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

EYTAN M. STEIN, STEPHANE DE BOTTON, THOMAS CLUZEAU, ARNAUD PIGNEUX, JANE L. LIESVELD, RACHEL J. COOK, PHILIPPE ROUSSELOT, DAVID A. RIZZIERI, THORSTEN BRAUN, GAIL J. ROBOZ, DELPHINE LEBON, MAEL HEIBLIG, KRISTEN BAKER, ANGELA VOLKERT, SOFIA PAUL, NISHA RAJAGOPAL, DAVID A. ROTH, MICHAEL KELLY & PIERRE PETERLIN
LEUKEMIA & LYMPHOMA
DOI: 10.1080/10428194.2023.2243356
AUGUST 2023

ERYTHROID LINEAGE CHROMATIN ACCESSIBILITY MAPS FACILITATE IDENTIFICATION AND VALIDATION OF NFIX AS A FETAL HEMOGLOBIN REPRESSOR

MUDIT CHAAND, CHRIS FIORE, BRIAN JOHNSTON, ANTHONY D’IPPOLITO, DIANE H. MOON, JOHN P. CARULLI, JEFFREY R. SHEARSTONE
COMMUNICATIONS BIOLOGY: DOI 10.1038/S42003-023-05205-4
2023

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)

DEJAN JURIC, DEBRA L. RICHARDSON, BABAR BASHIR, MANISH SHARMA, KYRIAKOS P. PAPADOPOULOS, SARA MATHEWS, GRAEME HODGSON, SUSAN HENRY, SOFIA PAUL, TERENCE HALL, DAVID A. ROTH, MICHAEL KELLY, TANYA ABDUL MALAK, VIRGINIA KLIMEK

ASCO ANNUAL MEETING
ABSTRACT NUMBER: 3081
JUNE 2023

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

BABAR BASHIR, MANISH SHARMA, DEJAN JURIC, KYRIAKOS P. PAPADOPOULOS, ERIKA P. HAMILTON, DEBRA L. RICHARDSON, GEOFFREY SHAPIRO, VAIBHAV SAHAI, NIHARIKA B. METTU, ZEV A. WAINBERG, OLATUNJI B. ALESE, TOMISLAV DRAGOVICH, GRAEME HODGSON, SUSAN HENRY, TERENCE HALL, SOFIA PAUL, DAVID A. ROTH, MICHAEL KELLY, TANYA ABDUL MALAK, VIRGINIA KLIMEK

ASCO ANNUAL MEETING
ABSTRACT NUMBER: 3080
JUNE 2023

TARGETING RARA OVEREXPRESSION WITH TAMIBAROTENE, A POTENT AND SELECTIVE RARΑ AGONIST, IS A NOVEL APPROACH IN AML

Stéphane de Botton, Thomas Cluzeau, Carlos Enrique Vigil, Rachel Cook, Philippe Rousselot, David A Rizzieri, Jane L Liesveld, Pierre Fenaux, Thorsten Braun, Anne Banos, Joseph G. Jurcic, Mikkael A. Sekeres, Michael R. Savona, Gail J. Roboz, Dale Bixby, Kate Madigan, Angela Volkert, Kristin Stephens, Qing Kang-Fortner, Kristen Baker, Sofia Paul, Michael Robert McKeown, John P Carulli, Matthew Lucas Eaton, Graeme Hodgson, Christopher Fiore, Michael Kelly, David A. Roth, Eytan M. Stein
Blood Advances
doi: 10.1182/bloodadvances.2022008806
December 2022

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

Suman Kambhampati, Christine McMahon, Alireza Eghtedar, Daniel Pollyea, Stephane de Botton, Arnaud Pigneux, Mohamad Cherry, Brian Ball, Gautam Borthakur, Thomas Cluzeau, Gary Schiller, Beibei Hu, Angela Volkert, Joanie Aasen Gausman, Graeme Hodgson, David A. Roth, Erica Warlick, Michael J. Kelly, Eytan M. Stein
64th American Society of Hematology (ASH) Annual Meeting
Abstract 1444
2022

