Abstract
Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insights into structure and mechanism of Pglycoprotein may aid in design of potent inhibitors. P >
Keywords: Cyclic peptide P-glycoprotein inhibitor, ATP-binding cassette, Nucleotide binding domain, Transmembrane domain, Central nervous system, Blood brain barrier, Breast cancer related protein, Positron emission tomography, Single-photon emission computed tomography, Cytochrome P450-3A4, Multidrug resistance, MDR, Protein-ligand interaction fingerprints, Serotonine reuptake transporter, Dopamine transporter, Norepinephrine transporter, Structure activity relationship, Radiolabeled P-gp substrates, SAV1866, Ligand docking, Quinazolinones, GABAA receptor, Pharmacophore modeling, NCI-60 screening, ATPbinding site, Tyrosine kinases (TKs), Nilotinib, Dasatinib, Bosutinib, ATPases
Current Topics in Medicinal Chemistry
Title: Using Structural and Mechanistic Information to Design Novel Inhibitors/Substrates of P-Glycoprotein
Volume: 10 Issue: 17
Author(s): Freya Klepsch, Thomas Stockner, Thomas Erker, Markus Muller, Peter Chiba and Gerhard F. Ecker
Affiliation:
Keywords: Cyclic peptide P-glycoprotein inhibitor, ATP-binding cassette, Nucleotide binding domain, Transmembrane domain, Central nervous system, Blood brain barrier, Breast cancer related protein, Positron emission tomography, Single-photon emission computed tomography, Cytochrome P450-3A4, Multidrug resistance, MDR, Protein-ligand interaction fingerprints, Serotonine reuptake transporter, Dopamine transporter, Norepinephrine transporter, Structure activity relationship, Radiolabeled P-gp substrates, SAV1866, Ligand docking, Quinazolinones, GABAA receptor, Pharmacophore modeling, NCI-60 screening, ATPbinding site, Tyrosine kinases (TKs), Nilotinib, Dasatinib, Bosutinib, ATPases
Abstract: Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insights into structure and mechanism of Pglycoprotein may aid in design of potent inhibitors. P >
Export Options
About this article
Cite this article as:
Klepsch Freya, Stockner Thomas, Erker Thomas, Muller Markus, Chiba Peter and F. Ecker Gerhard, Using Structural and Mechanistic Information to Design Novel Inhibitors/Substrates of P-Glycoprotein, Current Topics in Medicinal Chemistry 2010; 10 (17) . https://dx.doi.org/10.2174/156802610792928004
DOI https://dx.doi.org/10.2174/156802610792928004 |
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
-
Inflammatory Reactions and Hydrocortisone in the Setting of Cardiac Surgery: An Overview
Cardiovascular & Hematological Agents in Medicinal Chemistry Relationship Between the Pharmacokinetics of Levosimendan and Its Effects on Cardiovascular System
Current Drug Metabolism Nimodipine Reappraised: An Old Drug With a Future
Current Neuropharmacology Hydromorphone: Analytical Methodologies for its Determination
Current Analytical Chemistry Rediscovery of Caffeine: An Excellent Drug for Improving Patient Outcomes while Fighting WARS
Current Medicinal Chemistry Impaired Neural Transmission and Synaptic Plasticity in Superior Cervical Ganglia from β-Amyloid Rat Model of Alzheimers Disease
Current Alzheimer Research Analysis of Current Antifungal Agents and Their Targets within the Pneumocystis carinii Genome
Current Drug Targets Cardiac Workup of Ischemic Stroke
Current Cardiology Reviews Inflammatory Caspases: Targets for Novel Therapies
Current Pharmaceutical Design Long-Acting Antipsychotic Medications
Current Drug Targets Insulin and Endothelial Function: Physiological Environment Defines Effect on Atherosclerotic Risk
Current Diabetes Reviews Static Cerebral Blood Flow Autoregulation in Humans
Current Hypertension Reviews Genetics of Polygenic Hypertension from Animal Models to Humans
Current Hypertension Reviews Innovative Cancer Treatments that Augment Radiotherapy or Chemotherapy by the Use of Immunotherapy or Gene Therapy
Recent Patents on Anti-Cancer Drug Discovery Biochemical Markers of Renal Function
Current Medicinal Chemistry Protective Effects of Curcumin against Iron-induced Toxicity
Current Pharmaceutical Biotechnology The Role of NPY and Ghrelin in Anorexia Nervosa
Current Pharmaceutical Design A Review of the Chemical and Pharmacological Aspects of the Genus Marrubium
Current Pharmaceutical Design B-Type Natriuretic Peptide: Endogenous Regulator of Myocardial Structure, Biomarker and Therapeutic Target
Current Molecular Medicine Hypoxia Inducible Factor-1 as a Therapeutic Target in Cerebral Ischemia
Current Signal Transduction Therapy