Abstract
Chemical genomics is a drug discovery strategy that relies heavily on high-throughput screening (HTS) and therefore benefits from functional assay platforms that allow HTS against all relevant genomic targets. Receptor Selection and Amplification Technology (R-SAT™) is a cell-based, high-throughput functional assay where the receptor stimulus is translated into a measurable cellular response through an extensive signaling cascade occurring over several days. The large biological and chronological separation of stimulus from response provides numerous opportunities for enabling assays and increasing assay sensitivity. Here we review strategies for building homogeneous assay platforms across large gene families by redirecting and/or amplifying signal transduction pathways.
Keywords: Receptor Selection and Amplification Technology, G-protein coupled receptor (GPCR), GPCR assay, fluorescence polarization (FP), histone acetylase transfer activity (HAT)
Current Pharmaceutical Design
Title: Integrative Functional Assays, Chemical Genomics and High Throughput Screening: Harnessing Signal Transduction Pathways to a Common HTS Readout
Volume: 12 Issue: 14
Author(s): Ethan S. Burstein, Fabrice Piu, Jian-Nong Ma, Jacques T. Weissman, Erika A. Currier, Norman R. Nash, David M. Weiner, Tracy A. Spalding, Hans H. Schiffer, Andria L. Del Tredici and Mark R. Brann
Affiliation:
Keywords: Receptor Selection and Amplification Technology, G-protein coupled receptor (GPCR), GPCR assay, fluorescence polarization (FP), histone acetylase transfer activity (HAT)
Abstract: Chemical genomics is a drug discovery strategy that relies heavily on high-throughput screening (HTS) and therefore benefits from functional assay platforms that allow HTS against all relevant genomic targets. Receptor Selection and Amplification Technology (R-SAT™) is a cell-based, high-throughput functional assay where the receptor stimulus is translated into a measurable cellular response through an extensive signaling cascade occurring over several days. The large biological and chronological separation of stimulus from response provides numerous opportunities for enabling assays and increasing assay sensitivity. Here we review strategies for building homogeneous assay platforms across large gene families by redirecting and/or amplifying signal transduction pathways.
Export Options
About this article
Cite this article as:
Burstein S. Ethan, Piu Fabrice, Ma Jian-Nong, Weissman T. Jacques, Currier A. Erika, Nash R. Norman, Weiner M. David, Spalding A. Tracy, Schiffer H. Hans, Del Tredici L. Andria and Brann R. Mark, Integrative Functional Assays, Chemical Genomics and High Throughput Screening: Harnessing Signal Transduction Pathways to a Common HTS Readout, Current Pharmaceutical Design 2006; 12 (14) . https://dx.doi.org/10.2174/138161206776873662
DOI https://dx.doi.org/10.2174/138161206776873662 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Approaches to Improve Efficiency of Dendritic Cell-based Therapy of High Grade Gliomas
Current Pharmaceutical Design Application of Biological Study for Met Expression to Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Review of Progress in Predicting Protein Methylation Sites
Current Organic Chemistry Impact of Immune Response on the Use of iPSCs in Disease Modeling
Current Stem Cell Research & Therapy The Protective Effect of Korean Red Ginseng Against Rotenone-Induced Parkinson’s Disease in Rat Model: Modulation of Nuclear Factor-κβ and Caspase-3
Current Pharmaceutical Biotechnology Development of RNA Aptamer-Based Therapeutic Agents
Current Medicinal Chemistry Targeting Insulin Amyloid Assembly by Aminosugars and Their Derivatives
Protein & Peptide Letters Life Cycle of Yeast Prions: Propagation Mediated by Amyloid Fibrils
Protein & Peptide Letters Biosynthetic and Metabolic Alterations in Cancer Growth
Current Angiogenesis (Discontinued) Mild Improvement in Mitochondrial Function After a 3-Year Antiretroviral Treatment Interruption Despite Persistent Impairment of Mitochondrial DNA Content
Current HIV Research Mechanisms in the Development of Multiple Sclerosis Lesions: Reconciling Autoimmune and Neurodegenerative Factors
CNS & Neurological Disorders - Drug Targets Effects of Synthetic Peptides on the Inflammatory Response and their Therapeutic Potential
Mini-Reviews in Medicinal Chemistry Ligand and Structure Based Virtual Screening Strategies for Hit-Finding and Optimization of Hepatitis C Virus (HCV) Inhibitors
Current Medicinal Chemistry 8-Hydroxyquinoline and Hydroxamic Acid Inhibitors of Botulinum Neurotoxin BoNT/A
Current Topics in Medicinal Chemistry A Mechanistic Study on Altered Pharmacokinetics of Irinotecan by St. Johns Wort
Current Drug Metabolism Sigma-1 Receptors and Selective Serotonin Reuptake Inhibitors: Clinical Implications of their Relationship
Central Nervous System Agents in Medicinal Chemistry Glycosaminoglycans, Protein Aggregation and Neurodegeneration
Current Protein & Peptide Science The Potential Role of Pro-Inflammatory and Anti-Inflammatory Cytokines in Epilepsy Pathogenesis
Endocrine, Metabolic & Immune Disorders - Drug Targets Experimental Drugs for Neuropathic Pain
Current Neuropharmacology Targeting Allosteric Control Mechanisms in Heat Shock Protein 70 (Hsp70)
Current Topics in Medicinal Chemistry