Abstract
Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however, no PROTAC acting against cancer has reached the clinical trials. The concept of PROTACs involves the reduction in the disease-causing protein by its degradation through the ubiquitin-proteasomal enzyme system. This concept has attracted a lot of attention from both industry and academia due to its potential in drug discovery (in the form of PROTACs), which can conquer the resistance associated with current treatments of cancer. Thus, it is the need of the hour to identify and synthesize more PROTACs for a viable treatment of cancer. This article reviews the design, activity and effects produced in cancer by some recently developed PROTACs.
Keywords: PROTACs, cancer, ubiquitin, anticancer, proteins, target.
Mini-Reviews in Medicinal Chemistry
Title:PROTACs in Treatment of Cancer: A Review
Volume: 21 Issue: 16
Author(s): Poonam Arora, Manjinder Singh, Varinder Singh, Shiveena Bhatia and Sandeep Arora*
Affiliation:
- Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, Punjab,India
Keywords: PROTACs, cancer, ubiquitin, anticancer, proteins, target.
Abstract: Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however, no PROTAC acting against cancer has reached the clinical trials. The concept of PROTACs involves the reduction in the disease-causing protein by its degradation through the ubiquitin-proteasomal enzyme system. This concept has attracted a lot of attention from both industry and academia due to its potential in drug discovery (in the form of PROTACs), which can conquer the resistance associated with current treatments of cancer. Thus, it is the need of the hour to identify and synthesize more PROTACs for a viable treatment of cancer. This article reviews the design, activity and effects produced in cancer by some recently developed PROTACs.
Export Options
About this article
Cite this article as:
Arora Poonam , Singh Manjinder , Singh Varinder , Bhatia Shiveena and Arora Sandeep *, PROTACs in Treatment of Cancer: A Review, Mini-Reviews in Medicinal Chemistry 2021; 21 (16) . https://dx.doi.org/10.2174/1389557521666210226150740
DOI https://dx.doi.org/10.2174/1389557521666210226150740 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Biodiversity, Ethnopharmacology, Biotechnology, Bioclimatology and Scientific Education Applied to Toxicology and One Health
Neglected Tropical Diseases (NTDs) are represented by a group of distinct illnesses that affect the most vulnerable segment of the population, negatively impacting the Economy and Public Health. For example, like snakebite, leishmaniasis disproportionately affects vulnerable populations in tropical and subtropical regions. The search for safe drugs against various diseases ...read more
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Chemistry of Materials and Emerging Techniques: Future of Drug Discovery and Medicinal Product Developments
In drug discovery, established knowledge of functional groups, their chemical behaviors, and structure-activity relationships favor chemists to achieve desired efficacy and safety profiles within the novel designed medicinal products. Here, judicious integration of different tools and techniques of chemistry also plays a fundamental role towards the selection of the processes ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
- Announcements
Related Articles
-
Phytogenic One-pot Synthesis and Spectroscopic Characterization of Novel
Mono Benzylated Resveratrol Hybrid Molecule Using Extracted Resveratrol
from Green Grape Peels: <i>In Silico</i> ADMET Study and <i>In Vitro</i> Antitumor
Activities Against Breast Cancer Cells
Current Bioactive Compounds Applications of Cellular Systems Biology in Breast Cancer Patient Stratification and Diagnostics
Combinatorial Chemistry & High Throughput Screening Natural Products as PI3K/ Akt Inhibitors: Implications in Preventing Hepatocellular Carcinoma
Current Molecular Pharmacology Targeted Delivery of Lipid Nanoparticles by Means of Surface Chemical Modification
Current Organic Chemistry Antiangiogenic Therapy
Current Pharmaceutical Design Preferentially Expressed Antigen in Melanoma (PRAME) and the PRAME Family of Leucine-Rich Repeat Proteins
Current Cancer Drug Targets Protein Engineering: A New Frontier for Biological Therapeutics
Current Drug Metabolism Neopterin as a Marker for Immune System Activation
Current Drug Metabolism Relevance of Drug Metabolizing Enzyme Activity Modulation by Tea Polyphenols in the Inhibition of Esophageal Tumorigenesis
Medicinal Chemistry A Systematic Review of Genes Involved in the Inverse Resistance Relationship Between Cisplatin and Paclitaxel Chemotherapy: Role of BRCA1
Current Cancer Drug Targets Expression and Function of the Endocannabinoid System in Glial Cells
Current Pharmaceutical Design A Facile and Microwave-assisted Rapid Synthesis of 2-Arylamino-4-(3′-indolyl)- thiazoles as Apoptosis Inducing Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Pharmacoinformatic Approaches to Design Natural Product Type Ligands of ABC-Transporters
Current Pharmaceutical Design Pharmacogenomic Approaches for Tailored Anti-Leukemic Therapy in Children
Current Medicinal Chemistry Design, In Silico Modelling, and Functionality Theory of Novel Folate Receptor Targeted Rutin Encapsulated Folic Acid Conjugated Keratin Nanoparticles for Effective Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Outcome-Dependent Global Similarity Analysis of Imbalanced Core Signaling Pathways in Ischemic Mouse Hippocampus
CNS & Neurological Disorders - Drug Targets Thalidomide: An Overview of its Pharmacological Mechanisms of Action
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 5-HT3 Receptors
Current Pharmaceutical Design Targeting Malignancies with Disulfiram (Antabuse): Multidrug Resistance, Angiogenesis, and Proteasome
Current Cancer Drug Targets Synthesis and Apoptotic Activities of New 2(3H)-benzoxazolone Derivatives in Breast Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry