Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor-Reference-Cited by-同舟云学术

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Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor

Published:2019 Issue:7 Volume:17 Page:2020-2027
ISSN:1477-0520
Container-title:Organic & Biomolecular Chemistry
language:en
Short-container-title:Org. Biomol. Chem.

Author:

Kirberger Steven E.¹²³⁴,Ycas Peter D.¹²³⁴,Johnson Jorden A.¹²³⁴,Chen Chen⁵⁶⁴,Ciccone Michael F.⁵⁶⁴,Woo Rinette W. L.⁷⁸⁹⁴,Urick Andrew K.¹²³⁴,Zahid Huda¹²³⁴,Shi Ke¹⁰¹¹¹²¹³³,Aihara Hideki¹⁰¹¹¹²¹³³,McAllister Sean D.⁷⁸⁹⁴,Kashani-Sabet Mohammed⁷⁸⁹⁴,Shi Junwei¹⁴¹⁵¹⁶¹⁷⁴,Dickson Alex¹⁸¹⁹²⁰⁴,dos Santos Camila O.⁵⁶⁴,Pomerantz William C. K.¹²³⁴^ORCID

Affiliation:

1. Department of Chemistry

2. University of Minnesota

3. Minneapolis

4. USA

5. Cold Spring Harbor Laboratory

6. Cold Spring Harbor

7. Center for Melanoma Research and Treatment

8. California Pacific Medical Center Research Institute

9. San Francisco

10. Department of Biochemistry

11. Molecular Biology

12. and Biophysics

13. University of Minnesota Twin Cities

14. Perelman School of Medicine

15. University of Pennsylvania

16. 3400 Civic Center Boulevard

17. Philadelphia

18. Department of Biochemistry & Molecular Biology

19. Michigan State University

20. East Lansing

Abstract

¹⁹F NMR-guided development of a BPTF chemical probe through SAR and ligand deconstruction.

Funder

National Cancer Institute

Rita Allen Foundation

Pershing Square Foundation

National Institutes of Health

University of Minnesota

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2019/OB/C8OB02599A

Reference29 articles.

1. Essential Role of Chromatin Remodeling Protein Bptf in Early Mouse Embryos and Embryonic Stem Cells

2. BPTF Maintains Chromatin Accessibility and the Self-Renewal Capacity of Mammary Gland Stem Cells

3. Identification and Characterization of BPTF, a Novel Bromodomain Transcription Factor

4. Recognition of a Mononucleosomal Histone Modification Pattern by BPTF via Multivalent Interactions

5. BPTF is required for c-MYC transcriptional activity and in vivo tumorigenesis

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1. Chromatin remodellers as therapeutic targets;Nature Reviews Drug Discovery;2024-07-16

2. BPTF Drives Gastric Cancer Resistance to EGFR Inhibitor by Epigenetically Regulating the C‐MYC/PLCG1/Perk Axis;Advanced Science;2023-10-20

3. BPTF in bone marrow provides a potential progression biomarker regulated by TFAP4 through the PI3K/AKT pathway in neuroblastoma;Biological Procedures Online;2023-05-11

4. Creating Maps of the Ligand Binding Landscape for Kinetics-Based Drug Discovery;Methods in Molecular Biology;2021-12-10

5. New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition;Journal of Medicinal Chemistry;2021-09-13

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