All Publications

SELECT-AML-1: PHASE 2 RANDOMIZED TRIAL OF TAMIBAROTENE IN COMBINATION WITH VENETOCLAX AND AZACITIDINE IN ADULT PATIENTS WITH PREVIOUSLY UNTREATED WITH RARA OVEREXPRESSION, WHO ARE INELIGIBLE FOR STANDARD INDUCTION THERAPY

Borate U, et al. SOHO Annual Meeting. 2024
Abstract Number: AML-347

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 2023
DOI 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

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