All Publications
USE OF TAMIBAROTENE, A POTENT AND SELECTIVE RARΑ AGONIST, IN COMBINATION WITH AZACITIDINE IN PATIENTS WITH RELAPSED AND REFRACTORY AML WITH RARA GENE OVEREXPRESSION
Stein E, et al. Leukemia & Lymphoma. AUGUST 2023
DOI: 10.1080/10428194.2023.2243356
ERYTHROID LINEAGE CHROMATIN ACCESSIBILITY MAPS FACILITATE IDENTIFICATION AND VALIDATION OF NFIX AS A FETAL HEMOGLOBIN REPRESSOR
CHAAND M, et al. COMMUNICATIONS BIOLOGY. June 2023DOI 10.1038/S42003-023-05205-4
TOLERABILITY AND PRELIMINARY ACTIVITY OF THE POTENT, SELECTIVE, ORAL CDK7 INHIBITOR SY-5609 IN COMBINATION WITH FULVESTRANT IN PATIENTS WITH ADVANCED HORMONE RECEPTOR-POSITIVE (HR+), HER2- BREAST CANCER (BC)
JURIC D, et al. ASCO ANNUAL MEETING. June 2023
ABSTRACT NUMBER: 3081
PHASE 1/1B STUDY OF SY-5609, A SELECTIVE AND POTENT CDK7 INHIBITOR, IN ADVANCED SOLID TUMORS AND IN 2L/3L PANCREATIC DUCTAL ADENOCARCINOMA (PDAC) IN COMBINATION WITH GEMCITABINE +/- NAB-PACLITAXEL
BASHIR B, et al. ASCO ANNUAL MEETING. June 2023
Abstract Number: 3080
TARGETING RARA OVEREXPRESSION WITH TAMIBAROTENE, A POTENT AND SELECTIVE RARΑ AGONIST, IS A NOVEL APPROACH IN AML
de Botton S, et al. Blood Advances. December 2022
doi: 10.1182/bloodadvances.2022008806
INITIAL RESULTS FROM SELECT-AML-1, A PHASE 2 STUDY OF TAMIBAROTENE IN COMBINATION WITH VENETOCLAX AND AZACITIDINE IN RARA-POSITIVE NEWLY DIAGNOSED AML PATIENTS INELIGIBLE FOR STANDARD INDUCTION CHEMOTHERAPY
Kambhampati S, et al. ASH Annual meeting. 2022
Abstract 1444
AN ORAL AND SELECTIVE CDK12 INHIBITOR DEMONSTRATES ROBUST ANTI-TUMOR ACTIVITY
HU S, et al. AACR ANNUAL MEETING. 2022
ABSTRACT NUMBER: 5392
SY-5609, A POTENT AND SELECTIVE CDK7 INHIBITOR, POTENTIATES BTK INHIBITOR ACTIVITY IN MANTLE CELL LYMPHOMA PRECLINICAL MODELS
JOHANNESSEN L, et al. ASH ANNUAL MEETING. 2021
Abstract Number: 1205
DISCOVERY OF SY-5609: A SELECTIVE, NONCOVALENT INHIBITOR OF CDK7
MARINEAU j, et al. J of Medicinal Chemistry. November 2021
DOI: 10.1021/acs.jmedchem.1c01171
TOLERABILITY AND PRELIMINARY CLINICAL ACTIVITY OF SY-5609, A HIGHLY POTENT AND SELECTIVE ORAL CDK7 INHIBITOR, IN PATIENTS WITH ADVANCED SOLID TUMORS
Sharma M, et al. ESMO congress. 2021
Oral Presentation
Abstract Number: 518MO
SY-5609, A HIGHLY POTENT AND SELECTIVE ORAL CDK7 INHIBITOR, EXHIBITS ROBUST ANTITUMOR ACTIVITY IN PRECLINICAL MODELS OF KRAS MUTANT CANCERS AS A SINGLE AGENT AND IN COMBINATION WITH CHEMOTHERAPY
Henry S, et al. ESMO Congress. 2021
Abstract Number: 13P
PRECLINICAL EVALUATION OF INTERMITTENT DOSING REGIMENS ON ANTITUMOR AND PD ACTIVITY OF SY-5609, A POTENT AND SELECTIVE ORAL CDK7 INHIBITOR, IN OVARIAN CANCER XENOGRAFTS
Johannessen L, et al. ESMO Congress. 2021
Abstract Number: 14P
SELECTION OF RARA-POSITIVE NEWLY DIAGNOSED UNFIT AML PATIENTS WITH ELEVATED RARA GENE EXPRESSION ENRICHES FOR FEATURES ASSOCIATED WITH PRIMARY RESISTANCE TO VENETOCLAX AND CLINICAL RESPONSE TO SY‑1425, A POTENT AND SELECTIVE RARΑ AGONIST, PLUS AZACITIDINE
Fiore C, et al. ASH annual meeting. 2020
Abstract Number: 137323
EARLY EVIDENCE OF DOSE-DEPENDENT PHARMACODYNAMIC ACTIVITY FOLLOWING TREATMENT WITH SY-5609, A HIGHLY SELECTIVE AND POTENT ORAL CDK7 INHIBITOR, IN PATIENTS WITH ADVANCED SOLID TUMORS
Papadopoulos K, et al. EORTC-NCI-AACR Symposium. 2020
Abstract Number: 180
ORAL ARSENIC TRIOXIDE ORH-2014 PHARMACOKINETIC AND SAFETY PROFILE IN PATIENTS WITH ADVANCED HEMATOLOGIC DISORDERS
RAVANDI F, et al. HAEMATOLOGICA. June 2020
SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, IN COMBINATION WITH AZACITIDINE DEMONSTRATES A HIGH COMPLETE RESPONSE RATE AND A RAPID ONSET OF RESPONSE IN RARA-POSITIVE NEWLY DIAGNOSED UNFIT ACUTE MYELOID LEUKEMIA
de Botton S, et al. ASH Annual Meeting. 2020
Abstract Number: 134600
INITIAL RESULTS FROM A BIOMARKER-DIRECTED PHASE 2 TRIAL OF SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, IN COMBINATION WITH AZACITIDINE IN RELAPSED/REFRACTORY ACUTE MYELOID LEUKEMIA
Stein E, et al. ASH Annual Meeting. 2020
Abstract Number: 134602
ACTIVITY OF SY-5609, AN ORAL, NONCOVALENT, POTENT, AND SELECTIVE CDK7 INHIBITOR, IN PRECLINICAL MODELS OF COLORECTAL CANCER
Johannessen L, et al. ASCO Annual Meeting. 2020
Abstract Number: 3585
FIRST-IN-HUMAN PHASE I STUDY OF SY-5609, AN ORAL, POTENT, AND SELECTIVE NONCOVALENT CDK7 INHIBITOR, IN ADULT PATIENTS WITH SELECT ADVANCED SOLID TUMORS
Papadopoulos K, et al. ASCO Annual Meeting. 2020
Abstract Number: TPS3662
A COMPUTATIONAL MODEL USING THE EPIGENOME AND TRAINED ON CRISPR DROP-OUT SCREENS CAN IDENTIFY ONCOGENIC DEPENDENCIES IN PRIMARY TUMOR SAMPLES
FIORE C, et al. KEYSTONE SYMPOSIA CANCER EPIGENETICS: NEW MECHANISMS AND THERAPEUTIC OPPORTUNITIES. 2020
ABSTRACT NUMBER: 2042
THE INTEGRATOR COMPLEX RNA HYDROLASE INTS11 IS A KEY DEPENDENCY AND THERAPEUTIC TARGET IN 1P36-DELETED CANCERS
D’IPPOLITO a, et al. KEYSTONE SYMPOSIA CANCER EPIGENETICS: NEW MECHANISMS AND THERAPEUTIC OPPORTUNITIES. 2020
ABSTRACT NUMBER: 1047
CDK7 AND CDK12 INHIBITION RESULT IN DISTINCT TRANSCRIPTIONAL EFFECTS
Rajagopal N, et al. Keystone Symposia Cancer Epigenetics: New Mechanisms and Therapeutic Opportunities. 2020
Abstract Number: 2041
