Deep mutational scanning of DNMT3A R882H reveals a self-assembly safeguard

Garcia, Emma M.; Lavidor, Olivia R.; Raval, Shaunak; Shekhar, Mrinal; Lue, Nicholas Z.;  Liang, Jessica K.; McFadden, Maeve; Hwang, Derek D.;  Zepeda, Marcanthony U.; Chen, Luke W.;  Carr, Steven A.;  Papanastasiou, Malvina; Liau, Brian B.#

Nature Chemical Biology Accepted in Principle
Preprint
‍ ‍

Covalent chemical rescue of a transcription factor-corepressor complex

Liu, Chao*; Yost, Karl*; Kwok, Hui Si; Caroli, Jonatan; Waterbury, Amanda L.; Gankhuyag, Nomin; Zhang, Olivia; Harry, Stefan A.; Hansen, Tobias N.; Roh, Heejin; Furui, Airi; Mattevi, Andrea; Liau, Brian B.#.

ACS Central Science 2026
Publication
‍ ‍

CRISPR-based functional screening of noncoding regulatory elements

Roh, Heejin; Liau, Brian B.#.

Current Opinion in Chemical Biology 2026 • Review
Publication

A HUWE1 regulatory helix gates ASCL1 degradation through its C-terminal phospho-degron in small cell lung cancer

Masuzawa, Keita*; Dong, Kevin D.*; Hu, Calvin X.; Peng, Ting; Myung, Yoochan; Singh, Shilpa; Li, Xinyue; Wang, Tianchu; Jin, Cyrus; Paulo, Joao A.; Yang, Ka; Schmid, Ernst W.; Booker, Matthew A.; Li, Yixiang; Hong, Deli; Lazo, Suzan; Tolstorukov, Michael Y.; Doench, John G.; Duplaquet, Leslie; Donovan, Katherine A.; Iqbal, Sumaiya; Fischer, Eric S.; Liau, Brian B.; Gygi, Steven P.; Oser, Matthew G.#

Genes and Development 2026
Publication
‍ ‍

Systematic Targeting of Protein Complexes with Molecular COUPLrs

Yang, Diane*; Harry, Stefan A.*; Chong, Harrison B.*; Khandelwal, Neha*; Zhang, Edwin*; Nordenfelt, Natalie S.; Chen, Nicholas; Lee, Christine; Kaluziak, Stefan T.; Codd, Elizabeth M.; Trivedi, Samay; Gohar, Magdy; McKnight, Giovan; Mitchell, Dawn R.; Ge, Maolin; Gao, Chengzhuo; Holmes, Zavontae; Yang, Wenxin; Smith, Abigail E.; Carlin, Alexander D.; Lazarov, Matthew J.; Ibrahim, Sufian M.; Takahashi, Mariko; Zhang, Siwen; Leong, Herman X.; Luna, Hector M.; Stevens, Reilly; Mullin, Paul S.; Ignashkina, Anastasia; Chearavanont, Zander; Emonds, Kim; Popoola, George; Barakat, Idris A.; Onozato, Maristela L.; Mahamdeh, Mohammed; Fujino, Toshio; Gerhartz, Jan; Ackerman, Emily E.; Koh, Huan Yee; Naranbhai, Vivek; Seo, Hyuk-Soo; Dhe-Paganon, Sirano; Sun, Zhen-Yu J.; Heffron, Gregory J.; Hata, Aaron N.; Soberman, Roy J.; Nowak, Radoslaw P.; Ott, Christopher J.; Liau, Brian B.; Iafrate, A. John; Bar-Peled, Liron#

Cancer Discovery 2026
Publication • Preprint
‍ ‍

Proximity-Induced Rewiring of Oncogenic Kinase Triggers Apoptosis

Merz, Manuel L.*; Shoba, Veronika M.*; Pergu, Rajaiah*; Severance, Zachary C.*; Munkanatta Godage, Dhanushka N. P.; Deb, Arghya; Kwok, Hui Si; Singh, Prashant; Singh, Sameek; Allen, Jonathan B.; Tian, Wenzhi; Gosavi, Pallavi M.; Chaudhary, Santosh K.; Anokhina, Viktoriya; Weisberg, Ellen L.; Payne, N. Connor; He, Yao; Dhaliwal, Rohil; Osadchey, Reilly; Shekhar, Mrinal; Mazitschek, Ralph; Rees, Matthew G.; Roth, Jennifer A.; Cui, Qiang; Griffin, James D.; Liau, Brian B.; Choudhary, Amit#

