Abstract
With the recently completed sequencing and annotation of the human genome, it has become clear that a significant portion of the genome encodes signal-transducing molecules including receptors, protein kinases, ion channels, transporters and coupling proteins. This review focuses on membrane-localized receptors, which represent the largest single group of signal-transducing molecules. Indeed, one can estimate that nearly 10% of the human genome encodes membrane- localized receptors (e.g. G-protein coupled receptors, ligand-gated ion channels and transporters). We have defined that portion of the human genome that encodes receptors the receptorome. In this article, we will demonstrate how the massively parallel screening of the receptorome provides a facile and under-utilized screening platform for drug discovery. Using case studies, we will show how receptorome-based screening elucidates the mechanisms responsible for serious side-effects of both approved and investigational medications. Additionally, we will provide evidence that receptorome- based screening provides insights into novel therapeutic indications of approved medications and serves to validate targets for therapeutic drug discovery.
Keywords: Obesity-Related Molecular Targets, In Silico Receptoromics, Receptor Databases, GPCR, NC-IUPHAR, Weight Gain
Current Pharmaceutical Design
Title: Screening the Receptorome Yields Validated Molecular Targets for Drug Discovery
Volume: 12 Issue: 14
Author(s): Wesley K. Kroeze and Bryan L. Roth
Affiliation:
Keywords: Obesity-Related Molecular Targets, In Silico Receptoromics, Receptor Databases, GPCR, NC-IUPHAR, Weight Gain
Abstract: With the recently completed sequencing and annotation of the human genome, it has become clear that a significant portion of the genome encodes signal-transducing molecules including receptors, protein kinases, ion channels, transporters and coupling proteins. This review focuses on membrane-localized receptors, which represent the largest single group of signal-transducing molecules. Indeed, one can estimate that nearly 10% of the human genome encodes membrane- localized receptors (e.g. G-protein coupled receptors, ligand-gated ion channels and transporters). We have defined that portion of the human genome that encodes receptors the receptorome. In this article, we will demonstrate how the massively parallel screening of the receptorome provides a facile and under-utilized screening platform for drug discovery. Using case studies, we will show how receptorome-based screening elucidates the mechanisms responsible for serious side-effects of both approved and investigational medications. Additionally, we will provide evidence that receptorome- based screening provides insights into novel therapeutic indications of approved medications and serves to validate targets for therapeutic drug discovery.
Export Options
About this article
Cite this article as:
Kroeze K. Wesley and Roth L. Bryan, Screening the Receptorome Yields Validated Molecular Targets for Drug Discovery, Current Pharmaceutical Design 2006; 12 (14) . https://dx.doi.org/10.2174/138161206776873680
DOI https://dx.doi.org/10.2174/138161206776873680 |
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
-
Multimodality Imaging in Cardiac Sarcoidosis: Is There a Winner?
Current Cardiology Reviews Loneliness and Social Isolation: Determinants of Cardiovascular Outcomes
Current Cardiology Reviews Heat Shock Proteins - Two Sides of a Coin
Current Cardiology Reviews Bilirubin Chemistry and Metabolism; Harmful and Protective Aspects
Current Pharmaceutical Design Coffee: A Dietary Intervention on Type 2 Diabetes?
Current Medicinal Chemistry Inhibition of Platelet Adhesion to Collagen as a New Target for Antithrombotic Drugs
Current Drug Targets - Cardiovascular & Hematological Disorders Effects of Verbascoside Administration on the Blood Parameters and Oxidative Status in Jennies and Their Suckling Foals: Potential Improvement of Milk for Human Use
Endocrine, Metabolic & Immune Disorders - Drug Targets Oral Antiplatelet Treatment in STEMI: Current Practice and Future Considerations
Current Pharmaceutical Design Single Emulsion-Solvent Evaporation Technique and Modifications for the Preparation of Pharmaceutical Polymeric Nanoparticles
Recent Patents on Drug Delivery & Formulation Electronic Noses in Medical Diagnostics
Current Medicinal Chemistry Fabry Disease and Cardiovascular Involvement
Current Pharmaceutical Design HDL Therapy: Two Kinds of Right?
Current Pharmaceutical Design A Pilot Study on Prostate Cancer Risk and Pro-Inflammatory Genotypes: Pathophysiology and Therapeutic Implications
Current Pharmaceutical Design Biomarkers of Chronic Kidney Disease - Mineral and Bone Disorder (CKD-MBD), A Review of Published Patents and Patent Applications
Recent Patents on Biomarkers Coarctation of the Aorta - The Current State of Surgical and Transcatheter Therapies
Current Cardiology Reviews Disease Modifying Osteoarthritis Drugs: Facing Development Challenges and Choosing Molecular Targets
Current Drug Targets Is Red Meat Required for the Prevention of Iron Deficiency Among Children and Adolescents?
Current Pediatric Reviews Immunocal® and Preservation of Glutathione as a Novel Neuroprotective Strategy for Degenerative Disorders of the Nervous System
Recent Patents on CNS Drug Discovery (Discontinued) High-Density Lipoprotein: Key Molecule in Cholesterol Efflux and the Prevention of Atherosclerosis
Current Pharmaceutical Design Nutritional Antioxidants Mechanisms of Action, Analyses of Activities and Medical Applications
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents