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Featured Publications
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Full list of publications
2024

High-throughput diversification of protein-ligand surfaces to discover chemical inducers of proximity.

James B. Shaum, Erica A. Steen, Miquel Muñoz i Ordoño, Daniela V. Wenge, Hakyung Cheong, Moritz Hunkeler, Eric M. Bilotta, Zoe Rutter, Paige A. Barta, Natalia Milosevich, Lauren M. Hargis, Jordan Janowski, Timothy R. Bishop, Trever R. Carter, Bryce da Camara, Matthias Hinterndorfer, Lucas Dada, Wen-Ji He, Fabian Offensperger, Hirotake Furihata, Sydney R. Schweber, Charlie Hatton, Yanhe (Crane) Wen, Benjamin F. Cravatt, Keary M. Engle, Bruno Melillo, Seiya Kitamura, Alessio Ciulli, Scott A. Armstrong, Eric S. Fischer, Georg E. Winter, Michael A. Erb.

bioRxiv (2024) – https://www.biorxiv.org/content/10.1101/2024.09.30.615685v1

Redirecting the pioneering function of FOXA1 with covalent small molecules.

Sang Joon Won*, Yuxiang Zhang*, Christopher J. Reinhardt, Lauren M. Hargis, Nicole S. MacRae, Kristen E. DeMeester, Evert Njomen, Jarrett R. Remsberg, Bruno Melillo, Benjamin F. Cravatt**, Michael A. Erb**.

Molecular Cell 84, 1-17 (2024).

Functional Investigations of p53 Acetylation Enabled by Heterobifunctional Molecules.

Li-Yun Chen, Soumya Jyoti Singha Roy, Appaso M Jadhav, Wesley W Wang, Pei-Hsin Chen, Timothy Bishop, Michael A Erb, Christopher G Parker.

ACS Chemical Biology 19, 1918−1929 (2024).

SuFEx-based chemical diversification for the systematic discovery of CRBN molecular glues.

Trever R. Carter, Natalia Milosevich, Lucas Dada, James B. Shaum, K. Barry Sharpless, Seiya Kitamura**, Michael A. Erb**.

Bioorganic and Medicinal Chemistry 104, 117699 (2024).

Inherited blood cancer predisposition through altered transcription elongation.

Jiawei Zhao, Liam D. Cato, Uma P. Arora, Erik L. Bao, Samuel C. Bryant, Nicholas Williams, Yuemeng Jia, Seth R. Goldman, Jyoti Nangalia, Michael A. Erb, Seychelle M. Vos, Scott A. Armstrong, Vijay G. Sankaran.

Cell 187, 642-658 (2024).

2023

Small-molecule tools for YEATS domain proteins

Michael A. Erb

Current Opinion in Chemical Biology 78, 102404 (2023).

Acetyl-CoA biosynthesis drives resistance to histone acetyltransferase inhibition.

Bishop TR, Subramanian C, Bilotta EM, Garnar-Wortzel L, Ramos AR, Zhang Y, Asiaban JN, Ott CJ, Rock CO, Erb MA.

Nature Chemical Biology 19, 1215–1222 (2023).

As featured in Nature Chemical Biology "News and Views"

Metabolic regulation of epigenetic drug resistance.

Nathaniel W. Snyder & Jordan L. Meier.

Collateral lethality between HDAC1 and HDAC2 exploits cancer-specific NuRD complex vulnerabilities.

Yuxiang Zhang, David Remillard, Ugoma Onubogu, Barbara Karakyriakou, Joshua N Asiaban, Anissa R Ramos, Kirsten Bowland, Timothy R Bishop, Paige A Barta, Stephanie Nance, Adama D Durbin, Christopher J Ott, Michalina Janiszewska, Benjamin F Cravatt, Michael A Erb.

Nature Structural & Molecular Biology 30, 1160–1171 (2023)

2021

Enabling cancer target validation with genetically encoded systems for ligand-induced protein degradation.

Zhang Y, Erb MA. 

Current Research in Chemical Biology 1, (2021)

Chemical inhibition of ENL/AF9 YEATS domains in acute leukemia.

Garnar-Wortzel L,* Bishop TR,* Kitamura S,* Milosevich N, Asiaban JN, Zhang X, Zheng Q, Chen E, Ramos AR, Ackerman CJ, Hampton EN, Chatterjee AK, Young TS, Hull MV, Sharpless KB, Cravatt BF, Wolan DW, Erb MA.

ACS Central Science 7, 815-830 (2021)

A short ORF-encoded transcriptional regulator.

Koh M, Ahmad I, Ko Y, Zhang Y, Martinez TF, Diedrich JK, Chu Q, Moresco JJ, Erb MA, Saghatelian A†, Schultz PG†, Bollong MJ†.

Proceedings of the National Academy of Sciences 118, e2021943118. (2021)

2020

Cell-Based Ligand Discovery for the ENL YEATS Domain.

