Abstract
S100B interacts with the p53 protein in a calcium-dependent manner and down-regulates its function as a tumor suppressor. Therefore, inhibiting the S100B-p53 interaction represents a new approach for restoring functional wild-type p53 in cancers with elevated S100B such as found in malignant melanoma. A discussion of the biological rational for targeting S100B and a description of methodologies relevant to the discovery of compounds that inhibit S100B-p53 binding, including computational techniques, structural biology techniques, and cellular assays, is presented.
Keywords: melanoma, p53 tumor suppressor protein, cyclin-dependent kinase inhibitor, epitope mapping, computer-aided drug design, fluorescence spectroscopy, std-nmr
Current Topics in Medicinal Chemistry
Title: Design of Inhibitors for S100B
Volume: 5 Issue: 12
Author(s): Joseph Markowitz, Alexander D. MacKerell Jr., France Carrier, Thomas H. Charpentier and David J. Weber
Affiliation:
Keywords: melanoma, p53 tumor suppressor protein, cyclin-dependent kinase inhibitor, epitope mapping, computer-aided drug design, fluorescence spectroscopy, std-nmr
Abstract: S100B interacts with the p53 protein in a calcium-dependent manner and down-regulates its function as a tumor suppressor. Therefore, inhibiting the S100B-p53 interaction represents a new approach for restoring functional wild-type p53 in cancers with elevated S100B such as found in malignant melanoma. A discussion of the biological rational for targeting S100B and a description of methodologies relevant to the discovery of compounds that inhibit S100B-p53 binding, including computational techniques, structural biology techniques, and cellular assays, is presented.
Export Options
About this article
Cite this article as:
Markowitz Joseph, MacKerell Jr. D. Alexander, Carrier France, Charpentier H. Thomas and Weber J. David, Design of Inhibitors for S100B, Current Topics in Medicinal Chemistry 2005; 5 (12) . https://dx.doi.org/10.2174/156802605774370865
DOI https://dx.doi.org/10.2174/156802605774370865 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
- Announcements
Related Articles
-
Application of Phage Display Technology to Cancer Research
Current Pharmaceutical Biotechnology Advancement of Mechanisms of Coxsackie Virus B3-Induced Myocarditis Pathogenesis and the Potential Therapeutic Targets
Current Drug Targets Role of ncRNAs in Development, Diagnosis and Treatment of Human Cancer
Recent Patents on Anti-Cancer Drug Discovery Nanostructural Hybrid Sensitizers for Photodynamic Therapy
Current Pharmaceutical Design Biological Effects of Curcumin and Its Role in Cancer Chemoprevention and Therapy
Anti-Cancer Agents in Medicinal Chemistry Therapeutic Potential of Natural Compounds that Regulate the Activity of Protein Kinase C
Current Medicinal Chemistry Novel Options for the Pharmacological Treatment of Chronic Anal Fissure – Role of Botulin Toxin
Current Clinical Pharmacology Synergistic Effect of α-Solanine and Cisplatin Induces Apoptosis and Enhances Cell Cycle Arrest in Human Hepatocellular Carcinoma Cells
Anti-Cancer Agents in Medicinal Chemistry Insights into the Design of p97-targeting Small Molecules from Structural Studies on p97 Functional Mechanism
Current Medicinal Chemistry Hierarchical Profiles of Signaling Pathways and Networks Reveal Two Complementary Pharmacological Mechanisms
CNS & Neurological Disorders - Drug Targets Pharmacologic Activation of p53 by Small-Molecule MDM2 Antagonists
Current Pharmaceutical Design Application of DODMA and Derivatives in Cationic Nanocarriers for Gene Delivery
Current Organic Chemistry Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy
Current Medicinal Chemistry A Phosphoproteomics Approach to Identify Candidate Kinase Inhibitor Pathway Targets in Lymphoma-Like Primary Cell Lines
Current Drug Discovery Technologies Lipids as Activators of Innate Immunity in Peptide Vaccine Delivery
Current Medicinal Chemistry Eph as a Target in Inflammation
Endocrine, Metabolic & Immune Disorders - Drug Targets Biochemical Mechanisms of Cisplatin Cytotoxicity
Anti-Cancer Agents in Medicinal Chemistry The use of Azoles Containing Natural Products in Cancer Prevention and Treatment: An Overview
Anti-Cancer Agents in Medicinal Chemistry Linking Inflammation to Cell Cycle Progression
Current Pharmaceutical Design In Vitro Evaluation of Antimicrobial and Antiproliferative Activities for Compounds Isolated from the Ficus Bubu Warb. (Moraceae) Fruits: Chemotaxonomic Significance
Drug Delivery Letters