Abstract
Background: Bromodomain and Extra Terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery.
Objective: This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases.
Method: BET proteins act as ‘epigenetic readers' and bind to acetylated lysine residues on the tails of histones H3 and H4. Inhibition of BET proteins for a wide array of therapeutic applications has led to the discovery and development of various BET inhibitors.
Results: The increasing significance of BET inhibitors as a potential anticancer therapeutic has led to an extensive patent activity both from academia and pharmaceutical industry. Several of the BET inhibitors are under clinical development for the treatment of various kinds of cancers.
Conclusion: The unmet needs and challenges associated with BET inhibition for cancer treatment have been portrayed in this review. An insight into the current developments and future prospects has been described as well.
Keywords: BET, BET inhibitors, BRDs, cancer, epigenetics, patent, therapeutic potential.
Recent Patents on Anti-Cancer Drug Discovery
Title:BET Inhibitors as Anticancer Agents: A Patent Review
Volume: 12 Issue: 4
Author(s): Imran Ali, Gildon Choi*Kwangho Lee*
Affiliation:
- Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 34114,Korea
- Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 34114,Korea
Keywords: BET, BET inhibitors, BRDs, cancer, epigenetics, patent, therapeutic potential.
Abstract: Background: Bromodomain and Extra Terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery.
Objective: This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases.
Method: BET proteins act as ‘epigenetic readers' and bind to acetylated lysine residues on the tails of histones H3 and H4. Inhibition of BET proteins for a wide array of therapeutic applications has led to the discovery and development of various BET inhibitors.
Results: The increasing significance of BET inhibitors as a potential anticancer therapeutic has led to an extensive patent activity both from academia and pharmaceutical industry. Several of the BET inhibitors are under clinical development for the treatment of various kinds of cancers.
Conclusion: The unmet needs and challenges associated with BET inhibition for cancer treatment have been portrayed in this review. An insight into the current developments and future prospects has been described as well.
Export Options
About this article
Cite this article as:
Ali Imran , Choi Gildon *, Lee Kwangho*, BET Inhibitors as Anticancer Agents: A Patent Review, Recent Patents on Anti-Cancer Drug Discovery 2017; 12 (4) . https://dx.doi.org/10.2174/1574892812666170808121228
DOI https://dx.doi.org/10.2174/1574892812666170808121228 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
The Relationship Between Oncogene Expression and Clinical Outcome in Endometrial Carcinoma
Current Cancer Drug Targets Camptothecin Resistance in Cancer: Insights into the Molecular Mechanisms of a DNA-Damaging Drug
Current Medicinal Chemistry Influence of Dietary Substances on Intestinal Drug Metabolism and Transport
Current Drug Metabolism Diphtheria Fusion Protein Therapy of Chemoresistant Malignancies
Current Cancer Drug Targets Role of Colloidal Drug Delivery Carriers in Taxane-mediated Chemotherapy: A Review
Current Pharmaceutical Design Analysis of Four Types of Leukemia Using Gene Ontology Term and Kyoto Encyclopedia of Genes and Genomes Pathway Enrichment Scores
Combinatorial Chemistry & High Throughput Screening EGFR Inhibitors and Radiation in HNSCC
Current Cancer Therapy Reviews Review of QSAR for DNA Polymerase Inhibitors and New Models for Heterogeneous Series of Compounds
Current Computer-Aided Drug Design Clinical Development of 17-Allylamino, 17-Demethoxygeldanamycin
Current Cancer Drug Targets Targeted Lipid Nanoparticles for Antisense Oligonucleotide Delivery
Current Pharmaceutical Biotechnology Drugs Made of RNA: Development and Application of Engineered RNAs for Gene Therapy
Mini-Reviews in Medicinal Chemistry Minimally Invasive Transoral Surgical Treatment for Oropharyngeal Carcinoma
Current Cancer Therapy Reviews Important Aspects of Post-Prandial Antidiabetic Drug, Acarbose
Current Topics in Medicinal Chemistry Rasburicase: A New Approach for Preventing and/or Treating Tumor Lysis Syndrome
Current Pharmaceutical Design Prediction of Essential Proteins in Prokaryotes by Incorporating Various Physico-chemical Features into the General form of Chou’s Pseudo Amino Acid Composition
Protein & Peptide Letters In Vitro High Throughput Phage Display Selection of Ovarian Cancer Avid Phage Clones for Near-Infrared Optical Imaging
Combinatorial Chemistry & High Throughput Screening Current Therapeutic Approaches in Inflammatory Bowel Disease
Current Pharmaceutical Design Pharmacogenomics of 5-Fluorouracil/Oxaliplatin in Colorectal Cancer
Current Pharmacogenomics Synthesis and Biological Potentials of 5-aryl-N-[4-(trifluoromethyl) phenyl]-1,3,4-oxadiazol-2-amines
Letters in Organic Chemistry Novel Biotransformation Process of Podophyllotoxin to 4 -Sulfur-Substituted Podophyllum Derivates with Anti-Tumor Activity by Penicillium purpurogenum Y.J. Tang
Current Medicinal Chemistry