ACS Central Science 2026
Publication • Preprint
‍ ‍

Nano-scaled, fully automated hydrogen/deuterium exchange for analysis of macromolecular assemblies reaching the MDa scale

Raval, Shaunak; Shi, Yuqi; Morriss, Julia W.; Ivanov, Alexander R.; Coales, Stephen; Aphasizheva, Inna; Aphasizhev, Ruslan; Liau, Brian B.; Carr, Steven A.#; Papanastasiou, Malvina#

Molecular & Cellular Proteomics 2026
Publication
‍ ‍

A chemical-genetic interaction between PAF1 and ENL/AF9 YEATS inhibition

Barta, Paige A.; Garnar-Wortzel, Leopold; Bishop, Timothy R.; Hayward, Rachel E.; Hargis, Lauren M.; Shaum, James B.; Kwok, Hui Si; Liau, Brian B.; Cravatt, Benjamin F.; Erb, Michael A.#

RSC Chem. Biol. 2026
Publication | Preprint
‍ ‍

2025

Coupling CRISPR scanning with targeted chromatin accessibility profiling using a double-stranded DNA deaminase

Roh, Heejin*; Shen, Simon P.*; Hu, Yan*; Kwok, Hui Si; Siegenfeld, Allison P.; Lee, Ceejay.; Zepeda, Marcanthony U.; Guo, Chun-Jie; Roseman, Shelby A.; Comenho, Caroline; Sankaran, Vijay G.; Buenrostro, Jason D.; Liau, Brian B.#

Nature Methods 2025
Publication • Preprint • Tweetorial • Nature Methods Research Briefing • Nature Biotechnology Research Highlight • Harvard Gazette
‍ ‍

Covalent adduct Grob fragmentation underlies LSD1 demethylase-specific inhibitor mechanism of action and resistance

Waterbury, Amanda L.*; Caroli, Jonatan*; Zhang, Olivia.; Tuttle, Paloma; Liu, Chao; Li, Jiaming; Park, Ji Sung; Hoenig, Samuel M.; Barone, Marco; Furui, Airi, Mattevi, Andrea#; Liau, Brian B.#

Nature Communications 2025
Publication
‍ ‍

DNA methylation insulates genic regions from CTCF loops near nuclear speckles

Roseman, Shelby A.*; Siegenfeld, Allison P.*; Lee, Ceejay; Lue, Nicholas Z.; Liau, Brian B.#

eLife 2025
Publication • Preprint
‍ ‍

Oxidation of retromer complex controls mitochondrial translation

Zhang, Junbing*; Ali, Md Yousef*; Chong, Harrison B.*; Tien, Pei-Chieh; Woods, James; Noble, Carolina; Vornbäumen, Tristan; Ordulu, Zehra; Possemato, Anthony P; Harry, Stefan A.; Fonticella, Jay M.; Fellah Lina; Harrison, Drew; Ge, Maolin; Khandelwal, Neha; Huang, Yingfei; Chauvin, Maëva; Bischof, Anica T.; Hambelton, Grace M.; Gohar, Magdy F.; Zhang, Siwen; Choi, MinGyu.; Bouberhan, Sara; Oliva, Esther; Mino-Kenudson, Mari; Pavlova, Natalya N.; Lawrence, Michael; Gainor, Justin F.; Beausoleil, Sean A.; Bardeesy, Nabeel; Mostolavsky, Raul; Pépin, David; Ott, Christopher J.; Liau, Brian B.; Bar-Peled L#