AN ORAL AND SELECTIVE CDK12 INHIBITOR DEMONSTRATES ROBUST ANTI-TUMOR ACTIVITY

SHANHU HU, DAVID MOEBIUS, WOJCIECH DWORAKOWSKI, ELLIOT COOPER, DEREK LAPLACA, SYDNEY ALNEMY, PHONE PERERA, JASON MARINEAU, CLAUDIO CHUAQUI, JOHN CARULLI, ERIC OLSON
AMERICAN ASSOCIATION FOR CANCER RESEARCH (AACR) ANNUAL MEETING 2022
ABSTRACT NUMBER: 5392
2022

SY-5609, A POTENT AND SELECTIVE CDK7 INHIBITOR, POTENTIATES BTK INHIBITOR ACTIVITY IN MANTLE CELL LYMPHOMA PRECLINICAL MODELS

LIV JOHANNESSEN, PRIYANKA SAWANT, ANTHONY D’IPPOLITO, NAN KE, ARIEL LEFKOVITH, MATTHEW EATON, WOJCIECH DWORAKOWSKI, MARIA ROSARIO, SUSAN HENRY, GRAEME HODGSON
63RD AMERICAN SOCIETY OF HEMATOLOGY (ASH) ANNUAL MEETING
Abstract Number: 1205
2021

DISCOVERY OF SY-5609: A SELECTIVE, NONCOVALENT INHIBITOR OF CDK7

JASON J. MARINEAU, KRISTIN B. HAMMAN, SHANHU HU, SYDNEY ALNEMY, JANESSA MIHALICH, ANZHELIKA KABRO, KENNETH MATTHEW WHITMORE, DANA K. WINTER, STEPHANIE ROY, STEPHANIE CIBLAT, NAN KE, ANNELI SAVINAINEN, ASHRAF WILSILY, GORAN MALOJCIC, ROBERT ZAHLER, DARBY SCHMIDT, MICHAEL J. BRADLEY, NIGEL J. WATERS, CLAUDIO CHUAQUI
DOI: 10.1021/acs.jmedchem.1c01171
November 2021

TOLERABILITY AND PRELIMINARY CLINICAL ACTIVITY OF SY-5609, A HIGHLY POTENT AND SELECTIVE ORAL CDK7 INHIBITOR, IN PATIENTS WITH ADVANCED SOLID TUMORS

Manish R. Sharma, Babar Bashir, Erika Hamilton, Dejan Juric, Kyriakos Papadopoulos, Debra Richardson, Geoffrey Shapiro, Graeme Hodgson, Nan Ke, Anthony D’Ippolito, Susan Henry, Li Zhu, Maria Rosario, Hina Jolin, David Roth, Virginia Klimek, Kate Madigan, Mike Kelly
ESMO Congress 2021
Oral Presentation
Abstract Number: 518MO
2021

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

Susan Henry, Liv Johannessen, Priyanka Sawant, Ariel Lefkovith, Nan Ke, Anthony D’Ippolito, Wojciech Dworakowski, Graeme Hodgson
ESMO Congress 2021
Abstract Number: 13P
2021

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

Liv Johannessen, Wojciech Dworakowski, Maria Rosario, Priyanka Sawant, Nan Ke, Ariel Lefkovith, Anthony D’Ippolito, Matthew Eaton, Susan Henry, Graeme Hodgson
ESMO Congress 2021
Abstract Number: 14P
2021

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

Christopher Fiore, Michael Kelly, Angela Volkert, Li Zhou, Kate Madigan, Matthew Eaton, Graeme Hodgson, David A. Roth, Qing Kang-Fortner
62nd American Society of Hematology (ASH) Annual Meeting
Abstract Number: 137323
2020

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

Kyriakos P. Papadopoulos, Manish R. Sharma, Erika Hamilton, Debra Richardson, Babar Bashir, Dejan Juric, Geoffrey Shapiro, Graeme Hodgson, Nan Ke, Anthony D’Ippolito, Liv Johannessen, Qing Kang-Fortner, Li Zhou, Maria Rosario, William Zamboni, Hina A. Jolin, Catherine Madigan, Michael J. Kelly, David A. Roth
32nd EORTC-NCI-AACR Symposium
Abstract Number: 180
2020

ORAL ARSENIC TRIOXIDE ORH-2014 PHARMACOKINETIC AND SAFETY PROFILE IN PATIENTS WITH ADVANCED HEMATOLOGIC DISORDERS

FARHAD RAVANDI, IPHIGENIA KOUMENIS, ANANDHI JOHRI, MARTIN TALLMAN, GAIL J. ROBOZ, STEPHEN STRICKLAND, GUILLERMO GARCIA-MANERO, GAUTAM BORTHAKUR, KIRAN NAQVI, MEGHAN MEYER, MADHU PUDIPEDDI, SIRISH NIDARMARTHY, KRIS VADDI AND HAGOP KANTARJIAN
HAEMATOLOGICA VOL. 105 NO. 6 (2020)
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

Stephane de Botton, Thomas Cluzeau, Carlos E. Vigil, Rachel J. Cook, Philippe Rousselot, David A. Rizzieri, Jane L. Liesveld, Pierre Fenaux, Thorsten Braun, Anne Banos, Michael Savona, Don Park, Michael Kelly, Angela Volkert, Li Zhou, Qing Kang-Fortner, David A. Roth, Eytan M. Stein
62nd American Society of Hematology (ASH) Annual Meeting
Oral Presentation
Abstract Number: 134600
2020

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

Eytan M. Stein, Stephane de Botton, Thomas Cluzeau, Arnaud Pigneux, Jane L. Liesveld, Rachel J. Cook, Philippe Rousselot, David A. Rizzieri, Thorsten Braun, Dale L. Bixby, Gail J. Roboz, Delphine Lebon, Mael Heiblig, Michael Kelly, Angela Volkert, Li Zhou, Qing Kang-Fortner, David A. Roth, Pierre Peterlin 62nd American Society of Hematology (ASH) Annual Meeting
Oral Presentation
Abstract Number: 134602
2020

ACTIVITY OF SY-5609, AN ORAL, NONCOVALENT, POTENT, AND SELECTIVE CDK7 INHIBITOR, IN PRECLINICAL MODELS OF COLORECTAL CANCER

Liv Johannessen, Nan Ke, Priyanka Sawant, Wojciech Dworakowski, Tony D’ippolito, Shanhu Hu, Nisha Rajagopal, Matthew Eaton, Graeme Hodgson
American Society of Clinical Oncology (ASCO20) Virtual Scientific Program
Abstract Number: 3585
2020

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

Kyriakos P. Papadopoulos, Manish R. Sharma, Erika Hamilton, Debra Richardson, Babar Bashir, Graeme Hodgson, Li Zhou, Angela Volkert, Hina A. Jolin, Catherine Madigan, Michael Kelly, David A. Roth
American Society of Clinical Oncology (ASCO20) Virtual Scientific Program
Abstract Number: TPS3662
2020

A COMPUTATIONAL MODEL USING THE EPIGENOME AND TRAINED ON CRISPR DROP-OUT SCREENS CAN IDENTIFY ONCOGENIC DEPENDENCIES IN PRIMARY TUMOR SAMPLES

CHRIS FIORE, MATTHEW L EATON, BRIAN JOHNSTON, MATT GUENTHER, CINDY COLLINS, MEI WEI CHEN, JOHN CARULLI, ERIC OLSON
KEYSTONE SYMPOSIA CANCER EPIGENETICS: NEW MECHANISMS AND THERAPEUTIC OPPORTUNITIES
ABSTRACT NUMBER: 2042
2020

THE INTEGRATOR COMPLEX RNA HYDROLASE INTS11 IS A KEY DEPENDENCY AND THERAPEUTIC TARGET IN 1P36-DELETED CANCERS

ANTHONY D’IPPOLITO, YOGESH CHUTAKE, BENOIT MOREAU, CHRISTINA KOLODZY, DANEYAL FAROUQ, JASON MARINEAU, MATTHEW EATON, KAI-LIEH HUANG, YONG SUNG PARK, REID T. POWELL, CLIFFORD C. STEPHAN, JOHN CARULLI, ERIC R. OLSON , ERIC J. WAGNER, MATTHEW G. GUENTHER
KEYSTONE SYMPOSIA CANCER EPIGENETICS: NEW MECHANISMS AND THERAPEUTIC OPPORTUNITIES
ABSTRACT NUMBER: 1047
2020