Asiaban JN, Milosevich N, Chen E, Bishop TR, Wang J, Zhang Y, Ackerman CJ, Hampton EN, Young TS, Hull MV, Cravatt BF, Erb MA.

ACS Chemical Biology 15, 895–903 (2020)

Processing for Destruction.

Erb, MA.

Nature Chemical Biology 16, 3–4 (2020) News and Views

2019

Pharmacological Modulation of Transcriptional Coregulators in Cancer.

Bishop, TR; Zhang, Y; Erb, MA.

Trends in Pharmacological Sciences 40, 388–402 (2019)

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Graduate publications
 
2018

Nabet, B; Roberts, JM; Buckley, DL; Paulk, J; Dastjerdi, S; Yang, A; Leggett, AL; Erb, MA; Lawlor, MA; Souza, A; Scott, TG; Vittori, S; Perry, JA; Qi, J; Winter, GE; Wong, K-K.; Gray, NS; Bradner, JE. The dTAG System for Immediate and Target-Specific Protein Degradation. Nat Chem Biol 2018, 14 (5), 431–441. https://doi.org/10.1038/s41589-018-0021-8.

Gechijian, LN; Buckley, DL; Lawlor, MA; Reyes, JM; Paulk, J; Ott, CJ; Winter, GE; Erb, MA; Scott, TG; Xu, M; Seo, H-S.; Dhe-Paganon, S; Kwiatkowski, NP; Perry, JA; Qi, J; Gray, NS; Bradner, J. E. Functional TRIM24 Degrader via Conjugation of Ineffectual Bromodomain and VHL Ligands. Nat Chem Biol 2018, 14 (4), 405–412. https://doi.org/10.1038/s41589-018-0010-y.

Zeid, R; Lawlor, MA; Poon, E; Reyes, JM; Fulciniti, M; Lopez, MA; Scott, TG; Nabet, B; Erb, MA; Winter, GE; Jacobson, Z; Polaski, DR; Karlin, KL; Hirsch, RA; Munshi, NP; Westbrook, TF; Chesler, L; Lin, CY; Bradner, JE. Enhancer Invasion Shapes MYCN-Dependent Transcriptional Amplification in Neuroblastoma. Nat Genet 2018, 463 (4), 899. https://doi.org/10.1038/s41588-018-0044-9.

Ishoey, M; Chorn, S; Singh, N; Jaeger, MG; Brand, M; Paulk, J; Bauer, S; Erb, MA; Parapatics, K; Müller, AC; Bennett, KL; Ecker, GF; Bradner, JE; Winter, GE. Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders. Acs Chem Biol 2018, 13 (3), 553–560. https://doi.org/10.1021/acschembio.7b00969.

Olson, CM; Jiang, B; Erb, MA; Liang, Y; Doctor, ZM; Zhang, Z; Zhang, T; Kwiatkowski, N; Boukhali, M; Green, JL; Haas, W; Nomanbhoy, T; Fischer, ES; Young, RA; Bradner, JE; Winter, GE; Gray, NS. Pharmacological Perturbation of CDK9 Using Selective CDK9 Inhibition or Degradation. Nat Chem Biol 2018, 14 (2), 163–170. https://doi.org/10.1038/nchembio.2538.

2017

Winter, GE*; Mayer, A*; Buckley, DL*; Erb, MA*; Roderick, JE; Vittori, S; Reyes, JM; Iulio, J di; Souza, A; Ott, CJ; Roberts, JM; Zeid, R; Scott, TG; Paulk, J; Lachance, K; Olson, CM; Dastjerdi, S; Bauer, S; Lin, CY; Gray, NS; Kelliher, MA; Churchman, LS; Bradner, JE. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell 2017, 67 (1), 5-18.e19. https://doi.org/10.1016/j.molcel.2017.06.004.

Erb, MA; Scott, TG.; Li, BE; Xie, H; Paulk, J; Seo, H-S; Souza, A; Roberts, JM; Dastjerdi, S; Buckley, DL; Sanjana, NE; Shalem, O; Nabet, B; Zeid, R; Offei-Addo, NK; Dhe-Paganon, S; Zhang, F; Orkin, SH; Winter, GE; Bradner, JE. Transcription Control by the ENL YEATS Domain in Acute Leukaemia. Nature 2017, 543(7644), 270–274. https://doi.org/10.1038/nature21688.

Wan, L; Wen, H; Li, Y; Lyu, J; Xi, Y; Hoshii, T; Joseph, JK; Wang, X; Loh, Y-HE; Erb, MA; Souza, AL; Bradner, JE; Shen, L; Li, W; Li, H; Allis, CD; Armstrong, SA; Shi, X. ENL Links Histone Acetylation to Oncogenic Gene Expression in Acute Myeloid Leukaemia. Nature 2017, 543 (7644), 265–269. https://doi.org/10.1038/nature21687.

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