Abstract
The protein kinase superfamily represents both an enormous opportunity and a unique challenge for drug discovery. Protein kinases play central roles in the cellular economy and it is well known that a large number of diseases involve aberrant protein kinase activity. This review discusses how fragment based screening strategies, such as virtual screening, NMR and high-throughput X-ray crystallography are being employed to identify new chemo-types to produce the next generation of protein kinase inhibitors.
Keywords: kinase inhibitors, x-ray crystallography, lead generation, structure-based drug design, virtual screening
Mini-Reviews in Medicinal Chemistry
Title: New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches
Volume: 4 Issue: 3
Author(s): Adrian Gill
Affiliation:
Keywords: kinase inhibitors, x-ray crystallography, lead generation, structure-based drug design, virtual screening
Abstract: The protein kinase superfamily represents both an enormous opportunity and a unique challenge for drug discovery. Protein kinases play central roles in the cellular economy and it is well known that a large number of diseases involve aberrant protein kinase activity. This review discusses how fragment based screening strategies, such as virtual screening, NMR and high-throughput X-ray crystallography are being employed to identify new chemo-types to produce the next generation of protein kinase inhibitors.
Export Options
About this article
Cite this article as:
Gill Adrian, New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches, Mini-Reviews in Medicinal Chemistry 2004; 4 (3) . https://dx.doi.org/10.2174/1389557043487385
DOI https://dx.doi.org/10.2174/1389557043487385 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
The use of Pseudotyped Coronaviruses for the Screening of Entry
Inhibitors: Green Tea Extract Inhibits the Entry of SARS-CoV-1, MERSCoV,
and SARS-CoV-2 by Blocking Receptor-spike Interaction
Current Pharmaceutical Biotechnology Fate of Influenza A Virus Proteins
Protein & Peptide Letters Peptide-Based Anticancer Vaccines: Recent Advances and Future Perspectives
Current Medicinal Chemistry Key Aspects of the Novartis Compound Collection Enhancement Project for the Compilation of a Comprehensive Chemogenomics Drug Discovery Screening Collection
Current Topics in Medicinal Chemistry Pharmacophore-Based Virtual Screening
Current Medicinal Chemistry N-(Sulfamoylbenzoyl)-L-proline Derivatives as Potential Non-β-lactam ESBL Inhibitors: Structure-Based Lead Identification, Medicinal Chemistry and Synergistic Antibacterial Activities
Medicinal Chemistry Effects of Salinomycin on Cancer Stem Cell in Human Lung Adenocarcinoma A549 Cells
Medicinal Chemistry Outcome of a HIV Positive Patient Infected with COVID-19 After an Autologous Bone Marrow Transplantation: A Case Report
Current HIV Research Role of Lipid Nanoparticles in COVID-19 in Repurposing Drugs and Vaccines
Current Nanoscience Recent Androgen Receptor Antagonists in Prostate Cancer
Mini-Reviews in Medicinal Chemistry Discovery of Inhibitors of Protein-Protein Interactions from Combinatorial Libraries
Current Topics in Medicinal Chemistry Curcumin-Based Anti-Prostate Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Periostin as a Heterofunctional Regulator of Cardiac Development and Disease
Current Genomics A Brief Review of Drug Discovery Research for Human African Trypanosomiasis
Current Medicinal Chemistry The Etiology of Hypertension in the Metabolic Syndrome Part Two: The Gene-Environment Interaction
Current Vascular Pharmacology The LSM 510 META - ConfoCor 2 System: An Integrated Imaging and Spectroscopic Platform for Single-Molecule Detection
Current Pharmaceutical Biotechnology Nitroisoxazolones Showing Diverse Chemical Behavior: A Use ful Building Block for Polyfunctionalized Systems
Current Medicinal Chemistry Andrographolide Derivative AL-1 Ameliorates LPS-induced Acute Lung Injury by Inhibiting NLRP3 Inflammasome and Lung Permeability
Current Pharmaceutical Design Endothelin Receptor Antagonists: Another Potential Alternative for Cardiovascular Diseases
Current Drug Targets - Cardiovascular & Hematological Disorders Plastid Molecular Pharming I. Production of Oral Vaccines via Plastid Transformation
Mini-Reviews in Medicinal Chemistry