PUBLICATIONS AND ABSTRACTS

sy-1425 (tamibarotene), a potent selective rara agonist, induces changes in the transcriptional regulatory circuit of aml cells leading to differentiation

Chris Fiore, Michael R. McKeown, Emily Lee, Matthew L. Eaton, Darren Smith, Kathryn Austgen, Mei Wei Chen, Matthew Guenther, M. Ryan Corces, Ravindra Majeti, Eric Olson and Christian Fritz

AACR Annual Hematologic Malignancies Meeting: Poster Section: 6 (2017).

sy-1425 (tamibarotene), a selective rara agonist, shows synergistic anti-tumor activity with hypomethylating agents in a biomarker selected subset of aml

Michael R. McKeown, Emily Lee, Chris Fiore, Matthew L. Eaton, Christian Fritz and Eric Olson

AACR Annual Meeting: Poster Section: 3, Abstract Number: 3085 (2017).

sy-1425, a selective rarα agonist, induces high levels of cd38 expression in rara-high aml tumors creating a susceptibility to anti-cd38 therapeutic antibody treatment

Kathryn Austgen, Michael R. McKeown, Darren Smith, Emily Lee, Chris Fiore, Matthew L. Eaton, Christian Fritz, Tracey Lodie and Eric Olson

AACR Annual Meeting: Poster Section: 26, Abstract Number: 2644 (2017).

aml patient clustering by super-enhancers reveals an rara associated transcription factor signalling partner

Michael R. McKeown, Matthew L. Eaton,  Chris Fiore, Emily Lee, Kathryn Austgen, Darren Smith, Ryan Corces, Ravindra Majeti and Christian Fritz

AACR Annual Meeting: Poster Section: 20, Abstract Number: 1511 (2017).

sy-1365, a potent and selective cdk7 inhibitor, exhbits promising anti-tumor activity in multiple preclnical models of AGGRESSIVE solid tumors

Shanhu Hu, Nan Ke, Yixuan Ren, Sofija Miljovska, Nisha Rajagopal, Michael McKeown, David Orlando, Kevin Sprott, Yoon Choi, Eric Olson and Christian Fritz 

AACR Annual Meeting: Poster Section: 4, Abstract Number: 1151 (2017).

targeting the transcriptional kinanses cdk12 AND CDK13 IN breast and Ovarian Cancer

Michael Bradley, Kristin Hamman, David Orlando, Shanhu Hu, Jason Marineau, Nan Ke, Sherry Ren, Yoon Choi, Christopher Roberts, Christian Fritz and Eric Olson

AACR Annual Meeting: Poster Section: 4, Abstract Number: 1143 (2017).

super-enhancer landscapes reveal novel epigenomic patient subtypes and druggable dependencies in human aml

Matthew L. Eaton, M. Ryan Corces, Michael R. McKeown, Chris Fiore, Jeremy T. Lopez, Katarzyna Piotrowska, Emily Lee, Mei Wei Chen, Darren Smith, Steven M. Chan, Julie L. Koening, Sarah K. Knutson, Kathryn Austgen, Matt G. Guenther, Dave Orlando, Jakob Loven, Christian Fritz and Ravindra Majeti.

CSHL Systems Biology Meeting: (2017).

Transcriptional Addiction in Cancer

James E. Bradner, Denes Hnisz, and Richard A. Young.

Cell ., doi: http://dx.doi.org/10.1016/j.cell.2016.12.013 (February 9, 2017).

A novel subgroup of estrogen receptor positive breast cancer may benefit from super-enhancer guided patient selection for retinoic acid receptor α agonist treatment

Michael R. McKeown, Chris Fiore, Emily Lee, Matthew L. Eaton, Dave Orlando, Matt G. Guenther, Cindy Collins, Mei Wei Chen, Christian Fritz and Emmanuelle di Tomaso

SABCS Annual Meeting: Session: Treatment: Novel Targets and Targeted Agents, Program Number: P6-11-18 (2016).

sy-1425 (tamibarotene) induces profound transcriptional changes in aml tumors with high retinoic acid receptor alpha

Chris Fiore, Michael McKeown, Emily Lee, Matthew L. Eaton, and Christian Fritz

ASH Annual Meeting: Poster Section: 128, Abstract Number: 1523 (2016).

Clinical pharmacodynamic markers and combinations with sy-1425 (tamibarotene) in a genomically-define subset of non-apl aml

Michael  R. McKeown, Chris Fiore, Emily Lee, Matthew L. Eaton, Kathryn Austgen, Darren Smith and Christian Fritz

ASH Annual Meeting: Poster Section: 128, Abstract Number: 2898 (2016).