Nature 2025
Publication
‍ ‍

Converging mechanism of UM171 and KBTBD4 neomorphic cancer mutations

Xie, Xiaowen*; Zhang, Olivia*; Yeo, Megan J.R.*; Lee, Ceejay*; Tao, Ran; Harry, Stefan A.; Payne, Connor N.; Nam, Eunju; Paul, Leena; Li, Yiran; Kwok, Hui Si; Jiang, Hanjie; Mao, Hiabin; Hadley, Jennifer L.; Lin, Hong; Batts, Melissa; Gosavi, Pallavi M.; D’Angiolella, Vincenzo; Cole, Philip A.; Mazitschek, Ralph; Northcott, Paul A.; Zheng, Ning#; Liau, Brian B.#

Nature 2025
Publication • Preprint • Tweetorial • Nature News & Views • Nature Reviews Drug Discovery Highlight • Cancer Discovery News • Molecular Cell Spotlight
‍ ‍

UM171 glues asymmetric CRL3-HDAC1/2 assembly to degrade CoREST corepressors

Yeo, Megan J.R.*; Zhang, Olivia*; Xie, Xiaowen*; Nam, Eunju*; Payne, Connor N.; Gosavi, Pallavi M.; Kwok, Hui Si; Iram, Irtiza; Lee, Ceejay; Li, Jiaming; Chen, Nicholas; Nguyen, Khanh; Jiang, Hanjie; Wang, Zhipeng A.; Lee, Kwangwoon; Mao, Haibin; Harry, Stefan A.; Barakat, Idris A.; Takahashi, Mariko; Waterbury, Amanda L.; Barone, Marco; Mattevi, Andrea; Carr, Steven A.; Udeshi, Namrata D.; Bar-Peled, Liron;  Mazitschek, Ralph; Cole, Philip A.; Liau, Brian B.#; Zheng, Ning#.

Nature 2025
Publication • Preprint • Tweetorial • Nature News & Views • Nature Reviews Drug Discovery Highlight • Cancer Discovery News • Molecular Cell Spotlight
‍ ‍

CTCF/RAD21 organize the ground state of chromatin-nuclear speckle association

Yu, Ruofan; Roseman, Shelby A.; Siegenfeld, Allison P.; Gardner, Zachary; Nguyen, Son C.; Joyce, Eric F.; Jain, Rajan; Liau, Brian B.; Krantz, Ian D.; Alexander, Katherine#; Berger, Shelley L.#

Nature Structural & Molecular Biology 2025
Publication • Preprint
‍ ‍

Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1

Lee, Kwangwoon; Barone, Marco; Waterbury, Amanda L.; Jiang, Hanjie; Nam, Eunju; DuBois-Coyne, Sarah E.; Whedon, Samuel D.; Wang, Zhipeng A.; Caroli, Jonatan; Neal, Katherine; Ibeabuchi, Brian; Dhoondia, Zuzer; Kuroda, Mitzi I.; Liau, Brian B.; Beck, Samuel#; Mattevi, Andrea#; Cole, Philip A.#

Nature Chemical Biology 2025
Publication
‍ ‍

Building the first base editors

Waterbury, Amanda L.; Iram, Irtiza; Liau, Brian B.#

Nature Chemical Biology 2025 • Invited perspective
Publication
‍ ‍

2024

An autoinhibitory switch of the LSD1 disordered region controls enhancer silencing

Waterbury, Amanda L.*; Kwok, Hui Si*; Lee, Ceejay*; Narducci, Domenic N.; Freedy, Allyson M.; Su, Cindy; Raval, Shaunak; Reiter, Andrew H.; Hawkins, William; Lee, Kwangwoon; Li, Jiaming; Hoenig, Samuel M.; Vinyard, Michael E.; Cole, Philip A.; Hansen, Anders S.; Carr, Steven A.; Papanastasiou, Malvina; Liau, Brian B.#

