Abstract
Extensive efforts since 1931, on the structural determination of the mammalian tachykinin SP by NMR, CD and IR have turned out to be inconclusive. Studies are now being concentrated on the structural properties and characteristics of various NK receptors (NK1, NK2 and NK3) with the help of genetics, cloning, receptor engineering, mutagenesis and modeling. This knowledge is now being fruitfully used in the development of non-peptide NK1 receptor antagonists that essentially block the pharmacological effects of SP. It is now being realized that the simultaneous blockade of two or more receptors gives promising results in emesis, depression and pulmonary obstructive diseases. In addition to the synthetic compounds, the discovery of antagonists from natural origin has added a great value to this field. In this review we have made an attempt to present the structural characteristics of SP, its analogs and antagonists, the structural characteristics of the NK receptor, and structure activity relationships that have helped to improve the therapeutic utilities of SP antagonists.
Keywords: Substance P, NK receptor, SAR of SP, Secondary structure, 2D-NMR, NK1 antagonists, QSAR
Current Topics in Medicinal Chemistry
Title: Substance P: Structure, Function, and Therapeutics
Volume: 4 Issue: 1
Author(s): Prasanna Datar, Sudha Srivastava, Evans Coutinho and Girjesh Govil
Affiliation:
Keywords: Substance P, NK receptor, SAR of SP, Secondary structure, 2D-NMR, NK1 antagonists, QSAR
Abstract: Extensive efforts since 1931, on the structural determination of the mammalian tachykinin SP by NMR, CD and IR have turned out to be inconclusive. Studies are now being concentrated on the structural properties and characteristics of various NK receptors (NK1, NK2 and NK3) with the help of genetics, cloning, receptor engineering, mutagenesis and modeling. This knowledge is now being fruitfully used in the development of non-peptide NK1 receptor antagonists that essentially block the pharmacological effects of SP. It is now being realized that the simultaneous blockade of two or more receptors gives promising results in emesis, depression and pulmonary obstructive diseases. In addition to the synthetic compounds, the discovery of antagonists from natural origin has added a great value to this field. In this review we have made an attempt to present the structural characteristics of SP, its analogs and antagonists, the structural characteristics of the NK receptor, and structure activity relationships that have helped to improve the therapeutic utilities of SP antagonists.
Export Options
About this article
Cite this article as:
Datar Prasanna, Srivastava Sudha, Coutinho Evans and Govil Girjesh, Substance P: Structure, Function, and Therapeutics, Current Topics in Medicinal Chemistry 2004; 4 (1) . https://dx.doi.org/10.2174/1568026043451636
DOI https://dx.doi.org/10.2174/1568026043451636 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Biomarkers for Systemic Therapy in Ovarian Cancer
Current Cancer Drug Targets The Need for Calcium Channels in Cell Proliferation
Recent Patents on Anti-Cancer Drug Discovery Therapeutic Potential of Curcumin in the Treatment of Glioblastoma Multiforme
Current Pharmaceutical Design Magnetic Nanoparticles in Brain Disease Diagnosis and Targeting Drug Delivery
Current Nanoscience Voltage-Gated Ion Channels, New Targets in Anti-Cancer Research
Recent Patents on Anti-Cancer Drug Discovery New Insights into Pre-, Intra- and Post-Operative Brain Mapping in Low- Grade Glioma Surgery: Towards a Longitudinal Study of Cerebral Plasticity
Current Medical Imaging Selected Approaches for Rational Drug Design and High Throughput Screening to Identify Anti-Cancer Molecules
Anti-Cancer Agents in Medicinal Chemistry Genistein Potentiates the Anti-cancer Effects of Gemcitabine in Human Osteosarcoma via the Downregulation of Akt and Nuclear Factor-κB Pathway
Anti-Cancer Agents in Medicinal Chemistry A Review of Nanocarrier-Based CNS Delivery Systems
Current Drug Delivery Current Limitations in the Treatment of Parkinson’s and Alzheimer’s Diseases: State-of-the-Art and Future Perspective of Polymeric Carriers
Current Medicinal Chemistry DNA Demethylation: Where Genetics Meets Epigenetics
Current Pharmaceutical Design Biospecies Capture and Detection at Low Concentration
Micro and Nanosystems Water and Ion Channels: Crucial in the Initiation and Progression of Apoptosis in Central Nervous System?
Current Neuropharmacology Advances in Helper-Dependent Adenoviral Vector Research
Current Gene Therapy VEGF/VEGFR Pathway Inhibitors as Anti-Angiogenic Agents: Present and Future
Current Cancer Drug Targets Biocompatible Targeting Hydrogels for Breast Cancer Treatment
Mini-Reviews in Medicinal Chemistry The Role of CD40 Expression in Dendritic Cells in Cancer Biology; A Systematic Review
Current Cancer Drug Targets Cancer Pharmacogenetics: The Move from Pharmacokinetics to Pharmacodynamics
Current Pharmacogenomics TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design Dual-Specificity MAP Kinase Phosphatases as Targets of Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry