaik, Debasis, Zhang, Tinghu, Huang, Hai-Tsang, Lucente, Diane E, Dickerson, Bradford C, Mitchison, Timothy J, Fischer, Eric S, Gray, Nathanael S, Haggarty, Stephen J

“…Tauopathies are neurodegenerative diseases characterized by aberrant forms of tau protein accumulation leading to neuronal death in focal brain areas. Positron…”
Get full text

Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2 by Du, Guangyan, Jiang, Jie, Wu, Qibiao, Henning, Nathaniel J., Donovan, Katherine A., Yue, Hong, Che, Jianwei, Lu, Wenchao, Fischer, Eric S., Bardeesy, Nabeel, Zhang, Tinghu, Gray, Nathanael S.

“…Aberrant activation of FGFR signaling occurs in many cancers, and ATP‐competitive FGFR inhibitors have received regulatory approval. Despite demonstrating…”
Get full text

INK4 Tumor Suppressor Proteins Mediate Resistance to CDK4/6 Kinase Inhibitors by Li, Qing, Jiang, Baishan, Guo, Jiaye, Shao, Hong, Del Priore, Isabella S, Chang, Qing, Kudo, Rei, Li, Zhiqiang, Razavi, Pedram, Liu, Bo, Boghossian, Andrew S, Rees, Matthew G, Ronan, Melissa M, Roth, Jennifer A, Donovan, Katherine A, Palafox, Marta, Reis-Filho, Jorge S, de Stanchina, Elisa, Fischer, Eric S, Rosen, Neal, Serra, Violeta, Koff, Andrew, Chodera, John D, Gray, Nathanael S, Chandarlapaty, Sarat

“…Cyclin-dependent kinases 4 and 6 (CDK4/6) represent a major therapeutic vulnerability for breast cancer. The kinases are clinically targeted via ATP…”
Get more information

MEN1 mutations mediate clinical resistance to menin inhibition by Perner, Florian, Stein, Eytan M., Wenge, Daniela V., Singh, Sukrit, Kim, Jeonghyeon, Apazidis, Athina, Rahnamoun, Homa, Anand, Disha, Marinaccio, Christian, Hatton, Charlie, Wen, Yanhe, Stone, Richard M., Schaller, David, Mowla, Shoron, Xiao, Wenbin, Gamlen, Holly A., Stonestrom, Aaron J., Persaud, Sonali, Ener, Elizabeth, Cutler, Jevon A., Doench, John G., McGeehan, Gerard M., Volkamer, Andrea, Chodera, John D., Nowak, Radosław P., Fischer, Eric S., Levine, Ross L., Armstrong, Scott A., Cai, Sheng F.

“…Chromatin-binding proteins are critical regulators of cell state in haematopoiesis 1 , 2 . Acute leukaemias driven by rearrangement of the mixed lineage…”
Get full text

Solenoid architecture of HUWE1 contributes to ligase activity and substrate recognition by Hunkeler, Moritz, Jin, Cyrus Y., Ma, Michelle W., Monda, Julie K., Overwijn, Daan, Bennett, Eric J., Fischer, Eric S.

“…HECT ubiquitin ligases play essential roles in metazoan development and physiology. The HECT ligase HUWE1 is central to the cellular stress response by…”
Get full text

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C by Zeng, Mei, Lu, Jia, Li, Lianbo, Feru, Frederic, Quan, Chunshan, Gero, Thomas W, Ficarro, Scott B, Xiong, Yuan, Ambrogio, Chiara, Paranal, Raymond M, Catalano, Marco, Shao, Jay, Wong, Kwok-Kin, Marto, Jarrod A, Fischer, Eric S, Jänne, Pasi A, Scott, David A, Westover, Kenneth D, Gray, Nathanael S

“…Targeted covalent small molecules have shown promise for cancers driven by KRAS G12C. Allosteric compounds that access an inducible pocket formed by movement…”
Get more information