CHROMATIN ACCESSIBILITY MAPPING OF PRIMARY ERYTHROID CELL POPULATIONS LEADS TO IDENTIFICATION AND VALIDATION OF NUCLEAR FACTOR I X (NFIX) AS A NOVEL FETAL HEMOGLOBIN (HBF) REPRESSOR
CHAAND M, et al. ASH Annual meeting. 2019
ABSTRACT NUMBER 124337
PRECLINICAL EVALUATION OF PK, PD, AND ANTI-TUMOR ACTIVITY OF THE ORAL, NON-COVALENT, POTENT AND HIGHLY SELECTIVE CDK7 INHIBITOR, SY-5609, PROVIDES RATIONALE FOR CLINICAL DEVELOPMENT IN MULTIPLE SOLID TUMOR INDICATIONS
JOHANNESSEN L, et al. EORTC-NCI-AACR MOLECULAR TARGETS AND CANCER SYMPOSIUM. 2019
ABSTRACT NUMBER: C091
SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, IN COMBINATION WITH AZACITIDINE DEMONSTRATES HIGH RESPONSE RATES AND A RAPID ONSET OF CLINICAL RESPONSES IN RARA-POSITIVE NEWLY DIAGNOSED UNFIT AML
de Botton S, et al. ESH Conference on AML. 2019
Abstract Number: 16081
DISCOVERY AND CHARACTERIZATION OF SY-1365, A SELECTIVE, COVALENT INHIBITOR OF CDK7
Hu S, et al. Cancer Research. May 2019
DOI: 10.1158/0008-5472.CAN-19-0119
SY-5609, AN ORALLY AVAILABLE SELECTIVE CDK7 INHIBITOR, DEMONSTRATES BROAD ANTI-TUMOR ACTIVITY IN VIVO
Hu S, et al. AACR Annual Meeting. 2019
Abstract Number: 4421
PROSPECTIVE IDENTIFICATION OF RB PATHWAY ALTERATIONS PREDICT RESPONSE TO SY-1365, A SELECTIVE CDK7 INHIBITOR, IN A PANEL OF HIGH-GRADE OVARIAN CANCER PATIENT-DERIVED XENOGRAFT MODELS
Ke N, et al. AACR Annual Meeting. 2019
Abstract Number: 4409
INHIBITION OF CDK7 OVERCOMES RESISTANCE TO CDK4/6 INHIBITORS IN HORMONE RECEPTOR POSITIVE BREAST CANCER CELLS
Guarducci C, et al. San Antonio Breast Cancer Symposium. 2018
Abstract Number 1008
EARLY RESULTS FROM A BIOMARKER-DIRECTED PHASE 2 TRIAL OF SY-1425 IN COMBINATION WITH AZACITIDINE OR DARATUMUMAB IN NON-APL ACUTE MYELOID LEUKEMIA (AML) AND MYELODYSPLASTIC SYNDROME (MDS)
Cook R, et al. ASH Annual Meeting. 2018
Abstract Number 2735
SUPER-ENHANCER LANDSCAPES OF OVARIAN CANCER REVEAL NOVEL EPIGENOMIC SUBTYPES AND TARGETS
Eaton ML, et al. EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium. 2018
Abstract Number 400
PROOF-OF-MECHANISM BASED ON TARGET ENGAGEMENT AND MODULATION OF GENE EXPRESSION FOLLOWING TREATMENT WITH SY-1365, A FIRST-IN-CLASS SELECTIVE CDK7 INHIBITOR IN PHASE 1 PATIENTS WITH ADVANCED CANCER
Juric D, et al. EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium. 2018
Abstract Number 11
SY-1365, A SELECTIVE CDK7 INHIBITOR, ENHANCES CARBOPLATIN ACTIVITY IN OVARIAN CANCER CELL LINES AND XENOGRAFTS, AND INHIBITS EFFECTORS OF HOMOLOGOUS RECOMBINATION REPAIR
Johannessen L, et al. EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium. 2018
Abstract Number 50
ANTITUMOR SYNERGY WITH SY-1425, A SELECTIVE RARα AGONIST, AND HYPOMETHYLATING AGENTS IN RETINOIC ACID RECEPTOR PATHWAY ACTIVATED MODELS OF ACUTE MYELOID LEUKEMIA
McKeown M, et al. Emmanuelle di Tomaso Haematologica. October 2018
DOI: 10.3324/haematol.2018.192807
TRIAL DESIGN OF A FIRST-IN-HUMAN PHASE 1 EVALUATION OF SY-1365, A FIRST-IN-CLASS SELECTIVE CDK7 INHIBITOR, WITH INITIAL EXPANSIONS IN OVARIAN AND BREAST CANCER
Shapiro G, et al. ASCO Annual Meeting. 2018
Abstract Number TPS2600
SY-1365, A SELECTIVE CDK7 INHIBITOR, EXHIBITS POTENT ANTI-TUMOR ACTIVITY AGAINST OVARIAN CANCER MODELS IN VITRO AND IN VIVO
Konstantinopoulos P, et al. AACR Annual Meeting. 2018
Abstract Number: 1525
SY-1365, A SELECTIVE CDK7 INHIBITOR, EXHIBITS POTENT ANTI-TUMOR ACTIVITY AGAINST OVARIAN CANCER MODELS IN VITRO AND IN VIVO
Konstantinopoulos P, et al. AACR Annual Meeting. 2018
Abstract Number: 1525
SY-1365, A POTENT AND SELECTIVE CDK7 INHIBITOR, EXHIBITS ANTI-TUMOR ACTIVITY IN PRECLINICAL MODELS OF HEMATOLOGIC MALIGNANCIES AND DEMOSTRATES INTERACTIONS WITH THE BCLXL/BCL2 MITOCHONDRIAL APOPTOSIS SIGNALING PATHWAY IN LEUKEMIA
Hodgson G, et al. ASH Annual Meeting. 2017
Abstract Number: 2651
EARLY RESULTS FROM A BIOMARKER-DIRECTED PHASE 2 TRIAL OF SY-1425 IN ACUTE MYELOID LEUKEMIA (AML) AND MYELODYSPLASTIC SYNDROME (MDS) DEMONSTRATE DHRS3 INDUCTION AND MYELOID DIFFERENTIATION FOLLOWING SY-1425 TREATMENT
Jurcic J, et al. ASH Annual Meeting. 2017.
Abstract Number: 2633
EPIGENOMIC ANALYSIS OF CANCER STEM CELL (CSC)-ENRICHED TRIPLE-NEGATIVE BREAST CANCER (TNBC) POPULATIONS REVEALS GENE REGULATORY CIRCUITRY AND NOVEL TUMOR CELL VULNERABILITIES
Guenther M, et al. San Antonio Breast Cancer Symposium. 2017
Abstract Number: 1548
BCL2L1 (BCLXL) EXPRESSION AND MYC SUPER-ENHANCER POSITIVITY PREDICT SENSITIVITY TO THE COVALENT CDK7 INHIBITOR SY-1365 IN TRIPLE NEGATIVE BREAST CANCER (TNBC) CELL LINES
Rajagopal N, et al. San Antonio Breast Cancer Symposium. 2017
Abstract Number: 1343
PK/PD MODELING OF THE FIRST-IN-CLASS, POTENT AND SELECTIVE COVALENT CDK7 INHIBITOR, SY-1365, PROVIDES MECHANISTIC BASIS FOR INTERMITTENT DOSING REGIMENS IN PRECLINICAL EFFICACY MODELS OF HEMATOLOGICAL AND SOLID TUMORS
Waters N, et al. AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Conference. 2017
Abstract Number: B171
CHARACTERIZING THE EPIGENETIC LANDSCAPE IDENTIFIES PUTATIVE THERAPEUTIC TARGETS IN THE PANCREATIC CANCER CHIMERA
Sood D, et al. American College Surgeons. 2017
SUPPRESSION OF ADAPTIVE RESPONSES TO TARGETED CANCER THERAPY BY TRANSCRIPTIONAL REPRESSION
Rusan M, et al. Cancer Discovery. October 2017.