Covalent targeting of remote cycteine residues to develop cdk12 and cdk13 inhibitors

Tinghu Zhang, Nicholas Kwiatkowski, Calla M Olson, Sarah E. Dixon-Clarke, Brian J. Abraham, Ann K. Greifenberg, Scott B. Fiacarro, Jonathan M. Elkins, Yanke Liang, Nancy M Hannett, Theresa Manz, Mingfeng Hao, Bartlomiej Bartkowiak, Arno L. Greenlead, Jarrod A Marto, Matthias Geyer, Alex N. Bullock, Richard A. Young, and Nathanael S. Gray.

Nature Chemical Biology., doi: 10,1038/NCHEMBIO.2166 (August 29, 2016).

SUPER-ENHANCER ANALYSIS DEFINES NOVEL AML AND MDS SUB-TYPES

Michael R. McKeown, Emily Lee, Chris Fiore, Matthew L. Eaton, Jeremy Lopez, Ryan Corces-Zimmerman, Ravindra Majeti,  Kristin Stephens, Christian Fritz, and Eric Olson

EHA 21st Congress: Oral Presentation: Hall A3, Abstract Number: s807(June 12, 2016).

FIRST-IN-CLASS CDK7 INHIBITOR, INDUCES ROBUST APOPTOSIS IN ACUTE MYELOID LEUKEMIA AND DEMONSTRATES DURABLE IN VIVO EFFICACY

Yoon Jong Choi, Shanhu Hu, Nan Ke, Yixuan Ren, Jeremy Lopez, Sofija Miljovska, David Orlando, Darby Schmidt, Michael Bradley, Kevin Sprott, Christian Fritz and Eric Olson

EHA 21st Congress: Poster Section: Biology 3, Abstract Number: P558 (2016).

SY-1425 IN GENOMICALLY DEFINED SUBSET OF AML AND MDS PATIENTS

Michael R. McKeown, Emily Lee, Chris Fiore, Matthew L. Eaton, Jeremy Lopez, Ryan Corces-Zimmerman, Ravindra Majeti, Christian Fritz, and Eric Olson

AACR Annual Meeting: Poster Section: 14, Abstract Number: 1187(2016).

CDK7 INHIBITION AS A NOVEL TREATMENT STRATEGY FOR ACUTE LEUKEMIAS

Shanhu Hu, Nan Ke, Yixuan Ren, Jeremy Lopez, Sofija Miljovska, David Orlando, Darby Schmidt, Michael Bradley, Kevin Sprott, Eric Olson, Christian C. Fritz, and Yoon Jong Choi

AACR Annual Meeting: Poster Section: 20, Abstract Number: 4820 (2016).

ACTIVATION OF PROTO-ONCOGENES BY DISRUPTION OF CHROMOSOME NEIGHBORHOODS

Hnisz D. et al.

Science;  doi: 10.1126/science.aad9024 (2016).

TARGETING TRANSCRIPTIONAL DEPENDENCY IN ACUTE MYELOID LEUKEMIA (AML) WITH A COVALENT INHIBITOR OF TRANSCRIPTIONAL KINASE CDK7

Yixuan Ren,  Victoria Brown,  Shanhu Hu,  Jeremy Lopez, Sofija Miljovska, Darby Schmidt, Michael Bradley, Kevin Sprott, Eric Olson, Christian C. Fritz and, Yoon Jong Choi

ASH Annual Meeting: Session: 616, Poster I (2015).


NO DRIVER BEHIND THE WHEEL? TARGETING TRANSCRIPTION IN CANCER

Hector L. Franco, Lee Kraus

Cell; doi:10.1016/j.cell.2015.09.013 (2015).

CDK7-DEPENDENT TRANSCRIPTIONAL ADDICTION IN TRIPLE-NEGATIVE BREAST CANCER

Yuboa Wang, Tinghu Zhang, Nicholas Kwitowski, Brian J. Abraham, Tong Ihn Lee, Shaozhen Xie, Haluk Yuzugulu, Thanh Von, Heyuan Li, Ziao Lin, Daniel G. Stover, Elgene Lim, Zhiagang C. Wang, J.Dirk Iglehart, Richard A. Young, Nathanael S. Gray, Jean J. Zhao

Cell; doi:10.1016/j.cell.2015.08.063 (2015).

TARGETING TRANSCRIPTION FACTORS IN CANCER

Anand S. Bhagwat, Christopher R. Vakoc.

Trends in Cancer; doi:10.1016/j.trecan.2015.07.001 (2015).

SUPER-ENHANCER LANDSCAPES SPECIFY MOLECULAR SUBTYPES AND NOVEL TARGETS IN ACUTE MYELOID LEUKEMIA

Matthew Eaton, Ryan Corces-Zimmerman, Jeremy Lopez, Christian Fritz, Eric Olson, Ravindra Majeti, Jakob Loven.

AACR Annual Meeting: 12.2212.23 (2015).

SUPER-ENHANCERS DEFINE BREAST CANCER SUBCLASSES AND IDENTIFY NOVEL TUMOR CELL VULNERABILITIES

Cindy Collins, Mei Wei Chen, Matthew Eaton, David Orlando, Michael McKeown, Christian Fritz, Eric Olson, Matthew Guenther.