Molecular Cell 2024
Publication • Tweetorial
‍ ‍

DrugMap: A quantitative pan-cancer analysis of cysteine ligandability

Takahashi, Mariko*; Chong, Harrison B*.; Zhang, Siwen*; Lazarov, Matthew J.; Harry, Stefan; Maynard, Michelle; White, Ryan; Murrey, Heather E.; Hilbert, Brendan; Neil, Jason R.; Gohar, Magdy; Ge, Maolin; Zhang, Junbing; Durr, Benedikt R.; Kryukov, Gregory; Tsou, Chih-Chiang; Brooijmans, Natasja; Alghali, Aliyu; Rubio, Karla; Vilanueva, Antonio; Harrison, Drew; Koglin, Ann-Sophie; Ojeda, Samuel; Karakyriakou, Barbara; Healy, Alexander; Assaad, Jonathan; Makram, Farah; Rachman, Inbal; Khandelwal, Neha; Tien, Pei-Chieh; Popoola, George; Chen, Nicholas; Vordermark, Kira; Richter, Marianne; Patel, Himani; Yang, Tzu-Yi; Griesshaber, Hanna; Hosp, Tobias; van den Ouweland, Sanne; Hara, Toshiro; Bussema, Lily; Dong, Rui; Shi, Lei; Rasmussen, Martin Q.; Domingues, Ana C.; Lawless, Aleigha; Fang, Jacy; Yoda, Satoshi; Nguyen, Linh P.; Reeves, Sarah M.; Wakefield, Farrah N.; Acker, Adam; Clark, Sarah E.; Dubash, Taronish; Fisher, David E.; Maheswaran, Shyamala; Haber, Daniel A.; Boland, Genevieve; Sade-Feldman, Moshe; Jenkins, Russel; Hata, Aaron; Bardeesy, Nabeel; Suva, Mario L.; Martin, Brent; Liau, Brian B.; Ott, Christopher; Rivera, Miguel N.; Lawrence, Michael S.#; Bar-Peled, Liron#

Cell 2024
Publication
‍ ‍

2023

Base editor screens for in situ mutational scanning at scale

Lue, Nicholas Z.; Liau, Brian B.#

Molecular Cell 2023 • Review
Publication • Tweetorial
‍ ‍

Base editor scanning reveals activating mutations of DNMT3A

Garcia, Emma M.; Lue, Nicholas Z.; Liang, Jessica K.; Lieberman, Whitney K.; Hwang, Derek D.; Woods, James; Liau, Brian B.#

ACS Chemical Biology 2023
Publication • Preprint
‍ ‍

Activity-based CRISPR scanning uncovers allostery in DNA methylation maintenance machinery

Ngan, Kevin C.; Hoenig, Samuel M.; Kwok, Hui Si; Lue, Nicholas Z.; Gosavi, Pallavi M.; Tanner, David A.; Garcia, Emma M.; Lee, Ceejay; Liau, Brian B.#

eLife 2023
Publication • Preprint • Tweetorial
‍ ‍

Systematic identification of anticancer drug targets reveals a nucleus-to-mitochondria ROS-sensing pathway

Zhang, Junbing#; Simpson, Claire M.; Berner, Jacqueline; Chong, Harrison B.; Fang, Jiafeng; Ordulu, Zehra; Weiss-Sadan, Tommy; Possemato, Anthony P.; Harry, Stefan; Takahashi, Mariko; Yang, Tzu-yi; Richter, Marianne; Patel, Himani; Smith, Abby E.; Carlin, Alexander D.; Hubertus de Groot, Adriaan F.; Wolf, Konstantin; Shi, Lei; Wei, Ting-Yu; Dürr, Benedikt R.; Chen, Nicholas J.; Vornbäumen, Tristan; Wichmann, Nina O.; Mahamdeh, Mohammed S.; Pooladanda, Venkatesh; Matoba, Yusuke; Kumar, Shaan; Kim, Eugene; Bouberhan, Sara; Oliva, Esther; Rueda, Bo R.; Soberman, Roy J.; Bardeesy, Nabeel; Liau, Brian B.; Lawrence, Michael; Stokes, Matt P.; Beausoleil, Sean A.; Bar-Peled, Liron#

Cell 2023
Publication
‍ ‍

Chromatin complex dependencies reveal targeting opportunities in leukemia

Najm, Fadi J.; DeWeirdt, Peter; Moore, Molly M.; Bevill, Samantha M.; El Farran, Chadi A.; Macias, Kevin A.; Hegde, Mudra; Waterbury, Amanda L.; Liau, Brian B.; van Galen, Peter; Doench, John G.; Bernstein, Bradley E.#

