Yu Shen

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Preclinical Development The Bcl-2 / Bcl-XL / Bcl-w Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.

L. Lam, Xin Lu, S. Rosenberg, 2017, Cancer research.

Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

L. Lam, T. Uziel, D. Albert, 2017, Molecular Cancer Therapeutics.

HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues

T. Uziel, D. Albert, Xiaoyu Lin, 2016, Molecular Cancer Therapeutics.

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

L. Lam, Chaohong Sun, S. Rosenberg, 2020, Nature.

Developing Lipid Nanoparticle-Based siRNA Therapeutics for Hepatocellular Carcinoma Using an Integrated Approach

S. Fesik, Xiaoyu Lin, A. Sarthy, 2013, Molecular Cancer Therapeutics.

Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes

P. Vijay, B. Riley-Gillis, Yu Shen, 2019, Molecular Cancer Therapeutics.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

Chaohong Sun, L. Hasvold, Chang H. Park, 2017, Journal of Medicinal Chemistry.

Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

T. Uziel, D. Albert, Emily J. Faivre, 2016, Molecular Cancer Research.

Discovery of N-ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET bromodomain inhibitor with selectivity for the second bromodomain.

K. Longenecker, P. Kovar, L. Hasvold, 2020, Journal of medicinal chemistry.

Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization

K. Glaser, S. Fesik, Mark G. Anderson, 2010, Proceedings of the National Academy of Sciences.

Evaluating hypoxia-inducible factor-1alpha as a cancer therapeutic target via inducible RNA interference in vivo.

M. Staver, S. Fesik, D. Semizarov, 2005, Cancer research.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, Chaohong Sun, P. Kovar, 2017, Journal of medicinal chemistry.

Overcoming obstacles to develop effective and safe siRNA therapeutics

Leiming Li, Yu Shen, 2009, Expert opinion on biological therapy.

Overcomingobstaclesto developeffectiveandsafesiRNA therapeutics

Leiming Li, Yu Shen, 2009 .

Overcoming obstacles to develop effective and safe siRNA therapeutics.

Leiming Li, Yu Shen, 2009, Expert opinion on biological therapy.

Superior efficacy of cotreatment with BET protein inhibitor and BCL2 or MCL1 inhibitor against AML blast progenitor cells

K. Rajapakshe, C. Coarfa, M. Konopleva, 2019, Blood Cancer Journal.

Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents in vitro and in vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation

S. Fesik, U. Warrior, M. Michaelides, 2008, Proceedings of the National Academy of Sciences.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011, Molecular Cancer Therapeutics.

Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML

G. Borthakur, M. Motwani, R. Gandour-Edwards, 2022, In Vivo.

Abstract 4960: First-in-class, highly BDII-selective BET family inhibitor ABBV-744 displays potent anti-tumor activity in androgen receptor positive prostate cancer models and an improved tolerability profile

Xin Lu, T. Uziel, D. Albert, 2018, Experimental and Molecular Therapeutics.

Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo.

Mikkel A. Algire, Chaohong Sun, J. Randolph, 2023, Journal of medicinal chemistry.

Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

L. Lam, M. Konopleva, Xin Lu, 2021, Molecular Cancer Therapeutics.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, Chaohong Sun, N. Soni, 2017, Bioorganic & medicinal chemistry letters.

Superior efficacy of cotreatment with BET protein inhibitor and BCL2 or MCL1 inhibitor against AML blast progenitor cells

K. Rajapakshe, C. Coarfa, M. Konopleva, 2019, Blood Cancer Journal.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

H. Maecker, S. Rosenberg, J. Leverson, 2011, Molecular Cancer Therapeutics.

‘Seed’ analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737

S. Fesik, S. Morgan-Lappe, L. Vernetti, 2007, Oncogene.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, P. Kovar, Chang H. Park, 2017, Journal of medicinal chemistry.

Advances in the development of siRNA-based therapeutics for cancer.

Yu Shen, 2008, IDrugs : the investigational drugs journal.

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Ana L. Aguirre, A. Bogdan, Justin D Dietrich, 2018, Bioorganic & medicinal chemistry letters.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, N. Soni, P. Kovar, 2017, Bioorganic & medicinal chemistry letters.

Chang H. Park, D. Albert, Emily J. Faivre, 2017, Journal of medicinal chemistry.

Abstract 4694: ABBV-075, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo

S. Rosenberg, P. Tapang, D. Albert, 2016 .