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Your search keyword '"Maureen H. Beresini"' showing total 15 results
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15 results on '"Maureen H. Beresini"'

2. Table S1 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

Bromodomain selectivity data for GNE-049 using BROMOscan® panel

Published
2023
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3. Figure S2 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

qPCR analysis of Myc expression after GNE-049 treatment, effects of GNE-049 combination treatment.

Published
2023
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5. Figure S4 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

Western blot analysis of AR mutant and over expressing LNCaP cells

Published
2023
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6. Figure S1 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

Western blots confirming siRNA knockdowns, GNE-049 compound properties.

Published
2023
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8. Data from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

Resistance invariably develops to antiandrogen therapies used to treat newly diagnosed prostate cancers, but effective treatments for castration-resistant disease remain elusive. Here, we report that the transcriptional coactivator CBP/p300 is required to maintain the growth of castration-resistant prostate cancer. To exploit this vulnerability, we developed a novel small-molecule inhibitor of the CBP/p300 bromodomain that blocks prostate cancer growth in vitro and in vivo. Molecular dissection of the consequences of drug treatment revealed a critical role for CBP/p300 in histone acetylation required for the transcriptional activity of the androgen receptor and its target gene expression. Our findings offer a preclinical proof of concept for small-molecule therapies to target the CBP/p300 bromodomain as a strategy to treat castration-resistant prostate cancer. Cancer Res; 77(20); 5564–75. ©2017 AACR.

Published
2023
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9. Figure S3 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

Western blot and ChIP seq analysis of GNE-049 impact on histone acetylation

Published
2023
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10. Table S2 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Karen E. Gascoigne, Steven Magnuson, F. Anthony Romero, Maureen H. Beresini, Susan Kaufman, Edna Choo, Justin Ly, Zora Modrusan, Peter M. Haverty, Ryan Raisner, Samir Kharbanda, Mark Merchant, Ehud Segal, Cecile de la Cruz, Emily Chan, Jesse Garcia, and Lingyan Jin

Abstract

RNA seq analysis of androgen stimulated LNCaP cells treated with GNE-049.

Published
2023
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12. High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRAS

Author

Ke Sherry, Li, John G, Quinn, Matthew J, Saabye, Jesus F Salcido, Guerrero, Jim, Nonomiya, Qihui, Lian, Wilson, Phung, Yevgeniy, Izrayelit, Benjamin T, Walters, Amy, Gustafson, Nicholas F, Endres, Maureen H, Beresini, and Melinda M, Mulvihill

Subjects
Proto-Oncogene Proteins p21(ras), Kinetics, Drug Discovery
Abstract

With recent advances and success in several drugs designed to treat acute and chronic diseases, targeted covalent inhibitors show a resurgence in drug discovery. As covalent inhibition is time-dependent, the preferred quantitative potency metric of irreversible inhibitors is the second-order rate constant

Published
2022

13. GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like

Author

Shumei Wang, Vickie Tsui, Terry D. Crawford, James E. Audia, Daniel J. Burdick, Maureen H. Beresini, Alexandre Côté, Richard Cummings, Martin Duplessis, E. Megan Flynn, Michael C. Hewitt, Hon-Ren Huang, Hariharan Jayaram, Ying Jiang, Shivangi Joshi, Jeremy Murray, Christopher G. Nasveschuk, Eneida Pardo, Florence Poy, F. Anthony Romero, Yong Tang, Alexander M. Taylor, Jian Wang, Zhaowu Xu, Laura E. Zawadzke, Xiaoyu Zhu, Brian K. Albrecht, Steven R. Magnuson, Steve Bellon, and Andrea G. Cochran

Subjects
0301 basic medicine, Models, Molecular, 010405 organic chemistry, Protein Conformation, 01 natural sciences, 0104 chemical sciences, 03 medical and health sciences, 030104 developmental biology, Protein Domains, Drug Design, Molecular Probes, Drug Discovery, Molecular Medicine, Humans, Benzimidazoles, Transcription Factor TFIID
Abstract

The biological functions of the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1(1,2)) remain unknown, although TAF1 has been identified as a potential target for oncology research. Here, we describe the discovery of a potent and selective in vitro tool compound for TAF1(2), starting from a previously reported lead. A cocrystal structure of lead compound 2 bound to TAF1(2) enabled structure-based design and structure-activity-relationship studies that ultimately led to our in vitro tool compound, 27 (GNE-371). Compound 27 binds TAF1(2) with an IC

Published
2018

14. Synthesis and Screening of Linear and Cyclic Oligocarbamate Libraries. Discovery of High Affinity Ligands for GPIIb/IIIa

Author

and Thomas Keough, Sari J. Paikoff, Lea T. Berleau, Maureen H. Beresini, Peter G. Schultz, Andrea R. Hebert, Corey W. Liu, Charles Y. Cho, R. Scott Youngquist, and David E. Wemmer

Subjects
chemistry.chemical_classification, Platelet aggregation, biology, Ligand, Stereochemistry, Integrin, Peptide, General Chemistry, Biochemistry, Combinatorial chemistry, Catalysis, chemistry.chemical_compound, GpIIb/IIIa, Colloid and Surface Chemistry, Monomer, chemistry, Snake venom, biology.protein, Clearance
Abstract

Synthetic methodology has been developed for the generation of large, diverse libraries of “unnatural” carbamate oligomers using the “one bead, one peptide” method. Using a pool of 27 structurally and functionally diverse monomers, one acyclic and two cyclic libraries were synthesized and screened for binding to the integrin GPIIb/IIIa. Several classes of oligocarbamate ligands for GPIIb/IIIa were discovered, and two cyclic ligands have activities that are within a factor of 3 of kistrin, a snake venom protein that effectively inhibits platelet aggregation. Preliminary pharmacokinetic characterization was performed on a linear oligocarbamate ligand, which was cleared from plasma with a half-life of 3.6 min.

Published
1998
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15. Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores

Author

Georgette M, Castanedo, Fredrick C, Sailes, Nathan J P, Dubree, John B, Nicholas, Lisa, Caris, Kevin, Clark, Susan M, Keating, Maureen H, Beresini, Henry, Chiu, Sherman, Fong, James C, Marsters, David Y, Jackson, and Daniel P, Sutherlin

Subjects
Models, Molecular, Integrins, Structure-Activity Relationship, Drug Design, Molecular Conformation, Combinatorial Chemistry Techniques, Enzyme-Linked Immunosorbent Assay, Indicators and Reagents, Integrin alpha4beta1
Abstract

Two structural classes of dual alpha4beta1/alpha4beta7 integrin antagonists were investigated via solid-phase parallel synthesis. Using an acylated amino acid backbone, lead compounds containing biphenylalanine or tyrosine carbamate scaffolds were optimized for inhibition of alpha4beta1/VCAM and alpha4beta7/MAdCAM. A comparison of the structure-activity relationships in the inhibition of the alpha4beta7/MAdCAM interaction for substituted amines employed in both scaffolds suggests a similar binding mode for the compounds.

Published
2002

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