CDK7 AND CDK12 INHIBITION RESULT IN DISTINCT TRANSCRIPTIONAL EFFECTS

Nisha Rajagopal, Sydney Alnemy, Anthony D'Ippolito, Jason Marineau, David Moebius, Elliot Cooper, Matthew Eaton, John Carulli, Claudio Chuaqui, Eric Olson, Shanhu Hu
Keystone Symposia Cancer Epigenetics: New Mechanisms and Therapeutic Opportunities
Abstract Number: 2041
2020

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

MUDIT CHAAND, CHRIS FIORE, BRIAN JOHNSTON, DIANE MOON, JOHN CARULLI, JEFF SHEARSTONE
61ST AMERICAN SOCIETY OF HEMATOLOGY (ASH) ANNUAL MEETING AND EXPOSITION
ORAL PRESENTATION
ABSTRACT NUMBER 124337
2019

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

LIV JOHANNESSEN, SHANHU HU, NAN KE, ANTHONY D’IPPOLITO, NISHA RAJAGOPAL, PRIYANKA SAWANT, KRISTIN HAMMAN, JASON MARINEAU, ANNELI SAVINAINEN, WILLIAM ZAMBONI, GRAEME HODGSON
31st EORTC-NCI-AACR MOLECULAR TARGETS AND CANCER SYMPOSIUM
ABSTRACT NUMBER: C091
2019

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

Stephane de Botton, Carlos E. Vigil, Thomas Cluzeau, Jane L. Liesveld, David A. Rizzieri, Tamara K. Moyo, Philippe Rousselot, Anne Banos, Don Park, Eytan M. Stein, Gail J. Roboz, Joseph G. Jurcic, Robert L. Redner, Dale L. Bixby, Jeffrey Baker, Pierre Fenaux, Gabrielle Roth-Guepin, Thorsten Braun, Jorge E. Cortes, Mikkael A. Sekeres, Michael Kelly, Angela Volkert, Li Zhou, Qing Kang, David A. Roth, Rachel J. Cook
European School of Haematology (ESH) Conference on AML
Abstract Number: 16081
2019

DISCOVERY AND CHARACTERIZATION OF SY-1365, A SELECTIVE, COVALENT INHIBITOR OF CDK7

Shanhu Hu, Jason J. Marineau, Nisha Rajagopal, Kristin B. Hamman, Yoon Jong Choi, Darby R. Schmidt, Nan Ke, Liv Johannessen, Michael J. Bradley, David A. Orlando, Sydney R. Alnemy, Yixuan Ren, Stephane Ciblat, Dana K. Winter, Anzhelika Kabro, Kevin T. Sprott, J. Graeme Hodgson, Christian C. Fritz, John P. Carulli, Emmanuelle di Tomaso and Eric R. Olson
Cancer Research
DOI: 10.1158/0008-5472.CAN-19-0119
May 2019

SY-5609, AN ORALLY AVAILABLE SELECTIVE CDK7 INHIBITOR, DEMONSTRATES BROAD ANTI-TUMOR ACTIVITY IN VIVO

Shanhu Hu, Jason Marineau, Kristin Hamman, Michael Bradley, Anneli Savinainen, Sydney Alnemy, John Carulli, Claudio Chuaqui and Eric Olson
American Association for Cancer Research (AACR) Annual Meeting
Abstract Number: 4421
2019

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

Nan Ke, Liv Johannessen, Nisha Rajagopal, David Orlando, John Carulli, Graeme Hodgson
American Association for Cancer Research (AACR) Annual Meeting
Abstract Number: 4409
2019

INHIBITION OF CDK7 OVERCOMES RESISTANCE TO CDK4/6 INHIBITORS IN HORMONE RECEPTOR POSITIVE BREAST CANCER CELLS

Cristina Guarducci, Agostina Nardone, Ariel Feiglin, Ilenia Migliaccio, Luca Malorni, Martina Bonechi, Matteo Benelli, Angelo Di Leo, Graeme Hodgson, Geoffrey I. Shapiro, Rachel Schiff, Myles Brown, Rinath Jeselsohn
San Antonio Breast Cancer Symposium
Abstract Number 1008
2018

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)

Rachel J. Cook, Tamara K. Moyo, Jane L. Liesveld, David A. Rizzieri, Eytan M. Stein, Stephane de Botton, Gail J. Roboz, Mikkael A. Sekeres, Joseph G. Jurcic, Azra Raza, Robert L. Redner, Dale L. Bixby, Jorge E. Cortes, Kristin Stephens, Angela Volkert, Qing Kang, Emmanuelle di Tomaso, David A. Roth, Carlos E. Vigil
60th American Society of Hematology (ASH) Annual Meeting and Exposition
Abstract Number 2735
2018

SUPER-ENHANCER LANDSCAPES OF OVARIAN CANCER REVEAL NOVEL EPIGENOMIC SUBTYPES AND TARGETS

Eaton ML, Johnston B, Piotrowska K, Collins C, Lopez J, Knutson S, di Tomaso E, Carulli J, Olson E 
30th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium
Abstract Number 400
2018

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

Dejan Juric, Kyriakos P. Papadopoulos, Anthony Tolcher, Erika Hamilton, Khanh T. Do, David Orlando, William Zamboni, Graeme Hodgson, Emmanuelle di Tomaso, Kristin Stephens, David A. Roth, Geoffrey I. Shapiro
30th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium
Oral Plenary Session 6
Abstract Number 11
2018

SY-1365, A SELECTIVE CDK7 INHIBITOR, ENHANCES CARBOPLATIN ACTIVITY IN OVARIAN CANCER CELL LINES AND XENOGRAFTS, AND INHIBITS EFFECTORS OF HOMOLOGOUS RECOMBINATION REPAIR

Liv Johannessen, Shanhu Hu, Nan Ke, Nisha Rajagopal, David Orlando, Sydney Alnemy, Anthony D'Ippolito, John Carulli, Emmanuelle di Tomaso, Graeme Hodgson
30th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium
Abstract Number 50
2018

ANTITUMOR SYNERGY WITH SY-1425, A SELECTIVE RARα AGONIST, AND HYPOMETHYLATING AGENTS IN RETINOIC ACID RECEPTOR PATHWAY ACTIVATED MODELS OF ACUTE MYELOID LEUKEMIA

Michael R. McKeown, Liv Johannessen, Emily Lee, Christopher Fiore, Emmanuelle di Tomaso Haematologica
DOI: 10.3324/haematol.2018.192807
October 2018

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

Geoffrey Shapiro, Kyriakos P. Papadopoulos, Khanh T. Do, Dejan Juric, Rinath Jeselsohn, Panagiotis Konstantinopoulos, Ursula Matulonis, Graeme Hodgson, Emmanuelle di Tomaso, Kristin Stephens, David A. Roth, Anthony Tolcher
American Society of Clinical Oncology (ASCO) Annual Meeting 
Abstract Number TPS2600
2018

SY-1365, A SELECTIVE CDK7 INHIBITOR, EXHIBITS POTENT ANTI-TUMOR ACTIVITY AGAINST OVARIAN CANCER MODELS IN VITRO AND IN VIVO

Panagiotis A. Konstantinopoulos, Graeme Hodgson, Nisha Rajagopal, Liv Johannessen, Joyce F. Liu, Paul T. Kirschmeier, Shan Zhou, Cam Anh Tran, Nan Ke, David Orlando, Christian Fritz, Emmanuelle di Tomaso, Ursula A. Matulonis
American Association for Cancer Research (AACR) Annual Meeting: Poster Discussion Session
Abstract Number: 1525
2018

SY-1365, A SELECTIVE CDK7 INHIBITOR, EXHIBITS POTENT ANTI-TUMOR ACTIVITY AGAINST OVARIAN CANCER MODELS IN VITRO AND IN VIVO

Panagiotis A. Konstantinopoulos, Graeme Hodgson, Nisha Rajagopal, Liv Johannessen, Joyce F. Liu, Paul T. Kirschmeier, Shan Zhou, Cam Anh Tran, Nan Ke, David Orlando, Christian Fritz, Emmanuelle di Tomaso, Ursula A. Matulonis
American Association for Cancer Research (AACR) Annual Meeting: Poster Session
Abstract Number: 1525
2018