DOI: 10.1158/2159-8290.CD-17-0461
RARA PATHWAY ACTIVATION BIOMARKERS IN STUDY SY-1425-201 DEFINE A NEW SUBSET OF AML AND MDS PATIENTS AND CORRELATE WITH MYELOID DIFFERENTIATION FOLLOWING EX VIVO SY-1425 TREATMENT
Vigil C, et al. ESH Conference on AML. 2017
Abstract Number: 8882
TARGETING THE NONCODING GENOME: SUPERENHANCERS MEET THEIR KRYPTONITE
Wang E, Aifantis I. Cancer Discovery. 2017
DOI: 10.1158/2159-8290.CD-17-0860
PHARMACODYNAMIC AND PHARMACOKINETIC EVALUATION OF SY-1425 (TAMIBAROTENE) IN BIOMARKER-SELECTED ACUTE MYELOID LEUKEMIA (AML) AND MYELODYSPLASTIC SYNDROME (MDS) PATIENTS
Bixby D, et al. ESMO Congress. 2017
Abstract Number: 1032P
A PHASE 1 STUDY OF SY-1365, A SELECTIVE CDK7 INHIBITOR, IN ADULT PATIENTS WITH ADVANCED SOLID TUMORS
Tolcher A, et al. ESMO Congress. 2017
Abstract Number: 425TiP
A BIOMARKER-DIRECTED PHASE 2 STUDY OF SY-1425, A SELECTIVE RETINOIC ACID RECEPTOR ALPHA AGONIST, IN ADULT PATIENTS WITH ACUTE MYELOID LEUKEMIA (AML) OR MYELODYSPLASTIC SYNDROME (MDS)
Cook R, et al. ASCO Annual Meeting. 2017
Abstract Number: TPS7071
SUPER-ENHANCER ANALYSIS DEFINES NOVEL EPIGENOMIC SUBTYPES OF NON-APL AML INCLUDING AN RARΑ DEPENDENCY TARGETABLE BY SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST
McKeown M. Et al.
Cancer Discovery
doi: 10.1158/2159-8290.CD-17-0399
2017
MECHANISTICALLY INFORMED COMBINATIONS OF SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, WITH HYPOMETHYLATING OR ANTI-CD38 TARGETED AGENTS IN AML AND MDS
McKeown M, et al. EHA. 2017
Abstract Number: P188
SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, REPROGRAMS AML CELLS FOR DIFFERENTIATION ALONG DISTINCT LINEAGES, UNCOVERING PD MARKERS FOR CLINICAL STUDIES
McKeown M, et al. EHA. 2017
Abstract Number: E884
THE EPIGENETIC LANDSCAPE OF T CELL SUBSETS IN SLE IDENTIFIES KNOWN AND POTENTIAL NOVEL DRIVERS OF THE AUTOIMMUNE RESPONSE
Karman J, et al. FOCIS Annual Meeting. June 2017.
Abstract Number: 319030
SY-1425 (TAMIBAROTENE), A POTENT SELECTIVE RARA AGONIST, INDUCES CHANGES IN THE TRANSCRIPTIONAL REGULATORY CIRCUIT OF AML CELLS LEADING TO DIFFERENTIATION
Fiore C, et al. AACR Annual Hematologic Malignancies Meeting. 2017
Poster Section: 6
EPIGENOMIC ANALYSIS OF PRIMARY BREAST CANCER TUMORS REVEALS NOVEL TUMOR CELL VULNERABILITIES AND THERAPEUTIC TARGETS
Guenther M, et al. IMPAKT Breast Cancer Conference. 2017
Abstract Number: 47P
SY-1425 (TAMIBAROTENE), A SELECTIVE RARA AGONIST, SHOWS SYNERGISTIC ANTI-TUMOR ACTIVITY WITH HYPOMETHYLATING AGENTS IN A BIOMARKER SELECTED SUBSET OF AML
McKeown M, et al. AACR Annual Meeting. 2017
Abstract Number: 3085
SY-1425, A SELECTIVE RARA AGONIST, INDUCES HIGH LEVELS OF CD38 EXPRESSION IN RARA-HIGH AML TUMORS CREATING A SUSCEPTIBILITY TO ANTI-CD38 THERAPEUTIC ANTIBODY TREATMENT
Austgen K, et al. AACR Annual Meeting. 2017
Poster Section: 26, Abstract Number: 2644
