Abstract
The molecular chaperone heat shock protein 90 (HSP90) is essential for the folding stability, intracellular disposition and proteolytic turnover of many of the key regulators of cell growth, differentiation and survival. These essential functions are used by the cells during the oncogenesis process to allow the tumor transformation and facilitate the rapid somatic evolution. Inhibition of HSP90 would provide combinatorial blockade of a range of oncogenic pathways, antagonizing many of the hallmark traits of cancer. Several HSP90 inhibitors are currently under clinical trial investigation for the treatment of cancer. This review summarizes the current state and progress achieved in the development of HSP90 inhibitors targeting the N-terminal ATP pocket, C-terminal domain, different compartmentalized isoforms, and protein (cochaperones and/or client proteins)/HSP90 interactions. In the context of drug discovery, the most relevant patents which appeared recently in the literature are discussed as well.
Keywords: Anticancer therapeutics, development of antitumor agents, drug discovery, heat shock proteins (HSPs), HSP90 inhibitors, HSP90 modulators, heat shock response, molecular chaperones
Recent Patents on Anti-Cancer Drug Discovery
Title:Heat Shock Protein 90 Inhibitors as Therapeutic Agents
Volume: 7 Issue: 3
Author(s): Isabel Gomez-Monterrey, Marina Sala, Simona Musella and Pietro Campiglia
Affiliation:
Keywords: Anticancer therapeutics, development of antitumor agents, drug discovery, heat shock proteins (HSPs), HSP90 inhibitors, HSP90 modulators, heat shock response, molecular chaperones
Abstract: The molecular chaperone heat shock protein 90 (HSP90) is essential for the folding stability, intracellular disposition and proteolytic turnover of many of the key regulators of cell growth, differentiation and survival. These essential functions are used by the cells during the oncogenesis process to allow the tumor transformation and facilitate the rapid somatic evolution. Inhibition of HSP90 would provide combinatorial blockade of a range of oncogenic pathways, antagonizing many of the hallmark traits of cancer. Several HSP90 inhibitors are currently under clinical trial investigation for the treatment of cancer. This review summarizes the current state and progress achieved in the development of HSP90 inhibitors targeting the N-terminal ATP pocket, C-terminal domain, different compartmentalized isoforms, and protein (cochaperones and/or client proteins)/HSP90 interactions. In the context of drug discovery, the most relevant patents which appeared recently in the literature are discussed as well.
Export Options
About this article
Cite this article as:
Gomez-Monterrey Isabel, Sala Marina, Musella Simona and Campiglia Pietro, Heat Shock Protein 90 Inhibitors as Therapeutic Agents, Recent Patents on Anti-Cancer Drug Discovery 2012; 7 (3) . https://dx.doi.org/10.2174/157489212801820066
DOI https://dx.doi.org/10.2174/157489212801820066 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
Call for Papers in Thematic Issues
Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...read more
- 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 Role of CXC-Chemokine IL-8, IL-6 and CXCR2 Receptor in Lymphoplasmacytic Lymphoma: Correlations with Microvascular Characteristics and Clinical Features
Current Angiogenesis (Discontinued) The Fate of Nanoparticles In Vivo and the Strategy of Designing Stealth Nanoparticle for Drug Delivery
Current Drug Targets Utilising Nanotechnology and Nanosystems for Treatment of Rare Diseases
Pharmaceutical Nanotechnology ChemoImmunoModulation: Immune Regulation by the Antineoplastic Chemotherapeutic Agents
Current Medicinal Chemistry Exploring Confluence-Related Signalling to Modulate the Expression of Oct4 – A Role in Facilitating Mouse Somatic Cell Reprogramming?
Current Stem Cell Research & Therapy Synthetic and Biological Attributes of Pyrimidine Derivatives: A Recent Update
Current Organic Synthesis Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy
Current Drug Discovery Technologies Potential and Perspectives of Cyclonucleosides
Current Medicinal Chemistry Laccases in Pharmaceutical Chemistry: A Comprehensive Appraisal
Mini-Reviews in Organic Chemistry ATP Site-Directed Inhibitors of Protein Kinase CK2: An Update
Current Topics in Medicinal Chemistry Impact of Leukemia Stem Cells Phenotype Expression on Response to Induction Therapy in Acute Myeloid Leukemia Patients
Cardiovascular & Hematological Disorders-Drug Targets On the Origin of Epidermal Cancers
Current Molecular Medicine Folate Receptor Targeted Liposomes Encapsulating Anti-Cancer Drugs
Current Pharmaceutical Biotechnology Editorial (Thematic Issue: Immunophilins, Protein Chemistry and Cell Biology of a Promising New Class of Drug Targets – Part II)
Current Molecular Pharmacology Signaling in Human B-Lymphoma Rafts
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Targeting Mitochondria in Fighting Cancer
Current Pharmaceutical Design Cancer Stem Cells in Prostate Cancer Chemoresistance
Current Cancer Drug Targets Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
Current Pharmaceutical Biotechnology Targeting Regulatory T Cells for Anticancer Therapy
Mini-Reviews in Medicinal Chemistry MicroRNA Expression in Coronary Artery Disease
MicroRNA