Nature Communications 2023
Publication
‍ ‍

2022

Base editor scanning charts the DNMT3A activity landscape

Lue, Nicholas Z.; Garcia, Emma M.; Ngan, Kevin C.; Lee, Ceejay; Doench, John G.; Liau, Brian B.#

Nature Chemical Biology 2022
Publication • Preprint • Tweetorial
‍ ‍

CRISPR-suppressor scanning for systematic discovery of drug-resistance mutations

Ngan, Kevin C.*; Lue, Nicholas Z.*; Lee, Ceejay; Liau, Brian B.#

Current Protocols 2022
Publication
‍ ‍

Polycomb-lamina antagonism partitions heterochromatin at the nuclear periphery

Siegenfeld, Allison P.*; Roseman, Shelby A.*; Roh, Heejin; Lue, Nicholas Z.; Wagen, Corin C.; Zhou, Eric; Johnstone, Sarah E.; Aryee, Martin J.#; Liau, Brian B.#

Nature Communications 2022
Publication • Preprint • Tweetorial
‍ ‍

Profiling the landscape of drug resistance mutations in neosubstrates to molecular glue degraders

Gosavi, Pallavi M.*; Ngan, Kevin C.*; Yeo, Megan J.R.; Su, Cindy; Li, Jiaming; Lue, Nicholas Z.; Hoenig, Samuel M.; Liau, Brian B.#

ACS Central Science 2022
Publication • Preprint • Tweetorial • ACS Central Science First Reactions
‍ ‍

2021

Discovering new biology with drug-resistance alleles

Freedy, Allyson M.; Liau, Brian B.#

Nature Chemical Biology 2021 • Review
Publication
‍ ‍

Discovery of C13-aminobenzoyl cycloheximide derivatives that potently inhibit translation elongation

Koga, Yumi*; Hoang, Eileen M.*; Park, Yongho; Keszei, Alexander F.A.; Murray, Jason; Shao, Sichen**; Liau, Brian B.#

Journal of the American Chemical Society 2021
Publication • Synfacts
‍ ‍

2020

Gain-of-function genetic alterations of G9a drive oncogenesis

Kato, S., Weng, Q.Y., Insco, M.L., Chen, K.Y., Muralidhar, S., Pozniak, J., Diaz, J.M.S., Drier, Y., Nguyen, N., Lo, J.A., van Rooijen, E., Kemeny, L.V., Zhan, Y., Feng, Y., Silkworth, W., Powell, C.T., Liau, B.B., Xiong, Y., Jin, J., Newton-Bishop, J., Zon, L.I., Bernstein, B.E., Fisher, D.E.

Cancer Discovery 2020
Publication
‍ ‍

2019

A versatile synthetic route to cycloheximide and analogues that potently inhibit translation elongation

Park, Yongho; Koga, Yumi; Su, Cindy; Waterbury, Amanda L.; Johnny, Christopher L.; Liau, Brian B.#

Angewandte Chemie International Edition 2019 | Publication
‍ ‍

Taking a STAP at core promoter–transcriptional cofactor specificity

Siegenfeld, Allison P.*; Lee, Ceejay*; Liau, Brian B.#

Biochemistry 2019 • Invited Commentary
Publication
‍ ‍

CRISPR-suppressor scanning reveals a nonenzymatic role of LSD1 in AML

Vinyard, Michael E.*; Su, Cindy*; Siegenfeld, Allison P.*; Waterbury, Amanda L.*; Freedy, Allyson M.*; Gosavi, Pallavi M.*; Park, Yongho; Kwan, Eugene E.; Senzer, Benjamin D.; Doench, John G.; Bauer, Daniel E.; Pinello, Luca; Liau, Brian B.#

Nature Chemical Biology 2019
Publication
‍ ‍

2017

Uncovering the cellular target of agelastatin A

Park, Yongho; Liau, Brian B.#

Cell Chemical Biology 2017 • Invited Commentary
Publication
‍ ‍

Transcription elongation factors represent in vivo cancer dependencies in glioblastoma