AML PATIENT CLUSTERING BY SUPER-ENHANCERS REVEALS AN RARA ASSOCIATED TRANSCRIPTION FACTOR SIGNALLING PARTNER
McKeown M, et al. AACR Annual Meeting. 2017
Poster Section: 20, Abstract Number: 1511
SY-1365, A POTENT AND SELECTIVE CDK7 INHIBITOR, EXHBITS PROMISING ANTI-TUMOR ACTIVITY IN MULTIPLE PRECLNICAL MODELS OF AGGRESSIVE SOLID TUMORS
Hu S, et al. AACR Annual Meeting. 2017
Poster Section: 4, Abstract Number: 1151
TARGETING THE TRANSCRIPTIONAL KINASES CDK12 AND CDK13 IN BREAST AND OVARIAN CANCER
Bradley M, et al. AACR Annual Meeting. 2017
Poster Section: 4, Abstract Number: 1143
SUPER-ENHANCER LANDSCAPES REVEAL NOVEL EPIGENOMIC PATIENT SUBTYPES AND DRUGGABLE DEPENDENCIES IN HUMAN AML
Eaton M, et al. CSHL Systems Biology Meeting. 2017
TRANSCRIPTIONAL ADDICTION IN CANCER
Bradner J, et al. Cell. February 2017
doi: http://dx.doi.org/10.1016/j.cell.2016.12.013
A NOVEL SUBGROUP OF ESTROGEN RECEPTOR POSITIVE BREAST CANCER MAY BENEFIT FROM SUPER-ENHANCER GUIDED PATIENT SELECTION FOR RETINOIC ACID RECEPTOR ALPHA AGONIST TREATMENT
McKeown M, et al. SABCS Annual Meeting. 2016
Program Number: P6-11-18
SY-1425 (TAMIBAROTENE) INDUCES PROFOUND TRANSCRIPTIONAL CHANGES IN AML TUMORS WITH HIGH RETINOIC ACID RECEPTOR ALPHA
Fiore C, et al. ASH Annual Meeting. 2016
Poster Section: 128, Abstract Number: 1523
CLINICAL PHARMACODYNAMIC MARKERS AND COMBINATIONS WITH SY-1425 (TAMIBAROTENE) IN A GENOMICALLY-DEFINE SUBSET OF NON-APL AML
McKeown M, et al. ASH Annual Meeting. 2016
Poster Section: 128, Abstract Number: 2898
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
AN ORAL AND SELECTIVE CDK7 INHIBITOR DEMONSTRATES SUBSTANTIAL ANTI-TUMOR EFFECT IN BREAST AND OVARIAN CANCER MODELS
Shanhu Hu, Jason Marineau, Michael Bradley, Kristin Hamman, Sydney Alnemy, Danielle Smith, John Carulli, Claudio Chuaqui
30th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium
Abstract Number 96
2018
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
Ren Y, et al. ASH Annual Meeting. 2015
Session: 616, Poster I
NO DRIVER BEHIND THE WHEEL? TARGETING TRANSCRIPTION IN CANCER
Franco H, Kraus L. Cell. 2015
doi:10.1016/j.cell.2015.09.013
CDK7-DEPENDENT TRANSCRIPTIONAL ADDICTION IN TRIPLE-NEGATIVE BREAST CANCER
Wang Y, et al. Cell. 2015
doi:10.1016/j.cell.2015.08.063
TARGETING TRANSCRIPTION FACTORS IN CANCER
Bhagwat A, Vakoc C. Trends in Cancer. 2015
doi:10.1016/j.trecan.2015.07.001
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
QUANTITATIVE CHIP-SEQ NORMALIZATION REVEALS GLOBAL MODULATION OF THE EPIGENOME
David A. Orlando, Mei Wei Chen, Victoria E. Brown, Snehakumari Solanki, Yoon J. Choi, Eric R. Olson,
Christian C. Fritz, James E. Bradner, and Matthew G. Guenther
Cell Reports, Volume 9, Issue 3, 1163 - 1170
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
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2010