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

Graeme Hodgson, Liv Johannessen, Nisha Rajagopal, Shanhu Hu, David Orlando, Matthew Eaton, Michael McKeown, Jeffrey Tyner, Stephen Kurtz, Kevin Sprott, Christian Fritz, Emmanuelle di Tomaso
American Society of Hematology Annual Meeting
Abstract Number: 2651
2017

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

Joseph G. Jurcic, Azra Raza, George Vlad, Eytan Stein, Mikhail Roshal, Dale Bixby, Daniel F. Boyer, Carlos E. Vigil, Sergei Syrbu, Mikkael A. Sekeres, Heesun J. Rogers, David Rizzieri, Anand S. Lagoo, Gail Roboz, Robert Redner, David P. Steensma, Rachel Cook, Tamara K. Moyo, Michael Savona, Michael R McKeown, Nigel J. Waters, Kristin Stephens, Angela Volkert, Emmanuelle di Tomaso, David A. Roth, Jorge Cortes
American Society of Hematology Annual Meeting
Abstract Number: 2633
2017

EPIGENOMIC ANALYSIS OF CANCER STEM CELL (CSC)-ENRICHED TRIPLE-NEGATIVE BREAST CANCER (TNBC) POPULATIONS REVEALS GENE REGULATORY CIRCUITRY AND NOVEL TUMOR CELL VULNERABILITIES

Matthew G. Guenther, Arthur W. Lambert, Christopher Fiore, Yogesh Chutake, Mei Wei Chen, David Orlando, Matthew Eaton, Brian Bierie, Robert Weinberg, Christian C. Fritz, Eric Olson
San Antonio Breast Cancer Symposium
Abstract Number: 1548
2017

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

Nisha Rajagopal, Graeme Hodgson, Liv Johannessen, Shanhu Hu, Nan Ke, Michael McKeown, Matthew Guenther, Alex Bush, Christian Fritz, David Orlando, Eric Olson, Emmanuelle di Tomaso
San Antonio Breast Cancer Symposium
Abstract Number: 1343
2017

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

Nigel J. Waters, Shanhu Hu, Brett Matzuka, Graeme Hodgson, Yixuan Ren, Yoon Choi, Kevin Dykstra, Christopher Roberts, Kevin Sprott, Emmanuelle di Tomaso, Christian C. Fritz
AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Conference
Abstract Number: B171
2017

CHARACTERIZING THE EPIGENETIC LANDSCAPE IDENTIFIES PUTATIVE THERAPEUTIC TARGETS IN THE PANCREATIC CANCER CHIMERA

Divya Sood MD, Kathryn Austgen PhD, Chris Fiore PhD, David Orlando PhD, Brian Johnston MS, Sofija Miljovska MS, Cindy Collins MS, Randall French PhD, Yu Shi PhD, Tony Hunter PhD, Tracey Lodie PhD, Andrew Lowy MD
American College Surgeons
2017

SUPPRESSION OF ADAPTIVE RESPONSES TO TARGETED CANCER THERAPY BY TRANSCRIPTIONAL REPRESSION

Maria Rusan, Kapsok Li, Yvonne Li, Camilla L. Christensen, Brian J. Abraham, Nicholas Kwiatkowski, Kevin A. Buczkowski, Bruno Bockorny, Ting Chen, Shuai Li, Kevin Rhee, Haikuo Zhang, Wankun Chen, Hideki Terai, Tiffany Tavares, Alan L. Leggett, Tianxia Li, Yichen Wang, Tinghu Zhang, Tae-Jung Kim, Sook-Hee Hong, Neermala Poudel-Neupane, Michael Silkes, Tenny Mudianto, Li Tan, Takeshi Shimamura, Matthew Meyerson, Adam J. Bass, Hideo Watanabe, Nathanael S. Gray, Richard A. Young, Kwok-Kin Wong and Peter S. Hammerman
Cancer Discovery DOI: 10.1158/2159-8290.CD-17-0461
October 20, 2017

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

Carlos E. Vigil, Joseph Jurcic, Azra Raza, Rachel Cook, Dale Bixby, Mikkael Sekeres, David Rizzieri, Eytan Stein, Robert L. Redner, David Steensma, Gail Roboz, Michael Savona, Michael McKeown, Chris Fiore, Angela Volkert, Curran Murphy, Kristin Stephens, David A. Roth, Emmanuelle di Tomaso, Jorge Cortes.
ESH Conference on AML
Abstract Number: 8882
2017

TARGETING THE NONCODING GENOME: SUPERENHANCERS MEET THEIR KRYPTONITE

Eric Wang and Ioannis Aifantis
Cancer Discovery (7) (10) 1065-1066; DOI: 10.1158/2159-8290.CD-17-0860
October 1, 2017

PHARMACODYNAMIC AND PHARMACOKINETIC EVALUATION OF SY-1425 (TAMIBAROTENE) IN BIOMARKER-SELECTED ACUTE MYELOID LEUKEMIA (AML) AND MYELODYSPLASTIC SYNDROME (MDS) PATIENTS

Dale Bixby, Carlos E. Vigil, Joseph Jurcic, Rachel Cook, Mikkael Sekeres, David Rizzieri, Jorge Cortes, Robert Redner, David Steensma, Gail Roboz, Tamara Moyo, Michael R McKeown, Nigel J. Waters, Kristin Stephens, Emmanuelle di Tomaso, David A. Roth, Eytan Stein
ESMO Congress
Abstract Number: 1032P
2017

A PHASE 1 STUDY OF SY-1365, A SELECTIVE CDK7 INHIBITOR, IN ADULT PATIENTS WITH ADVANCED SOLID TUMORS

Anthony Tolcher, Khanh T. Do, Emmanuelle di Tomaso, Nigel J. Waters, Kristin Stephens, David A. Roth, Geoffrey Shapiro
ESMO Congress
Abstract Number: 425TiP
2017

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)

Rachel Cook, Eytan Stein, David Steensma, Mikkael Sekeres, Dale Bixby, David Rizzieri, Joseph Jurcic, Carlos E. Vigil, Robert Redner, Gail Roboz, Michael Savona, Michael R. McKeown, Kristin Stephens, David A. Roth, Jorge Cortes
ASCO Annual Meeting
Abstract Number: TPS7071
2017

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

Michael R McKeown, Kathryn Austgen, Chris Fiore, Emily Lee, Darren Smith, Christian Fritz, Tracey Lodie, Emmanuelle di Tomaso, Eric Olson
EHA 22nd Congress
Abstract Number: P188
2017

SY-1425, A POTENT AND SELECTIVE RARΑ AGONIST, REPROGRAMS AML CELLS FOR DIFFERENTIATION ALONG DISTINCT LINEAGES, UNCOVERING PD MARKERS FOR CLINICAL STUDIES

Michael R McKeown, Chris Fiore, Kathryn Austgen, Emily Lee, Darren Smith, Mei Wei Chen, Matthew L Eaton, Angela Volkert, Curran Murphy, Kristin Stephens, Christian Fritz, Tracey Lodie, Emmanuelle di Tomaso and Eric Olson
EHA 22nd Congress
Abstract Number: E884
2017

THE EPIGENETIC LANDSCAPE OF T CELL SUBSETS IN SLE IDENTIFIES KNOWN AND POTENTIAL NOVEL DRIVERS OF THE AUTOIMMUNE RESPONSE

Jozsef Karman, Brian Johnston, Sofija Miljovska, David Orlando, Eric Olson and Tracey Lodie
Federation of Clinical Immunology Societies (FOCIS) 17th Annual Meeting: Late-breaking Oral Presentation
Abstract Number: 319030
June 16, 2017

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

EPIGENOMIC ANALYSIS OF PRIMARY BREAST CANCER TUMORS REVEALS NOVEL TUMOR CELL VULNERABILITIES AND THERAPEUTIC TARGETS

Matthew G. Guenther, Mei Wei Chen, Christina Kolodzy, Michael McKeown, Emily Lee, Cindy Collins, Matthew Eaton, David Orlando, Emmanuelle di Tomaso,
Christian C. Fritz, Eric R. Olson.
IMPAKT Breast Cancer Conference
Abstract Number: 47P
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 RARA 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 KINASES 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 ALPHA 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

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

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

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