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
-
Mice Brain Nitric Oxide Synthase Response Induced by Anaesthetics and Other Porphyrinogenic Drugs
Drug Metabolism Letters MicroRNAs: Key Players in Microglia and Astrocyte Mediated Inflammation in CNS Pathologies
Current Medicinal Chemistry Biosynthetic and Metabolic Alterations in Cancer Growth
Current Angiogenesis (Discontinued) Association Between Oxidative Stress and Altered Cholesterol Metabolism in Alzheimer’s Disease Patients
Current Alzheimer Research Using Endogenous Neural Stem Cells to Enhance Recovery from Ischemic Brain Injury
Current Neurovascular Research Editorial (Cellular Senescence and Inflammation: Advances and Therapeutic Targets in Aging and Major Age-Related Diseases)
Current Pharmaceutical Design Insulin Secretion and Interleukin-1β Dependent Mechanisms in Human Diabetes Remission After Metabolic Surgery
Current Medicinal Chemistry An Overview of Non-Neural Sources of Calcitonin Gene-Related Peptide
Current Medicinal Chemistry Perinatal Events Affecting the Onset of Allergic Diseases
Current Drug Targets - Inflammation & Allergy Transition Metal Complexes of Some Azamacrocycles and Their Use in Molecular Recognition
Current Organic Synthesis Diagnostic and Therapeutic Potentials of microRNAs in Heart Failure
Current Topics in Medicinal Chemistry Alpha-Secretase Cleavage of the Amyloid Precursor Protein: Proteolysis Regulated by Signaling Pathways and Protein Trafficking
Current Alzheimer Research Graphical Abstracts:
Central Nervous System Agents in Medicinal Chemistry Triheptanoin Supplementation to Ketogenic Diet Curbs Cognitive Impairment in APP/PS1 Mice Used as a Model of Familial Alzheimer’s Disease
Current Alzheimer Research Meet Our Co-Editor
Cardiovascular & Hematological Agents in Medicinal Chemistry Nasal Drug Delivery System-Factors Affecting and Applications
Current Drug Therapy An Update on Human Stem Cell-Based Therapy in Parkinson's Disease
Current Stem Cell Research & Therapy Mesenchymal Stem Cells of Dental Origin-Their Potential for Antiinflammatory and Regenerative Actions in Brain and Gut Damage
Current Neuropharmacology Development of COX-2 Selective Inhibitors - Therapeutic Perspectives
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Depressed Glucose Consumption at Reperfusion following Brain Ischemia does not Correlate with Mitochondrial Dysfunction and Development of Infarction: An in vivo Positron Emission Tomography Study
Current Neurovascular Research