Abstract
The application of NMR screening in drug discovery has recently attained heightened importance throughout the pharmaceutical industry. NMR screening can be applied at various points in a drug discovery program, ranging from very early in the program, when new targets can be screened long before an HTS enzymatic assay is developed, to later in the program, as in the case where no useful hits have been detected by HTS using biological assays. The binders determined in primary NMR screens are used to guide secondary screens, which can be either completely NMR driven or use NMR in combination with other biophysical techniques. In this review we briefly discuss the methods and techniques used in NMR screening. Then, we describe in detail the NMR screening strategies and their applications to specific targets, including successful examples from actual drug design programs at our own and other pharmaceutical companies.
Keywords: NMR Screening, HTS enzymatic assay
Current Topics in Medicinal Chemistry
Title: Application of NMR Screening in Drug Discovery
Volume: 3 Issue: 1
Author(s): Jasna Fejzo, Christopher Lepre and Xiaoling Xie
Affiliation:
Keywords: NMR Screening, HTS enzymatic assay
Abstract: The application of NMR screening in drug discovery has recently attained heightened importance throughout the pharmaceutical industry. NMR screening can be applied at various points in a drug discovery program, ranging from very early in the program, when new targets can be screened long before an HTS enzymatic assay is developed, to later in the program, as in the case where no useful hits have been detected by HTS using biological assays. The binders determined in primary NMR screens are used to guide secondary screens, which can be either completely NMR driven or use NMR in combination with other biophysical techniques. In this review we briefly discuss the methods and techniques used in NMR screening. Then, we describe in detail the NMR screening strategies and their applications to specific targets, including successful examples from actual drug design programs at our own and other pharmaceutical companies.
Export Options
About this article
Cite this article as:
Fejzo Jasna, Lepre Christopher and Xie Xiaoling, Application of NMR Screening in Drug Discovery, Current Topics in Medicinal Chemistry 2003; 3 (1) . https://dx.doi.org/10.2174/1568026033392796
DOI https://dx.doi.org/10.2174/1568026033392796 |
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
-
Viruses and Multiple Sclerosis
CNS & Neurological Disorders - Drug Targets Extracellular Level of GABA and Glu: In Vivo Microdialysis-HPLC Measurements
Current Topics in Medicinal Chemistry Targeted Anti-leukemic Therapy as Disease-stabilizing Treatment for Acute Myeloid Leukemia Relapse after Allogeneic Stem Cell Transplantation: Will it be Possible to Combine these Strategies with Retransplantation or Donor Lymphocyte Infusions?
Current Cancer Drug Targets Are Carbonic Anhydrase Inhibitors Suitable for Obtaining Antiobesity Drugs ?
Current Pharmaceutical Design The Relationship Between Cleft Lip, Maxillary Hypoplasia, Hypoxia and Phenytoin
Current Pharmaceutical Design Transitional Polytherapy: Tricks of the Trade for Monotherapy to Monotherapy AED Conversions
Current Neuropharmacology Potential Health Benefits of Passion Fruit Peel Flour
The Natural Products Journal AMPA Receptor Antagonists as Potential Anticonvulsant Drugs
Current Topics in Medicinal Chemistry The Interaction of DNA-Binding Ligands with Trinucleotide-Repeat DNA: Implications for Therapy and Diagnosis of Neurological Disorders
Current Topics in Medicinal Chemistry Recent Multiple Transition Metal Catalysed Single-Pot Reactions
Current Organic Synthesis Non-Antidepressant Treatment of Generalized Anxiety Disorder
Current Clinical Pharmacology Bridging Over the Troubled Heterogeneity of SPG-Related Pathologies: Mechanisms Unite What Genetics Divide
Current Molecular Medicine Protein-Protein Interactions and Subunit Composition of Ion Channels
CNS & Neurological Disorders - Drug Targets SLC1 Glutamate Transporters and Diseases: Psychiatric Diseases and Pathological Pain
Current Molecular Pharmacology An Update on Autoinflammatory Diseases
Current Medicinal Chemistry Patent Selections:
Recent Patents on Regenerative Medicine Calcium Channels and Prostate Cancer
Recent Patents on Anti-Cancer Drug Discovery AMPA Receptor Antagonists: Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Novel Pyrimidine based Semicarbazones: Confirmation of Four Binding Site Pharmacophoric Model Hypothesis for Antiepileptic Activity
Central Nervous System Agents in Medicinal Chemistry Physiology, Pharmacology and Pathophysiology of the pH Regulatory Transport Proteins NHE1 and NBCn1: Similarities, Differences, and Implications for Cancer Therapy
Current Pharmaceutical Design