Abstract
Drug development is a long and expensive process. It starts from the identification of a small molecule (hit compound) endowed with the ability to suppress a cellular or viral enzyme essential for the development of a given disease and proceeds through subsequent rounds of structural changes and optimization until the desired pharmacological properties are reached (lead compound). At any point of the hit-to-lead optimization process, it is of essence to monitor the behavior of the intermediate molecules with respect to their molecular targets. This involves precise mechanism of action studies as well as quantitative measurement of the performance of the compound against its target. Enzyme kinetic studies are thus an essential component of the drug development process. Relevant examples of the power of enzyme kinetics in the antiviral drug development process will be discussed in the context of anti-HIV chemotherapy.
Keywords: Enzyme kinetics, Virtual screening, SAR, Inhibitors, Antiviral drugs.
Current Pharmaceutical Biotechnology
Title:The Power of Enzyme Kinetics in the Drug Development Process
Volume: 14 Issue: 5
Author(s): Alberta Samuele, Emmanuele Crespan, Anna Garbelli, Laura Bavagnoli and Giovanni Maga
Affiliation:
Keywords: Enzyme kinetics, Virtual screening, SAR, Inhibitors, Antiviral drugs.
Abstract: Drug development is a long and expensive process. It starts from the identification of a small molecule (hit compound) endowed with the ability to suppress a cellular or viral enzyme essential for the development of a given disease and proceeds through subsequent rounds of structural changes and optimization until the desired pharmacological properties are reached (lead compound). At any point of the hit-to-lead optimization process, it is of essence to monitor the behavior of the intermediate molecules with respect to their molecular targets. This involves precise mechanism of action studies as well as quantitative measurement of the performance of the compound against its target. Enzyme kinetic studies are thus an essential component of the drug development process. Relevant examples of the power of enzyme kinetics in the antiviral drug development process will be discussed in the context of anti-HIV chemotherapy.
Export Options
About this article
Cite this article as:
Samuele Alberta, Crespan Emmanuele, Garbelli Anna, Bavagnoli Laura and Maga Giovanni, The Power of Enzyme Kinetics in the Drug Development Process, Current Pharmaceutical Biotechnology 2013; 14 (5) . https://dx.doi.org/10.2174/138920101405131111105023
DOI https://dx.doi.org/10.2174/138920101405131111105023 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
- 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
Related Articles
-
Emerging Role of Stem Cells - Derived Exosomes as Valuable Tools for Cardiovascular Therapy
Current Stem Cell Research & Therapy Application of NMR Metabolomics to Search for Human Disease Biomarkers
Combinatorial Chemistry & High Throughput Screening New Drug Targets for Genomic Cancer Therapy Successes, Limitations, Opportunities and Future Challenges
Current Cancer Drug Targets Current State of the Art of New Tubulin Inhibitors in the Clinic
Current Clinical Pharmacology The Pathogenesis, Complications and Therapeutic Strategy for Hepatitis C Virus-associated Insulin Resistance in the Era of Anti-viral Treatment
Reviews on Recent Clinical Trials Anti-CD20 Antibody in Primary Sjogren's Syndrome Managemen
Current Pharmaceutical Biotechnology Potential Molecular Targeted Therapeutics: Role of PI3-K/Akt/mTOR Inhibition in Cancer
Anti-Cancer Agents in Medicinal Chemistry Cisplatin Resistance and Transcription Factors
Current Medicinal Chemistry - Anti-Cancer Agents The Weal and Woe of Costimulation in the Adoptive Therapy of Cancer with Chimeric Antigen Receptor (CAR)-Redirected T Cells
Current Molecular Medicine Discovery of Novel NAMPT Inhibitors Based on Pharmacophore Modeling and Virtual Screening Techniques
Combinatorial Chemistry & High Throughput Screening Innate Immune System Modulation During Aging: Contributions of Macrophages and Dendritic Cells
Current Immunology Reviews (Discontinued) Genetic Variations in Telomere Maintenance, with Implications on Tissue Renewal Capacity and Chronic Disease Pathologies
Current Pharmacogenomics and Personalized Medicine Near-Infrared Dyes: Probe Development and Applications in Optical Molecular Imaging
Current Organic Synthesis Curcumin Activates the Nrf2 Pathway and Induces Cellular Protection Against Oxidative Injury
Current Molecular Medicine How Immune-inflammatory Processes Link CNS and Psychiatric Disorders: Classification and Treatment Implications
CNS & Neurological Disorders - Drug Targets An Update on Hypersensitivity Pneumonitis
Current Respiratory Medicine Reviews Acknowledgements to Contributors
Recent Patents on Anti-Cancer Drug Discovery Synthetic Androgens as Designer Supplements
Current Neuropharmacology Gene Therapy for Haemophagocytic Lymphohistiocytosis
Current Gene Therapy Antibody-Targeted Immunoliposomes for Cancer Treatment
Mini-Reviews in Medicinal Chemistry