AACR Annual Meeting: 4.3837.20 (2015).

CONVERGENCE OF DEVELOPMENTAL AND ONCOGENIC SIGNALING PATHWAYS AT TRANSCRIPTIONAL SUPER-ENHANCERS

Denes Hnisz, Jurian Schuijers, Charles Y. Lin, Abraham S. Weintraub, Brian J. Abraham, Tong Ihn Lee, James E. Bradner, Richard A. Young.

Molecular Cell; doi: 10.1016/j.molcel.2015.02.014 (2015).

TARGETING TRANSCRIPTIONAL ADDICTIONS IN SMALL CELL LUNG CANCER WITH A COVALENT CDK7 INHIBITOR

Camilla L. Christensen, Nicholas Kwiatkowski, Brian J. Abraham, Julian Carretero, Fatima Al-Shahrour, Tinghu Zhang, Edmond Chipumuro, Grit S. Herter-Sprie, Esra A. Akbay, Abigail Altabef, Jianming Zhang, Takeshi Shimamura, Marzia Capelletti, Jakob B. Reibel, Jillian D. Cavanaugh, Peng Gao, Yan Liu, Signe R. Michaelsen, Hans S. Poulsen, Amir R. Aref, David A. Barbie, James E. Bradner, Rani E. George, Nathanael S. Gray, Richard A. Young, Kwok-Kin Wong.

Cancer Cell; doi: 10.1016/j.cell.2014.10.019 (2014).


 

GENOME-WIDE LOCALIZATION OF SMALL MOLECULES

Anders, L., Guenther, M.G., Qi,J., Fan, Z.P., Marineau, J.J., Rahl, P.B., Loven, J, Sigova, A.A., Smith, W.B., Lee, T.I., Bradner, J.E., and Young, R.A.

Nature Biotechnology; doi:10.1038/nbt.2776 (2013)

DISCOVERY AND CHARACTERIZATION OF SUPER-ENHANCER-ASSOCIATED DEPENDENCIES IN DIFFUSE LARGE B CELL LYMPHOMA

Chapuy,B., McKeown, M.R., Lin, C.Y., Monti, S., Roemer, M.G.M., Qi,J., Rahl, P.B., Sun, H.H., Yeda, K.T., Doench, J.G., Reichert,E., Kung, A.L., Rodig,S.J., Young,R.A., Shipp, M.A., and Bradner, J.E.

Cancer Cell 24:777-790 (2013).

RICHARD YOUNG INVITED NIH SEMINAR: SUPER-ENHANCERS CONTROL CELL IDENTITY AND DISEASE DRIVERS

(2013)

SUPER-ENHANCERS IN THE CONTROL OF CELL IDENTITY AND DISEASE

Hnisz,D., Abraham, B.J., Lee, T.I., Lau, A., Saint-Andre,V., Sigova, A.A., Hoke, H.A., and Young, R.A.

Cell 155: 1-14 (2013).

SELECTIVE INHIBITION OF TUMOR ONCOGENES BY DISRUPTION OF SUPER-ENHANCERS

Lovén, J., Hoke, H.A.,  Lin, C.Y., Lau, A., Orlando, D.A.,  Vakoc, C.R., Bradner, J.E., Lee, T.I., and Young, R.A.

Cell 153: 320-334 (2013).

MASTER TRANSCRIPTION FACTORS AND MEDIATOR ESTABLISH SUPER-ENHANCERS AT KEY CELL IDENTITY GENES

Whyte, W.A., Orlando, D.A., Hsnisz, D., Abraham, B.J., Lin, C.Y., Kagey, M.H.,  Rahl, P.B., Lee, T.I., and Young, R.A.

Cell 153: 307-319 (2013).

TRANSCRIPTIONAL REGULATION AND ITS MISREGULATION IN DISEASE

Lee,T.I., and Young, R.A.

Cell 152: 1237-1251 (2013).


REVISITING GLOBAL GENE EXPRESSION ANALYSIS

Lovén, J., Orlando, D.A., Sigova, A.A., Lin, C.Y., Rahl, P.B., Burge, C.B., Levens, D.L., Lee, T.I., and Young, R.A.

Cell 151: 476-482 (2012).

TRANSCRIPTIONAL AMPLIFICATION IN TUMOR CELLS WITH ELEVATED C-MYC

Lin, C.Y., Lovén, J., Rahl, P.B., Paranal, R.M., Burge, C.B., Bradner, J.E., Lee, T.I., and Young, R.A.

Cell 151: 56-67 (2012).

CONTROL OF THE EMBRYONIC STEM CELL STATE

Young, R.A.

Cell 144: 940-954 (2011).

C-MYC REGULATES TRANSCRIPTIONAL PAUSE RELEASE

Rahl, P.B., Lin, C.Y., Seila, A.C., Flynn, R.A., McCuine, S., Burge, C.B., Sharp, P.A., and Young, R.A.

Cell 141: 432–445 (2010).