Search Results - "Fischer, Eric"

Structural basis of lenalidomide-induced CK1α degradation by the CRL4(CRBN) ubiquitin ligase by Petzold, Georg, Fischer, Eric S, Thomä, Nicolas H

“…Thalidomide and its derivatives, lenalidomide and pomalidomide, are immune modulatory drugs (IMiDs) used in the treatment of haematologic malignancies. IMiDs…”
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Beyond Cavity Born–Oppenheimer: On Nonadiabatic Coupling and Effective Ground State Hamiltonians in Vibro-Polaritonic Chemistry by Fischer, Eric W., Saalfrank, Peter

“…The emerging field of vibro-polaritonic chemistry studies the impact of light–matter hybrid states known as vibrational polaritons on chemical reactivity and…”
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Structural basis of regulated m7G tRNA modification by METTL1–WDR4 by Li, Jiazhi, Wang, Longfei, Hahn, Quentin, Nowak, Radosław P., Viennet, Thibault, Orellana, Esteban A., Roy Burman, Shourya S., Yue, Hong, Hunkeler, Moritz, Fontana, Pietro, Wu, Hao, Arthanari, Haribabu, Fischer, Eric S., Gregory, Richard I.

“…Chemical modifications of RNA have key roles in many biological processes 1 – 3 . N 7 -methylguanosine (m 7 G) is required for integrity and stability of a…”
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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…”
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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…”
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Structures of BIRC6-client complexes provide a mechanism of SMAC-mediated release of caspases by Hunkeler, Moritz, Jin, Cyrus Y, Fischer, Eric S

“…Tight regulation of apoptosis is essential for metazoan development and prevents diseases such as cancer and neurodegeneration. Caspase activation is central…”
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Development of Dual and Selective Degraders of Cyclin‐Dependent Kinases 4 and 6 by Jiang, Baishan, Wang, Eric S., Donovan, Katherine A., Liang, Yanke, Fischer, Eric S., Zhang, Tinghu, Gray, Nathanael S.

“…Cyclin‐dependent kinases 4 and 6 (CDK4/6) are key regulators of the cell cycle, and there are FDA‐approved CDK4/6 inhibitors for treating patients with…”
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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…”
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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…”
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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…”
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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…”
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Targeted protein degradation: from mechanisms to clinic by Tsai, Jonathan M., Nowak, Radosław P., Ebert, Benjamin L., Fischer, Eric S.

“…Targeted protein degradation refers to the use of small molecules to induce the selective degradation of proteins. In its most common form, this degradation is…”
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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…”
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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…”
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METTL1-mediated m7G modification of Arg-TCT tRNA drives oncogenic transformation by Orellana, Esteban A., Liu, Qi, Yankova, Eliza, Pirouz, Mehdi, De Braekeleer, Etienne, Zhang, Wencai, Lim, Jihoon, Aspris, Demetrios, Sendinc, Erdem, Garyfallos, Dimitrios A., Gu, Muxin, Ali, Raja, Gutierrez, Alejandro, Mikutis, Sigitas, Bernardes, Gonçalo J.L., Fischer, Eric S., Bradley, Allan, Vassiliou, George S., Slack, Frank J., Tzelepis, Konstantinos, Gregory, Richard I.

“…The emerging “epitranscriptomics” field is providing insights into the biological and pathological roles of different RNA modifications. The RNA…”
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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…”
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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…”
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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,…”
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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…”
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Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling by You, Inchul, Erickson, Emily C, Donovan, Katherine A, Eleuteri, Nicholas A, Fischer, Eric S, Gray, Nathanael S, Toker, Alex

“…The PI3K/AKT signaling cascade is one of the most commonly dysregulated pathways in cancer, with over half of tumors exhibiting aberrant AKT activation…”
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