Miller, T.E., Liau, B.B., Wallace, L.C., Morton, A.R., Xie, Q., Dixit, D., Factor, D.C., Kim, L.Y.J., Morrow, J.J., Wu, Q., Mack, S.C., Hubert, C.G., Gillespie, S.M., Flavahan, W.A., Hoffmann, T., Thummalapalli, R., Hemann, M.T., Paddison, P.J., Horbinski, C.M., Zuber, J., Scacheri, P.C., Bernstein, B.E., Tesar, P.J., Rich, J.N.#

Nature 2017
Publication
‍ ‍

Adaptive chromatin remodeling drives glioblastoma stem cell plasticity and drug tolerance

Liau, B.B.*, Sievers, C.*, Donohue, L.K., Gillespie, S.M., Flavahan, W.A., Miller, T.E., Venteicher, A.S., Hebert, C.H., Carey, C.D., Rodig, S.J., Shareef, S.J., Najm, F.J., van Galen, P., Wakimoto, H., Cahill, D.P., Rich, J.N., Aster, J.C., Suvà, M.L., Patel, A.P.#, Bernstein, B.E.#

Cell Stem Cell 2017
Publication
‍ ‍

Prior to Liau Lab

RBPJ maintains brain tumor-initiating cells through CDK9-mediated transcriptional elongation

Xie, Q., Wu, Q., Kim., L., Miller, T.E., Liau, B.B., Mack, S.C., Yang, K., Factor, D.C., Fang, X., Huang, Z., Zhou, W., Alazem, K., Wang, X., Bernstein, B.E., Bao, S., Rich, J.N#

Journal of Clinical Investigation 2016
Publication
‍ ‍

Insulator dysfunction and oncogene activation in IDH mutant gliomas

Flavahan, W.A.*, Drier, Y.*, Liau, B.B., Gillespie, S.M., Venteicher, A.S., Stemmer-Rachamimov, A.O., Suvà, M.L., Bernstein, B.E.#

Nature 2016
Publication • Nature News and Views
‍ ‍

A multiplexed system for quantitative comparisons of chromatin landscapes

van Galen, P., Viny, A.D., Ram, O., Ryan, R.J.H., Cotton, M.J., Donohue, L., Sievers, C., Drier, Y., Liau, B.B., Gillespie, S.M., Carroll, K.M., Cross, M.B., Levine, R.L., Bernstein, B.E.#

Molecular Cell 2016
Publication
‍ ‍

Mediator kinase inhibition further activates super-enhancer-associated genes in AML

Pelish, H.E.*, Liau, B.B.*, Nitulescu, I.I., Tangpeerachaikul, A., Poss, Z.C., Da Silva, D.H., Caruso, B.T., Arefolov, A., Fadeyi, O., Christie, A.L., Du, K., Banka, D., Schneider, E.V., Jestel, A., Zou, G., Si, C., Ebmeier, C.C., Bronson, R.T., Krivtsov, A.V., Myers, A.G., Kohl, N.E., Kung, A.L., Armstrong, S.A., Lemieux, M.E., Taatjes, D.J., Shair, M.D.#

Nature 2015
Publication
‍ ‍

A unified strategy for the synthesis of 7-membered-ring-containing Lycopodium alkaloids

Lee, A.S., Liau, B.B., Shair, M.D.#

Journal of the American Chemical Society 2014
Publication
‍ ‍

Total syntheses of HMP-Y1, hibarimicinone, and HMP-P1

Liau, B.B., Milgram, B.C., Shair, M.D.#

Journal of the American Chemical Society 2012
Publication
‍ ‍

Gram-scale synthesis of the A'B'-subunit of angelmicin B

Milgram, B.C., Liau, B.B., Shair, M.D.#

Organic Letters 2011
Publication
‍ ‍

Total synthesis of (+)-fastigiatine

Liau, B.B., Shair, M.D.#

Journal of the American Chemical Society 2010
Publication • Nature Chemistry News and Views
‍ ‍

A study of the effect of Z- and E-olefinic geometry on the rates of ring closure of 13-membered dienes

Liau, B.B., Gnanadesikan, V., Corey, E.J.#

Organic Letters 2008
Publication