Abstract
Dopamine β-monooxygenase (DBM) catalyses the conversion of dopamine to norepinephrine in the catecholamine biosynthetic pathway. The substrate specificity of DBM is wide and the enzyme is capable of performing a variety of oxidations. While the crystal structure of DBM is not yet available, various indirect data allow insight into the enzymes machinery. Considered an attractive therapeutic target for the treatment of hypertension and congestive heart failure, DBM and its inhibitors have received attention by medicinal chemists over the last four decades. Although several QSAR models for DBM inhibitors have been generated, these models are actually unable to explain the exceptionally high potency of the latest generation of inhibitors.
Keywords: Dopamine β-monooxygenase, dopamine β-hydroxylase, inhibitor, imidazolethione, nepicastat, BIA 5-453, CHF
Current Enzyme Inhibition
Title: Dopamine β-Monooxygenase: Mechanism, Substrates and Inhibitors
Volume: 5 Issue: 1
Author(s): Alexandre Beliaev, Humberto Ferreira, David A. Learmonth and Patricio Soares-da-Silva
Affiliation:
Keywords: Dopamine β-monooxygenase, dopamine β-hydroxylase, inhibitor, imidazolethione, nepicastat, BIA 5-453, CHF
Abstract: Dopamine β-monooxygenase (DBM) catalyses the conversion of dopamine to norepinephrine in the catecholamine biosynthetic pathway. The substrate specificity of DBM is wide and the enzyme is capable of performing a variety of oxidations. While the crystal structure of DBM is not yet available, various indirect data allow insight into the enzymes machinery. Considered an attractive therapeutic target for the treatment of hypertension and congestive heart failure, DBM and its inhibitors have received attention by medicinal chemists over the last four decades. Although several QSAR models for DBM inhibitors have been generated, these models are actually unable to explain the exceptionally high potency of the latest generation of inhibitors.
Export Options
About this article
Cite this article as:
Beliaev Alexandre, Ferreira Humberto, Learmonth A. David and Soares-da-Silva Patricio, Dopamine β-Monooxygenase: Mechanism, Substrates and Inhibitors, Current Enzyme Inhibition 2009; 5 (1) . https://dx.doi.org/10.2174/157340809787314265
DOI https://dx.doi.org/10.2174/157340809787314265 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
- 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
-
CEST MRI for Molecular Imaging of Brain Metabolites
Current Molecular Imaging (Discontinued) A Mini-Review on Cardiovascular and Hematological Complications of COVID-19
Coronaviruses Localisation of Endothelin-1 and its Receptors in Vascular Tissue as Seen at the Electron Microscopic Level
Current Vascular Pharmacology MicroRNAs as Candidate Drug Targets for Cardiovascular Diseases
Current Drug Targets Possible Role of NUCB2/nesfatin-1 in Adipogenesis
Current Pharmaceutical Design Cell Hierarchy, Metabolic Flexibility and Systems Approaches to Cancer Treatment
Current Pharmaceutical Biotechnology Cardiovascular Effects of Liraglutide
Current Hypertension Reviews Serum Albumin Concentration and Cognitive Impairment
Current Alzheimer Research Dexmedetomidine Use in General Anaesthesia
Current Drug Targets Curcumin and Curcumin-like Molecules: From Spice to Drugs
Current Medicinal Chemistry Effective Agents Targeting the Mitochondria and Apoptosis to Protect the Heart
Current Pharmaceutical Design Appropriate Anti-Thrombotic/Anti-Thrombin Therapy for Thrombotic Lesions
Current Cardiology Reviews Incretin-Based Therapies in Patients with Type 2 Diabetes
Current Drug Therapy Regulation and Function of Rankl in Arterial Calcification
Current Pharmaceutical Design Exploring New CGRP Family Peptides and their Receptors in Vertebrates
Current Protein & Peptide Science Susceptibility Genes in Hypertension
Current Pharmaceutical Design Stroke Prevention in Atrial Fibrillation: Concepts and Controversies
Current Cardiology Reviews Key Role of Mitochondria in Alzheimer’s Disease Synaptic Dysfunction
Current Pharmaceutical Design High-Throughput Structural Biology in Drug Discovery: Protein Kinases
Current Pharmaceutical Design Flavonoid Rich Fraction of Dioscorea bulbifera Linn. (Yam) Enhances Mitochondrial Enzymes and Antioxidant Status, Thereby Protects Heart from Isoproterenol Induced Myocardial Infarction
Current Pharmaceutical Biotechnology